Pharmacology BY: Hermie M. Pueyo M.D., R.N. Pharmacology
Pharmacology BY: Hermie M. Pueyo M.D., R.N. Pharmacology
Pharmacology BY: Hermie M. Pueyo M.D., R.N. Pharmacology
Pharmacology
- most simply defined as study of drug.
Fundamentals of Pharmacology
1. Pharmacokinetics
- study of drug’s changes as it enters and passes through the body.
a. absorption
b. distribution
c. biotransformation
d. excretion
2. Pharmacodynamics
- mechanism by which drugs produce changes in body tissue.
a. desired effect - intended action of drugs
b. adverse effect - harmful unintended reactions
c. side effects – consequence reactions
d. toxicity – the degree which something is poisonous
digoxin = 0.5 – 2.0 ng/mL
lithium = 0.5 – 1.5 mEq/L
Eye medications :
- administer eyedrops first then ointment.
- use a separate bottle for each client.
- instruct the client to tilt the head backward, open eyes and look up.
- avoid contact of medication bottle to the eyeball.
- place prescribed dose in the lower conjunctival sac.
- instruct the client to press the inner canthus for 30-60 seconds.
- instruct the client to close the eye gently.
Ear drops
- in infant and children younger than 3 y.o, pull pinna downward and backward.
- in older children and adult, upward and backward.
- direct the solution on the wall of the ear canal, not directly on the ear drum.
CLASSIFICATIONS Of DRUGS
Anticonvulsants
Prototype :
a. Hydantoins - phenytoin (Dilantin)
b. Barbiturates - phenobarbital ( Luminal)
c. Miscellaneous
- carbamazepine (Tegretol), diazepam, clorazepate (Tranxene),
valproic acid (Dapakene), ethosuximide (Zarontin).
Mechanism of action :
- treat seizures by depressing abnormal neuronal activity in motor cortex.
Adverse effects :
- sedation & drowsiness, gingival hyperplasia
- diplopia, nystagmus, vertigo, dizziness
- thrombocytopenia, aplastic anemia
Nursing considerations :
1. Advise female clients to use contraceptives.
2. Inform clients taking phenytoin that harmless urine discoloration is common.
3. Warn clients with diabetes that hydantoins may increase blood sugar level and that
valproic acid may produce a false positive result in urine ketone test.
4. Teach clients receiving carbamazepine to identify symptoms of bone marrow
depressions.
5. Reassure that barbiturates are not addictive at a low dosage.
6. Avoid taking alcohol with barbiturates.
7. Administer IV phenytoin slowly to avoid cardiotoxicity.
8. Avoid mixing other drugs in same syringe with phenytoin.
Antiparkinsonian Agents
Prototype :
a. Anticholinergic agents
- trihexyphenidyl (Artane), benztropine (Congentin)
b. Dopaminergic agents
- Levodopa, carbidopa-levodopa (Sinemet), amantidine (Symmetrel),
pergolide (Permax), selegiline (Eldepryl), bromocriptine.
Mechanism of actions :
a. anticholinergic agents
- inhibit cerebral motor centers.
b. dopaminergic agents
- increasing dopamine concentrations or
enhancing neurotransmitter functioning.
Adverse effects of dopaminergic agents:
a. levodopa – nausea, vomiting, anorexia, orthostatic hypotension,
dark-colored urine and sweat
b. amantidine – ankle edema, constipation
c. bromocriptine – palpitations, tachycardia
Nursing considerations :
1. Give dopaminergic agents after meals to reduce GI symptoms.
2. Reassure client that levodopa may cause harmless darkening of urine and sweat.
3. Avoid taking Vit B6 (pyridoxine) with levodopa because it speed up metabolism.
4. Educate clients to minimize orthostatic hypotension.
5. Elevate leg to reduce ankle edema.
Central Nervous System Stimulants
Prototype :
- amphetamines, methylphenidate (Ritalin)
Mechanism of actions :
- increase excitatory CNS neurotransmitter activity and blocks inhibitory impulses.
Indications :
- for obesity (amphetamines)
- attention deficit hyperactivity disorders
- narcolepsy
- drug-induced respiratory depressions.
Adverse effects :
- nervousness, insomnia, restlessness
- hypertension, tachycardia, headache
- anorexia, dry mouth.
