Drug File

DRUGS USED IN OBSTETRICS
INTRODUCTION
Drugs used in obstetrics have a huge impact on the outcome of both mother and baby. Drugs used during
first trimester can produce congenital malformation and the period of greatest risk is from the third to eleven
weeks of pregnancy. During second and third trimester drugs can affect the growth and functional
development of the fetus or they can have toxic effect on fetus tissues.
CLASSIFICATION OF DRUGS USED IN PREGNANCY:
S. NO. DRUG CLASSIFICATION
1. Commonly users  Folic Acid

 Iron
 Calcium
2. Anti-hypertensive drugs  Methyldopa

 Labetalol
 Propranolol (Inderal)
 Hydralazine
 Nifedipine
 Diazoxide
 Sodium Nitroprusside
 Prazosin
 Nitroglycerine
 Captopril
3. Tocolytic Agents  Betamimetics:

 Isoxuprine Hydrochloride
 Ritrodrine Hydrochloride
 terbutaline
 Indomethacin
 Calcium channel blockers
 Nifidepine
 Magnesium antagonists
 Oxytocin antagonists
 Atosiban
 Nitric oxide (NO) donors
4. Diuretics  Furosemide (Lasix)
 Hydrochlorothiazide
 Spironolactone (Aldactone)
5. Anticoagulants  Heparin sodium
 Warfarin sodium (cumadin)
6. Analgesics  Pethidine ( mereridine)
 Fenetanyl
 Promethazine ( phenergan)
7. Oxytocin  Oxytocin
 Ergot derivatives
 prostaglandins
8. Anticonvulsant drugs  Magnesium sulfate
 Diazepam
 Phenytoin ( dilantin)
 Phenobarbitone ( luminal)
9. Teratogenic agents
Emergency drugs used in
neonates
PREGNANCY & ITS EFFECTS ON PHARMACOKINETICS: -

The remarkable physiological changes occurring in pregnancy have an impact on the absorption,
distribution, metabolism and elimination.
Absorption:
1. Decreased gastrointestinal motility in pregnancy reduced gastric emptying delays the appearance of
orally administered drugs in the plasma.
2. Vasodilation in pregnancy: this helps in efficient absorption of drugs administered through
intramuscular injection as the tissue perfusion increased because of vasodilation.
Distribution
1. Increase body fluid: a larger space is created as a result of increase in total body water upto 8 L. This
enhances better distribution of water-soluble drugs.
2. Haemodilution in pregnancy: plasma albumin declines by 10 g/L from a normal range of 33-55g/L
This results in increased free concentration of drugs binding to albumin.
Metabolism
 Increased hepatic metabolism: although the blood flow to the liver does not increase significantly in
pregnancy, there is an increase in the hepatic metabolism. This increase in metabolism results in
increased clearance of drugs like phenytoin.
Elimination
 Increased renal plasma flow in pregnancy which doubles in pregnancy. This causes rapid loss of
drugs through kidney excretion.
EFFECTS OF DRUGS ON PREGNANCY, LABOUR & PUERPERIUM: -
Effects of medications during pregnancy:
Effects of consuming drugs in pregnancy depend on factors like the following:
 Dose of drugs consumed
 Period of pregnancy when the drug was consumed.
 Existing health ailments the woman has
 Drug interactions.
 Self treatment and consuming over the counter drugs without consultation with a health care provider
which is harmful.
 Harmful drugs which have teratogenic effects on the unborn fetus resulting in birth defects.
 Pregnant woman having already existing conditions like asthma and epilepsy, in which case they
should adhere to the treatment to keep the condition under control, otherwise severity of the
condition might affect fetal outcome.
Effects of medications during labour:

 Common medications used in labour are analgesics as well as anaesthetics. Anaesthetics like opioids
cause nausea and vomiting in the women & have effects the breathing of the fetus causing
drowsiness. Sometimes they cause respiratory distress. Some analgesics and anaesthetics need to be
tested with dose before administration.
Effects of drugs in puerperium:
 Drugs, even if they are herbal supplements, consumed during puerperium should be taken with
caution after consultation with a physician as they have a tendency to pass through breast milk.
DRUGS & BREASTFEEDING:

Any medication consumed by the mother may be present in the breast milk. Drug concentration in the breast
milk is lesser concentration levels in the mother.
Drugs that are low molecular weight, nonionized and lipid soluble are usually passed through breast milk.
Drugs affecting lactation
 Oral pill (combined): lactation suppression
 Ergot derivatives: lactation suppression.
 Bromocriptine lactation suppression
Drugs affecting neonate
 Antithyroid drugs: hypothyroidism, goitre & agranulocytes
 Metronidazole: blood dyscrasias, irritability & anorexia
 Sedatives, anticonvulsants & narcotics: poor sucking reflex Tetracycline: tooth staining and delayed
bone growth
 Warfarin and heparin: safe
 Corticosteroids: sale
MISOPROSTOL
INTRODUCTION
Brand name- Cytotec
Misoprostol is a synthetic PGE1 analog that has been found to be effective and inexpensive agent for
cervical ripening as well as labor induction.
Although it has been used as an effective agent for that purpose in viable pregnancies, it is not approved by
the US Food and Drug Administration for cervical ripening and labor induction.
PHARMACOLOGY:
The initial effect of both vaginal and oral misoprostol is increase in uterine tonus. The onset of action of oral
misoprostol is more rapid and initial increase is more pronounced. Oral misoprostol has a rapid onset of
action and peak and shorter duration of action than misoprostol administered by vaginal route. The half-life
of oral misoprostol is 30 minutes and time to peak plasma concentration is 30 minutes as compared to 80
minutes of vaginal misoprostol. Thus, vaginal misoprostol has a more sustained action.
INDICATIONS OF USE
 Used for cervical ripening and labor induction.
 Used for medical association
CONTRAINDICATION:
 Misoprostol is contraindicated for induction of labor in women with previous cesarean section.
 The use of misoprostol in prior uterine surgery or cesarean delivery is avoided in third trimester.
DOSAGE:
 The 25-100 µg doses have been tried and compared in various trials, with different dosing intervals
Usually 25 µg every 4-6 hours interval to a maximum of 6 doses is given.
ROUTES OF ADMINISTRATION:
Misoprostol may be administered orally or vaginally. Although it can be used by buccal or sublingual routes,
these routes are not recommended.
ADVERSE EFFECTS:
 Uterine hyperstimulation (3-8%).
 Use of misoprostol may lead to adverse fetal heart changes, twice as compared to dinoprostone. The
incidence is closely related to the dose and frequency of misoprostol.
 When used for cervical ripening and labor induction, it significantly reduces cesarean rates and need
for oxytocin induction. In addition, it results in shorter intervals to vaginal delivery thus increasing
the number of vaginal births within 12-24 hours. However, use of oral misoprostol in trials have
shown lower risk of Apgar score <7 at 5 minutes of life.
 Since the best dose and route of misoprostol for labor induction with a live fetus are not known and
there are concerns regarding hyperstimulation, misoprostol use for induction of labor should be
within clinical trials.
COMPLICATIONS:-
 Tachysystole
 FHS changes
 Meconium-stained liquor
 uterine
NURSING RESPONSIBILTY:-
 Give to patients at high risk for developing NSAID use-induced gastric ulcers, give for the full term
of the NSAID use.
 Arrange for oral and written explanation of the risk to pregnancy; appropriate contractive.
 Measures must be taken; begin therapy on the second or third day of a normal menstrual period.
DINOPROSTONE
INTRODUCTION
Preinduction cervical ripening is the most important predictor of successful labor induction. Labor induction
is an exhausting process, unripe cervix is associated with higher chances of chorioamnionitis, prolonged
labor and cesarean delivery. The most commonly used index to assess cervical favorability is Bishop's score.
The success of induction depends on five components, consistency, position, effacement and dilatation of
cervix and the station of presenting part. Each parameter is scored out of 2 or 3 and total score is given out
of 13. Poor Bishop's score (<6) is indicator unfavorable cervix and thus the need for cervical ripening
agents. Thus, cervical ripening facilitates more successful outcome during induction of labor.³ Table 13.1
enlists the drugs used for preinduction cervical ripening.
Prostaglandins
Prostaglandin analogs are most commonly used for the purpose of cervical ripening. Prostaglandins facilitate
cervical ripening by mainly altering the extracellular ground substance of the cervix and increasing the
activity of collagenase in the cervix. Risks associated with the use of prostaglandins include uterine
hyperstimulation and maternal side effects such as nausea, vomiting, diarrhea and fever.
DINOPROSTONE (PGE2)
Generic name- Dinoprostone
Brand name- cervidil, prepidil, prostin E2
Pharmacology:
Dinoprostone is a derivative of prostanoic acid. PGE2 has an important role in the events leading to the
initiation of labor. The half-life of dinoprostone is 2.5-5 minutes. The rate limiting step for inactivation is
regulated by the enzyme 15-hydroxyprostaglandin dehydrogenase. Any PGE2 that escapes local inactivation
is rapidly cleared to the extent of 95% on the first pass through the pulmonary circulation.
PGE2 is endogenously secreted in the body by the fetal membranes and placenta and play an important role
in spontaneous initiation of labor.
It acts as a local hormone and enables ripening of the cervix by a number of different mechanisms. It softens
the cervix by altering the extracellular ground substance of cervix by increasing the activity of collagenase
in the cervix, thus causes an increase in elastase, glycosaminoglycan, dermatan sulfate, and hyaluronic acid
levels. The relaxation of cervical smooth muscle facilitates dilation. It also causes an increase in intracellular
calcium levels, leads to gap junction formation, necessary for the coordinated uterine contractions during
labor.
PHARMACODYNAMICS
Dinoprostone is equivalent to prostaglandin E2. It stimulate labor and delivery by stimulating the uterine,
and thus terminates pregnancy. Dinoprostone is also capable of stimulating the smooth muscle of the
gastrointestinal tract of man.
MECHANISM OF ACTION
Dinoprostone administered intravagially stimulate the myometrium of the gravid uterus to contract in a
manner that is similar to the contraction seen in the term uterus during labor, resulting in the evacuation of
the product of conception from the uterus.
INDICATIONS OF USE
 Most common use is for preinduction cervical ripening at term pregnancy
 Used for cervical ripening in following conditions
 Termination of pregnancy from 12 to 20 gestational weeks
 Missed abortion or intrauterine fetal death
 Nonmetastatic gestational trophoblastic disease.
CONTRAINDICATIONS
These are some of the relative contraindications:
 Asthma.
 Increased intraocular glaucoma. pressure, e.g. Compromised CVS, renal or hepatic function.
ADVERSE EFFECTS:
It is generally a safe drug and has few adverse effects:
 Nausea, vomiting and fever
 Placental abruption and scar dehiscence due to uterine hyperstimulation may sometimes occur if
drug is inappropriately introduced high up beyond internal Os of cervix.
DRUGINTERACTIONS:
Dinoprostone may increase activity of oxytocin, therefore both should not be used concomitantly. After
intracervical gel instillation, oxytocin infusion should only be started after atleast 6-8 hours.
DOSAGE AND PREPARATIONS:
Dinoprostone is available in many preparations. It is available as gel for both intracervical and intravaginal
use, vaginal tablets (pessary, suppositories) and vaginal inserts.
Intracervical gel: This 0.5 mg dinoprostone is available in 2.5 mL base in prefilled syringe.
The dose may be repeated every 6 hours to a maximum of 3 doses in 24 hours.6
METHOD OF INSTILLATION:
It should be confirmed that the patient is not febrile, there is no active vaginal bleeding and FHR pattern is
reassuring. The fetal heart rate and uterine activity should be closely monitored 15-30 min before and 30-
120 min after instillation of dinoprostone. Gel should be inserted below the internal Os, in the cervical canal,
either blindly or under visualization with speculum. Patient should remain recumbent for 30 minutes after
PGE2 gel instillation.
Preparations: Cerviprime gel, dinoripe gel-all contain 0.5 mg dinoprostone.
Intravaginal gel: In cases of unfavorable cervix in primigravida, one application of 2 mg dinoprostone gel is
inserted into the vagina. A repeat dose of 2 mg can be used after 6 hours. Maximum of only 2 doses are
recommended.
Preparation: Prostin E2 contains 2 mg dinoprostone.
Intravaginal tablet: Vaginal tablet containing 3 mg dinoprostone is inserted followed by another tablet after
6-8 hours if necessary. Maximum dose of 6 mg can be given.
Preparation: Prostin E2 vaginal tablet contains 3 mg dinoprostone.
Intravaginal insert: It is a controlled-release prostaglandin E2 vaginal insert. It contains 10 mg
dinoprostone which is released slowly at rate of 0.3 mg per hour for 24 hours. Vaginal insert is a thin
polymeric wafer held within a polyester sac, with a long tail to allow easy removal. The patient is kept
recumbent for 2 hours after insertion under strict FHR and 1 uterine activity monitoring. It is removed after
12 hours or with labor onset. It is used as a single dose and a single application
It is approved and available for use in USA, Canada and Europe.
Preparation: Cervidil dinoprostone. contains 10 mg
Stempel et al. conducted a randomized trial for comparing efficacy and safety of intracervical versus
intravaginal gel for preinduction cervical ripening and found intravaginal gel to be more favorable as
compared to intracervical gel.
STORAGE/STABILITY: Dinoprostone gel is stored in refrigerator at 36°-46°F. Suppository is stored in

