DRUG
CONSULT
1
111
IIII
New Cholesterol-Lowcring Drugs BY
CAROL
A.
MILLER
ince the mid-1980s, drug therapy has been used in
S conjunction with dietary interventions to reduce the risk of coronary artery disease in people with elevated
cholesterol and lipoproteins. 1 Categories of antihyperlipidemic agents include the following: bile acid resins (cholestyramine and colestipol hydrochloride), nicotinic acid (niacin), dextrothyroxine, clofibrate, gemfibrozil, probucol, and HMG-CoA reductase inhibitors (see drug card). The selection of a drug is based, in part, on the degree of elevation of cholesterol, triglycerides, and specific lipoproteins. In 1987, lovastatin (Mevacor) was the first FDAapproved drug in a category of cholesterol-lowering agents called HMG-CoA reductase inhibitors. In late 199 I, two additional cholesterol-lowering drugs of this type, pravastatin (Pravachol) and simvastatin (Zocor), were approved for use in the United States. Lovastatin, pravastatin, and simvastatin are used in the treatment of C A R O L A, MILLER, RN-C, MSN, is a gerontological nurse specialist with Care & Counseling, Miller/Wetzler Associates, Cleveland, Ohio.
34/1/36806
CATEGORY: HMG-CoA reductase inhibitor, cholesterol-lowering agent. BRAND NAME: Pravachol (Bristol-Myers Squibb) DOSAGE FORMS: White, round, biconvex tablets, 10 mg (marked "154") and 20 mg (marked "178"). DOSE: Recommended starting dose is 10 or 20 mg at bedtime. Geriatric dosage considerations: Start with I 0 mg at bedtime. In the elderly, maximum reductions in low-density l i p o p r o t e i n cholesterol may be achieved with daily doses of 20 mg or less. USE: As an adjunct to diet for the reduction of elevated lotal and low-density lipoprotein choleslerol levels in patients with primary hypercholesterolemia (types Ila and lib) when the response In a diet restricted in saturated fat and cholesterol has not been adequate. ACTION: Inhibits HMG-CoA reductase activity in the liver, which leads to increased elim-
Types IIa and IIb primary hypercholesterolemia, which is characterized by elevated cholesterol, normal or elevated triglycerides, elevated low-density lipoprotein, and normal high-density lipoprotein. All three drugs are similar in their action of reducing total and low-density lipoprotein cholesterol. The drugs interfere with the biosynthesis of cholesterol by inhibiting HMG-CoA reductase, which is the key enzyme necessary for the production of cholesterol. Because cholesterol synthesis follows a circadian rhythm with peak synthesis occurring during sleep, these drugs are administered in the evening. Lovastatin should be administered with a meal, but pravastatin and simvastatin can be taken with or without food. Recent studies of pravastatin suggest that oncedaily dosing at bedtime is as effective as twice-daily dosing. 2 REFERENCES I. Lipid Research Clinics Program. The Lipid Research Clinics coronary primary prevention trial results. 11. The relationship of reduction in incidence of coronary heart disease to cholesterol lowering. JAVA 1984;251:365. 2. Jones PH, Farmer JA, Cressman hiD, et al. Once-daily pravastatin in patients with primary hypercholesterolemia: a dose-response study. Clin Cardiol 1991;14:146-51,
ination of low-density lipoproteins from the blood. Also inhibits hepatic synthesis of verylow-density lipoproteins, which diminishes the production of low-density tipoprotein. PHARMACOKINETICS: Rapidly absorbed with peak plasma levels within 1 to 1.5 hours after ingestion, lipid-lowering effects are similar whelher taken with, before, or without food. Average oral absorption is 34%, and absolute bioavailabilily is 17%. Approximately 50% of the circulating drug is bound to plasma proteins. SIDE/ADVERSE EFFECTS: Adverse effects attributed to the drug in clinical trials of pravastotin: rash and headache. Adverse effects of HMG-CoA reductase inhibitors: progression of cataracts, ophtholmoplegia, myopathy, rhabdomyolysis, cranial nerve dysfunctions, tremor, vertigo, memory loss, paresthesia, peripheral neuropathy, peripheral nerve palsy, anorexia, vomiting, poncreotitis, hepolitis, gynecomastia, loss of libido, erectile dysfunction. Geriatric Nursing March/April 1992 119
CONSULT
1
111
IIII
New Cholesterol-Lowcring Drugs BY
CAROL
A.