Nursing considerations :
1. Should be given at morning.
2. Don’t stop amphetamine abruptly to avoid withdrawal symptoms.
3. Monitor blood pressure and pulse.
4. Ice chips or sugarless gum for dry mouth.
5. Watch out for growth retardation in children taking methylphenidate.
General Anesthetics
Prototype :
a. Inhalation anesthetics
- enflurane (Ethrane), halothane
- isoflurane (Forane), nitrous oxide
b. Injection anesthetics
- fentanyl (Sublimaze), ketamine (Ketalar),
thiopental Na (Penthotal), etomidate (Amidate)
Mechanism of actions :
- cause CNS depression, by producing loss of consciousness, unresponsiveness to pain
stimuli, and muscle relaxation.
Nursing considerations :
1. Instruct client NPO for 8 hours before administration.
2. Monitor cardio pulmonary depression and hypotension.
3. Monitor urinary retention.
4. Monitor body temperature
- malignant hyperthermic crisis :
dantrolene (antidote)
5. Avoid alcohol or CNS depressants for 24 hours after anesthesia.
6. In patient who received halothane, monitor signs of hepatic fatal side effects :
- rash, fever, nausea, vomiting
- jaundice and altered liver function.
Anticoagulants
Prototype :
- Heparin (SQ and IV)
Warfarin (Orally)
Mechanism of actions :
a. Heparin
- prevents thrombin from converting fibrinogen to fibrin.
b. Warfarin
- suppress coagulation by acting as an
antagonist of vitamin K after 4-5 days.
Hemostasis :
Bleeding/injury
I
Vasoconstriction Plasminogen
I I
Platelet aggregation Plasmin
( temporary plug) I
I I
Clotting factor activation -------------- I
I I I
Intrinsic pathway (8,9,10,11,12) Extrinsic pathway (3,7,10) I
(PTT ) (PT) Vit K dep. I
I I I
I Prothrombin activation I I
I I
Thrombin I
I I
Fibrinogen ------------Fibrin threads ------------- Fibrin split products
(coagulation) ( Removed by liver & spleen )
Indications :
- thrombosis, pulmonary embolism, myocardial infarction
Adverse effect :
- bleeding
Nursing considerations :
1. HEPARIN sodium
- if given SQ don’t aspirate or rub the injection site (above the scapula - best site).
- therapeutic level 1.5-2.5 times normal PTT;
normal PTT is 20-35 sec. = 50-85 sec.
- antidote : (protamine sulfate)
Antiplatelet Medications
Prototype: aspirin, Dipyridamole (Persantin)
Clopidoigrel (Plavix), Ticlopidine
Mechanism of action :
- inhibit the aggregation of platelet thereby prolonging bleeding time.
Indications :
- used in the prophylaxis of long-term complication following M.I, coronary
revascularization, and thrombotic CVA.
Nursing considerations :
- Monitor bleeding time ( NV = 1-9 mins)
- Take the medication with food.
Cardiac Glycosides
Prototype:
- digoxin (Lanoxin) and digitoxin (Crystodigin)
Mechanism of actions :
- increase intracellular calcium, which causes the heart muscle fibers to contract more
efficiently, producing positive inotropic & negative chronotropic action.
Indications :
- use for CHF, atrial tachycardia and fibrillation
Nursing considerations :
- Monitor for toxicity as evidence by :
nausea, vomiting, anorexia, halo vision, confusion, bradycardia and heart blocks .
- Do not administer if pulse is less than 60 bpm.
- Should be caution in patient with hypothyroidism and hypokalemia.
- Antidote : Digi-bind
- Phenytoin is the drug of choice to manage
digitalis-induced arrhythmia.
Nitrates
Prototype :
- isosorbide dinitrate (Isordil)
- nitroglycerine (Deponit, Nitrostat)
Mechanism of action :
- produce vasodilatation including coronary artery.
Indications :
- angina pectoris, MI, peripheral arterial occlusive disease.
Adverse effects:
- headache, orthostatic hypotension .
Nursing Considerations :
1. Transdermal patch
- apply the patch to a hairless area using a new patch and different site each day.
- remove the patch after 12-24 hours, allowing 10-12 hours “patch free” each day to
prevent tolerance.