freezer below -4°F and inserts between -4° and -14°F. Inserts are stable for a period of 3 years when stored
in a freezer.
MONITORING: The fetal heart rate and uterine activity should be closely monitored 15-30 minutes before
and 30-120 minutes after instillation of dinoprostone.
SAFETY DURING PREGNANCY: It a FDA category C drug. It is used only when termination of
pregnancy is indicated. It is not used during lactation.
NURSING RESPONSIBILTY:-
BEFORE:-
 Explain the process.
 Before administering the medication, the nurse must evaluate, confirm, and apply critical thinking
skills to the pharmaceutical order.
 The patients medication, the clients position and health in terms of contraindications, pertinent test
results, relevant information including vital sign, client allergies, and potential drug interactions
should be documented.
 Observe and exercise appropriate precautions for handling, preparation, administration, and disposal
of hazardous drugs.
 Use double chemotherapy gloves and a protective gown.
 Eye/ face and respiratory protection may be needed during preparation and administration.
DURING
 The vaginal insert must be kept frozen until it is time to use it. Do not thaw it up first.
 Securely place the vaginal insert between the middle and index fingers.
 Immediately after removing the insert from the packaging, place it transversely in the posterior
fornix of the vagina.
 Without a retrieval system, do not use.
 To prevent the vaginal insert from shifting from its ideal position, tuck part of the surplus retrieval
system into the vagina. Leave a little portion of the retrieval system outside the vagina to facilitate
retrieval.
 Following insertion, the patient should stay in a supine position for 2 hours, after that, they may
become mobile.
 Removal: pull the tape slowly from the vagina to remove the vaginal implant.
 Once said, throw the vaginal insert away.
AFTER
 Monitor the vital sign.
 Monitor signs symptoms of anaphylaxis, such as skin reaction or pulmonary symptoms (such as
pressure in the chest, coughing or dyspnea).
OXYTOCIN
INTRODUCTION:-
Oxytocin is a nonapeptide. It is synthesized in the supraoptic and paraventricular nuclei of the
hypothalamus. By nerve axons it is transported from the hypothalamus pituitary where it is stored and
eventually released. to the posterior.
Oxytocin has a half-life of 3-4 minutes and a duration of action of approximately 20 minutes, It is rapidly
metabolized and degraded by oxytоставе
Trade names: Pitocin, Syntocin Available dose: 5 units 1 ampulc
Action: Initiates myometrial contractions
MODE OF ACTION:
Myometrial oxytocin receptor concentration increases maximum (100-200 fold) during labor Oxytocin acts
through receptor and voltage-mediated calcium channels to initiate myometrial pontractions
It stimialates amniotic and decidual prostaglandin production. Beund intracellular calcium is eventually
mobdized from the sarcoplasmic reticulum to activate the contractile protein. The aterine commenons are
physiological, Le. causing l'andal contraction with relaxation of the zervis.
PREPARATIONS USED:
(i) Synthetic oxytocin (Syntocinon Sandoz or Pitocin-Parke-Davis) is widely used. It has only got oxytocie
effect without any vasopressor action.The Sentocinon a available in ampoules containing 5 IU/ml Pitocm 5
U
(ii) Syntometrine (Sandez) A combination of syntocinon 5 units and ergometrine 0.5 mg. (1) Desamuno-
oxytocin It is not machvated by oxytocinase and is 50-100 more effective than oxytocin. It is used as buccal
tablets containing 50 IU.
(iv) Oxytocin nasal solution contains 40 units/ml.
EFFECTIVENESS:
In the first trimester, the uterus is almost refractory in oxytocin. is the second trimester, relative refl
refractoriness persists, and, as such, oxytocin can only supplement other abortifacient agents in induction of
abortion. In later months of pregnancy and during labor in purticular, it is highly sensitive to oxytocin even
in small doses.
Oxytocin loses its effectiveness unless preserved at the correct temperature (hetween 2°C and 8°C)
INDICATIONS:
conveniently used in pregnancy, labor or puerperinm The indications are grouped as follows:
Oxytocin may be
Therapeutic:
 Pregnancy
 Labor
 Puerperium
 Pregnancy Early
THERAPEUTIC:
 Diagnostic:
o To accelerate abortion inevitable or missed and to expedite expulsion of hydatidiform
mole To stop bleeding following evacuation of the uterus
o Used as an adjunct to induction of abortion along with other abortifacient agents
(PGEL of PGE2)
 Late:
o To induce labor
o To ripen the cervix before induction.
o Augmentation of laber.
o Uterine inertia
 Labor
o Inactive management of third stage of labor
o Following expulsion of placenta as an alternative to crgometrine
 Puerperium:
To munimize blood loss and to control postpartum hemorrhage.
DIAG NOSTIC:
 Contraction stress test: To assess the foetal wellbeing during pregnancy I m/min which is stepped
up at interval of 20 mimites until effective uterine contractions established.
 Oxytocin sensitivity test: To assess the irritability of sdcrus following administration of oxytocin.
0.01 units of oxytocin is injected intravenously at the end of spontaneous uterine contrachons, at one
minnate intervals until an induced contraction starts.
SIDE EF FFECTS:
Maternal
 Uterine hyperstimulation
 Water intoxication.
 Antidiuresis
 Reflex tachycardia
 Rhinorrhoea
 Uterine bleeding
 Spasm
 Uterine rupture
 Hypotension
 Transient hypotension
 Nasal irritation
 Lachrymation (following nasal admin)
 Hypertonicity
 Nausesa
 Vomiting
Foetal
 Foetal hypoxia
 Retinal haemorrhage
 Foetal death
 Jaundice
 Arrhythmias
 Bradycardia
 Foetal distress
 Seizure
 Low Apgar score
Contracted pelvis
Inco-ordinate uterine contractions
CONTRAINDICATIONS:
 Grand maltipara
 Contracted pelvis
 Inco-ordinate uterine contractions
 History of caesarean section
 Obstructed labour
 Malpresentation
 Foetal distress
 Hypovolemic state
 Contraindicated vaginal delivery (Cardiac diseases, Invasive cervical cancer, Active genital herpes,
Prolapse of the cord, Cord presentation. Total placenta previa or Vasa previa)
 Severe pre-eclamptic toxaemia
DANGERS OF OXYTOCIN:
The dangers are particularly noticed when the drug is administered late in pregnancy or during labor.
Maternal
i. Uterine hyperstimulation (overactivity)-is a frequently observed side effect. There may be
excessive duration of r nterine contraction (hypertonia) 1 or increased frequency 6 in 10 min tame)
of contractions (polysystole). It is often associated with abnorinal FHR pattern.
ii. Uterine rupture-may be seen with violent uterine contraction common. High-risk cases are: grand
multipara, malpresentation, contracted pelvis, prior uterine scar (hysterotomy) and excessive
oxytocin use.
iii. Water intoxication is due to its antidiuretic function when used in high dose (30 40 mlU/min),
Water intexication is mansfested by hyponatremia, confusion, coma, convulsions, congestive cardiac
failure and death. It is prevented by strict fhuid intake and output record, use of salt solution and by
avoiding high dose oxytocin fat a long time.
iv. Hypotension. Bolus IV injections of oxytocin cuuse hypotension especially when patient is
hypovolemic or with a heart disense. Occasionally oxytocin may produce anginal pain
v. Antidiuresis: Antidiuretic effect is observed when exytocin infiacion rate is high 140- 50 mlU/min)
and continued for a long time
FETAL:
Fetal distress, fetal hypoxin or even fetal deuth may occur due to uterine hyperstimulation Uterine
hypertonis or polysystole causes reduced placented blood flow.
ROUTES OF ADMINISTRATION
 Controlled intravenous infusion is the widely used method.
 Bolus IV or IM-5-10 units after the birth of the baby as an alternative to ergometrine
 Intramuscular the preparation used is syndometrine
 Puccal tablets or nasal spray Limited use on trial basis.
METHODS OF ADMINISTRATION OF OXYTOCIN:

Controlled intravenous infusion Intramuscular
Controlled Intravenous Infusion:
Oxytocin infusion should be ideally by infusion pump. Fluid load should be minimum. It is started at low
dose rates (1-2 mlU/min) and increased gradually.
For induction of labor
PRINCIPLES:
Because of safery, the oxytocin should be started with a low dose and is escalated at an interval of 20-30
minutes where there is no response, When the optimal response is achieved (uterine contraction sustained
for about 45 seconds and numbering 3 contractions in 10 minutes), the administration of the particular
concentration in mlU/minute is to be continued. This is called oxytocin titration technique.
The objective of oxytocin administration is not only to initiate effective uterine contractions but also to
maintain the normal pattern of uterine activity till delivery and at least 30-60 minutes beyond that.
Calculation of the infused dose:-
Nowadays the infusion is expressed in terms of milliunits per minute. This can give an accurate idea about
the exact amount administered per minute irrespective of the concentration of the solution.
Regulation of the drip:
The drip is regulated by-
(1) Manually, counting the drops per minute commonly practiced
(2) oxytocin infution pump which automatically controls the amount of fluid to be infused.
Convenient regime:
Because of wide variation in response, It is a sound practice to start with a low dose (1-2 mIU/min) and
to escalate by 1-2 mIU/min at every 20 min intervals up to 8 mIU/min. The patient should preferably lie
on venacaval corupression.
High-dose oxytocin begins with 4 mlU/min and increased 4 mlU/min at every 20-30 min interval. It is
mainly used for augmentation of labor and in active management of labor. Risks of uterine hyperstimulation
and fetal heart irregularities. with high-dose regime.
In majority of cases a dose of less than 16 mlU/min (2 units in 500 ml. Ringer solution with drop rate of 60
minute) is enough to achieve the objective. Conditions where fluid overload is to be avoided, Infusion with
high concentration and reduced drop rate is preferred
For augmentation of labor
Oxytocin infusion is used during labor in userine inertia or fise augmentation of labor or in the active
managment of labor. The procedure consists of low riture of the membranes followed by oxytocin influsion
when the liquor is clear, Fetopelvic disproportion must be ruled out beforehand.
Indications of stopping the infusion

1. Nature of uterine contractions
 Abnormal uterine contractions occurring frequently (every 2 minutes or less) hyperstimulation) or
polysystole lasting more than 60 sec
 Increased tonus in between contractions
2. Evidences of fetal distress
3. Appearance of untoward maternal symptoms
NURSE'S RESPONSIBILITIES:
1. Maintain the rate of flow of infusion according to the uterine response, to avoid hyper stimulation
2. Uterine contractions number of contractions per 10 min dilution of contraction and period of
relaxation are noted.
3. Peak intrauterine pressure should be monitored by using intrauterine pressure monitor. Peak
intrauterine pressure of 50-60 min 11g with a resting tone 10-15 mm Hg is optimize when
intrauterine pressure monitoring is used.
4. FHR monitoring should be done by auscultation at every 15 minutes interval or by continuous
electronic foetal monitoring.
5. Assessment of progress of labour should be done (descent of the bead and rate of cervical dilatation)
6. Help the client to use breathing exercises to manage her contractions (pain).
7. After achieving the adequate number of contractions, Oxytocin infusion should he
8. maintained in a slow (<10 drops) Rate of flow of infusion by counting the drops per minutes on
monitoring the pamp.
PROGESTERONES
INTRODUCTION (PRETERM LABOR)
Progesterone is used in prevention of preterm labor as it causes uterine muscle quiescence.
Pharmacology:-
Progesterone has been extensively studied and found to act at various levels detailed below.
Myometrium and cervix:- progesterone differentially regulates expression of 2 major isoform viz
progesterone receptor (PR)-A and PR-B. at term, there is alteration of PR-/PR-B ratio that favors
myometrial contractility and cervical effacement. It also alters the expression of PR coactivators and histone
acetylation within myometrial cells, which are key regulators of myometrial contractility. Further it
interferes with oxytocin binding and signaling in a nongenomic fashion by binding with transmembrane
oxytocin receptors.
Placenta : it interferes with cortisol- mediated regulation of placental gene expression. The most important
result of this is increase in corticotrophin releasing hormones (CRH) which thereby regulate the timing of
labor.
Amniotic fluid:- it increase endogenous inhibitor of phospholipase A2 thereby decreasing the availability of
arachidonic acid which ultimately leads to decreased production of prostaglandin.
The half of vaginal progesterone is 13 hours. It has high bioavailability.
The half-life of injectable 17-HPC is 7 days.
INDICATION:-
Women with previous history of preterm delivery.
Asymptomatic women with short cervical length of less than 16 mm in routine ultrasound done in 2 nd
trimester between 20-24 weeks.
CONTRAINDICATION :-
 Current or past history of thrombophlebitis, thromboembolic disorder or cerebral apoplexy.
 Liver dysfunction or disease.
 Known or suspected malignancy of breast or genital organs.
DOSAGE:-
In case of prior spontaneous preterm birth, injection 17-hydroxyprogesterone caproate 250 mg IM is given
weekly from 16-20 weeks through 36 weeks.
In patients with short cervical length, progesterone suppository of 90-200 mg vaginally is advised since
diagnosis through 36 weeks.
ADVERSE DRUG REACTION
Common side effects include fatigue, headache, malaise.
PREPARATION:-
Micronized progesterone that can be used either orally or intravaginally ( preparations nidagen, susten,
endogest, wisrone).
Injectable 17- hydroxyprogestrone caproate (HPC) (injection proluton depot, HPC depot, proguard,
uniprogestin depot 250 or 500 mg).
Progesterone is not recommended in multiple gestation as it neither prolongs gestation as it neither prolongs
gestation as it neither prolongs gestation nor improves perinatal outcome.
MENOPAUSE
Menopause occurs due to cessation of ovarian function and consequent decline in its hormonal secretion.
The usual age for menopause is around 50-51 years. Thus, with growing life expectancy a woman is
expected to spend about one third of her life in menopausal state.
Though menopause is a physiological event, a woman at this stage of life often manifests symptoms that
occur due to cessation of ovarian hormone secretion particularly estrogen. The postmenopausal symptoms
mainly comprise of vasomotor symptoms (hot flashes) and clinical manifestation of urogenital atrophy. The
other important issue is that of osteoporosis which E is not manifest clinically but makes the bones ( fragile
and prone to fractures on minimal a trauma. Aging related other problems also need to be dealt with in
postmenopausal women.
Rh (D) IMMUNOGLOBULIN)
INTRODUCTION
Brand Name- Hyperrho, Micrhogram, Rhogam, Ohophylac, Winrho
Generic Name- Human Rho (D) Immune Globulin
Human Rho(D) immune globulin is a solution of antibodies used to prevent isoimmunization of Rho(D)
negative patients exposed to Rho(D) positive blood in pregnancy or transfusion.
INDICATION
 Indicated for suppression of rhesus (Rh) isoimmunization in nonsensitized Rho (D)-negative women
with an Rh-incompatible pregnancy, or in Rho (D)-negative individuals transfused with Rho(D)-
positive red blood cells (RBCs) or blood components containing Rho(D)-positive RBCs.
 Also indicated in Rho(D)-positive, non-splenectomized adult patients with chronic immune
thrombocytopenic purpura (ITP) to raise platelet counts.
PHARMACODYNAMICS
 15000 international unit (IU) contains sufficient anti-Rho (D) to effectively suppress the immunizing
potential of approximately 17mL of Rho (D) (D- positive) red blood cells.
 Human Rho(D) immune globulin therapy prevents immunization to Rho (D)- positive red blood cells
(RBC) by inducing antibody-mediated immunosuppression (AMIS) effectively clearing Rho-positive
RBCs by rapidly binding to them.
 This prevents Rho-negative mothers to produce alloantibodies to paternally inherited RhD antigen
expressed on fetal erythrocytes and cause haemolytic diseases of the newborn. Rho immune globulin
increase platelet into and reduce bleeding in Rho-positive with ITP by inhibiting autoantibody-
mediated platelet clearance.
MECHANISM OF ACTION
 The mechanism of action of Rho(D) immune globulin therapy is unclear.
 It is suggested that Rho immune globulin predominantly prevents the antibody response during
incompatible pregnancy by accelerating the phagocytosis of RBC's and clearance from the
circulation before the recognition by the immune system.
 IgG-opsonized RBCs may interact with activating IgG receptors (FcyRs) on effector cells and elicit
phagocytosis via mononuclear phagocytic system, primarily by macrophages.
 IgG may also stimulate complement activation on the RBC surface, followed by RBC lysis or
complement receptor-mediated phagocytosis but to smaller extent.
ABSORPTION
In patients undergoing therapy for Rh isoimmunization suppression, Rho(D) immune globulin titers were
detected in all women up to at least 9 weeks following either intravenous or intramuscular administration.
Following intravenous administration of a single 1500 IU (300 mcg) dose, peak serum levels of Rho(D)
immune globulin ranged from 62 to 84 ng/mL after first day. The levels ranged from 7 to 46 ng/mL and
were achieved between 2 and 7 days following intramuscular injection. The absolute bioavailability
achieved following IM administration is 69%.
NURSING CONSIDERATIONS
 Patient with immunoglobulin A deficiency may develop immunoglobulin A antibodies and have
anaphylactic reaction prescribe must high benefit of treatment against risk of hypersensitivity
reaction before giving.
 Obtain history of alleries and reaction to immunization keep epinephrine 1:1000 ready to treat
anaphylaxis.
 Immediately after delivery send a sample of neonates cord blood to laboratory for testing and cross
matching confirm if mother is Rho(D) OR Dpositive.
 This immune serum provides passive fetal blood during pregnancy and prevents formation of
maternal antibody which would indanger future.
 Postpan volination with live virus vaccine for 3 months after administration or Rho(D) Ig.
ANTICOAGULANTS
HEPARIN SODIUM
Heparin, also known unfractionated heparin, is a medication and naturally occurring glycosaminoglycan. As
a medication it is used as an anticoagulant. Specifically it is also used in the pregnancy, treatment of heart
attacks and unstable angina. It is given by injection into a vein or under the skin.
Mechanism of Action
Heparin binds to the enzyme inhibitor antithrombin III (AT), causing a conformational change that result
activation through increase in the flexibility of its reactive site loop. The activated AT then inactivates
thrombin, factor Xa and other proteases. Prevents canversion of fibrinogen to fibrin.
INDICATIONS
 Deep vein thrombosis.
 Theomboembolism
 Disseminated intravascular coagulation
 Patients with prosthetic valves in the heart.
CONTRAINDICATION
 An increased risk of a clot forming during pregnancy or after birth
 Recurrent thrombosis.
DOSAGE AND ROUTE
 Parentally: Initially 5,000 7,000 IU to be administered as IV push
 In case of failure of initial dose by 2,500 units subcutaneously every 24 hours
SIDE EFFECTS
 Leukopenin
 Thrombocytopenia
 Osteoporosis
 Hemorrhage
 Alopecia
Assess
 Blood studies: Hematocrit, platelets, occult blood in stools, Partial prothrombin time
 Blood pressure: Signs of hypertension.
Administer
 At same time, each day to maintain steady blood level.
 Avoid all IM injections that may cause bleeding.
Evaluate
 Therapeutic response: Decrease of deep vein thrombosis
 Bleeding gums, petechiae, ecchymosis, black tarry stools, hematuria
 Fever, skin rash urticaria
Teach Patient Family
 To avoid use of drugs unless prescribed by physician
 To use soft bristle toothbrush to avoid bleeding gums
 To comply with instructions
 To recognize and to sign of bleeding-gums, under skin, urine, stool.
WARFARIN SODIUM (COUMADIN)
Warfarin is an anticoagulant (Blood thinner) Warfarin reduces the formation of blood clots. Warfarin is used
to treat or prevent blood clot in veins or arteries, which can reduce the risk of stroke, heart attack, or other
serious conditions.
MECHANISM OF ACTION
Interferes with blood clotting by indirect means-depresses hepatic synthesis of stumia K dependent
coagulation factors (II, VII, IX, XI).
INDICATIONS
 Deep vein thrombosis.
 Pulmonary embolism.
CONTRAINDICATION
 Recent brain, eye, or spinal cord injury or surgery.
 Severe liver or kidney disease
 Uncontrolled hypertension
 Creuses placenta and may cause fatal hemorrhage in the fetus.
DOSAGE AND ROUTE

