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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 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 client’s 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 (Parasympathomemitics) 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 client’s 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 (Sympathomimetics) 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 - inhibits action of a-receptors in vascular smooth muscle to cause vasodilatation. b. beta blockers - compete with epinephrine in b-receptors in heart, pulmonary airways, peripheral circulation and CNS. Indications : - Raynaud’s disease, hypertension, pheochromocytoma. - angina, arrhythmias, mitral valve prolapse, glaucoma Adverse effects : - orthostatic hypotension, bradycardia, CHF - depression, insomnia and vertigo - bronchospasm and dyspnea, nasal stuffiness, cold extremities Nursing considerations : 1. Administer oral alpha-blockers with milk to minimize GI side effects. 2. Administer oral beta-blockers before meals and at a.m. if insomnia occurs. 3. Check client’s apical pulse rate before drug administration, refer if below 60 bpm. 4. Hypotensive precautions. 5. Warn clients not to drive or operate dangerous machinery until he/she has adjusted to medications. Prototype : Skeletal Muscle Relaxants Agents - methacarbamol (Robaxin), baclofen (Lioresal), dantrolene (Dantrium), metaxalone (Skelaxin), orphanedrine (Norgesic), chlorzoxazone Mechanism of actions: - depress CNS - inhibit calcium ion release in the muscle - enhance the inhibitory action of GABA (gamma-amino butyric acid) Indications : - for acute musculoskeletal pain - for muscle spasticity associated with multiple sclerosis, cerebral palsy, CVA, and spinal cord injury. Adverse effects : - hypotonia, ataxia, hypotension, drowsiness - blurred vision, bradycardia, depression, urine retention Nursing considerations : 1. Caution clients that mental alertness may be impaired. 2. Monitor neuromuscular status, bowel and bladder functions. 3. Inform clients that maximum benefit of baclofen is attained for 1-2 months. 4. Reduce baclofen dosage gradually because of associated withdrawal symptoms : Confusion, hallucinations, paranoia & rebound spasticity. 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. Prototype : ANTIPARKINSONIAN AGENTS 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. 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 don’t shake the ampules of barbiturates. Don’t 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 - incr...
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