2. Sublingual medications :
- note the BP before giving the medication.
- offer sips of water before giving because dryness may inhibit absorption.
- one tablet for pain and repeat every 5 mins. for a total of three doses; if not relieved
after 15 mins., seek medical help.
- stinging or burning sensation indicates that the tablet is fresh.
- instruct patient not to swallow the pill
- sustained release medications should be swallowed and not to be crush.
- protect the pills from light.
Anti-arrhythmic Drugs
Class I (block Na channels)
IA - quinidine, procainamide
IB - lidocaine
IC - flecainamide
Class II (Beta-blockers)
propanolol, esmolol
Class III (block K channels)
amiodarone, bretylium
Class IV (block Ca channels)
verapramil, diltiazem
Nursing considerations :
1. Watch out for signs of CHF.
2. Have client weigh themselves and report
weight gain.
3. Watch out for signs of lidocaine toxicity :
- confusion and restlessness
Antilipemics
Prototype :
a. cholesterol-lowering agents
- cholestyramine, colestipol, lovastatin
b. triglyceride-lowering agents
- gemfibrozil, clofibrate
Mechanism of actions :
- interfere with cholesterol synthesis as well as
decreasing lipoprotein & triglyceride synthesis.
Nursing considerations :
- monitor liver functions while using statins.
- prevent constipation, flatulence, cholelithiasis
- encourage increase fluid and fiber intake.
ANTI – HYPERTENSIVE
Diuretics
- usually given at morning
CARBONIC ANHYDRASE INHIBITORS
- Acetazolimide (Diamox)
- increase Na+, K+, & HCO3 secretion, along with it is H2O
- metabolic acidosis
OSMOTIC DIURETIC
- Mannitol
- Increase osmotic pressure of the glomerular filtrate.
- hypotension
THIAZIDE DIURETICS
- hydrochlorothiazide
- blocks Na and K reabsorption; reabsorb Ca
- hypercalcemia
LOOP DIURETICS
- Furosemide (Lasix)
- blocks Na, K, and Ca reabsorption
- hypocalcemia
POTASSIUM SPARING DIURETICS
- Spironolactone (Aldactone)
- excrete Na and water but it reabsorb K
- hyperkalemia
RESPIRATORY MEDICATIONS
Bronchodilators
Prototype :
Symphatomimetic Xanthines
- albuterol, salbutamol - aminophylline
- isoproterenol, salmeterol - theophylline
- terbutaline
Mechanism of actions:
- sympathomimetic (b-receptor agonist) bronchodilators, dilate airways.
- xanthine bronchodilators, stimulate CNS for respiration.
Indications :
- bronchospasm, asthma, bronchitis, COPD.
Adverse effects :
- palpitations and tachycardia
- restlessness, nervousness, tremors
- anorexia, nausea and vomiting, headache, dizziness.
Nursing considerations :
- Contraindicated hyperthyroidism, cardiac dysrhythmia, or uncontrolled seizure
disorder.
- Should be used with caution in patient with HPN and narrow-angle glaucoma.
Glucocorticoids (Corticosteroids)
Prototype :
- dexamethasone, budesonide, fluticasone, prednisone, beclomethasone.
Mechanism of actions :
- act as anti-inflammatory agents and reduce edema of the airways, as well as
pulmonary edema.
Adverse effects :
- Cushing’s syndrome, neutropenia. osteoporosis
Nursing considerations :
- Take drugs at meal time or with food.
- Eat foods high in potassium, low in sodium.
- Instruct client to avoid individuals with RTI.
- Instruct client not to stop medication abruptly, it should be tapered to prevent
adrenal insufficiency
- Avoid taking NSAID while taking steroids.
- Take inhaled bronchodilators first before taking inhaled steroids, and rinse mouth
after using.
Mast Cell Stabilizers
Prototype : cromolyn sodium (Intal)
Mechanism of action :
- stabilize mast cells that release histamine triggering asthmatic attacks.
Nursing Consideration:
- Should be given before asthmatic attacks.
- Administer oral capsule at least 30 mins before meals for better absorption.
- Drink a few sips of water before & after inhalation to prevent cough & unpleasant taste
- Assess for lactose-intolerance.
