Lescol


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fluvastatin sodium

Lescol, Lescol XL

Pharmacologic class: HMG-CoA reductase inhibitor

Therapeutic class: Antihyperlipidemic

Pregnancy risk category X

Action

Competitively inhibits HMG-CoA reductase, an enzyme needed to synthesize cholesterol. This inhibition reduces cholesterol concentration in hepatic cells, which in turn increases synthesis of low-density lipoprotein (LDL) receptors, enhances LDL uptake, and ultimately reduces plasma cholesterol concentration.

Availability

Capsules: 20 mg, 40 mg

Tablets (extended-release): 80 mg

Indications and dosages

Adjunctive therapy to diet to reduce elevated total cholesterol (TC), LDL-C, apolipoprotein B (Apo B), and triglyceride levels; to increase HDL-C in patients with primary hypercholesterolemia and mixed dyslipidemia; to reduce risk of undergoing revascularization procedures in patients with clinically evident coronary heart disease (CHD); to slow progression of atherosclerosis in patients with CHD

Adults: Initially, 40 mg (capsule) P.O. in evening or b.i.d. Don't give two 40-mg capsules at one time. Or, 80 mg (extended-release tablet) P.O. as a single dose at any time of day.

Adjunctive therapy to diet to reduce elevated TC, LDL-C, and Apo B levels in boys and postmenarchal girls with heterozygous familial hypercholesterolemia after failing adequate trial of diet therapy

Children ages 10 to 16: Initially, 20 mg (capsule) P.O. May increase dosage to maximum daily dose: 40 mg (capsule) P.O. b.i.d. or one 80-mg extended-release tablet once daily at 6-week intervals. Individualize dosages according to goal of therapy.

Dosage adjustment

• Concurrent use of cyclosporine, fluconazole, or lipid-modifying doses (1 g/day or greater) of niacin

Contraindications

• Hypersensitivity to drug or its components
• Active hepatic disease or unexplained, persistent serum transaminase elevations
• Patients who are pregnant or may become pregnant
• Breastfeeding patients

Precautions

Use cautiously in:
• severe renal impairment, history of liver disease or heavy alcohol use, uncontrolled hypothyroidism
• concurrent use of gemfibrozil (avoid use)
• concurrent use of cyclosporine, other fibrates, drugs that may decrease levels of endogenous steroid hormones (such as ketoconazole, spironolactone, cimetidine)
• elderly patients (advanced age a predisposing factor for myopathy)
• children younger than age 9 (safety not established).

Administration

• Know that before starting drug, patient should be on standard cholesterol-lowering diet and weight-control and physical exercise programs, if appropriate.
• Check liver enzyme test values before starting drug.
• Give with or without food.
• If patient is also receiving bile-acid resin, give fluvastatin at bedtime at least 4 hours after resin.

Adverse reactions

CNS: headache, dizziness, insomnia, fatigue

CV: syncope, hypertension, intermittent claudication, atrial fibrillation

EENT: sinusitis, nasopharyngitis

GI: nausea, vomiting, diarrhea, constipation, dyspepsia, flatulence, abdominal pain, gastric disorder

GU: urinary tract infection, myoglobinuria, acute renal failure

Hepatic: abnormal liver function tests

hepatitis (rare), hepatic failure

Metabolic: hyperglycemia

Musculoskeletal: joint pain, arthritis, extremity pain, myalgia, myopathy, rhabdomyolysis

Respiratory: exertional dyspnea, bronchitis

Other: flulike symptoms, tooth disorder, accidental trauma, peripheral edema, allergic reaction

Interactions

Drug-drug.Cholestyramine: decreased fluvastatin blood level

Antifungals, erythromycin, colchicine, gemfibrozil and other fibrates, lipid-modifying doses of niacin, other HMG-CoA inhibitors: increased risk of myopathy

Cimetidine, diclofenac, omeprazole, ranitidine: increased fluvastatin blood level

Cyclosporine, fluconazole: increased fluvastatin exposure

Glyburide, phenytoin: increased blood levels of both drugs

Rifampin: increased fluvastatin metabolism, decreased blood level

Drug-diagnostic tests.Alanine aminotransferase, aspartate aminotransferase, creatine kinase, fasting serum glucose, HbA1c: increased levels

Drug-behaviors.Alcohol use: increased risk of hepatotoxicity

Patient monitoring

• Watch for allergic reaction to drug.

