PHARMACOLOGY Pharmacology - most simply defined as study of drug. Fundamentals of Pharmacology 1.

Pharmacokinetics - study of drugs 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 Safety and Efficacy Nursing Principles : 1. Always verify the Five Rights . a. the right medications b. the right client c. the right dosage d. the right form, route and technique e. the right time 2. Chart drug administration only after its been given, never before. 3. Never leave the medication on cart or tray unattended. 4. Chart observed therapeutic and adverse effects accurately and fully. 5. Check history for allergies and potential drug interactions before administering a newly ordered drug. 6. Inform the prescribing physician of any observed adverse effects; if cannot be located, inform the nursing supervisor 7. Question drug orders that are unclear, that appear to contain errors, or that have potential to harm. 8. Take the following actions if an error occurs : a. immediately notify the nursing supervisor, the prescribing physician, and the pharmacist. b. assess the clients condition and provide any necessary care. 9. For postpartum women, advice to take drugs after breastfeeding. Administration of Drugs : Routes and Nursing considerations: 1. Enteral oral, sublingual, rectal, gastric tubes - capsulated pill, sustained release and enteric coated should not be crushed. 2. Parenteral IV, IM, SQ, ID, IT, IA, epidural. - vastus lateralis (safest site for IM) 3. Topical skin, inhalants, mucus membrane. 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 DRUGS AFFECTING THE CENTRAL AND AUTONOMIC SYSTEM Cholinergic Agents(Parasympa thomemitics )

Prototype : - synthetic acetylcholine, pilocarpine, carbachol, bethanecol (Urocholine), edrophonium (Tensilon), neostigmine (Prostigmine), pyridostigmine (Mestinon). Mechanism of action : - stimulates cholinergic receptors by mimicking acetylcholine or inhibition of enzyme cholinesterase. Indications : - glaucoma, urine retention, Myasthenia Gravis - antidote to neuromuscular blocking agents : tricyclic antidepressants and atropine Adverse effects : - blurring of vision, miosis - increase in salivation, intestinal cramps - bronchoconstriction, wheezing, DOB - hypotension and bradycardia Nursing considerations : 1. Warn & monitor clients of the side effects. 2. Have atropine available for use as antidote. Cholinergic Blocking Agents (Parasympatholytics, Anticholinergics) Prototype : - atropine, scopalamine (Triptone), dicyclomine (Bentyl), propantheline (Pro-Banthine). Mechanism of actions : - block the binding of acetylcholine in the receptors of parasympathetic nerves. Indications : - use preoperatively to dry up secretions. - treat spasticity of GI or urinary tract. - use for treatment of bradycardia, asthma, parkinsonism. - use for antidote in organophosphate poisoning. Adverse effects : - dry mouth , dilatation of pupils, tachycardia - urinary retention, ileus, heat stroke Nursing considerations : 1. Keep clients in cool environment. 2. Watch out for signs of heatstroke and dehydration. 3. Encourage clients to increase fluid intake and use of sugarless gum/candy for dry mouth. 4. For GI spasticity, administer 30 minutes before meals and at bed time. Adrenergic Agents(Sympa thomimetics ) Prototype : - epinephrine, norepinephrine, ephedrine, dopamine, dobutamine, phenylephrine, terbutaline, albuterol, isoproterenol. Mechanism of actions : - stimulate alpha and beta adrenergic receptor directly or trigger the release of catecholamines indirectly causing sympathetic effects. Indications : - cardiopulmonary arrest, hypotension - COPD and asthma, nasal congestions - allergic reaction, anaphylactic shock Adverse effects : - restlessness, insomnia, tremors, nausea - palpitations, angina, tachycardia, HPN Nursing considerations : 1. Contraindicated in clients w/ hyperthyroidism, pheochromocytoma & cardiovascular disease. 2. Monitor vital signs and advice precautions. 3. Should be taken with food. Adrenergic Blocking Agents Prototype : a. Alpha blockers - phentolamine (Regintine), phenoxybenzamine, prazosin (Minipress), reserpine (Serpasil), terazosin (Hytrin) - clonidine (Catapress), methyldopa (Aldomet) b. Beta blockers

- atenolol (Tenormin), esmolol (Brevibloc), metoprolol (Lopressor), nadolol (Corgard), propanolol (Inderal), timolol ( Blocadren) Mechanism of actions : a. alpha blockers Prototype : a. Hydantoins - phenytoin (Dilantin) b. Barbiturates - phenobarbital ( Luminal) c. Miscellaneous 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. Dont 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. DRUGS AFFECTING MENTAL FUNCTIONING Sedatives, Hypnotics, and Anxiolytics Prototype : a. Benzodiazepines - diazepam (Valium), lorazipam (Ativan), alprazolam (Xanax), flurazepam (Dalmane) b. Barbiturates - amobarbital, phenobarbital, secobarbital c. Miscellaneous - chloral hydrate (Noctec), buspirone (Buspar), paraldehyde (Paral) Mechanism of actions :