Anti-tuberculosis
Prototype :
First line Second line
- Isoniazid (INH) - Cycloserine
- Rifampicin (Rifadin) - Kanamycin
- Ethambutol - Ethonamide
- Pyrazinamide - Para-aminosalicylic acid
- Streptomycin
- active tuberculosis are treated with drug combination for 6-9 mos.
- multidrug-resistant strain (MDR-TB) are medicated for 1 year up to 2 years
- given before meals
Isoniazid
- should be given 1 hr before or 2 hrs after meals because food may delay absorption.
- should be given at least 1 hr before antacids.
- instruct to notify physician for signs of hepatoxicity (jaundice), and neurotoxicity
numbness of extremities.
- administer with Vitamin B6 to counteract the neurotoxic side effects.
- avoid alcohol.
Rifampicin
- given on an empty stomach with 8 0z. of water, 1 hour before or 2 hours after meals
and avoid taking antacids with medications.
- hepatotoxic thus avoid alcohol.
- instruct the client that urine, feces, sweat, and tears will be red-orange in color.
Pyrazinamide
- given for 2 months.
- increase serum uric acid and cause photosensitivity.
Ethambutol
- contraindicated in children under 13 years old.
- obtain a baseline visual acuity because it can cause optic neuritis.
- Instruct the client to notify the physician immediately if any visual problems occurs.
Streptomycin
- aminoglycoside antibiotic given IM.
- nephrotoxic and ototoxic.
- obtain baseline audiometric test and repeat every 1-2 months because the
medications impairs the CN VIII.
DRUGS AFFECTING GASTROINTESTINAL SYSTEM
Antacids
Prototype :
- aluminum/magnesium compounds (Maalox)
- sodium bicarbonate (Alka-Seltzer)
- calcium carbonate (Tums)
- magnesium hydroxide (Milk of Magnesia).
Mechanism of actions :
- neutralize the stomach acidity.
Adverse effects :
- metabolic alkalosis, stone formation
- electrolyte imbalance
- diarrhea (magnesium), constipation (aluminum).
Nursing considerations :
- Give 1 hr after meals.
- Avoid giving medications within 1-2 hrs of antacid administration
(decreases absorption).
- Take fluids to flush after intake of antacid suspensions.
- Monitor for changes of bowel patterns.
Histamine – 2 blockers
Prototype :
- cimetidine (Tagamet), ranitidine (Zantac),
famotidine (Pepcid), nizatidine (Axid).
Mechanism of action:
- blocks H2 receptors in the stomach, reducing
acid secretions.
Nursing considerations :
- Given before or with meals
- Avoid giving other drugs with cimetidine
- Gynecomastia may developed with chronic use of cimetidine.
Anti-diarrheal Agents
Prototype :
- diphenoxylate (Lomotil), loperamide (Imodium), kaolin/pectin mixture (Kaopectate).
Mechanism of actions :
- decrease stomach motility and peristalsis.
Nursing considerations :
- Monitor for rebound constipation.
- Be cautious taking if with infectious diarrhea.
- Monitor atropine toxicity with diphenoxylate.
- Clay, white or pale stool is common with kaopectate.
Laxatives
a. lactulose (Cephulac), Na biphosphate (Fleet
enema) & magnesium salt (Milk of Magnesia)
- retain fluid and distend intestine
b. ducosate (Dialose)
- emulsify fecal fat and water
c. bisacodyl (Dulcolax) & senna (X-prep)
- irritates intestinal mucosa and
stimulate intestinal smooth muscles
d. bulk-forming laxative (Metamucil)
- increase fecal bulk and water content
e. mineral oil
- lubricates & prevent colon absorption
Emetics
Prototype : ipecac syrup, apomorphine
Mechanism of actions :
- induce vomiting through stimulation of vomiting center of medulla.
Indications :
- ingestion of poisonous or toxic substances.
Nursing considerations :
- Consult poison control center before induction of vomiting.
- Administer ipecac syrup with large amount of fluid.
DRUGS AFFECTING THE ENDOCRINE SYSTEM
Thyroid Agents
Prototype :
- Proloid (thryroglobulin )
- Synthroid (levothyroxine)
- Cytomel ( liothyronine).
