Pharmacology

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CNS and CVD Drugs

Drug Classification
Drugs Affecting CNS (Central Nervous System) and PNS (Peripheral Nervous System)
Peripheral Nervous System
1. Sensory
2. Motor
a. Voluntary
b. Involuntary ( Autonomic )
 Sympathetic
 Parasympathetic
Major Neurotransmitters
1. Acetylcholine - muscle contractions and parasympathetic
2. Norepinephrine & epinephrine - sympathetic
3. Serotonin - mood
4. Dopamine - involuntary motor
5. Prostaglandin - mediates pain
6. Enkephalin and endorphins - inhibits pain
7. GABA (Gamma Amino-Butyric Acid) – inhibitory

Cholinergic Agents (Parasympathomemitics)


Prototype :
- pilocarpine, donepezil (Aricept)
- carbachol, bethanechol (Urocholine)
- pyridostigmine (Mestinon)
neostigmine (Prostigmine)
edrophonium (Tensilon)
Myasthenia gravis
Mechanism of action :
- stimulates cholinergic receptors or inhibition of enzyme cholinesterase.
Indications :
- glaucoma, urine retention, Myasthenia Gravis, and Alzheimer’s
Adverse effects :
- blurring of vision due to miosis
- increase in salivation, intestinal cramps
- bronchoconstriction, wheezing, DOB
- hypotension and bradycardia
Nursing considerations :
1. While giving this drugs, prepare oxygen, suction machine and atropine.
2. Myasthenic medications given on the right time each day to prevent crisis
Myasthenic crisis - under dose
Cholinergic crisis - overdose

Cholinergic Blocking Agents (Parasympatholytics, Anticholinergics)


Prototype :
- atropine, scopalamine (Triptone), dicyclomine (Bentyl) and Hyoscine, propantheline (Pro-
Banthine), trihexyphenidyl (Artane), benztropine (Congentin)
Mechanism of actions :
- block the binding of acetylcholine
Indications :
- use preoperatively to dry up secretions.
- use for treatment of bradycardia
- given before cataract surgery and eye examination
- treat spasticity of GI or urinary tract.
- use for treatment of parkinsonism.
Adverse effects :
- dry mouth , dilatation of pupils,
- tachycardia, urinary retention, ileus
Nursing considerations :
1. Encourage clients to increase fluid intake and use of sugarless gum/candy for dry mouth.
2. Precautions with coronary artery disease.
3. High fiber diet

Adrenergic Agents (Sympathomimetics)


Prototype :
- epinephrine, norepinephrine, phenylephrine, ephedrine, dopamine, dobutamine, albuterol,
terbutaline, isoproterenol, salbutamol
Mechanism of actions :
- stimulate alpha and beta adrenergic receptor
Indications :
- cardiopulmonary arrest
- anaphylactic shock, cardiogenic shock
- COPD and asthma, nasal congestions
Adverse effects :
- restlessness, insomnia, tremors
- palpitations, angina pectoris, tachycardia, HPN
Nursing considerations :
- precautions in clients w/ hyperthyroidism, pheochromocytoma & CVD.

Adrenergic Blocking Agents


Prototype :
a. Alpha blockers - phentolamine (Regintine), clonidine (Catapress), methyldopa (Aldomet)
b. Beta blockers -
Selective - atenolol (Tenormin), metoprolol (Lopressor)
Non selective - nadolol (Corgard), propranolol (Inderal), timolol (Blocadren)
Mechanism of actions :
a. alpha blockers - inhibits action of a-receptors in vascular smooth muscle to cause vasodilatation.
b. beta blockers - compete with epinephrine in b-receptors in heart (B1) and pulmonary airways
(B2)
Indications :
- Raynaud’s disease, HPN, pheochromocytoma
- angina pectoris, arrhythmias, glaucoma
Adverse effects :
- orthostatic hypotension, bradycardia
- bronchospasm and dyspnea, nasal stuffiness
Nursing considerations :
1. Hold if apical pulse is below 60 bpm.
2. Hypotensive precautions.
- avoid long standing
- use of elastic stockings
- don’t rise standing up from bed quickly
- avoid warmth situations (warm bath)
Take precautions on COPD patients

Anticonvulsants
Prototype :
a. Hydantoins - phenytoin (Dilantin)
b. Barbiturates - phenobarbital ( Luminal)
c. Others or Miscellaneous - carbamazepine (Tegretol), diazepam, valproic acid (Dapakene)
Mechanism of action :
- treat seizures by depressing abnormal neuronal activity in motor cortex.
- increasing the effect of GABA
Adverse effects :
- sedation & drowsiness, dizziness
- gingival hyperplasia, cleft lip, urine discoloration (phenytoin)
- aplastic anemia and Steven-Johnson’s Syndrome (carbamazepine)
Nursing considerations :
1. Advise female clients to use contraceptives.
2. Inform clients taking phenytoin that harmless urine discoloration is common.
3. Protect phenytoin from light.
Avoid taking alcohol with barbiturates.