MILLER
ince the mid-1980s, drug therapy has been used in
S conjunction with dietary interventions to reduce the risk of coronary artery disease in people with elevated
cholesterol and lipoproteins. 1 Categories of antihyperlipidemic agents include the following: bile acid resins (cholestyramine and colestipol hydrochloride), nicotinic acid (niacin), dextrothyroxine, clofibrate, gemfibrozil, probucol, and HMG-CoA reductase inhibitors (see drug card). The selection of a drug is based, in part, on the degree of elevation of cholesterol, triglycerides, and specific lipoproteins. In 1987, lovastatin (Mevacor) was the first FDAapproved drug in a category of cholesterol-lowering agents called HMG-CoA reductase inhibitors. In late 199 I, two additional cholesterol-lowering drugs of this type, pravastatin (Pravachol) and simvastatin (Zocor), were approved for use in the United States. Lovastatin, pravastatin, and simvastatin are used in the treatment of C A R O L A, MILLER, RN-C, MSN, is a gerontological nurse specialist with Care & Counseling, Miller/Wetzler Associates, Cleveland, Ohio.
34/1/36806
CATEGORY: HMG-CoA reductase inhibitor, cholesterol-lowering agent. BRAND NAME: Pravachol (Bristol-Myers Squibb) DOSAGE FORMS: White, round, biconvex tablets, 10 mg (marked "154") and 20 mg (marked "178"). DOSE: Recommended starting dose is 10 or 20 mg at bedtime. Geriatric dosage considerations: Start with I 0 mg at bedtime. In the elderly, maximum reductions in low-density l i p o p r o t e i n cholesterol may be achieved with daily doses of 20 mg or less. USE: As an adjunct to diet for the reduction of elevated lotal and low-density lipoprotein choleslerol levels in patients with primary hypercholesterolemia (types Ila and lib) when the response In a diet restricted in saturated fat and cholesterol has not been adequate. ACTION: Inhibits HMG-CoA reductase activity in the liver, which leads to increased elim-
Types IIa and IIb primary hypercholesterolemia, which is characterized by elevated cholesterol, normal or elevated triglycerides, elevated low-density lipoprotein, and normal high-density lipoprotein. All three drugs are similar in their action of reducing total and low-density lipoprotein cholesterol. The drugs interfere with the biosynthesis of cholesterol by inhibiting HMG-CoA reductase, which is the key enzyme necessary for the production of cholesterol. Because cholesterol synthesis follows a circadian rhythm with peak synthesis occurring during sleep, these drugs are administered in the evening. Lovastatin should be administered with a meal, but pravastatin and simvastatin can be taken with or without food. Recent studies of pravastatin suggest that oncedaily dosing at bedtime is as effective as twice-daily dosing. 2 REFERENCES I. Lipid Research Clinics Program. The Lipid Research Clinics coronary primary prevention trial results. 11. The relationship of reduction in incidence of coronary heart disease to cholesterol lowering. JAVA 1984;251:365. 2. Jones PH, Farmer JA, Cressman hiD, et al. Once-daily pravastatin in patients with primary hypercholesterolemia: a dose-response study. Clin Cardiol 1991;14:146-51,
ination of low-density lipoproteins from the blood. Also inhibits hepatic synthesis of verylow-density lipoproteins, which diminishes the production of low-density tipoprotein. PHARMACOKINETICS: Rapidly absorbed with peak plasma levels within 1 to 1.5 hours after ingestion, lipid-lowering effects are similar whelher taken with, before, or without food. Average oral absorption is 34%, and absolute bioavailabilily is 17%. Approximately 50% of the circulating drug is bound to plasma proteins. SIDE/ADVERSE EFFECTS: Adverse effects attributed to the drug in clinical trials of pravastotin: rash and headache. Adverse effects of HMG-CoA reductase inhibitors: progression of cataracts, ophtholmoplegia, myopathy, rhabdomyolysis, cranial nerve dysfunctions, tremor, vertigo, memory loss, paresthesia, peripheral neuropathy, peripheral nerve palsy, anorexia, vomiting, poncreotitis, hepolitis, gynecomastia, loss of libido, erectile dysfunction. Geriatric Nursing March/April 1992 119