 Tablets: 10 to 15 mg orally daily fir 3 days,
 Followed by 2-10 mg at the same time each day depending upon the prothrombin time.
SIDE EFFECTS
Mother
 Hemorrhage.
 Optic atrophy
Fetus
 Fetal Skeletal and facial
 deformities
 Microcephaly
 Allergic reactions
 Liver problems
 Low blood pressure
 Swelling
 Low red blood cells
 Pileness
 Fever
PHARMACOKINETICS
 Absorption: Completely from the GI tract.
 Metabolism: liver
 Excretion 80% the total dose is excreted in the wine with the remaining 20% appearing in the feces.
 Blood studies: Hematocrit, platelets, occult blood in stools
 Prothrombin time BP: Watch for signs of hypertension.
Administer
 At same time, each day to maintain steady blood levels.
 Alone do not give with food.
 Avoid all IM infections that may cause bleeding,
Perform/Provide
 Storage in tight container.
Evaluate
 Therapeutic response: Decrease of deep vein thoumbosis
 Bleeding gums, perechine, ecchymosis, black tarry stools, hematuria, fever, skin rashes, urticaria.
Teach Patient/Family
 To avoid over the counter (OTC) preparations unless prescribed by physician.
 Drug may be held during menstruation.
 To use soft-bristle booth brush Stress client compliance.
 To report any sign of bleeding.
HEPARINE
Introduction :Heparin, also known as unfractionated heparin (UFH), is a medication and naturally
occurring glycosaminoglycan.Heparin is a blood anticoagulant that increases the activity of antithrombin.It
is used in the treatment of heart attacks and unstable angina. It can be given intravenously or by injection
under the skin. Its anticoagulant properties make it useful to prevent blood clotting in blood specimen test
tubes and kidney dialysis machines.
Pharmacological classification: anti coagulants
Pharmacological name: unfractionated heparin

Therapeutic Action:decrease the clotting ability of the blood and help prevent harmful clots from forming
in blood vessels.
Availability :Heparin is available in vials at strengths of 1000, 5000, 10,000 and 20,000 units per ml.
Indication:
 Hemorrhage
 Heparin-Induced Thrombocytopenia and Heparin-Induced Thrombocytopenia with
Thrombosis
 Thrombocytopenia
 Heparin Resistance
 Hypersensitivity
 Hyperkalemia
 Elevations of Serum Aminotransferase
Route :intravenous
Dose : as prescribed by physcian
Contraindication :
 The platelet count is 100,000/mm or lower.

 The patient cannot have routine monitoring tests performed to monitor therapeutic heparin.
 The patient has an active, uncontrollable bleed except for disseminated intravascular coagulation
(DIC).
 Patients with a history of heparin-induced thrombocytopenia should also avoid heparin use.
Mechanism of action :
once administered

heparin binds to several proteins; however, it is binding to an antithrombin that is important,

as this causes a surface change and inactivates thrombin. Binding to antithrombin blocks several different
factors of the clotting cascade, but two are predominant: thrombin (Factor IIa) and Factor Xa. By
inactivating thrombin,

it blocks the conversion of fibrinogen to fibrin; this prevents the formation of clots and prolongs the clotting
time of blood.

Heparin does not affect bleeding time, but it does prolong the time that blood takes to clot.
Pharmacokinetics :
Absorption
Heparin is not absorbed through the gastrointestinal tract and therefore administered via parenteral route. Peak plasma
concentration and the onset of action are achieved immediately after intravenous administration.
Distribution
Heparin is highly bound to antithrombin, fibrinogens, globulins, serum proteases and lipoproteins. The volume of
distribution is 0.07 L/kg.
Elimination
Metabolism
Heparin does not undergo enzymatic degradation.
Excretion
Heparin is mainly cleared from the circulation by liver and reticuloendothelial cells mediated uptake into extravascular
space. Heparin undergoes biphasic clearance, a) rapid saturable clearance (zero order process due to binding to proteins,
endothelial cells and macrophages) and b) slower first order elimination. Low doses of heparin are cleared mostly by a
saturable, rapid, zero-order process. Slower first order elimination usually occurs with very high doses of heparin and is
dependent on renal function. The plasma half-life is dose-dependent, and it ranges from 0.5 to 2 h.
Nursing implication :
 Review patient allergies.

 Review and reconcile prescribed medications.
 Identify possible adverse effects of medications.
 Identify potential interactions with other medications.
 Determine route of administration.
 Determine time of administration.
 Develop patient education regarding medication administration.
 terbutaline and benzphetamine both increase sympathetic (adrenergic) effects, including increased
blood pressure and heart rate.
 Liver damage and haemopoietic disorders have been associated with phenytoin therefore baseline
liver function tests and full blood count should be taken when commencing phenytoin treatment.
 if patient is on an anticoagulant, you need to watch for signs of bleeding and bruising.
 If patient is on an antibiotic, you need to watch for signs of allergic reactions.
 Do not stop taking the anti-inflammatory medicine even if your asthma seems better, unless you are
told to do so by your doctor.
PHENETOIN
Introduction : Phenytoin (PHT), sold under the brand name Dilantin among others, is an anti-seizure
medication. It is useful for the prevention of tonic- clonic seizures and partial seizures, but not absence
seizures. The intravenous form is used for status epilepticus that does not improve with benzodiazepines. It
may also be used for certain heart arrhythmias or neuropathic pain. It can be taken intravenously or by
mouth.
Pharmacological classification : anticonvulsants
Pharmacological name : phenytoin or phenytoin sodium.
Therapeutic action : decreasing abnormal electrical activity in the brain.
Availability :
capsule, immediate-release
 30mg
 100mg
capsule, extended-release
 100mg
 200mg
 300mg
tablet, chewable
 50mg
oral suspension
 125mg/5mL
injectable solution
 50mg/mL
Indication : epilepsy, generalized tonic-clonic seizures, complex partial seizures, and status epilepticus.
Route : The drug should be injected slowly intravenously at a rate not exceeding 1-3 mg/kg/min or 50 mg
per minute, oral.
Dose : Usual Adult Dose for Seizures:
oral Initial dose: 100 mg extended release orally 3 times a day.

Maintenance dose: 100 mg orally 3 to 4 times a day.
IV: Do not exceed the infusion rate of 50 mg/min.

Loading dose: 10 to 15 mg/kg IV slowly.
Maintenance dose: 100 mg IV every 6 to 8 hours.
Usual Adult Dose for Arrhythmias: Loading Dose:

1.25 mg/kg IV every 5 minutes. May repeat up to a loading dose of 15 mg/kg, or
250 mg orally 4 times a day for 1 day, then 250 mg twice daily for 2 days
Maintenance Dose:
300 to 400 mg/day orally in divided doses 1 to 4 times a day
Usual Adult Dose for Status Epilepticus:
Loading dose: Manufacturer recommends 10 to 15 mg/kg by slow IV administration
Maintenance dose: IV or Oral: 100 mg every 6 to 8 hours.
Usual Pediatric Dose for Seizures:
Status Epilepticus: Loading Dose:- Infants, Children: 15 to 20 mg/kg IV in a single or divided doses
Usual Pediatric Dose for Arrhythmias:
Greater than 1 year:

Loading Dose: 1.25 mg/kg IV every 5 minutes. May repeat up to a loading dose of 15 mg/kg.
Maintenance Dose: 5 to 10 mg/kg/day orally or IV in 2 to 3 divided doses
Mechanisam of action :
Phenytoin

Delays recovery of Na+ channels from inactivation

Blocks Na+ channels in activated state

Blocks high frequency firing

Stabilizes the neuronal membrane

Inhibits generation of action potentials

Inhibits spread of seizures

Antiepileptic activity
Adverse effect : Headaches, Feeling drowsy, sleepy or dizzy. As your body gets used to phenytoin, these
side effects should wear off, Feeling nervous, unsteady or shaky, Feeling or being sick (nausea or
vomiting) , Constipation. , Sore or swollen gums
Contraindication : hypersensitivity, bradycardia, heart blocks, hypoglycemia.
Pharmacokinetics :
Absorption : May vary between different manufacturers; dependent on formulation Onset: 1 week (PO); 2-
24 hr (PO with loading dose); 0.5-1 hr (IV)
Peak plasma time: 1.5-3 hr (immediate-release); 4-12 hr (extended-release)
Distribution - Protein bound: 95% (adults); 85% (infants); 80% (neonates) , 0.6-0.7 L/kg (adults); 0.7 L/kg
(children); 0.7-0.8 L/kg (infants); 0.8-0.9 L/kg (full-term neonate); 1-1.2 L/kg (premature neonate)
Metabolism - Metabolized by hepatic P450 enzyme CYP2C9
Excretion: Urine

 Monitor BP, ECG, and respiratory function continuously during administration of IV phenytoin
and throughout period when peak serum phenytoin levels occur (15–30 min after administration).
 Instruct patient to take phenytoin as directed, at the same time each day.
 May cause drowsiness or dizziness.
 Caution patient to avoid alcohol and CNS depressants.
PROMETHAZINE HYDROCHLORIDE
Introduction : it is a medication used to manage and treat allergic conditions, nausea and vomiting,
motion sickness, and sedation. Promethazine also has off-label uses for nausea and vomiting in pregnancy.
Promethazine is a phenothiazine derivative with antidopaminergic, antihistamine, and anticholinergic
properties.
Pharmacological classification : phenothiazines. first-generation antihistamine, antipsychotic,

sedative, and antiemetic
Pharmacological name : Phenergan Prorex Provigan Zipan.
Therapeutic action : central and peripheral dopaminergic blockade.
Availability : This medicine is only available with your doctor's prescription .This product is available in
the following dosage forms:
 Promethazine hydrochloride injection solution: 25 mg/mL; 50 mg/mL.
 Promethazine hydrochloride oral solution: 6.25 mg/5 mL.
 Promethazine hydrochloride suppository: 12.5 mg; 25 mg; 50 mg.
 Promethazine hydrochloride oral syrup: 6.25 mg/5 mL.
 Promethazine hydrochloride oral tablets: 12.5 mg, 25 mg, 50 mg
Indication :
 Allergic conditions: Promethazine is a first-generation antihistamine, and thus it is indicated for
various allergic conditions, including seasonal allergic rhinitis and allergic conjunctivitis,
uncomplicated skin manifestations of urticaria, and angioedema. Promethazine is also indicated as
adjunctive therapy to epinephrine for anaphylactic reactions.
 Nausea and vomiting: Phenothiazines such as promethazine have substantial antiemetic activity.
Clinicians use promethazine to control nausea and vomiting associated with anesthesia or
chemotherapy.Promethazine is commonly used postoperatively as an antiemetic. The antiemetic
activity increases with increased dosing; however, side effects also increase, often limiting maximal
dosing.
 Motion sickness: Promethazine can serve as prophylactic therapy for motion sickness; it is most
effective when given 30 minutes to 1 hour before the triggering event.
 Sedation: Promethazine can be used as adjunctive therapy with other analgesics to provide
preoperative, postoperative, or obstetric sedation.
Route : oral, rectal, intramuscular, and intravenous. .
Dose : For oral dosage form (tablets):
 For allergy symptoms:

 Adults and teenagers—12.5 milligrams (mg) before meals and at bedtime; or 25 mg at bedtime as
needed.
 Children 2 years of age and older—Your doctor will determine dose based on the weight and/or
size of the child. The dose is usually 6.25 to 12.5 mg three times a day; or 25 mg at bedtime as
needed.
 Children younger than 2 years of age—Use and dose must be determined by your doctor .
 For prevention of motion sickness:
 Adults and teenagers—25 mg twice daily; this initial dose should be taken one-half to one hour
before traveling. The dose may be repeated eight to twelve hours later if needed. On other days of
travel, 25 mg may be taken on arising and again before the evening meal.
size of the child. The dose is usually 12.5 to 25 mg one-half to one hour before traveling. The
dose may be repeated eight to twelve hours later if needed.
 For nausea and vomiting:
 Adults and teenagers—25 mg for the first dose, then 12.5 to 25 mg every four to six hours if
needed.
size of the child. The dose is usually 0.5 mg per pound of body weight (1.1 mg per kg) or 12.5 to
25 mg every four to six hours as needed.
 For sedation:
 Adults and teenagers—25 to 50 mg.
size of the child. The dose is usually 12.5 to 25 mg.
 For control of pain or anxiety before or after surgery:
 Adults and teenagers—50 mg the night before surgery; 25 to 50 mg after surgery.
size of the child. The dose is usually 0.5 mg per pound of body weight (1.1 mg per kg) or 12.5 to
25 mg the night before surgery or after the surgery.
Mechanisam of action :
Promethazine

Promethazine works as a direct antagonist at the mesolimbic dopamine receptors and alpha-
adrenergic receptors in the brain.

exhibits its antihistamine effects as an H1-receptor blocker.