Antiparkinsonian Agents
 Degeneration of basal ganglia
 Decrease in dopamine
 Increase in acetylcholine
Prototype :
a. Anticholinergic agents
- propantheline (Pro-Banthine)
- trihexyphenidyl (Artane)
- benztropine (Congentin)
b. Dopaminergic agents
- Levodopa
- carbidopa-levodopa (Sinemet)
Nursing considerations :
1. Reassure client that levodopa may cause harmless darkening of urine and sweat.
2. Avoid taking Vit B6 (pyridoxine) with levodopa because it speed up metabolism.
3. Anticholinergic agents are used as antidote for EPS (extrapyramidal symptoms)of antipsychotic
drugs.

Hypnotics, Sedatives and Anxiolytics ( Minor Tranquilizer)


Prototype :
a. Benzodiazepines ZZZZZZZZZZZZZ
- diazepam (Valium), alprazolam (Xanax), lorazepam (Ativan) – drug of choice for SE
chlordiazepoxide (Librium) -delirium tremens
b. Barbiturates
- amobarbital, phenobarbital, secobarbital
c. Miscellaneous
- chloral hydrate (Noctec), Zolpidem (Stilnox)
Mechanism of actions :
- enhance GABA (gamma-amino butyric acid)
- depressing the RAS (reticular activating system)
Indications :
- induce sleep, sedate and calm clients
Adverse effects :
- hangover-effect, dizziness, CNS depression
- respiratory depression, drug-dependency
Nursing considerations :
1. Warn clients of injuries and falls.
2. Warn clients not to discontinue medications abruptly without consulting a physician.
3. Avoid alcohol while taking these drugs.
4. Prepare flumazenil for benzodiazepine toxicity
Antipsychotic drugs (Neuroleptics or Major Tranquilizer)
Prototype :
a. Phenothiazines
- chlorpromazine (Thorazine) trifluoperazine (Stelazine), thioridazine (Mellaril) and promethazine
(Phenergan)
b. Other Agents
- clozapine (Clozaril), haloperidol (Haldol)
Mechanism of action :
- block dopamine receptor in the limbic system, hypothalamus, and medulla oblongata.
Indications :
psychoses, vomiting and anxiety
Adverse effects :
- Extra-pyramidal symptoms such as dystonia, akinesia, pseudo-parkinsonism, and irreversible
tardive dyskinesia as manifested by :
a. lip smacking
b. fine wormlike tongue movement
c. involuntary movements of arms and leg.
Nursing considerations :
1. Teach family members the signs of EPS and report to physician immediately. In case with EPS,
prepare antidote :
(anti-cholinergic/anti-parkinsonism drugs)
a. propantheline (Pro-Banthine)
b. trihexyphenidyl (Artane)
c. benztropine (Cogentin)
d. diphenhydramine (Benadryl)
e. biperidine (Akineton)
2. Normalization of symptoms may not occur for several weeks after beginning of therapy

Antidepressants (Mood Elevators)


