simvastatin(redirected from Ranzolont)
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Pharmacologic class: HMG-CoA reductase inhibitor
Therapeutic class: Antihyperlipidemic
Pregnancy risk category X
Inhibits hepatic enzyme HMG-CoA reductase, interrupting cholesterol synthesis and low-density lipoprotein (LDL) consumption. Net effect is total cholesterol and serum triglyceride reductions.
Tablets: 5 mg, 10 mg, 20 mg, 40 mg, 80 mg
Indications and dosages
➣ Adjunct to diet to reduce risk of coronary heart disease (CHD) deaths, cardiovascular events, and hyperlipidemia
Adults: Initially, 10 to 20 mg P.O. daily in the evening. For patients at high risk for a CHD event due to existing CHD, diabetes, peripheral vessel disease, or history of stroke or other cerebrovascular disease, initial dosage is 40 mg/day. Range is 5 to 40 mg/day. Restrict use of 80-mg dose to patients who have been taking simvastatin 80 mg long term (for example, for 12 months or more) without evidence of muscle toxicity. Patients unable to achieve their LDL-C goal utilizing 40-mg dose should not be titrated to 80-mg dose, but should be placed on alternative LDL-C-lowering treatment that provides greater LDL-C lowering effects.
➣ Adjunct to other lipid-lowering treatments (such as LDL apheresis) or if such treatments are unavailable for patients with homozygous familial hypercholesterolemia
Adults: 40 mg/day P.O. in the evening.
➣ Heterozygous familial hypercholesterolemia after failure of an adequate trial of diet therapy
Adolescent boys and postmenarchal girls ages 10 to 17: Initially, 10 mg P.O. daily in the evening. Range is 10 to 40 mg/day; maximum dose is 40 mg/day. Adjust at intervals of 4 weeks or longer.
• Severe renal impairment
• Concurrent use of amiodarone, amlodipine, diltiazem, fibrates, niacin, ranolazine, verapamil, or voriconazole
• Elderly patients
• Hypersensitivity to drug or its components
• Active hepatic disease or unexplained persistent serum transaminase elevations
• Concurrent use of cyclosporine, danazol, gemfibrozil, or strong CYP3A4 inhibitors
• Women who are pregnant or may become pregnant
• Breastfeeding patients
Use cautiously in:
• severe renal impairment; severe acute infection; hypotension; severe metabolic, endocrine, or electrolyte problems; uncontrolled seizures; visual disturbances; myopathy; major surgery; trauma; alcoholism
• history of hepatic disease, liver enzyme abnormalities
• concurrent use of amiodarone, amlodipine, colchicine, digoxin, diltiazem, and lipid-modifying dosages (1 g/day or more) of niacincontaining products, other fibrates, ranolazine, verapamil, or warfarin
• concurrent use of simvastatin in dosages exceeding 20 mg/day with lipid-modifying dosages (1 g/day or more) of niacin-containing products in Chinese patients (avoid use)
• large quantities of grapefruit juice (avoid use)
• elderly patients
• children younger than age 10 (safety not established).
• Check liver function tests before starting therapy.
• Give with evening meal. Don't give with large amounts of grapefruit juice.
CNS: headache, asthenia
GI: nausea, vomiting, diarrhea, constipation, abdominal pain or cramps, flatulence, dyspepsia
Musculoskeletal: myalgia, rhabdomyolysis
Respiratory: upper respiratory infection
Drug-drug. Amiodarone, calcium channel blockers (such as amlodipine, diltiazem, verapamil), colchicine, other lipid-lowering drugs (such as fibrates or lipid-modifying doses of niacin-containing products), ranolazine, voriconazole: increased risk of myopathy including rhabdomyolysis
Cyclosporine, danazol, diltiazem, gemfibrozil, nefazodone, strong CYP3A4 inhibitors (clarithromycin, erythromycin, HIV protease inhibitors, itraconazole, ketoconazole, posaconazole, telithromycin): increased risk of severe myopathy or rhabdomyolysis
Digoxin: slightly increased digoxin blood level
Warfarin: modestly increased anticoagulant effects
Drug-diagnostic tests. Alanine aminotransferase, aspartate aminotransferase: increased levels
Drug-food. Grapefruit juice (more than 1 qt daily): increased drug blood level, greater risk of adverse reactions
Drug-behaviors. Alcohol use: increased risk of hepatotoxicity
☞ Watch closely for myositis and other adverse musculoskeletal reactions. Know that drug may cause rhabdomyolysis.
• Monitor liver function tests, CBC, and lipid levels.
• In patients receiving warfarin concurrently, closely monitor prothrombin time and International Normalized Ratio.
• Advise patient to take with evening meal, but not with large amounts of grapefruit juice.
• Tell patient drug may take up to 4 weeks to be effective.
☞ Caution patient to stop taking drug and contact prescriber if she suspects she is pregnant.
☞ Teach patient to recognize and report signs and symptoms of myopathy or hepatic disorders.
• Instruct patient to avoid alcohol use.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.
simvastatin/sim·va·stat·in/ (sim´vah-stat″in) an antihyperlipidemic agent that acts by inhibiting cholesterol synthesis, used in the treatment of hypercholesterolemia and other forms of dyslipidemia and to lower the risks associated with atherosclerosis and coronary heart disease.
simvastatinA lipid-lowering HMG-CoA reductase inhibitor used to improve lipid profiles and reduce mortality from coronary heart diseasse, diabetes and stroke.
Decreases total cholesterol by 27%, LDL-C by 35–60%, triglycerides by 20–37%, and increases HDL-C by 5–9%.
Constipation, flatulence, dyspepsia, abdominal pain, myalgia, muscle weakness.
simvastatinZocor® Therapeutics A lipid-lowering HMG-CoA reductase inhibitor used in hypercholesterolemia, to improve lipid profiles and ↓ mortality from CAD, DM, TIAs, stroke Adverse effects Constipation, flatulence, dyspepsia, abdominal pain, myalgia, muscle weakness. See Cholesterol-lowering drugs, Gemfibrozil, HMG-CoA reductase inhibitors, Hypercholesterolemia, Statin.
simvastatinA statin drug used to treat raised blood cholesterol levels. A very large seven-year trial of the drug suggested that it reduces the chances of a heart attack or a stroke by one third. A brand name is Zocor. See STATINS for an account of the drug's action.
drug class: cholesterol-lowering agent;
action: inhibits 3hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase enzyme, which reduces cholesterol synthesis;
use: as an adjunct in primary hypercholesterolemia types IIa and IIb.