Inhibits action of histamine

Antiemetic activity
Adverse effect :
 Convulsions (seizures)
 difficult or unusually fast breathing
 fast heartbeat or irregular pulse
 high fever
 high or low (irregular) blood pressure
 increased sweating
 loss of bladder control
 severe muscle stiffness
 unusually pale skin
 unusual tiredness or weakness
Contraindication :
Hypersensitivity : it is contraindicated in patients with hypersensitivity.
Pregnancy : Using promethazine late in pregnancy might increase the chance of slowed breathing
(respiratory depression) in newborns. It is important that your healthcare providers know you are taking
promethazine so that if respiratory depression happens your baby can get appropriate care.
Seizures: Promethazine should be used cautiously in patients with seizure disorders or in persons taking
concomitant medications, which may also lower seizure threshold (ie, narcotics, local anesthetics, etc).
Bone-Marrow Depression: Promethazine should be used cautiously in patients with bone marrow
depression (Leukopenia and agranulocytosis). The risk is higher when it is coadministered with other known
marrow-toxic agents.
Neuroleptic Malignant Syndrome: A potentially fatal NMS is reported in patients using promethazine
alone or combined with other antipsychotic drugs.
Pharmacokinetics :
Absorption : The absorption of promethazine from the gastrointestinal tract exceeds 80% in most subjects..
Distribution – The volume of distribution of promethazine is approximately 970L or 30L/kg. Promethazine

is 93% protein bound in serum, 5 mostly to albumin.
Metabolism - Minimal metabolism by the gastrointestinal mucosa is implicated
Excretion: 0.64% eliminated in the urine as the unchanged parent drug, 0.02-2.02% in the urine as
desmethylpromethazine, 10% in the urine as promethazine sulfoxide. The elimination half life of
promethazine is approximately 12-15h.

 Before taking promethazine, tell your doctor or pharmacist if you are allergic to it,
 Monitor BP, pulse, and respiratory rate frequently before anfd after, in patients receiving IV doses.
 Assess level of sedation after administration.
 Risk of sedation and respiratory depression are increased when administered concurrently with other
drugs that cause CNS depression.
 This drug may make you dizzy or drowsy or blur your vision. Alcohol or marijuana (cannabis) can
make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness or
clear vision until you can do it safely.
TERBTALIN
Introduction: Terbutaline belongs to the family of medicines known as bronchodilators. Bronchodilators

are medicines that relax the muscles in the bronchial tubes (air passages) of the lungs. They relieve cough,
wheezing, shortness of breath, and troubled breathing by increasing the flow of air through the bronchial
tubes.
Pharmacological classification:selective beta-2 adrenergic agonist
Pharmacological name:Bronclyn, Brethine, Bricanyl, Brethaire, Marex, and Terbulin.
Therapeutic Action: relaxing and opening the airways, making it easier to breathe.
Availability:capsule, immediate-release - 30mg100mg capsule, extended-release100mg200mg300mg,

Tablet - 50mg, oral suspension - 125mg/5mL, injectable solution -50mg/mL
Indication :epilepsy, generalized tonic-clonic seizures, complex partial seizures, and status epilepticus.
Route :The drug should be injected slowly intravenously at a rate not exceeding 1-3 mg/kg/min or 50 mg
per minute, oral.
dose: (adult)- 15-20 mg/kg , (child)- 5mg/kg/day
Mechanisam of action:
Terbutalin

Act on beta 2 adrenergic receptors

Increase cAMP levels results in relaxation of bronchial and smoothmucles

Wide air passage allows more air to flow in and out of lungs

Increase air flow and reduces shortness of breath
Adverse effect:Headaches, Feeling drowsy, sleepy or dizzy. As your body gets used to phenytoin, these
side effects should wear off, Feeling nervous, unsteady or shaky, Feeling or being sick (nausea or
vomiting) ,Constipation. , Sore or swollen gums
Contraindication :hypersensitivity, bradycardia, heart blocks, hypoglycemia.
Pharmacokinetics:
Absorption :In humans, around 45% of an oral dose is absorbed; peak bronchial effects occur within 2–3 h
and last approximately 8 h.
Distribution - Terbutaline has a mean volume of distribution of 1.6 L/kg.
Metabolism - Terbutaline is extensively metabolized to the glucuronic acid conjugate which is eliminated
via bile (40% of the dose) and urine (25% of the dose).
Excretion: more than 90% of a parenteral dose is eliminated in the urine.Less than 1% of the dose is
excreted in the bile.

 terbutaline and benzphetamine both increase sympathetic (adrenergic) effects, including increased
blood pressure and heart rate.
 if patient is on an anticoagulant, you need to watch for signs of bleeding and bruising.
 If patient is on an antibiotic, you need to watch for signs of allergic reactions.
 Do not stop taking the anti-inflammatory medicine even if your asthma seems better, unless you are
told to do so by your doctor.
NIFEDIPINE
INTRODUCTION
Nifedipine is a first generation calcium channel blocker used to treat hypertension and angina pectoris.
Nifedipine therapy is associated with a low rate of serum enzyme elevations and has been linked to several
instances of clinically apparent acute liver injury.
GENERIC NAME:- Nifedipine
TRADE NAME:- Adalat CC, Adalat XL, Nifedical XL, Procardia
CONTENT: Nifedipine
PHARMACOLOGICAL CLASSIFICATION THERAPEUTIC

THERAPEUTIC: Anti-hypertensive, Anti-hypertensive
PHARMACOLOGIC : - Calcium channel blocker , Antiarrhythmic , Vasodilator
PREGNANCY CATEGORY: C
MECHANISM OF ACTION
Inhibits the movement of calcium ions across the membranes of cardiac and arterial muscle cells,
inhibition of transmembrane calcium flow results in the depression of impulse formation in specialized
cardiac pacemaker cells,
in slowing of the velocity of the conduction of the cardiac muscle impulse,
in the depression of the of myocardial contractility and in the dilation of coronary arteries, arterioles.
These effects lead to decreased cardiac work, decreased cardiac energy consumption,
and increased delivery of oxygen to myocardial cells.
INDICATION
 Angina
 Hypertension
 Raynaud’s phenomenon . ( nifedipine is the mainstay of medical treatment ).
 Superventricular tachycardias, including atrial fibrillation.
 Ischemic neurological deficit after subarachnoid haemorrhage .
 Delay of preterm labour (prevent premature labour has been with nifedipine )
 Prophylaxis for cluster headache .
ROUTE / DOSE :-
 For oral dosage form (capsules):
 Adults-At first, 10 milligrams (mg) three times a day. Your doctor may increase your dose as
needed.
 Children-Use and dose must be determined by your doctor.
 For oral dosage form (extended-release tablets):
 Adults-At first, 30 or 60 milligrams (mg) once a day. Your doctor may increase your dose as needed.
However, the dose is usually not more than 90 mg once a day.
 Children-Use and dose must be determined by your doctor.
ADVERSE REACTION :-
CNS: headache, asthenia, dizziness, fatigue, nervousness, sleep disturbances.
CV: peripheral edema, angina, hypotension, arrhythmias, AV block, asystole
Dermatologic: Flushing, rash, pruritus, dermatitis
GI: nausea, Constipation, diarrhea, cramps, flatulence
OTHER: nasal congestion, cough, fever, chills, shortness of breath, muscle cramps
CONTRAINDICATION :-
Contraindicated in patients who are allergic to nifedipine.
PRECAUTION:
Use cautiously with patients who are lactating and pregnant.
PHARMECOKINETICS
NIFEDIPINE (PROCARDIA) PHARMACOKINETICS
Conventional Extended Release
Bioavailability: 40- 77% Bioavailability: 65- 89%
Onset: 20 minutes Onset: 30 minutes
Duration: 8 hours Duration: 24 hours
NIFEDIPINE (PROCARDIA) PHARMACOKINETICS
Metabolized by the liver by CYP3A4
Has a 2-7 hour half life
Excreted through the urine (60-80%) and feces (20-40%)

Usual dosage: 30-60 mg daily
NURSING RESPONSIBILITIES :-
Before:
 Assess the history of allergies to nifedipine and also pregnancy and lactation.
 teach significant others of the patient the common side effects of the drug and to report any severe
effects at once.
 Ensure that patient does not chew or divide sustained-release of tablet.
During:
 perform rights of medication.

 advise patient to drink medication as directed.
 Monitor patient's v/s and cardiac output carefully.
 Monitor BP carefully during titration period. Patient may become severely hypotensive, especially if
also taking other drugs known to lower BP. Withhold drug and notify physician if systolic BP <90.
 Monitor blood sugar in diabetic patients. Nifedipine has diabetogenic properties.
 Monitor for gingival hyperplasia and report promptly.
This is a rare but serious adverse effect (similar to phenytoin-induced hyperplasia).
After:
 advise patient not to take more than prescribed.

 document findings.
Patient & Family Education
 Inspect gums visually every day. Changes in gingivae may be gradual, and bleeding may be
exhibited only with probing.
 Seek prompt treatment for symptoms of gingival hyperplasia (easy bleeding of gingivae and gradual
enlarging of gingival mass, especially on buccal side of lower anterior teeth). Drug will be
discontinued if gingival hyperplasia occurs.
SODIUM NITROPRUSSIDE
Sodium Nitroprusside is approved for the treatment of acute hypertension, to induce controlled hypotension
to decrease postoperative bleeding, and to manage the acute heart failure.
GENERIC NAME :- nitroprusside
BRAND NAME :- Nipride , Nipride RTU, Nitropress
TRADE NAME :- Nipride , Nitropress
Sodium nitroprusside is a potent vasodilator commonly used in medical settings to manage acute
hypertensive crises and to reduce blood pressure during surgery. It is also utilized in the treatment of heart
failure and certain cases of pulmonary hypertension. Here are key points about sodium nitroprusside:
Chemical Properties
- Chemical Formula: Na2[Fe(CN)5NO]·2H2O
- Molecular Weight: 297.95 g/mol
- Appearance: Red crystalline powder
PHARMACOLOGICAL CLASSIFICATION
- Vasodilator: Specifically, a direct-acting vasodilator.
- Nitric Oxide Donor: Releases nitric oxide (NO), which is a key mediator in vasodilation.
- Antihypertensive Agent: Reduces systemic blood pressure.
THERAPEUTIC CLASSIFICATION
- Antihypertensive: Used for the rapid reduction of blood pressure in hypertensive emergencies.
- Heart Failure Therapy: Administered to decrease the workload on the heart in acute heart failure.
- Controlled Hypotensive Agent: Employed during surgical procedures to induce hypotension and minimize
bleeding.
MECHANISM OF ACTION
1. Release of Nitric Oxide (NO): Upon administration, sodium nitroprusside rapidly breaks down in the
bloodstream to release nitric oxide.
2. Activation of Guanylate Cyclase: Nitric oxide activates the enzyme guanylate cyclase in vascular smooth
muscle cells.
3. Increase in Cyclic GMP (cGMP): Activated guanylate cyclase catalyzes the conversion of guanosine
triphosphate (GTP) to cyclic guanosine monophosphate (cGMP).
4. Smooth Muscle Relaxation: Elevated levels of cGMP lead to a series of intracellular events that result in
the dephosphorylation of myosin light chains, reducing their interaction with actin. This process causes
relaxation of the smooth muscle cells in the vessel walls.
5. Vasodilation: The relaxation of vascular smooth muscles results in the dilation of both arteries and veins.
This reduces systemic vascular resistance (afterload) and venous return (preload).
6. Reduction in Blood Pressure: The overall effect is a significant reduction in blood pressure due to
decreased peripheral resistance and venous pooling.
AVAILABILITY
Sodium nitroprusside is available in the following forms and strengths:
Formulation
- Injectable Solution: Sodium nitroprusside is typically supplied as a lyophilized powder that needs to be
reconstituted with a suitable solvent (usually sterile water for injection) before intravenous administration.
Concentration
- Common Concentration: 50 mg per vial. Once reconstituted, it is diluted further in a suitable intravenous
fluid (e.g., 5% dextrose) before administration.
Packaging
- Vials: The reconstituted solution must be protected from light and used promptly to maintain its potency
and safety.
Storage
- Storage Conditions: Unopened vials should be stored at room temperature and protected from light. The
reconstituted solution should be used within a specific timeframe, typically within 24 hours, and also
protected from light.
INDICATION
Primary Indications
1. Hypertensive Emergencies: Rapid reduction of blood pressure in acute hypertensive crises where
immediate intervention is necessary to prevent organ damage.
2. Controlled Hypotension During Surgery: Induction of hypotension to decrease bleeding during surgical
procedures, facilitating a clearer surgical field.
3. Acute Heart Failure: Management of acute congestive heart failure to reduce cardiac workload by
decreasing both preload and afterload, improving cardiac output and reducing symptoms.
Other Indications
4. Hypertensive Encephalopathy: When severe hypertension leads to cerebral edema and encephalopathy,
sodium nitroprusside can help quickly lower blood pressure to prevent further neurological damage.
5. Aortic Dissection: Used in conjunction with beta-blockers to rapidly lower blood pressure and reduce the
shear stress on the aortic wall.
ROUTE OF ADMINISTRATION
- Intravenous (IV): Sodium nitroprusside is administered exclusively via intravenous infusion. Due to its
potency and the need for rapid titration, it is given through a controlled IV infusion, typically using an
infusion pump.
DOSAGE
The dosage of sodium nitroprusside must be individualized based on the patient's response and the clinical
situation. Here are general guidelines:
1. Starting Dose:
- Typically, the infusion is started at 0.3 mcg/kg/min.
2. Titration:
- The dose can be titrated in increments of 0.5 mcg/kg/min every few minutes based on the desired blood
pressure response. Adjustments should be made cautiously to avoid excessive hypotension.
3. Maximum Dose:
- The maximum recommended infusion rate is 10 mcg/kg/min. However, this high dose should not be
maintained for more than 10 minutes to avoid the risk of cyanide toxicity.
4. Maintenance Dose:
- Once the desired blood pressure reduction is achieved, the infusion rate is typically adjusted to the lowest
effective dose that maintains stable blood pressure.
ADMINISTRATION CONSIDERATIONS
- Continuous Monitoring: Patients receiving sodium nitroprusside require continuous blood pressure
monitoring, ideally with intra-arterial pressure measurements.
- Light Protection: The solution must be protected from light at all times to prevent degradation.
- Short Duration of Use: Because of the risk of cyanide toxicity, prolonged use (over 24-48 hours) should
be avoided if possible, and alternative antihypertensive therapies should be considered for long-term
management.
ADVERSE REACTION
Common Adverse Reactions

