Pharmacology Mnemonics - Flash Cards

Name: Losartan (Cozaar)

Class: Angiotensin II Antagonist

Mechanism: Competitive inhib. of angiotensin II ® smooth muscle relaxation (vasodilation), ¯ Na⁺ & H₂0, ¯ plasma volume ® ¯ BP.

Absorption: Oral.

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Toxicity/S.E.s: Hyperkalemia, fetal toxicity (c/i in 2^nd & 3^rd trimesters).

Utility: Treat hypertension.

Special Features: Angioneurotic edema and dry cough of ACE inhibitors not manifested.

Name: Lisinopril (Zestril, Prinivol)

Class: ACE Inhibitor

Mechanism: Inhib. production of angiotensin II ® block of vasoconstriction and aldosterone stim. ® ¯ TPR, ¯ Na⁺/H₂0 retention ® ¯ BP. Also blocks inactivation of bradykinin ® vasodilation. Diminishes normal ­ in epinephrine and aldosterone seen in CHF.

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Toxicity/S.E.s: Postural hypotension, renal insufficiency, hyperkalemia, persistent dry cough, rash, angioneurotic edema. C/i in 2^nd & 3^rd trimesters of pregnancy. Prob. not a great idea for 1^st trimester either.

Utility: Treat HTN, CHF, MI.

Special Features: Lysine derivative of enalaprilat.

Name: Enalapril (Vasotec)

Class: ACE Inhibitor

Mechanism: Inhib. production of angiotensin II ® block of vasoconstriction and aldosterone stim. ® ¯ TPR, ¯ Na⁺/H₂0 retention ® ¯ BP. Also blocks inactivation of bradykinin ® vasodilation. Diminishes normal ­ in epinephrine and aldosterone seen in CHF.

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Toxicity/S.E.s: Postural hypotension, renal insufficiency, hyperkalemia, persistent dry cough, rash, angioneurotic edema. C/i in 2^nd & 3^rd trimesters of pregnancy. Prob. not a great idea for 1^st trimester either.

Utility: Treat HTN, CHF, MI.

Special Features: Inactive prodrug. Converted to enalaprilat (acts like captopril).

Name: Captopril (Capoten)

Class: ACE Inhibitor

Mechanism: Inhib. production of angiotensin II ® block of vasoconstriction and aldosterone stim. ® ¯ TPR, ¯ Na⁺/H₂0 retention ® ¯ BP. Also blocks inactivation of bradykinin ® vasodilation. Diminishes normal ­ in epinephrine and aldosterone seen in CHF.

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Toxicity/S.E.s: Postural hypotension, renal insufficiency, hyperkalemia, persistent dry cough, rash, angioneurotic edema. C/i in 2^nd & 3^rd trimesters of pregnancy. Prob. not a great idea for 1^st trimester either.

Utility: Treat HTN, CHF, MI.

Special Features:

Name: Labetalol (Trandate)

Class: Nonselective b and a1 Blocking Agent

Mechanism: Competitive blockade of b1, b2, and a receptors.

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Toxicity/S.E.s: CV—orthostatic hypotension, sexual dysfxn, bradycardia, c/i for AV block. Resp—c/i in asthmatics, COPD, bronchitis, allergic rhinitis. Metabolism—caution w/diabetics (masks sign of hypoglycemia: tachycardia). CNS—weakness, fatigue, nightmares, depression. GI—n/v (uncommon). Hypersens—rash, hematologic disorders (rare). Also a effects.

Utility: Hypertension (¯ CO ® ¯ BP; blocks renin release). Angina pectoris (prophylactic ® ­ exercise tolerance due to ¯ O₂ demand). Cardiac arrhythmias (esp. supravent. tachyarrhyths). Acute MI (prophylaxis and reduction of infarct size and failure). Pheochromocytoma (in comb. w/alpha blocker). Essential tremor. Migraine headache (prophylaxis). Performance anxiety.

Features: Abrupt w/drawal may trigger MI. More a side effects. Widely used.