Prototype :
a. Tricyclic antidepressants (TCA)
- protriptyline (Vivactil), amitriptyline (Elavil)
- imipramine (Tofranil), desipramine
b. Monoamine oxidase inhibitors (MAOI)
- tranylcypromine (Pernate),
- isocarboxazid (Marplan), phenelzine (Nardil)
c. Selective serotonin reuptake inhibitors (SSRI)
- fluoxetine (Prozac)
d. Lithium
Adverse effects :
- hypertensive crisis (MAOI)
- dehydration, nausea and vomiting (Lithium).
Nursing considerations :
1. Explain to client that full response of TCA may take several weeks
2. Inform physician and withhold fluoxetine if client develop rashes.
3. Client taking MAO inhibitors should avoid tryptophan or tyramine-rich foods to avoid
hypertensive crisis.
- aged cheese, sour cream, yogurt, beer, wine, chocolate, soy sauce and yeast
- phentolamine (Regintine) an a-blocker for hypertensive crisis.
4. Take lithium with food to reduce GI effects
- > 1.5 mEq/L blood level may cause toxicity manifested by tremors, lethargy, seizure (manage by
diuretics and dialysis)
- maintain salt and adequate fluid intake
Analgesics (Pain reliever)
Prototype :
a. Narcotic analgesics (CNS) – hydrocodone, codeine, meperidine (Demerol), morphine,
butorphanol (Stadol), nalbuphine (Nubain)
b. Non – narcotic analgesic (PNS)
 NSAIDs - aspirin (Aspilet), naproxen mefenamic acid (Ponstan), ibuprofen, ketoprofen (Orudis),
coxibs
 steroids
c. Miscellaneous
paracetamol and acetaminophen (Tylenol)
Mechanism of actions :
a. Narcotic analgesics - alter pain perception by binding to opioid receptors in CNS.
b. Non- narcotic analgesic - relieves pain and fever by inhibiting the prostaglandin pathway.
Nursing considerations :
1. Monitor respiratory depression & hypotension
2. Accident precautions in narcotic analgesic.
3. Warn clients about possibility of dependency, and do not discontinue narcotics abruptly in the
narcotic-dependent clients.
a. opiates overdose symptoms :
- morphine overdose cause pupil constriction
Naloxone is antidote for narcotic overdose.
4. Advice clients to take NSAIDs and steroids with food and monitor bleeding complications.
5. Aspirin is contraindicated in clients below 18 years old with flu-like symptoms & pregnant.
6. Monitor hearing loss in clients taking aspirin and ibuprofen.
7. Monitor liver function in clients taking acetaminophen.
8. N-acetylcysteine (mucolytic) is antidote for paracetamol and acetaminophen overdose.
- It should be taken with flavored iced drink through a straw to disguised its pervasive flavor of a
rotten egg

Drugs Affecting Cardiovascular System

Anticoagulants
Prototype :
- Heparin (SQ and IV)
- Warfarin (Orally)
Mechanism of actions :
- they prevent clot formation
Indications :
- thrombosis (DVT)
- pulmonary embolism
- myocardial infarction
Adverse effect :
- bleeding
Nursing considerations :
1. HEPARIN sodium
- if given SQ don’t aspirate or rub
- therapeutic level 1.5-2.5 times normal PTT
- normal PTT is 20-35 sec. = 50-85 sec.
- antidote : (protamine sulfate)
2. WARFARIN sodium (coumadin)
- warfarin is used for long-term .
- onset of action is 4-5 days.
- therapeutic level is 1.5-2.0 times normal PT; normal PT = 9.6 -11.8 sec. = 20 – 24 sec.
- should be taken at the same time of the day to maintain at therapeutic level.
- reduce intake of green leafy vegetables.
- antidote : Vitamin K ( Aquamephyton)

Thrombolytics
Prototype :
Streptokinase, Urokinase
Mechanism of actions :
- activates plasminogen to generates plasmin (enzyme that dissolve clots).
Indications :
- use early in the course of MI (within 4-6 hours of the onset)
Nursing considerations :
- monitor bleeding
- antidote : Aminocaproic acid

Cardiac Glycosides
Prototype:
- digoxin (Lanoxin)
- digitoxin (Crystodigin)
Mechanism of actions :
- increase intracellular calcium, 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 <60
- Should be caution in patient with hypokalemia
- If > 12 hours missing the dose, don’t give a double dose on the next dose.
- Antidote : Digi-bind

Nitrates
Prototype :
- isosorbide dinitrate (Isordil), isosorbide mononitrate (Imdur)
- nitroglycerine (Deponit, Nitrostat)
Mechanism of action :
- produce vasodilatation including coronary artery
Indications :
- angina pectoris and MI (myocardial infarction)
Adverse effects: (3 H’s)
- headache, hypotension
Nursing Considerations :
1. Transdermal patch
- apply the patch to a hairless area and free of skin-folds
- remove the patch after 12-14 hours, to prevent tolerance.
- rotate the application site
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
minutes, seek medical help.
- stinging or burning sensation indicates that the tablet is fresh.
- sustained release medications : should be swallowed and not to be crash.
- protect the pills from light.
Antihypertensive Drugs
Angiotensin-Converting Enzyme (ACE) Inhibitors
Prototype :
captopril (Capoten), enalapril (Vasotec), quinapril, lisinopril
Mechanism of actions :
- prevent peripheral vasoconstriction by blocking conversion of angiotensin I to angiotensin II
decreasing peripheral resistance.
Indications :
- hypertension, CHF (decrease afterload)
Adverse effect :
- it cause hyperkalemia
- induce chronic cough
Nursing considerations :
- precautions in patients with COPD
- for hyperkalemia :
a. avoid using K+ sparing diuretics.
b. avoid potassium rich food : banana, oranges, potato
c. can give insulin and glucose
d. Kayexalate enema ( Na polysterene sulfonate)