1. Hypotension: Excessive blood pressure reduction can occur, leading to symptoms such as dizziness,
lightheadedness, or fainting.
2. Reflex Tachycardia: A compensatory increase in heart rate may occur in response to the sudden drop in
blood pressure.
3. Headache: Due to vasodilation of cerebral vessels.
Serious Adverse Reactions

1. Cyanide Toxicity: Prolonged infusion or high doses of sodium nitroprusside can lead to the accumulation
of cyanide, a byproduct of its metabolism. Symptoms of cyanide toxicity include:
- Metabolic acidosis
- Confusion or altered mental status
- Seizures
- Cardiac arrhythmias
- Lactic acidosis
- Coma and potentially death if untreated
2. Thiocyanate Toxicity: Cyanide is metabolized to thiocyanate, which can accumulate, especially in

patients with renal impairment. Symptoms of thiocyanate toxicity include:
- Weakness
- Disorientation
- Muscle spasms
- Tinnitus
- Nausea and vomiting
3. Methemoglobinemia: Elevated levels of methemoglobin can impair the ability of blood to carry oxygen,
leading to hypoxia. Symptoms include:
- Cyanosis (bluish discoloration of the skin)
- Shortness of breath
- Fatigue
- Confusion
Other Adverse Reactions

- Nausea and Vomiting: Gastrointestinal upset can occur with rapid blood pressure changes.
- Flushing: Due to vasodilation.
- Sweating: Excessive sweating can occur as a result of vasodilation and hypotension.
CONTRAINDICATIONS
ABSOLUTE CONTRAINDICATIONS
1. Severe Hypotension: Patients with very low blood pressure should not receive sodium nitroprusside as it
can further lower blood pressure to dangerous levels.
2. Compensatory Hypertension: Situations where high blood pressure is compensating for a critical
condition, such as in patients with an arteriovenous shunt or severe aortic stenosis.
3. Leber's Hereditary Optic Neuropathy: Patients with this condition are at increased risk of cyanide toxicity.
4. Tobacco Amblyopia: Patients with tobacco amblyopia (a condition associated with vision loss due to
toxic optic neuropathy) should not use sodium nitroprusside because they are at a higher risk of cyanide
toxicity.
RELATIVE CONTRAINDICATIONS
1. Renal Impairment: Caution is required in patients with renal dysfunction due to the increased risk of
thiocyanate accumulation and toxicity. Frequent monitoring of thiocyanate levels is necessary if use is
unavoidable.
2. Liver Impairment: Reduced hepatic function can impair the metabolism of cyanide to thiocyanate,
increasing the risk of cyanide toxicity.
3. Pregnancy and Breastfeeding: Sodium nitroprusside should be used during pregnancy only if the potential
benefit justifies the potential risk to the fetus. It should be used with caution in breastfeeding women due to
the potential risk to the infant.
4. Vitamin B12 Deficiency: Patients with low levels of vitamin B12 are at higher risk of cyanide toxicity as
vitamin B12 is required for the detoxification of cyanide.
OTHER CONSIDERATIONS
- Head Trauma or Cerebral Hemorrhage: Sodium nitroprusside should be used with caution in these patients
because of the risk of increasing intracranial pressure.
- Acute Heart Failure due to Mechanical Obstruction: For example, in cases of pericardial tamponade or
severe valvular stenosis, sodium nitroprusside may worsen hemodynamic status.
Given these contraindications and the drug's potent effects, the use of sodium nitroprusside should be
carefully considered and closely monitored by healthcare professionals.
The pharmacokinetics of sodium nitroprusside involve its absorption, distribution, metabolism, and
excretion, which are critical for understanding its onset of action and duration of effect.
ABSORPTION
- Intravenous Administration: Sodium nitroprusside is administered intravenously, ensuring 100%
bioavailability. The drug acts rapidly, with an almost immediate onset of action.
DISTRIBUTION
- Plasma Distribution: It is rapidly distributed in the blood and quickly reaches its site of action in the
vascular smooth muscle.
- Volume of Distribution (Vd): The volume of distribution is relatively low since it stays predominantly
within the vascular compartment.
METABOLISM
- Nitric Oxide Release: In the bloodstream, sodium nitroprusside releases nitric oxide (NO), the active
moiety responsible for its vasodilatory effects.
- Cyanide Formation: As a byproduct, cyanide ions are produced, which are rapidly converted to thiocyanate
in the liver by the enzyme rhodanase, using sulfur donors from the body.
- Thiocyanate Metabolism: Thiocyanate is much less toxic than cyanide and is gradually excreted by the
kidneys.
EXCRETION
- Renal Excretion: Thiocyanate, the major metabolite, is eliminated primarily through the kidneys. The half-
life of thiocyanate is about 3-7 days in patients with normal renal function.
- Cyanide Excretion: Cyanide is also excreted in small amounts via the kidneys and can be detoxified by
conversion to less harmful substances such as thiocyanate.
PHARMACOKINETIC PARAMETERS
- Onset of Action: Immediate (within seconds to minutes) after intravenous administration.
- Duration of Action: The hypotensive effect dissipates quickly after the infusion is stopped, usually within
1-10 minutes, due to rapid distribution and metabolism.
- Half-Life: The half-life of sodium nitroprusside itself is very short (about 2 minutes), while the half-life of
thiocyanate can range from 3 to 7 days depending on renal function.
CLINICAL CONSIDERATIONS
- Rapid Onset and Offset: This rapid pharmacokinetic profile allows for tight control of blood pressure,
which is crucial during hypertensive emergencies and surgeries.
- Risk of Accumulation: Prolonged infusions can lead to the accumulation of cyanide and thiocyanate,
especially in patients with renal or hepatic impairment. Regular monitoring of blood cyanide and
thiocyanate levels is essential to prevent toxicity.
NURSING IMPLICATIONS
The administration of sodium nitroprusside requires careful monitoring and specific nursing interventions to
ensure patient safety and therapeutic effectiveness. Here are key nursing implications:
Monitoring and Assessment

1. Blood Pressure: Continuous monitoring of blood pressure is crucial. Use an arterial line for accurate and
real-time measurements.
2. Heart Rate: Monitor for reflex tachycardia or bradycardia.
3. Signs of Hypotension: Observe for symptoms such as dizziness, fainting, or altered mental status.
4. Cyanide and Thiocyanate Levels: Monitor these levels, especially in prolonged use or in patients with
renal or hepatic impairment.
5. Oxygenation: Monitor oxygen saturation and respiratory status, as severe hypotension can lead to
hypoxia.
Administration
1. Intravenous Infusion: Administer via an IV infusion pump for precise control of the infusion rate.
2. Protect from Light: Ensure the solution and infusion set are protected from light to prevent degradation.
3. Titrate Dose Carefully: Start at a low dose and titrate upwards based on blood pressure response,
avoiding rapid changes to prevent hypotension.
4. Emergency Equipment: Have resuscitation equipment readily available due to the risk of rapid blood
pressure changes.
Patient Education
1. Explain Procedure: Inform the patient about the purpose of the drug and the need for frequent blood
pressure monitoring.
2. Report Symptoms: Instruct the patient to immediately report symptoms of dizziness, headache, or chest
pain.
Safety Precautions
1. Frequent Assessment: Conduct frequent assessments of mental status, renal function, and overall
cardiovascular status.
2. Fluid Balance: Monitor input and output to assess for signs of fluid overload or deficit, especially in
heart failure patients.
3. Watch for Toxicity: Be vigilant for signs of cyanide or thiocyanate toxicity, such as confusion, metabolic
acidosis, or muscle spasms.
Coordination with Healthcare Team

1. Communicate Findings: Regularly update the healthcare team about the patient’s response to treatment
and any adverse effects.
2. Adjustments: Collaborate with the prescribing physician to adjust dosages as needed based on
monitoring results.
CAPTOPRIL
INTRODUCTION
Captopril is a medication widely used in the treatment of high blood pressure (hypertension) and heart
failure. It belongs to the class of drugs known as ACE inhibitors (Angiotensin-Converting Enzyme
inhibitors), which are pivotal in cardiovascular medicine. Since its introduction in the early 1980s, captopril
has become a cornerstone therapy for managing hypertension and heart failure, and for protecting kidney
function in patients with diabetes.
PHARMACOLOGICAL CLASSIFICATION:
Class: ACE Inhibitor (Angiotensin-Converting Enzyme Inhibitor)
Therapeutic Class: Antihypertensive, Cardiovascular Agent
mechanism of action
1. Inhibition of ACE: Captopril specifically inhibits ACE, which is responsible for converting angiotensin I
(an inactive peptide) into angiotensin II (a potent vasoconstrictor).
2. Reduction of Angiotensin II: By inhibiting ACE, captopril decreases the production of angiotensin II.
This leads to several beneficial effects:
 Vasodilation: Angiotensin II causes blood vessels to constrict. Lower levels of angiotensin II result
in vasodilation, reducing blood pressure.
 Decreased Aldosterone Secretion: Angiotensin II stimulates the release of aldosterone from the
adrenal glands. Aldosterone promotes sodium and water retention, which increases blood volume
and pressure. By reducing angiotensin II, captopril lowers aldosterone levels, leading to decreased
sodium and water retention.
3. Bradykinin: Captopril also inhibits the degradation of bradykinin, a peptide that promotes vasodilation.
Increased levels of bradykinin contribute further to the lowering of blood pressure.
4. Cardiovascular Effects: The combined effects of reduced angiotensin II and increased bradykinin lead to
decreased peripheral resistance, reduced blood volume, and ultimately lower blood pressure. This decreases
the workload on the heart and can improve symptoms of heart failure and increase survival after a heart
attack.
AVAILABILITY
1. Prescription Requirement: Captopril is a prescription medication, meaning it must be prescribed
by a healthcare provider.
2. Formulations: It is typically available in tablet form in various dosages, including 12.5 mg, 25 mg, 50
mg, and 100 mg.
3. Brand Names: While captopril is often dispensed as a generic, it is also sold under several brand
names. Some common brand names include Capoten and Acepress.
4. Pharmacy Availability: Captopril can be found in most pharmacies, both physical and online. It is
commonly stocked due to its widespread use in managing hypertension and heart failure.
5. Cost: As a generic drug, captopril is generally affordable. The cost may vary based on the pharmacy,
insurance coverage, and location. Many insurance plans cover captopril, and patient assistance programs
may be available for those without insurance.
6. International Availability: Captopril is available in many countries around the world, though the
specific brand names and formulations may differ.
INDICATION
1. Hypertension (High Blood Pressure): Captopril is used to lower blood pressure, helping to
reduce the risk of complications such as stroke, heart attack, and kidney problems.
2. Heart Failure: It is prescribed to manage heart failure, improving symptoms, and enhancing the
quality of life by making it easier for the heart to pump blood.
3. Post-Myocardial Infarction (Heart Attack): Captopril is used to improve survival and reduce
the risk of heart failure after a heart attack by preventing the heart from being overworked.
4. Diabetic Nephropathy (Kidney Problems in Diabetes): For patients with type 1 diabetes and
proteinuria (excessive protein in urine), captopril can help protect kidney function and slow the progression
of kidney disease.
5. Left Ventricular Dysfunction: Captopril is indicated for patients with asymptomatic left
ventricular dysfunction to reduce the risk of symptomatic heart failure and subsequent complications.
Route / dose
1. Hypertension:
- Initial Dose: 25 mg taken two or three times daily.
- Maintenance Dose: The dose can be adjusted based on blood pressure response, usually ranging from 25
mg to 50 mg two or three times daily.
- Maximum Dose: Generally, up to 450 mg per day, divided into multiple doses.
2. Heart Failure:
- Initial Dose: 6.25 mg to 12.5 mg taken two or three times daily.