Mechanism of action :
- function as natural or synthetic hormones.
Nursing considerations :
- Taken in the morning.
- Caution with coronary artery disease.
- Monitor for signs of hyperthyroidism and refer for decreasing the dose.
Parathyroid Agents
Prototype :
a. calcitonin (Calcimar), etidronate (Didronel),
b. calcitrol (Rocaltrol), calcifediol (Calcedrol)
Mechanism of action :
a. reduce bone resorption
b. promotes calcium absorption
Nursing considerations :
- Monitor signs of calcium imbalance
- Report for bone pains.
- Remain sitting upright after taking etidronate.
Oral Hypoglycemic Agents (OHA)
1. Sulfonylureas
- stimulate insulin secretions and increase tissue sensitivity to insulin.
First Generation :
Chlorpropamide (Diabenese)
- disulfiram precautions
Tolbutamide (Orinase)
- congenital defect
Second Generation :
Glypizide, Glymepiride
2. Biguanides
- facilitates insulin action on the peripheral receptor site.
Metformin and Glucophage (Glucovance)
- side effect is lactic acidosis
3. Alpha-glucosidase inhibitors
- delay carbohydrate absorption in the intestinal system.
Acarbose (Precose) – side effect is diarrhea
4. Thiazolinidine
- increase tissue sensitivity of insulin.
Rosiglitazone (Avandia)
5. Meglitinides
- stimulate insulin release in pancreatic B-cells.
Repaglinide (Prandin)
Nursing considerations :
- Effective only for type II DM.
- Contraindicated to pregnant & breastfeeding.
- Given before meals.
- Monitor for signs of hypoglycemia.
Insulin
Insulin Onset Peak Duration
Lactation Suppressants
Prototype :
- bromocriptine (Parlodel)
Mechanism of action :
- decrease serum prolactin levels
Adverse effects :
- drowsiness, headache, nausea, palpitations
DRUGS FOR TREATING INFECTION
Antibacterial Agents
1. Cell wall inhibitors
a. penicillins - pen G, amoxicillin, cloxacillin
b. cephalosphorins - cephalexin, cefaclor
c. glycopeptide - vancomycin
2. Protein synthesis inhibitors
a. aminoglycosides - amikacin, gentamycin
b. macrolide - erythromycins, roxithromycin
c. lincosamides - clindamycins
d. chloramphenicol, tetracyclines
3. Antimetabolites - blocks folic acid synthesis
a. Sulfonamides - cotrimoxazole
4. DNA synthesis inhibitors
a. quinolones - ciprofloxacin, ofloxacin
b. metronidazole
Adverse effects :
1. Aminoglycoside - nephrotoxicity & ototoxicity
2. Sulfonamides - Steven-Johnson’s syndrome, photosynsetivity
3. Quinolones - insomnia
4. Tetracyclines - bone problems
5. Chloramphenicol - Gray syndrome, bone marrow depression
6. Erythromycin - hepatitis
Nursing considerations :
1. Collect appropriate specimen for C & S before starting antibiotics.
2. Check client’s history of allergies.
3. Avoid administering erythromycin and quinolones with food.
4. Pregnant precautions.
5. Report for diarrhea - pseudomembranous colitis (clindamycin)
6. Monitor adverse effects.
Antiviral Agents
Prototype :
- acyclovir (Zovirax), ganciclovir (Cytovene),
vidarabine (Vira-A), amantidine (Symmetrel),
ribavirin (Virazole), zidovidine (Retrovir).
Mechanism of actions :
- inhibits virus specific enzymes involve in DNA
synthesis. They only control the growth of
virus but it does not cure.
Adverse effects :
- granulocytopenia, thrombocytopenia, nausea,
nervousness, headache, nephrotoxicity.
Nursing consideration :
- Pregnant and breastfeeding precautions.
- Administer IV antivirals to avoid crystallization in renal tubules.
- Give ribavirin only with aerosol generator.
- Monitor CBC and creatinine level.
- Refer for signs of bleeding.
- Take amantidine after meals.
Antifungal Agents
Prototype :
- amphotericin B (Fungisone), nystatin,
fluconazole (Diflucan), ketoconazole (Nizoral).
Mechanism of actions :
- inhibit the synthesis of fungal sterol.