Angiotensin II Receptor Blockers (ARB)


Prototype :
valsartan , irbesartan, olmesartan, losartan, eprosartan, telmisartan
Mechanism of action :
block the receptors of angiotensin II causing the same effects with ACE – inhibitors
Indications :
good for hypertensive type II diabetes mellitus because it protect the renal system
Nursing considerations :
- same with ACE - inhibitors

Calcium-Channel Blockers
Prototype :
- nifedipine (Calcibloc, Adalat, Procardia), amlodipine (Norvasc), felodipine (Plendil), verapramil
(Isoptin), diltiazem
Mechanism of action :
- decrease cardiac contractility and the workload of the heart, thus decreasing the need for O2.
- it also promote vasodilatation of the coronary and peripheral vessels.
Indications :
- hypertension, angina, arrhythmia
Adverse effects :
- bradycardia, hypotension, headache
- reflex tachycardia, constipation
Nursing considerations :
- Administer between meals to enhance absorption.
- Take client’s pulse rate before each dose; withhold if pulse is below 60 bpm.
- Refer for signs of congestive heart failure.

Diuretics (Water pill)


- usually given at morning
CARBONIC ANHYDRASE INHIBITORS
- Acetazolamide (Diamox)
- increase Na+, K+, & HCO3 secretion, along with it is H2O
- metabolic acidosis

OSMOTIC DIURETIC
- Mannitol (Osmitrol)
- Increase osmotic pressure of the glomerular filtrate.
- hypotension
THIAZIDE DIURETICS
- hydrochlorothiazide
- blocks Na and K reabsorption; reabsorb Ca
- hypercalcemia
LOOP DIURETICS
- Furosemide, Bumetanide - most potent
- blocks Na, K, and Ca reabsorption
- hypocalcemia
POTASSIUM SPARING DIURETICS
- Spironolactone (Aldactone)
- excrete Na and water but it reabsorb K
- hyperkalemia
Nursing considerations :
- Mannitol decreases ICP by reduce cerebral edema.
- Before giving furosemide and thiazides, check BUN and K level.
- Give IV potassium (KCl) in case of hypokalemia
a. don’t give IV bolus
b. watch out for cardiac arrest and thrombophlebitis
Give IV calcium (Ca gluconate ) in case of hypocalcemia
a. monitor cardiac rate before and during administration

Respiratory and Digestive Drugs

Respiratory Drugs
Bronchodilators
Prototype :
Sympathomimetic Xanthine
- albuterol, salbutamol
- aminophylline
- isoproterenol, salmeterol
- theophylline
- terbutaline
Mechanism of actions:
- sympathomimetic bronchodilators (b-receptor agonist) dilate airways.
- xanthine bronchodilators, stimulate CNS to increase respiratory drive.
Indications :
- bronchospasm, asthma, bronchitis, COPD.
Adverse effects :
- palpitations and tachycardia
- restlessness, nervousness, tremors
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, reduce airway and pulmonary edema.
Adverse effects :

- Cushing’s syndrome, neutropenia, growth retardation, hypertension, GI bleeding, hyperglycemia,


bone demineralization, adrenal suppression.
Nursing considerations :
- Take drugs at meal time or with food.
- Eat foods high in potassium, low in sodium.
- Instruct client to avoid individuals with infections.
- Instruct client not to stop medication abruptly, it should be tapered to prevent adrenal
insufficiency
- Take inhaled bronchodilators first before taking inhaled steroids, and rinse mouth after using.
- Regular eye examination & growth monitoring.