- Maintenance Dose: The dose can be gradually increased to 50 mg to 100 mg two or three times daily,
depending on the patient's tolerance and response.
- Maximum Dose: Up to 450 mg per day, divided into multiple doses.
3. Post-Myocardial Infarction:
- Initial Dose: 6.25 mg, then 12.5 mg three times daily.
- Maintenance Dose: The dose is typically increased to 25 mg to 50 mg three times daily over several
weeks.
4. Diabetic Nephropathy:
- Typical Dose: 25 mg taken three times daily.
5. Left Ventricular Dysfunction:
- Initial Dose: 6.25 mg to 12.5 mg three times daily.
- Maintenance Dose: Typically increased to 25 mg to 50 mg three times daily as tolerated.
Adverse reaction
1. Cough: A persistent dry cough is a common side effect of ACE inhibitors like captopril.
2. Dizziness and Lightheadedness: Often occurs due to a drop in blood pressure, especially when starting
the medication or increasing the dose.
3. Taste Alterations: Some patients experience a metallic or salty taste.
4. Skin Rash: A mild skin rash can occur, typically early in treatment.
5. Fatigue: Feeling unusually tired or weak.
Serious Adverse Reactions

1. Angioedema: Swelling of the face, lips, tongue, throat, or extremities. This is a medical emergency and
requires immediate attention.
2. Hyperkalemia: Elevated potassium levels in the blood, which can cause dangerous heart rhythm
problems.
3. Renal Impairment: Worsening kidney function or acute kidney failure, particularly in patients with
preexisting kidney conditions or those taking other medications that affect kidney function.
4. Neutropenia/Agranulocytosis: A significant decrease in white blood cells, increasing the risk of

infections. This is more common in patients with renal impairment or collagen vascular disease.
5. Hypotension: Severely low blood pressure, particularly after the first dose or dose increases, especially in
patients who are volume-depleted or on diuretics.
6. Liver Dysfunction: Rarely, captopril can cause elevated liver enzymes and, in severe cases, liver injury.
Other Potential Adverse Reactions

1. Gastrointestinal Issues: Nausea, vomiting, diarrhea, or abdominal pain.
2. Headache: Common but generally mild.
3. Chest Pain: Non-specific chest pain not related to the heart.
Contraindications
1. Hypersensitivity:
Allergy to Captopril or ACE Inhibitors: Patients who have previously had an allergic reaction to captopril
or any other ACE inhibitors should not take this medication.
2. History of Angioedema:
 Related to Previous ACE Inhibitor Therapy: Patients with a history of angioedema related to
previous ACE inhibitor use should avoid captopril.
 Hereditary or Idiopathic Angioedema: Those with hereditary or idiopathic angioedema should not
take captopril due to the increased risk of severe swelling.
3. Pregnancy:
Second and Third Trimesters: Captopril is contraindicated during the second and third trimesters of
pregnancy due to the risk of fetal toxicity, including hypotension, neonatal skull hypoplasia, anuria, renal
failure, and death.
4. Severe Renal Impairment:

Patients with severe renal artery stenosis: Particularly bilateral or in a single kidney, as captopril can worsen
renal function.
5. Hyperkalemia:
High Blood Potassium Levels: Patients with hyperkalemia (high potassium levels) should not take captopril
because it can further increase potassium levels.
6. Hypotension:
Patients with Low Blood Pressure: Those with hypotension or conditions that lead to low blood pressure
(such as volume depletion) should avoid captopril unless under strict medical supervision.
PHARMACOKINETICS
Absorption
 Oral Bioavailability: Captopril is rapidly absorbed from the gastrointestinal tract, with an oral
bioavailability of about 60-75%.
 Peak Plasma Concentration: The peak plasma concentration is reached approximately 1 hour after
oral administration.
 Effect of Food: The presence of food in the stomach can reduce the absorption of captopril by about
30-40%, so it is typically recommended to take it one hour before meals.
Distribution
 Volume of Distribution (Vd): The volume of distribution is around 0.7 L/kg, indicating moderate
distribution into body tissues.
 Plasma Protein Binding: Approximately 25-30% of captopril is bound to plasma proteins, primarily
albumin.
Metabolism
 Metabolic Pathway: Captopril undergoes partial metabolism in the liver. The main metabolites are
captopril disulfide and captopril-cysteine disulfide.
 Active Metabolites: The metabolites of captopril are pharmacologically inactive.
Excretion
 Renal Excretion: Captopril and its metabolites are primarily excreted by the kidneys. Approximately
50% of an oral dose is excreted unchanged in the urine.
 Half-Life: The elimination half-life of captopril is relatively short, around 2-3 hours in patients with
normal renal function.
 Renal Impairment: In patients with impaired renal function, the elimination half-life is prolonged,
necessitating dose adjustments.
NURSING IMPLICATIONS
Assessment
1. Baseline Data: Obtain a thorough baseline assessment, including blood pressure, heart rate, renal
function (BUN, creatinine), and electrolyte levels (especially potassium).
2. History: Review the patient's medical history for contraindications such as angioedema, renal
impairment, or pregnancy. Assess for any history of drug allergies, particularly to ACE inhibitors.
Administration
1. Timing: Administer captopril one hour before meals to enhance absorption.
2. Dosage Adjustment: Be aware that dosages may need adjustment in patients with renal impairment or
the elderly. Follow the prescribed dosing regimen carefully.
Monitoring
1. Blood Pressure: Regularly monitor blood pressure to assess the effectiveness of the medication and
adjust the dosage as needed.
2. Renal Function: Periodically monitor renal function tests (BUN, creatinine) to detect any signs of renal
impairment.
3. Electrolytes: Check electrolyte levels, particularly potassium, to identify hyperkalemia, a potential side
effect of captopril.
4. Signs of Adverse Reactions: Watch for signs of angioedema (swelling of the face, lips, tongue, or
throat), a persistent dry cough, or symptoms of hypotension (dizziness, lightheadedness).
Patient Education
1. Medication Adherence: Emphasize the importance of taking captopril exactly as prescribed, even if the
patient feels well.
2. Reporting Symptoms: Instruct patients to report any signs of angioedema, persistent cough, dizziness, or
swelling immediately.
3. Lifestyle Modifications: Educate patients on lifestyle changes that can enhance the effectiveness of
captopril, such as dietary modifications (low-sodium diet), regular exercise, and avoiding smoking and
excessive alcohol consumption.
4. Hydration: Advise patients to stay adequately hydrated but to avoid excessive salt substitutes or
potassium supplements unless directed by their healthcare provider.
Safety Precautions
1. First Dose Hypotension: Be aware of the risk of significant hypotension after the first dose, particularly
in patients who are volume-depleted or on diuretics. Monitor these patients closely after the initial dose.
2. Renal Impairment: Use caution in patients with renal artery stenosis or severe renal impairment.
Monitor renal function closely and adjust doses accordingly.
3. Pregnancy: Ensure female patients of childbearing age are aware of the risks of taking captopril during
pregnancy and advise them to use effective contraception.
Coordination of Care
1. Communication: Communicate with other healthcare providers involved in the patient’s care to
coordinate treatment plans and monitor for potential drug interactions.
2. Follow-up: Schedule regular follow-up visits to monitor the patient’s response to therapy, adjust dosages
if necessary, and ensure adherence to the treatment plan.
NITROGLYCERINE
INTRODUCTION
Nitroglycerin is a medication commonly used to treat and prevent chest pain (angina) caused by heart
disease. It belongs to a class of drugs known as nitrates and works by relaxing and widening blood vessels,
which improves blood flow to the heart. This helps to reduce the heart's workload and the oxygen demand of
heart muscles.
Nitroglycerin belongs to the pharmacological class of drugs known as nitrates. Nitrates are vasodilators,
meaning they relax and widen blood vessels. This action primarily affects veins, leading to decreased
venous return to the heart and reduced cardiac preload, which ultimately decreases myocardial oxygen
demand.
Additionally, nitrates dilate coronary arteries, improving blood flow to the heart muscle. This dual
mechanism of action makes nitrates, including nitroglycerin, effective in relieving angina symptoms by
increasing oxygen supply and decreasing demand in the heart.
Furthermore, nitroglycerin is classified as an organic nitrate and is often used as a first-line treatment for
acute angina attacks and as a long-term preventive measure in individuals with chronic stable angina or heart
failure.
The therapeutic classification of nitroglycerin falls under several categories:
1. Anti-Anginal Agent: Nitroglycerin is primarily used to relieve and prevent angina pectoris, a type of
chest pain caused by reduced blood flow to the heart muscle. It achieves this by dilating blood vessels,
improving blood flow to the heart, and reducing myocardial oxygen demand.
2. Vasodilator: Nitroglycerin is a potent vasodilator, meaning it relaxes and widens blood vessels. This
action helps to decrease cardiac preload (the amount of blood returning to the heart) and afterload (the
resistance the heart must overcome to eject blood), leading to reduced cardiac workload and improved
cardiac function.
3. Anti-Ischemic Agent: By increasing blood flow to the heart muscle, nitroglycerin helps to alleviate
myocardial ischemia, a condition characterized by insufficient blood supply to the heart. This makes
nitroglycerin an important therapeutic agent in the management of ischemic heart disease.
4. Treatment for Heart Failure: In some cases, nitroglycerin may be used as adjunctive therapy in the
treatment of heart failure. By reducing preload and afterload, it can improve cardiac output and alleviate
symptoms of heart failure, such as dyspnea and exercise intolerance.
5. Hypertensive Crisis Management: Nitroglycerin can be used to lower blood pressure in hypertensive
emergencies or acute pulmonary edema, where rapid reduction of blood pressure is necessary to prevent
organ damage and improve patient outcomes.
MECHANISM OF ACTION
1. Nitric Oxide (NO) Production: Nitroglycerin is metabolized in the body to release nitric oxide (NO), a
potent vasodilator. Nitric oxide activates the enzyme guanylate cyclase in vascular smooth muscle cells.
2. Guanylate Cyclase Activation: Activation of guanylate cyclase leads to the conversion of guanosine
triphosphate (GTP) to cyclic guanosine monophosphate (cGMP).
3. cGMP-Mediated Effects: Increased levels of cGMP cause relaxation of vascular smooth muscle cells,
leading to vasodilation of both arterial and venous blood vessels.
4. Arterial Vasodilation: Vasodilation of arterial vessels reduces systemic vascular resistance (afterload),
thereby decreasing cardiac workload and myocardial oxygen demand.
5. Venous Vasodilation: Vasodilation of venous vessels reduces venous return to the heart (preload), which
reduces ventricular filling pressure and further decreases myocardial oxygen demand.
6. Coronary Vasodilation: Nitroglycerin also dilates coronary arteries, improving blood flow to the heart
muscle (myocardium), which helps alleviate myocardial ischemia and angina symptoms.
AVAILABILITY
1. Sublingual Tablets or Sprays: These are used for rapid relief of acute angina symptoms. They are
placed under the tongue (sublingually) for quick absorption into the bloodstream.
2. Oral Tablets or Capsules: Oral formulations are available for long-term prevention of angina attacks.
These are taken by mouth and provide sustained release of nitroglycerin.
3. Transdermal Patches: Patches containing nitroglycerin are applied to the skin and deliver a controlled
dose of the medication over a period of time, typically 24 hours. They are used for chronic angina
management.
4. Ointments: Nitroglycerin ointments are applied to the skin, usually on the chest area, and absorbed
through the skin to provide relief from angina symptoms.
5. Intravenous (IV) Formulation: Nitroglycerin is also available for intravenous administration in hospital
settings for the management of hypertensive emergencies, acute heart failure, and perioperative
hypertension.
INDICATION
1. Angina Pectoris: Nitroglycerin is primarily used to treat angina, a type of chest pain or discomfort
caused by reduced blood flow to the heart muscle. It can be used to relieve acute episodes of angina (acute
angina) or prevent angina attacks from occurring (chronic stable angina).
2. Acute Coronary Syndrome (ACS): Nitroglycerin may be administered to patients with acute coronary
syndrome, which includes conditions like unstable angina and myocardial infarction (heart attack), to relieve
chest pain and improve blood flow to the heart.
3. Heart Failure: In some cases, nitroglycerin may be used as adjunctive therapy in the management of
heart failure, particularly in cases where there is evidence of fluid overload and pulmonary congestion. It
helps to reduce preload and afterload, improving cardiac function and symptoms.
4. Hypertensive Emergencies: Nitroglycerin can be used in hypertensive crises, such as hypertensive

emergencies or acute pulmonary edema, to rapidly lower blood pressure and improve cardiac function.
5. Perioperative Hypertension: Nitroglycerin may be used during surgery to control blood pressure and
reduce myocardial oxygen demand in patients with hypertension.
6. Coronary Artery Disease (CAD): Nitroglycerin may be prescribed as part of the management of
coronary artery disease to alleviate symptoms and improve exercise tolerance in patients with stable angina.
DOSE AND ROUTE

1. Sublingual Tablets or Sprays (Immediate Relief of Angina):
 Sublingual tablets: 0.3 to 0.6 milligrams (mg) may be administered every 5 minutes as needed for
acute relief of angina symptoms. The tablet is placed under the tongue and allowed to dissolve.
 Sublingual sprays: 1 to 2 sprays (0.4 mg per spray) may be administered every 5 minutes as needed
for acute relief of angina symptoms. The spray is administered under the tongue.
2. Oral Tablets or Capsules (Long-term Prevention of Angina):
 The usual oral dosage for chronic stable angina is 2.5 to 6.5 mg taken 3 to 4 times daily, with dosing
intervals of at least 4 to 6 hours. The tablets or capsules are swallowed with water.
3. Transdermal Patches (Chronic Angina Management):
 Transdermal patches typically deliver nitroglycerin at a rate of 0.1 to 0.4 mg per hour. Patch
application sites are rotated to prevent skin irritation, and patches are typically applied once daily for
12 to 14 hours and removed for a 10 to 12-hour "patch-free" period.
4. Ointments (Chronic Angina Management):
 Nitroglycerin ointment is typically applied in a thin layer (usually about 1 inch in length) to the skin
over the chest or upper arm. The initial dosage is usually 0.5 inches of ointment, applied every 6 to 8
hours, with subsequent dosage adjustments based on individual response.
5. Intravenous Infusion (Hypertensive Emergencies or Acute Heart Failure):
 Intravenous nitroglycerin is administered as a continuous infusion, typically starting at a low dose

(e.g., 5 to 10 micrograms per minute) and titrated upwards based on blood pressure response.
Infusion rates are adjusted carefully to achieve the desired reduction in blood pressure without
causing hypotension.
ADVERSE REACTION
1. Headache: This is one of the most common side effects of nitroglycerin and can range from mild to
severe. It often occurs due to the vasodilatory effects of the medication.
2. Hypotension (Low Blood Pressure): Nitroglycerin can cause a drop in blood pressure, leading to
symptoms such as dizziness, lightheadedness, or fainting. This effect is more likely to occur with higher
doses or rapid administration.
3. Reflex Tachycardia: In response to a drop in blood pressure, the body may increase heart rate
(tachycardia) as a compensatory mechanism. This can lead to palpitations or a sensation of rapid heartbeat.
4. Flushing: Some individuals may experience flushing or redness of the skin, particularly in the face, neck,
or chest, as a result of peripheral vasodilation.
5. Nausea or Vomiting: Nitroglycerin may cause gastrointestinal upset in some individuals, leading to
symptoms such as nausea or vomiting.
6. Syncope (Fainting): Severe hypotension induced by nitroglycerin can occasionally lead to syncope or
loss of consciousness.
7. Allergic Reactions: Rarely, individuals may experience allergic reactions to nitroglycerin, which can
manifest as rash, itching, or swelling of the face, lips, or throat.
8. Tolerance: Prolonged use of nitroglycerin can lead to tolerance, where the medication becomes less
effective over time. This may necessitate dosage adjustments or changes in treatment.
9. Paradoxical Bradycardia: In rare cases, nitroglycerin may paradoxically slow the heart rate
(bradycardia), especially in patients with pre-existing bradycardia or conduction abnormalities.
10. Methemoglobinemia: Extremely rare, but nitroglycerin can potentially cause methemoglobinemia, a
condition where the blood contains elevated levels of methemoglobin, reducing its ability to carry oxygen.
CONTRAINDICATIONS
1. Hypersensitivity: Nitroglycerin is contraindicated in individuals with a known hypersensitivity or allergy
to nitroglycerin or other nitrates.
2. Severe Anemia: Nitroglycerin should be used with caution or avoided in individuals with severe anemia
because it can further reduce oxygen-carrying capacity in the blood.
3. Increased Intracranial Pressure (ICP): Nitroglycerin is contraindicated in patients with suspected or

known increased intracranial pressure, as it can worsen cerebral edema and neurological symptoms.
4. Severe Hypotension: Nitroglycerin is contraindicated in patients with severe hypotension (low blood
pressure), as it can further lower blood pressure and lead to hemodynamic instability.
5. Phosphodiesterase Inhibitors: Nitroglycerin should not be used concurrently with phosphodiesterase