Name: Metoprolol (Lopressor)

Class: Cardioselective b1-Blocking Agent

Mechanism: Selective blockade of b1 (heart, kidney) w/rel. sparing of b2. No a effect.

Absorption: Good oral (>95%). Bioavailability ~50%. Plasma levels vary 10x btwn. patients.

Dist.: 12% bound to protein. Metabolism.: Hepatic Excretion, t½: Short t½ (3-4 hr).

Toxicity/S.E.s: CV—hypotension, bradycardia, c/i for AV block. Resp—c/i in asthmatics, COPD, bronchitis, allergic rhinitis. Metabolism—caution w/diabetics (masks sign of hypoglycemia: tachycardia). CNS—weakness, fatigue, nightmares, depression. GI—n/v (uncommon). Hypersens—rash, hematologic disorders (rare).

Utility: Hypertension (¯ CO ® ¯ BP; blocks renin release). Angina pectoris (prophylactic ® ­ exercise tolerance due to ¯ O₂ demand). Cardiac arrhythmias (esp. supravent. tachyarrhyths). Acute MI (prophylaxis and reduction of infarct size and failure). Pheochromocytoma (in comb. w/alpha blocker). Essential tremor. Migraine headache (prophylaxis). Performance anxiety.

Name: Pindolol (Visken)

Class: Nonselective b-Blocking Agent (Partial Agonist)

Mechanism: Partial agonists of b1 and b2 receptors. No a effect. Some intrinsic sympathomimetic activity.

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Toxicity/S.E.s: Mild chronic fatigue, low exercise tolerance, sedation, nightmares, depression, ­ airway resistance (b2 effect).

Utility: Hypertension (esp. HTN w/moderate bradycardia).

Special Features: Much less effect on HR and CO compared to other b-blockers. Less disturbance of lipid and carbohydrate Metabolism. compared to other b-blockers.

Name: Timolol (Blocadren)

Class: Nonselective b-Blocking Agent

Mechanism: Competitive blockade of b1 and b2 receptors. No a effect.

Absorption: Good oral (>90%). High bioavailability ~75%. Plasma levels vary 7x btwn. patients. b-blocking plasma conc. 5-10 ng/mL (low). Eye drops.

Dist.: 10% bound to protein. Excretion, t½: Hepatic, renal. Short t½ (3-4 hr).

Toxicity/S.E.s: CV—hypotension, bradycardia, c/i for AV block. Resp—c/i in asthmatics, COPD, bronchitis, allergic rhinitis. Metabolism—caution w/diabetics (masks sign of hypoglycemia: tachycardia). CNS—weakness, fatigue, nightmares, depression. GI—n/v (uncommon). Hypersens—rash, hematologic disorders (rare).

Utility: Hypertension (¯ CO ® ¯ BP; blocks renin release). Angina pectoris (prophylactic ® ­ exercise tolerance due to ¯ O₂ demand). Cardiac arrhythmias (esp. supravent. tachyarrhyths). Acute MI (prophylaxis and reduction of infarct size and failure). Pheochromocytoma (in comb. w/alpha blocker). Essential tremor. Migraine headache (prophylaxis). Performance anxiety. Eyedrops for open-angle glaucoma (¯ production of aqueous humor).

Spec. Features: Abrupt w/drawal may trigger MI. 6-10x as potent orally as others.

Name: Nadolol (Corgard)

Class: Nonselective b-Blocking Agent

Mechanism: Competitive blockade of b1 and b2 receptors. No a effect.

Absorp.: Poor oral (>30%). Low bioavail: ~30%. Plasma levels vary 7x btwn. pts.

Dist.: 30% bound to protein.

Metabolism.: Excretion, t½: Renal. Long t½ (14-24 hr). Unchanged in urine.

Toxicity/S.E.s: CV—hypotension, bradycardia, c/i for AV block. May exacerbate angina (unopposed a receptor action). Resp—c/i in asthmatics, COPD, bronchitis, allergic rhinitis. Metabolism—caution w/diabetics (masks sign of hypoglycemia: tachycardia). CNS—weakness, fatigue, nightmares, depression. GI—n/v (uncommon). Hypersens—rash, hematologic disorders (rare).

