Lescol

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.