inhibitors (e.g., sildenafil, tadalafil, vardenafil) due to the risk of severe hypotension and cardiovascular
collapse.
6. Acute Myocardial Infarction with Low Filling Pressures: Nitroglycerin is contraindicated in patients
with acute myocardial infarction (heart attack) who have low filling pressures (e.g., right ventricular
infarction or obstructive cardiomyopathy), as it can exacerbate hypotension and worsen cardiac function.
7. Closed-Angle Glaucoma: Nitroglycerin is contraindicated in patients with closed-angle glaucoma, as it
can exacerbate intraocular pressure and precipitate an acute glaucoma attack.
8. Use of Riociguat: Concomitant use of nitroglycerin with riociguat, a medication used to treat pulmonary
arterial hypertension, is contraindicated due to the risk of hypotension.
9. Traumatic Brain Injury (TBI): Nitroglycerin should be used with caution or avoided in patients with
traumatic brain injury, as it can worsen cerebral perfusion and increase intracranial pressure.
PHARMACOKINETICS
1. Absorption: Nitroglycerin can be absorbed through various routes depending on the formulation.
Sublingual administration provides rapid absorption through the mucous membranes under the tongue. Oral
tablets are absorbed in the gastrointestinal tract, while transdermal patches deliver the medication through
the skin. Absorption through the skin and mucous membranes is facilitated by the lipid solubility of
nitroglycerin.
2. Distribution: Nitroglycerin is rapidly distributed throughout the body following absorption. It readily
crosses cell membranes due to its lipophilic nature. Distribution is primarily to vascular smooth muscle
cells, where nitroglycerin exerts its pharmacological effects by releasing nitric oxide and activating
guanylate cyclase.
3. Metabolism: Nitroglycerin undergoes extensive metabolism primarily in the liver. The primary
metabolic pathway involves the conversion of nitroglycerin to nitric oxide (NO) and other metabolites, such
as 1,2-glyceryl dinitrate and 1,3-glyceryl dinitrate. These metabolites are less potent vasodilators than
nitroglycerin itself. The metabolism of nitroglycerin is rapid, leading to a short half-life.
4. Elimination: Metabolites of nitroglycerin are eliminated primarily through renal excretion. The short
half-life of nitroglycerin and its metabolites results in rapid clearance from the body. The elimination half-
life of nitroglycerin is typically in the range of 1 to 4 minutes.
5. Duration of Action: The duration of action of nitroglycerin varies depending on the formulation and
route of administration. Sublingual nitroglycerin provides rapid onset of action within minutes but has a
short duration of action, typically lasting 30 minutes to 1 hour. Transdermal patches provide sustained
release of nitroglycerin over a 24-hour period.
NURSING IMPLICATION
1. Assessment:
 Perform a thorough assessment of the patient's cardiovascular status, including vital signs, cardiac
rhythm, and oxygen saturation.
 Assess the patient's history of angina, previous nitroglycerin use, and response to treatment.
 Evaluate for contraindications or potential drug interactions, such as concurrent use of
phosphodiesterase inhibitors or riociguat.
 Assess the patient's ability to self-administer nitroglycerin and their understanding of its use.
2. Education:
 Provide patient education on the purpose of nitroglycerin, its mechanism of action, and expected
therapeutic effects.
 Instruct patients on the correct administration technique for sublingual tablets or sprays, emphasizing
the importance of placing the medication under the tongue and not swallowing it.
 Educate patients on the appropriate timing and frequency of nitroglycerin administration for acute
relief of angina symptoms.
 Teach patients about potential adverse effects of nitroglycerin, including headache, hypotension, and
dizziness, and when to seek medical attention.
3. Monitoring:
 Monitor the patient's vital signs, particularly blood pressure and heart rate, before and after
nitroglycerin administration.
 Assess the patient for signs and symptoms of angina relief, such as decreased chest pain or
discomfort.
 Monitor for adverse reactions, including headache, hypotension, nausea, and syncope, and intervene
appropriately.
 Regularly assess the effectiveness of nitroglycerin therapy in relieving angina symptoms and
improving quality of life.
4. Safety Considerations:
 Emphasize the importance of caution when changing positions, especially from lying to standing,
due to the risk of orthostatic hypotension.
 Advise patients to avoid sudden changes in posture and to rise slowly from a sitting or lying position.
 Instruct patients to store nitroglycerin tablets or sprays in their original containers, away from
moisture and heat, and to check expiration dates regularly.
 Educate patients on the proper disposal of expired or unused nitroglycerin medications according to
local regulations.
5. Documentation:
 Document the administration of nitroglycerin, including the dose, route, time, and patient response.
 Record vital signs, angina symptoms, adverse reactions, and any interventions provided in the
patient's medical record.
 Maintain accurate and up-to-date documentation to facilitate communication among healthcare team
members and ensure continuity of care.
METHARGINE
INTRODUCTION
Methargine, also known as methylergometrine or methylergonovine, is a medication used primarily to
prevent or control excessive bleeding following childbirth, known as postpartum hemorrhage. It is an ergot
alkaloid that works by causing the muscles of the uterus to contract, thereby reducing bleeding.
 Class: Ergot alkaloid
 Class: Uterotonic agent
MACHANISM OF ACTION
1. Receptor Interaction:
 Adrenergic Receptors: Methylergometrine acts as a partial agonist at alpha-adrenergic receptors,
leading to vasoconstriction and increased smooth muscle tone.
 Serotonin Receptors: It also stimulates serotonin receptors, particularly the 5-HT2 subtype, which
contributes to uterine smooth muscle contraction.
 Dopaminergic Receptors: Methylergometrine can interact with dopaminergic receptors, although this
action is less pronounced in its uterotonic effects.
2. Uterine Smooth Muscle Contraction:

 Direct Stimulation: By directly stimulating the smooth muscle of the uterus, methylergometrine
increases the strength, duration, and frequency of uterine contractions.
 Calcium Mobilization: The drug facilitates the mobilization of intracellular calcium in uterine
smooth muscle cells. Increased intracellular calcium concentration is essential for muscle
contraction.
3. Hemostatic Effect:
 Reducing Bleeding: The increased uterine contractions help compress blood vessels within the
uterine wall, reducing blood flow and aiding in hemostasis (the process that stops bleeding).
 Involution of the Uterus: Promotes the involution (shrinking) of the uterus post-delivery, which helps
in reducing postpartum hemorrhage.
Availability
1. Oral Tablets:
- Typically available in 0.125 mg or 0.2 mg tablets.
2. Injectable Form:
- Available as an intramuscular (IM) or intravenous (IV) injection, often in 1 mL ampoules containing 0.2
mg/mL of methylergometrine maleate.
Brand Names
- Methergine
- Methargin
- Ergometrine
- Syntometrine (often combined with oxytocin)
Storage
- Tablets: Should be stored at room temperature, away from light and moisture.
INDICATION
Primary Indications
1. Prevention and Treatment of Postpartum Hemorrhage (PPH):
- Used to control and prevent excessive bleeding following childbirth by promoting uterine contractions.
2. Management of Uterine Atony:
- Employed in cases where the uterus fails to contract adequately after delivery, leading to bleeding.
Secondary Indications
1. Post-Abortion Hemorrhage:
- Utilized to control bleeding following a miscarriage or abortion by contracting the uterus.
2. Uterine Subinvolution:
- Helps in conditions where the uterus does not return to its pre-pregnancy size at the expected rate
postpartum.
Specific Use Cases

- During the Third Stage of Labor:
- Sometimes administered during the third stage of labor to facilitate placental expulsion and reduce
bleeding.
- After Cesarean Section:
- Can be used to manage bleeding and ensure uterine contraction following a cesarean delivery.
Off-Label Uses
- Gynecological Surgery:
- Occasionally used in certain gynecological surgeries to reduce intraoperative and postoperative bleeding.
DOSE AND ROUTE

Oral Administration:
- Dose: 0.2 mg
- Frequency: Every 6-8 hours
- Duration: Typically for 2-7 days postpartum
Intramuscular (IM) Injection:
- Dose: 0.2 mg
- Frequency: Every 2-4 hours as needed
- Maximum: Up to 5 doses
Intravenous (IV) Injection:
- Dose: 0.2 mg
- Administration: Slowly over at least 1 minute
- Frequency: Only if IM administration is not possible and should be limited to severe cases due to the risk
of severe hypertension and other side effects
POST-ABORTION HEMORRHAGE
Intramuscular (IM) Injection:
- Dose: 0.2 mg
- Frequency: Every 2-4 hours as needed
- Maximum: Up to 5 doses
Special Considerations
- Timing: For prevention of postpartum hemorrhage, the first dose is often given immediately after the
delivery of the placenta.
- Monitoring: Blood pressure should be monitored during treatment, especially if administered
to ergot alkaloids.
ADVERSE REACTION
1. Gastrointestinal
- Nausea
- Vomiting
- Abdominal pain
2. Central Nervous System
- Headache
- Dizziness
Cardiovascular Reactions
1. Hypertension
- Elevated blood pressure, which can be severe
2. Peripheral Vasoconstriction
- Resulting in cold extremities or paresthesia (tingling or numbness)
3. Chest Pain
- Angina or myocardial infarction (rare but serious)
Severe and Rare Adverse Reactions

1. Stroke
- Due to severe hypertension or vasospasm
2. Seizures
- Related to severe hypertensive episodes or cerebrovascular events
3. Myocardial Infarction
- Heart attack, particularly in patients with preexisting cardiovascular conditions
Allergic Reactions
1. Hypersensitivity Reactions
- Rash
- Pruritus (itching)
- Anaphylaxis (rare but potentially life-threatening)
Other Reactions
1. Uterine Cramping
- Although desired to some extent, can be excessively painful
2. Diaphoresis
- Excessive sweating
CONTRAINDICATIONS
Absolute Contraindications
1. Hypertension:
- Uncontrolled or severe hypertension
2. Preeclampsia and Eclampsia:
- Conditions associated with high blood pressure and potential for seizures
3. Cardiovascular Disease:
- Coronary artery disease, history of myocardial infarction, angina pectoris
4. Peripheral Vascular Disease:
- Conditions involving poor blood circulation in the limbs
5. Hypersensitivity:
- Known allergy or hypersensitivity to methylergometrine or any ergot alkaloids
6. Septic Conditions:
- Presence of infection, especially if associated with childbirth or abortion
7. Obstructed Labor:
- Situations where there is an obstruction preventing the passage of the baby
Relative Contraindications (Use with Caution)

1. Renal Impairment:
- Reduced kidney function can affect drug clearance
2. Hepatic Impairment:
- Liver diseases affecting drug metabolism
3. Severe Raynaud’s Phenomenon:
- A condition causing extreme vasoconstriction in the extremities
4. Migraine:
- Especially those with aura, due to potential for exacerbation

5. History of Drug Sensitivity:
- Caution with individuals who have had adverse reactions to similar drugs
Important Considerations
- Drug Interactions:
- Avoid concurrent use with other vasoconstrictive agents, including certain triptans used for migraines, as
well as other ergot alkaloids.
- Use cautiously with medications that can increase blood pressure or cause significant vasoconstriction.
- Pregnancy:
- Methylergometrine is not used during pregnancy except in specific circumstances like postpartum
hemorrhage management.
PHARMACOKINETICS
Absorption
- Oral Administration: Methylergometrine is well absorbed from the gastrointestinal tract when taken orally.
- Intramuscular (IM) Injection: Rapidly absorbed into the bloodstream.
- Intravenous (IV) Injection: Provides immediate drug availability in the bloodstream.
Distribution
- Protein Binding: Methylergometrine binds significantly to plasma proteins, which affects its distribution in
the body.
- Tissue Distribution: It is widely distributed in body tissues, particularly in the smooth muscle tissues of the
uterus.
Metabolism
- Liver Metabolism: Methylergometrine is extensively metabolized in the liver. It undergoes hepatic
biotransformation primarily through the cytochrome P450 enzyme system.
Excretion
- Biliary and Fecal Excretion: A significant portion of the drug and its metabolites are excreted via bile and
subsequently eliminated in the feces.
- Renal Excretion: A smaller fraction is excreted in the urine.
NURSING IMPLICATION
Pre-Administration Assessment
1. Patient History:
- Assess for contraindications such as hypertension, preeclampsia, cardiovascular diseases, and
hypersensitivity to ergot alkaloids.
- Review the patient's medication history for potential drug interactions.
2. Baseline Vital Signs:
- Measure and record baseline blood pressure, heart rate, and respiratory rate.
- Assess for any signs of uterine atony or postpartum hemorrhage.
Administration Considerations
1. Route of Administration:
- Oral: Administer with or without food; typically given every 6-8 hours for several days postpartum.
- Intramuscular (IM): Use aseptic technique; given in the deltoid or gluteal muscle.
- Intravenous (IV): Administer slowly over at least 1 minute; ensure the patient is monitored closely for
adverse effects.
2. Dosing:
- Follow the prescribed dosing regimen carefully.
- Be prepared to administer repeated doses every 2-4 hours if needed, especially in cases of persistent
bleeding, but do not exceed recommended maximum doses.
Monitoring During Treatment

1. Vital Signs:
- Regularly monitor blood pressure, heart rate, and respiratory rate, particularly after IV administration.
- Be vigilant for signs of hypertension and other cardiovascular reactions.
2. Uterine Response:
- Assess the firmness and position of the uterus regularly.
- Monitor the amount and nature of vaginal bleeding.
3. Adverse Effects:
- Watch for common side effects such as nausea, vomiting, headache, dizziness, and abdominal pain.
- Be alert for serious adverse reactions like severe hypertension, chest pain, severe headache, and signs of
stroke or myocardial infarction.
Patient Education
1. Information:
- Explain the purpose of methylergometrine and how it helps manage postpartum hemorrhage.
- Inform about potential side effects and the importance of reporting any severe or unusual symptoms
immediately.
2. Instructions:
- Advise on the correct oral dosing schedule if the patient is being discharged with a prescription.
- Emphasize the importance of adhering to follow-up appointments for monitoring.
Documentation
1. Record Keeping:
- Document the drug name, dose, route, time of administration, and the patient’s response to the
medication.
- Note any adverse reactions and the actions taken in response to them.
2. Ongoing Assessment:
- Record ongoing assessments of vital signs, uterine tone, and bleeding status.
- Ensure thorough documentation of patient education and discharge instructions.
Emergency Preparedness
- Be prepared to manage acute adverse reactions, such as severe hypertension or anaphylaxis, with
appropriate emergency medications and interventions.
- Ensure emergency equipment and medications are readily available when administering
methylergometrine, especially via IV route.
CALCIUM GLUCONATE
INTRODUCTION
Calcium gluconate is a medication used to treat conditions caused by low calcium levels in the body, such as
bone loss, weak bones, and decreased activity of the parathyroid gland. It's often given intravenously in
emergency situations, like severe hypocalcemia or certain overdoses. Always consult a healthcare
professional for proper usage and dosage information.
PHARMACOKINETICS AND THERAPEUTICS CLASSIFICATION