Adverse effects :
- nephrotoxicity and neurotoxicity
- bone marrow depression
- chills, fever, joint pains, abdominal pain and headache.
Nursing considerations :
- Dilute amphotericin B with sterile water solution not with electrolyte solution.
- Tell clients that fever, chills, GI upset, joint and muscle pain will subside as
amphotericin B continues.
- With oral candidiasis, let nystatin tablet dissolve in mouth rather than swallowing it.
- Refrain ketoconazole with antacids.
- Report for signs of bleeding, infection & fatigue.
Antiparasitic agents
Prototype :
a. Antimalarial
- chlroquine, mefloquine, primaquine,
quinine, pyrimethamine
b. Antiamebiasis
- metronidazole (Flagyl), iodoquinol,
furozolidone (Furoxone).
Mechanism of actions :
a. antimalarial – alters protozoal DNA, depleting folates, & reducing nucleic acid
production
b. antiamoeba – block protein synthesis.
Nursing considerations :
1. Administer anti-malarial drugs with food.
2. Take seizure precautions while administering
antimalarial drugs.
3. Refer cinchonism during quinine treatment:
- tinnitus, headache, vertigo, fever, and visual changes.
4. Inform clients that iodoquinol falsify thyroid function test for up to 6 months.
Antihelmintic
Prototype :
- mebendazole (Vermox), thiabendazole,
niclosamide (Niclocide), piperazine (Antepar),
praziquantel (Biltricide).
Mechanism of actions :
- paralyze larva and adult helmints by acting on parasite microtubules.
Adverse effects :
- GI upset, urinary odor (thiabendazole)
- headache, dizziness, fatigue
Nursing considerations :
1. Treat all the family members for nematodes infection to prevent recurrence.
2. Praziquantel must swallowed rapidly because of its bitter taste to avoid gagging.
3. Other antihelmintics should be chewed.
ANTI-NEOPLASTIC DRUGS
General considerations :
- kills or inhibit the reproduction of neoplasmic cells but as well as normal cells.
- it could be cell cycle phase specific or cell cycle non-specific.
- preferably given through IV route.
Prototype :
1. Alkylating Agents
- inhibits cell production by causing cross linking of DNA
a. Busulfan – hyperuricemia
b. Chlorambucil – gonadal suppression
c. Cisplatin – ototoxicity and nephrotoxicity
d. Cyclophosphamide – hemorrhagic cystitis.
2. Antitumor Antibiotic Agents
- interfere in DNA and RNA synthesis
a. Plicamycin – affects bleeding time
b. Doxurubicin – cardiotoxicity
c. Bleomycin – pulmonary toxicity.
3. Antimetabolites
- replace normal proteins required for DNA synthesis by inhibiting the S phase
a. Cytarabine – hepatotoxicity
b. 5-flourouracil – phototoxicity reaction and cerebellar dysfunctions
c. 6-marcaptopurine – hyperuricemia
d. Methotrexate – photosensitivity
- given with leucoverin to lessen its toxicity.
4. Mitotic Inhibitors (Vinca Alkaloids)
- prevent mitosis acting on the M phase causing cell death
a. Vincristine sulfate – neurotoxicity, numbness
5. Hormonal Medications and Enzymes
- block the normal hormones in hormone sensitive tumors
a. Tamoxifen citrate – visual problems
– elevate cholesterol & triglycerides level
b. Diethylstilbestrol – impotence and gynecomastia in men.
Side Effects:
stomatitis
- bland diet, avoid strong mouthwash
- soft tooth brush, ice chips
diarrhea, nausea and vomiting
- anti-emetic, replace fluids and electrolytes
alopecia
- reassure that it is temporary
- encourage o wear wigs, hats and head scarf
skin pigmentation
- inform that it is only temporary
tumor lysis syndrome
- hyperuricemia & hyperkalemia
- force fluids
infection
- notify physician if WBC is <2000/mm3
- monitor for signs of infection
- reverse isolation
- low bacteria diet
anemia
- iron, B-12, folic acid rich food
- provide rest periods
bleeding
- avoid NSAIDs
- minimize invasive procedures
- use soft toothbrush and electric razor
menstrual changes
- reassure that menstruation will resume.
THE END