a. Benzodiazepines - increase the effect of inhibitory neuro transmitter GABA (gamma-amino butyric acid) b. Barbiturates and Miscellaneous agents - depress CNS Indications : - induce sleep, sedate and calm clients Adverse effects : - hangover-effect, dizziness, CNS depression - respiratory depression, drug-dependence Nursing considerations : 1. Warn clients of injuries and falls. 2. Brief period of confusion and excitement upon waking up is common with benzodiazepines. 3. Warn clients not to discontinue medications abruptly without consulting a physician. 4. Avoid alcohol while taking these drugs. 6. Rotate and dont shake the ampules of barbiturates. Dont mix with other drugs. 7. Warn female clients that diazepam is associated with cleft lip. ANTIDEPRESSANTS AND MOOD DISORDER DRUGS Prototype : a. Tricyclic antidepressants - amitriptyline (Elavil), protriptyline (Vivactil), - imipramine (Tofranil), desipramine b. MAO (monoamine oxidase inhibitors ) - isocarboxazid (Marplan), phenelzine (Nardil), tranylcypromine (Pernate) c. Second-generation antidepressants - fluoxetine (Prozac), trazodone (Desyrel) d. Lithium Mechanism of actions : a. Tricyclic antidepressants - increase receptor sensitivity to serotonin and/or norepinephrine. b. MAO inhibitors - inhibit the enzyme MAO that metabolize the neurotransmitters norepinephrine and serotonin. c. Second generation antidepressants - inhibits the reuptake of serotonin. d. Lithium - increase serotonin & norepinephrine uptake Adverse effects : - dry mouth, blurred vision, urine retention, constipation (anticholinergic effects) - orthostatic hypotension, insomnia - hypertensive crisis (MAO) - dehydration (Lithium). Nursing considerations : 1. Caution client to rise slowly to reduce the effects of orthostatic hypotension. 2. Take antidepressant with food to enhance absorption 3. Explain to client that full response may take several weeks (2 weeks). 4. Assess client for constipation resulting from tricyclic antidepressant use. 5. Client taking MAO inhibitors should avoid tyramine-rich foods to avoid hypertensive crisis. - aged cheese, sour cream, yogurt, beer, wine, chocolate, soy sauce and yeast - pentholamine (Regintine) is the drug of choice for hypertensive crisis. - carbamazepine (Tegretol), diazepam, clorazepate (Tranxene), valproic acid (Dapakene), ethosuximide (Zarontin). Mechanism of action : - cause CNS depression, by producing loss of consciousness, unresponsiveness to pain stimuli, and muscle relaxation. 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. LOCAL AND TOPICAL ANESTHETIC Prototype : local : bupivacaine, lidocaine, tetracaine, procaine, mepivacaine, prilocaine topical : benzocaine, butacaine, dibucaine,lignocaine Mechanism of action : - block transmission of impulses across nerve cell membrane. Adverse effects : - cardiac dysrhythmias Nursing considerations : - lignocaine + prilocaine (EMLA cream) should be applied topically 60 minutes before procedure. - administer cautiously to the areas of large broken skin. - observe for fetal bradycardia in pregnant clients. ANALGESICS Prototype : a. Narcotic analgesics - codeine, meperidine (Demerol) morphine, butorphanol (Stadol) nalbuphine (Nubain) b. Non narcotic analgesic NSAIDs aspirin (aminosalicylic acid), mefenamic acid (Ponstan), ibuprofen (Motrin), naproxen, ketoprofen (Orudis), ketorolac. paracetamol and acetaminophen (Tylenol) Mechanism of actions : a. Narcotic analgesics - alter pain perception by binding to opiod receptors in CNS. b. Non- narcotic analgesic - relieves pain and fever by inhibiting the prostaglandin pathway. Nursing considerations : 1. Monitor respiratory depression & hypotension in clients taking narcotic analgesic. 2. Injury and accident precautions in clients taking narcotic analgesic. 3. Warn clients about possibility of dependency,and do not discontinue narcotics abruptly in the arcotic-dependent clients. 4. Naloxone is antidote for narcotic overdose. 5. Advice clients to take NSAIDs with food and monitor bleeding complications. 6. Aspirin is contraindicated in clients below 18 years old with flu-like symptoms. 7. Monitor hearing loss in clients taking aspirin. 8. Monitor liver function in clients taking acetaminophen. 9. N-acetylcysteine is antidote for paracetamol overdose. DRUGS AFFECTING THE CARDIOVASCULAR SYSTEM 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. Indications : - thrombosis, pulmonary embolism, myocardial infarction Adverse effect : - bleeding Nursing considerations : 1. HEPARIN sodium - if given SQ dont 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)

2. WARFARIN sodium (coumadin) - warfarin is used for long-term HEMOSTASIS : Bleeding/injury Vasoconstriction Plasminogen Platelet aggregation Plasmin ( temporary plug) Clotting factor activation-- --- --- --- --Intrinsic pathway (8,9,10,11,12) Extrinsic pathway (3,7,10) (PTT ) (PT) Vit K dep. Prothrombin activation Thrombin Fibrinogen- --- --- --- --Fibrin threads- --- --- --- --- Fibrin split products (coagulation) ( Removed by liver & spleen - onset of action is 4-5 days. - therapeutic level is 1.5-2.5 times normal PT; normal PT = 9.6 -11.8 sec. = 25 - 30 sec. INR = 2 - 3 - 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 : Aminocarpic acid 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.