Calcium gluconate falls under the pharmacological classification of minerals and electrolytes, specifically
calcium supplements.
Therapeutically, it is classified as a mineral supplement and is used to treat conditions related to low calcium
levels in the body.
MACHANISM OF ACTION
The mechanism of action of calcium gluconate involves replenishing calcium levels in the body.
Calcium is essential for various physiological processes, including muscle contraction, nerve transmission,
blood clotting, and bone health.
Calcium gluconate provides a readily available source of calcium ions, which can help restore normal
calcium levels and support these essential functions.
AVAILABILITY
Calcium gluconate is typically available in various formulations, including oral tablets, oral solutions, and
injectable solutions for intravenous or intramuscular administration. It can be found in pharmacies and
healthcare facilities, often with a prescription but sometimes over-the-counter depending on the formulation
and concentration. Always follow the guidance of a healthcare professional regarding the availability and
appropriate usage of calcium gluconate.
INDICATION
Calcium gluconate is indicated for the treatment of conditions caused by low calcium levels in the body,
such as hypocalcemia (low blood calcium levels). It may also be used to manage conditions associated with
calcium deficiency, including osteoporosis, osteomalacia, and certain cases of hypoparathyroidism.
Additionally, it can be administered in emergency situations, such as calcium channel blocker toxicity or
hyperkalemia (high blood potassium levels), to counteract their effects on the heart and muscles. Always
consult a healthcare professional for proper diagnosis and treatment recommendations.
DOSE AND ROUTE

For oral supplementation, typical doses range from 500 mg to 2 g of elemental calcium per day, divided into
multiple doses as prescribed by a healthcare professional.
For intravenous administration, doses may vary widely depending on the severity of hypocalcemia or the
specific emergency situation. A common intravenous dose for adults with acute hypocalcemia is 8.8 to 10
grams (approximately 90 to 100 mL of a 10% solution) administered over 10 to 20 minutes, but this should
be adjusted based on individual patient factors and response to treatment.
ADVERSE REACTION
1. Nausea
2. Vomiting
3. Constipation
4. Diarrhea
5. Hypercalcemia (high blood calcium levels)
6. Flushing or feeling of warmth
7. Injection site reactions (with intravenous or intramuscular administration)
Rare but serious adverse reactions may include:
1. Allergic reactions (rash, itching, swelling, difficulty breathing)
2. Arrhythmias (irregular heartbeats)
3. Hypercalciuria (increased calcium levels in urine)
4. Tissue necrosis or extravasation (with improper intravenous administration)
CONTRAINDICATIONS
Contraindications to the use of calcium gluconate include:
1. Hypercalcemia (high blood calcium levels)
2. Hypercalciuria (high levels of calcium in the urine)
3. Severe renal impairment or kidney failure
4. Calcium-containing kidney stones
5. Hypersensitivity or allergy to calcium gluconate or any of its components
PHARMACOKINETICS
The pharmacokinetics of calcium gluconate involve its absorption, distribution, metabolism, and excretion
in the body:
1. Absorption: When taken orally, calcium gluconate is absorbed in the gastrointestinal tract. However,
the absorption rate is relatively low compared to other calcium salts.
2. Distribution: Once absorbed, calcium ions from calcium gluconate are distributed throughout the body
via the bloodstream. Calcium is primarily stored in bones and teeth, but it also plays essential roles in
various physiological processes in tissues and organs.
3. Metabolism: Calcium gluconate itself does not undergo significant metabolism in the body. However,
calcium ions participate in various metabolic processes, including muscle contraction, nerve transmission,
and blood clotting.
4. Excretion: Excess calcium is primarily excreted via the kidneys in the urine. The rate of excretion is
influenced by factors such as kidney function, hydration status, and hormonal regulation.
NURSING IMPLICATION
1. Assessment: Nurses should assess the patient's calcium levels, renal function, and overall health status
before administering calcium gluconate. Monitoring vital signs, including heart rate and rhythm, is also
essential.
2. Administration: Nurses should follow the prescribed dosage, route, and rate of administration for
calcium gluconate. For intravenous administration, it should be given slowly to avoid adverse reactions such
as bradycardia or hypotension.
3. Monitoring: Nurses should monitor for signs and symptoms of adverse reactions, such as nausea,
vomiting, or allergic reactions, during and after administration. Continuous cardiac monitoring may be
necessary for patients receiving intravenous calcium gluconate.
4. Patient Education: Nurses should educate patients about the purpose of calcium gluconate therapy,
potential side effects, and any necessary precautions. Patients should be encouraged to report any adverse
reactions promptly.
5. Documentation: Nurses should accurately document the administration of calcium gluconate,

including the dose, route, time, and patient response. This documentation ensures continuity of care and
assists in monitoring the patient's progress.
6. Follow-up: Nurses should collaborate with other healthcare team members to assess the patient's
response to calcium gluconate therapy and adjust the treatment plan as necessary.
DIAZEPAM
INTRODUCTION
Diazepam is a medication primarily used to treat anxiety, muscle spasms, and seizures. It belongs to a class
of drugs called benzodiazepines, which work by enhancing the effects of a neurotransmitter called GABA in
the brain, resulting in a calming effect. It's important to use diazepam as prescribed by a healthcare
professional, as it can be habit-forming and has potential for misuse.
PHARMACOLOGICAL AND THERAPEUTICS CLASSIFICATION

Diazepam belongs to the pharmacological class of benzodiazepines and is classified therapeutically as an
anxiolytic, sedative-hypnotic, anticonvulsant, and muscle relaxant medication.
MACHANISM OF ACTION
1. Start with GABA Receptors: Begin with a representation of GABA receptors on the surface of a
neuron in the brain.
2. Diazepam Binding: Depict diazepam molecules (perhaps as small shapes) approaching and binding
to these GABA receptors.
3. Enhanced Inhibition: Show the diazepam-bound GABA receptors leading to an increased influx of
chloride ions into the neuron, hyperpolarizing it. This enhanced inhibition reduces the neuron's excitability
and activity.
4. Resulting Effects: Represent the downstream effects of this enhanced inhibition, such as reduced
neuronal firing, muscle relaxation, and sedation.
AVAILABILITY
Diazepam is available in various formulations, including tablets, oral solutions, injectable solutions, and
rectal gels. It's typically prescribed by healthcare professionals and can be obtained from pharmacies with a
prescription. The availability may vary depending on the country's regulations and healthcare system.
INDICATION
Diazepam is indicated for the management of anxiety disorders, short-term relief of anxiety symptoms, acute
alcohol withdrawal symptoms, muscle spasms, seizure disorders, and as a premedication for medical or
dental procedures. It is important to use diazepam strictly according to a healthcare professional's
instructions and for the prescribed indications due to its potential for misuse and dependence.
DOSE AND ROUTE

1. Anxiety Disorders: Oral doses typically range from 2 to 10 mg, taken 2 to 4 times daily.
2. Muscle Spasms: Oral doses usually range from 2 to 10 mg, taken 3 to 4 times daily. Intramuscular
injections may also be administered in severe cases, with doses ranging from 5 to 10 mg, repeated every 3 to
4 hours if necessary.
3. Seizure Disorders: Oral doses for adults typically range from 2 to 10 mg, taken 2 to 4 times daily.
Intravenous or intramuscular injections may be used for acute seizure episodes, with doses ranging from 5 to
10 mg, repeated as needed.
4. Premedication for Medical or Dental Procedures: Oral doses of 5 to 15 mg are commonly given 1 to 2
hours before the procedure.
Rectal gel formulations are also available for certain indications, such as acute seizure episodes, with doses
typically ranging from 5 to 20 mg, depending on the patient's age and weight.
ADVERSE REACTION
Adverse reactions to diazepam can vary in severity and may include:
1. Drowsiness: Feeling excessively tired or sleepy.
2. Sedation: Feeling overly relaxed or lethargic.
3. Confusion: Difficulty thinking clearly or concentrating.
4. Dizziness: Feeling lightheaded or unsteady.
5. Muscle Weakness: Reduced muscle strength or coordination.
6. Ataxia: Difficulty with balance and coordination.
7. Memory Impairment: Difficulty forming new memories or recalling information.
8. Respiratory Depression: Reduced breathing rate, especially when combined with other depressant drugs
like opioids.
9. Hypotension: Low blood pressure, which can cause dizziness or fainting.
10. Paradoxical Reactions: Unusual reactions such as increased anxiety, agitation, or aggression.
11. Dependence and Withdrawal: Risk of physical dependence with prolonged use, leading to withdrawal
symptoms upon discontinuation.
CONTRAINDICATIONS
Diazepam is contraindicated in individuals with:
1. Hypersensitivity: Known hypersensitivity to diazepam or other benzodiazepines.
2. Severe Respiratory Insufficiency: Including severe chronic obstructive pulmonary disease (COPD) or
sleep apnea.
3. Severe Hepatic Insufficiency: Due to the risk of drug accumulation and prolonged effects.
4. Acute Narrow-Angle Glaucoma: As diazepam can increase intraocular pressure.
5. Myasthenia Gravis: Due to the potential for exacerbating muscle weakness.
6. Severe Depression: Especially when accompanied by suicidal tendencies or psychosis.
7. History of Substance Abuse: Due to the potential for addiction and misuse.
8. Pregnancy and Breastfeeding: Diazepam should be avoided during pregnancy, especially during the first
trimester, and avoided or used with caution during breastfeeding due to the potential for sedation and
adverse effects on the infant.
PHARMACOKINETICS
1. Absorption: Diazepam is well-absorbed after oral administration, with peak plasma concentrations
typically reached within 1 to 1.5 hours. Rectal administration results in rapid absorption.
2. Distribution: Diazepam is highly lipophilic and rapidly distributes into tissues, including the brain. It
crosses the blood-brain barrier and placenta, and it is also found in breast milk. It has a large volume of
distribution, indicating extensive tissue distribution.
3. Metabolism: Diazepam is extensively metabolized in the liver by the cytochrome P450 enzyme
system, primarily through the CYP3A4 and CYP2C19 pathways. The major metabolite is
desmethyldiazepam, which has a longer half-life than diazepam itself. Other metabolites include oxazepam
and temazepam.
4. Excretion: The elimination half-life of diazepam is typically around 20 to 50 hours, while that of
desmethyldiazepam is longer, ranging from 36 to 200 hours. Both diazepam and its metabolites are excreted
primarily in the urine, with small amounts excreted in the feces.
NURSING IMPLICATION
1. Assessment: Nurses should assess the patient's medical history, current medications, allergies, and
vital signs before administering diazepam. Special attention should be given to respiratory status, liver
function, and any history of substance abuse.
2. Administration: Diazepam should be administered according to the prescribed dosage and route.
Intravenous administration requires careful monitoring of vital signs and the patient's response due to the
rapid onset of action.
3. Monitoring: Nurses should monitor for signs of adverse reactions, such as sedation, respiratory
depression, hypotension, and paradoxical reactions. Regular assessment of the patient's level of
consciousness, respiratory rate, blood pressure, and oxygen saturation is essential, especially during the
initial stages of treatment.
4. Patient Education: Nurses should educate patients and their caregivers about the proper use of
diazepam, including dosage, potential side effects, and precautions. Patients should be advised not to drive
or operate machinery while taking diazepam due to its sedative effects.
5. Withdrawal Management: For patients who have been on long-term diazepam therapy, nurses
should monitor for signs of withdrawal symptoms if the medication is discontinued or tapered. Withdrawal
symptoms may include rebound anxiety, insomnia, agitation, and seizures.
6. Interactions: Nurses should be aware of potential drug interactions with diazepam, especially with
other central nervous system depressants such as opioids, alcohol, and sedative-hypnotics. Close monitoring
and dose adjustments may be necessary when diazepam is co-administered with other medications.
7. Documentation: Accurate documentation of diazepam administration, patient response, vital signs,

and any adverse reactions is essential for continuity of care and communication among healthcare providers.

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DRUGS USED IN OBSTETRICS

CLASSIFICATION OF DRUGS USED IN PREGNANCY:

S. NO. DRUG CLASSIFICATION

1. Commonly users  Folic Acid

2. Anti-hypertensive drugs  Methyldopa

3. Tocolytic Agents  Betamimetics:

PREGNANCY & ITS EFFECTS ON PHARMACOKINETICS: -

Effects of medications during labour:

DRUGS & BREASTFEEDING:

Brand name- Cytotec

 Used for cervical ripening and labor induction.

 Used for medical association

 Uterine hyperstimulation (3-8%).

STORAGE/STABILITY: Dinoprostone gel is stored in refrigerator at 36°-46°F. Suppository is stored in

o To ripen the cervix before induction.

o Following expulsion of placenta as an alternative to crgometrine

METHODS OF ADMINISTRATION OF OXYTOCIN:

Indications of stopping the infusion

Progesterone is used in prevention of preterm labor as it causes uterine muscle quiescence.

The half of vaginal progesterone is 13 hours. It has high bioavailability.

The half-life of injectable 17-HPC is 7 days.

Women with previous history of preterm delivery.

 Current or past history of thrombophlebitis, thromboembolic disorder or cerebral apoplexy.

 Liver dysfunction or disease.

 Known or suspected malignancy of breast or genital organs.

ADVERSE DRUG REACTION

Common side effects include fatigue, headache, malaise.

DOSAGE AND ROUTE

Pharmacological classification: anti coagulants

Pharmacological name: unfractionated heparin

Dose : as prescribed by physcian

 The platelet count is 100,000/mm or lower.

 Review patient allergies.

Pharmacological classification : anticonvulsants

Pharmacological name : phenytoin or phenytoin sodium.

Therapeutic action : decreasing abnormal electrical activity in the brain.

oral Initial dose: 100 mg extended release orally 3 times a day.

IV: Do not exceed the infusion rate of 50 mg/min.

Usual Adult Dose for Arrhythmias: Loading Dose:

Usual Adult Dose for Status Epilepticus:

Loading dose: Manufacturer recommends 10 to 15 mg/kg by slow IV administration

Maintenance dose: IV or Oral: 100 mg every 6 to 8 hours.

Usual Pediatric Dose for Seizures:

Usual Pediatric Dose for Arrhythmias:

Greater than 1 year:

Peak plasma time: 1.5-3 hr (immediate-release); 4-12 hr (extended-release)

Metabolism - Metabolized by hepatic P450 enzyme CYP2C9

 Review patient allergies.

Pharmacological classification : phenothiazines. first-generation antihistamine, antipsychotic,

Pharmacological name : Phenergan Prorex Provigan Zipan.

Therapeutic action : central and peripheral dopaminergic blockade.

 Promethazine hydrochloride oral tablets: 12.5 mg, 25 mg, 50 mg

Route : oral, rectal, intramuscular, and intravenous. .

Dose : For oral dosage form (tablets):

 For allergy symptoms:

Hypersensitivity : it is contraindicated in patients with hypersensitivity.

Distribution – The volume of distribution of promethazine is approximately 970L or 30L/kg. Promethazine

Metabolism - Minimal metabolism by the gastrointestinal mucosa is implicated

 Review patient allergies.