Assess for myositis. If patient has muscle pain, monitor CK level. Discontinue drug if myopathy is diagnosed or suspected.
• Monitor lipid levels and liver function test results, particularly in patients with history of liver disease or heavy alcohol use.
• Be aware that bleeding or increased prothrombin times have occurred in patients taking coumarin anticoagulants concurrently with other HMG-CoA reductase inhibitors. Monitor prothrombin times closely in patients receiving warfarin-type anticoagulants when fluvastatin is initiated or dosage is changed. Watch for bleeding tendencies.
• In patients receiving phenytoin, or glyburide, closely monitor drug's effects on phenytoin or glyburide levels when fluvastatin is initiated or fluvastatin dosage is changed.

Patient teaching

• Instruct patient to take once-daily dosages in evening for best effect.
• Tell patient to take drug with or without food.
• Tell patient not to open capsules and not to break, crush, or chew extended-release tablets.
• Advise patient to maintain standard cholesterol-lowering diet and weight-control and physical exercise programs, as appropriate.

Instruct patient to immediately report irregular heart beat, muscle aches or pains, yellowing of eyes or skin, or unusual tiredness.

Teach patient how to recognize and report signs and symptoms of allergic response, renal dysfunction, or myopathy.
• Advise patient to notify prescriber if he drinks more than two glasses of alcohol daily.
• Advise women of childbearing age to use effective contraception and to stop drug immediately and notify prescriber if pregnancy occurs.
• Tell patient that full effect of drug may take up to 4 weeks.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.

Lescol

(lĕs′kōl′)
A trademark for the drug fluvastatin sodium.

Lescol®

Fluvastatin, see there.

Lescol

A brand name for FLUVASTATIN.
References in periodicals archive ?
The strong safety and efficacy profile of Lescol offers physicians an important tool in managing cholesterol.
First FDA Half-life in Brand name Generic name approval the body Mevacor Lovastatin 1987 Less than 2 hours Zocor Simvastatin * 1991 Less than 2 hours Pravachol Pravastatin 1991 2 hours Lescol Fluvastatin 1993 Less than 3 hours Lipitor Atorvastatin 1996 14 hours Crestor Rosuvastatin 2003 19 hours Lipophilic or Manufacturer and Brand name lipophobic derivation Mevacor Lipophilic Merck, natural compounds Zocor Lipophilic Merck, natural compounds Pravachol Lipophobic Bristol-Myers Squibb, natural compounds Lescol Lipophilic Novartis, synthetic Lipitor Lipophilic Pfizer, synthetic Crestor Lipophobic Pharmaceuticals, synthetic * Low-dose pill approved for over-the-counter sales in U.
The leading statin drugs are Lipitor (generic name atorvastatin), Crestor (rosuvastatin), Mevacor (lovastatin), Pravacol (pravastatin), Zocor (simvastatin) and Lescol (fluvastatin).
An analysis of data from the large-scale Women's Health Initiative showed that while hydrophilic statins such as Pravachol, Lipitor, and Crestor did not confer any reduction in breast cancer risk, the hydrophobic statins such as Zocor, Mevacor, and Lescol were associated with an 18% reduction in the relative risk of breast cancer.
xx Advicor, Altocor, Altoprev, Caduet, cholestyramine, cholestyramine light, Colestid, Crestor, fenofibrate, gemfibrozil, Lescol, Lescol XL, Lipitor, Locholest, Lofibra, Lopid, lovastatin, Mevacor, Niaspan, Pravachol, Pravigard PAC, Prevalite, Questran, Questran Light, Tricor, Welchol, Zetia, Zocor Depression 296.
market: Lipitor (atorvastatin), Lescol (fluvastatin), Mevacor (lovastatin), Pravachol (pravastatin), and Zocor (simvastatin).
Wyke Farms' Lescol brand, which is said to have 90% less cholesterol than Cheddar, is enjoying buoyant sales.
For all other statins (including Lipitor, Zocor, Lescol, Pravachol and Mevacor), there have been 27 cases of acute renal failure or renal insufficiency reported from January 1, 2001, through September 30, 2004, out of 316 million prescriptions filled-a rate of .
This group of medications includes Zocor, Lipitor, Pravachol, Mevacor, Crestor, and Lescol.
This brand, in combination with our currently marketed cardiovascular brands Lescol, Lescol XL, DynaCirc, DynaCirc CR and the recently approved InnoPran XL, substantially leverages our sales and marketing capacity.
For instance, seniors who spend $120 a month for Zocor can learn that the lesser-known Lescol is just as effective at lowering their cholesterol and costs about half as much - $63 a month.
There is also evidence for the cholesterol-lowering drugs called statins (Lipitor, Lescol, Mevacor, Pravachol and Zocor) that, when started in middle to later middle-age years, they reduce the risk of dementia, type 2 diabetes and osteoporosis.