Utility: Hypertension (¯ CO ® ¯ BP; blocks renin release). Angina pectoris (prophylactic ® ­ exercise tolerance due to ¯ O₂ demand). Cardiac arrhythmias (esp. supravent. tachyarrhyths). Acute MI (prophylaxis and reduction of infarct size and failure). Pheochromocytoma (in comb. w/alpha blocker). Essential tremor. Migraine headache (prophylaxis). Performance anxiety.

Special Features: Abrupt w/drawal may trigger MI. Better pt. compliance than w/propranolol.

Name: Propranolol (Inderal)

Class: Nonselective b-Blocking Agent

Mechanism: Competitive blockade of b1 and b2 receptors. No a effect. Decreases conversion of T₄ to T₃ by inhibiting hepatic monodeiodinase.

Absorp.: Good oral (>90%). Low bioavail.: ~30%. Plasma levels vary 20x btwn. patients.

Dist.:93% bound to protein. Enters CNS. Metabolism.: Hepatic Excret., t½: Short t½ (3.5-6 hr).

Toxicity/S.E.s: CV—hypotension, bradycardia. C/i for AV. May exacerbate angina (unopposed a receptor action). Resp—c/i in asthmatics, COPD, bronchitis, allergic rhinitis. Metabolism—caution w/diabetics (masks sign of hypoglycemia: tachycardia). CNS—weakness, fatigue, nightmares, depression. GI—n/v (uncommon). Hypersens—rash, hematologic disorders (rare).

Utility: Mild-mod HTN (¯ CO ® ¯ BP; blocks renin release). Adjunct to direct vasodilators for severe HTN (prevents reflex tachycardia). Angina pectoris (prophylactic ® ­ exercise tolerance 2° to ¯ O₂ demand). Cardiac arrhythmias (esp. supravent. tachyarrhyths). Acute MI (prophylaxis & reduction of infarct size and failure). Modifies risk factors assoc. w/atherosclerosis. Increases O₂ delivery to ischemic cardiac tissue.

Name: Prazosin (Minipress)

Class: a-Blocking Agent

Mechanism: Blocks a1 receptors in vasculature ® ¯ phospholipase C activation, ¯ IP₃ formation, ¯ Ca²⁺ released from intracellular stores ® arteriolar & venous vasodilation.

Absorption: Oral. 50% bioavailability

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Excretion, t½: 3 hr.

Toxicity/S.E.s: 1st dose syncope (1%), dizziness, headaches, weakness.

Utility: Treat periph. vasc. disease (Raynaud’s Disease), hypertension (lowers BP w/o producing sig. tachycardia), pheochromocytoma (phenoxybenz. is best), benign prostatic hyperplasia (relieves obstruction symptoms).

Special Features: Prazosin-type a blockers are the only clinically useful anti-hypertensive a-receptor antagonists. Produce less tachycardia than do direct vasodilators. Readily combined w/other drugs.

Name: Guanethidine (Ismelin)

Class: Adrenergic Neuron Blocking Agent

Mechanism: Taken up at NE nerve terminal by NE transport system. Blocks release of NE by action potential or indirect agents. Eventually depletes NE. Causes ¯ BP, some bradycardia. No adrenal effect.

Absorption: Poor oral.

Dist.: No CNS.

Metabolism.:

Excretion, t½: 5 days.

Toxicity/S.E.s: Marked postural & exercise hypotension, bradycardia, fluid retention, asthma aggravation, diarrhea, inhib. of ejaculation. But no CNS effects. C/I for pheochromocytoma (supersens), impending CHF or partial heart block, bronchial asthma. Not to be used in comb. w/MAO inhibitors or sympathomimetics. TCAs block uptake into nerve terminals.

Utility: Mod.-severe hypertension (very effective, but last resort due to severe side effects).

Special Features: Supersensitivity develops (­ effect of direct acting, but ¯ effect of indirect). Onset 1-3 wks. No longer considered very useful.