Anti-histamines (H-1 blockers)


Protoytype
 Brompheniramine (Dimetapp),
 Chlorphineramine (Antamin),
 Cetirizine (Iterax), Celestamine (Tavist),
 Diphenhydramine (Benadryl),
 Loratidine (Claritin) less hypnotic effect
Mechanism of action :
- decrease nasopharyngeal secretions and decrease nasal itching by blocking histamine in H1-
receptor.
Indications :
- common colds, rhinitis, urticaria, allergies sleeplessness, nausea and vomiting, EPS
(diphenhydramine).
Nursing Considerations :
- Precautions in handling machine and driving .
- Ice chips or candy for dry mouth
- H1 blockers are withhold for 3 days if patient is for skin test.

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.

Expectorant
Prototype :
guaifenesin (Robitusin Expectorant)
Mechanism of action:
- increase production of respiratory tract fluids
Indications :
- COPD, bronchitis, minor bronchial irritation

Antitussives
Prototype :
dextromethrophan
codeine & hydrocodone
Mechanism of actions :
- suppress the cough center in the medulla
Indications :
- for irritating, dry and exhausting cough
- before bronchoscopy

Adverse reactions :
- dizziness, addiction, respiratory arrest
Nursing considerations :
- not all cough should be suppress.
- opioids antitussive should be used cautiously in the patient with current or previous opioids
addiction.
- monitor for bradypnea.

Anti-tuberculosis
Prototype :
First line
- Rifampicin (Rifadin) - Red - orange
- Isoniazid (INH) - Neurotoxic/ hepatoxic - Vit B 6 (pyridoxine)
- Pyrazinamide - Pain in joints
- Ethambutol - Eye problem
- Streptomycin - Renal and ototoxic
a. Active tuberculosis are treated with drug combination for 6-9 mos.
b. Multi drug-resistant strain (MDR-TB) are treated for 1 year up to 2 years

Gastro-intestinal Drugs
Antacids
Prototype :
- aluminum/magnesium OH (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).
- 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.

Proton – Pump Inhibitors (PPI)


Prototype :
- omeprazole (Losec), Lansoprazole (Lanz), pantoprazole (Pantoloc)
Mechanism of action :
- inhibit the proton H+ to combine with Cl- to form hydrochloric acid
Nursing considerations :
- Given before meals

Mucosal Barriers
Prototype :
- sucralfate (Carafate)
- misoprostol (Cytotec)
Mechanism of action :
- coats the mucosa to prevent ulcerations
Nursing consideration :
- Given before meals
- Misoprostol is contraindicated for pregnant
- Sucralfate cause constipation.

Anti-diarrheal Agents
Prototype :
- diphenoxylate (Lomotil),
- loperamide (Imodium)
- kaolin/pectin mixture (Kaopectate)
Mechanism of actions :
- decrease GI motility and peristalsis
Nursing considerations :
- monitor for rebound constipation.
- be cautious taking if with infectious diarrhea.

Laxatives
Hyperosmolar laxatives
- lactulose (Cephulac), Na biphosphate (Fleet enema)
- magnesium salt (Milk of Magnesia)
Emollient laxatives (stool softeners)
- ducosate (Dialose)
Stimulant laxatives
- bisacodyl (Dulcolax), senna (X-prep), castor oil
Bulk-forming laxatives
- psyllium (Metamucil), methyllcelulose
Lubricant laxatives - mineral oil
Nursing considerations :
- Laxatives should not be used for long term therapy.
- Maintain stools to 2-3 times per/day
- Maintain fluid intake while on laxatives
- Abdominal discomfort is expected particularly in stimulant laxative.

Emetics
Prototype :
ipecac syrup, apomorphine
Mechanism of actions :
- stimulates the vomiting center in medulla
Indications :
- ingestion of poisonous or toxic substances
Nursing considerations :
- Consult poison control center before induction of vomiting (not use for corrosive poisoning)

Antiemetic
Prototype :
antihistamine - diphenhydramine, meclizine, trimethobenzamide
phenothiazine - chlorpromazine, promethazine

serotonin receptor antagonist - ondansteron


miscellaneous – metoclopramide
Mechanism of action :
they block the dopamine and serotonin receptor in the chemoreceptor trigger zone
Indications :
- Meniere’s disease and motion sickness (antihistamine)
- Post-operative and post-chemotherapy
induced nausea and vomiting (phenothiazine and serotonin antagonist)
Adverse effects :
- depression Endolymphatic
Hydrops
 Vertigo
 Tinnitus
 Hearing loss

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