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Lescol, Lescol XL
Pharmacologic class: HMG-CoA reductase inhibitor
Therapeutic class: Antihyperlipidemic
Pregnancy risk category X
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.
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.
• Concurrent use of cyclosporine, fluconazole, or lipid-modifying doses (1 g/day or greater) of niacin
• 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
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).
• 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.
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
Musculoskeletal: joint pain, arthritis, extremity pain, myalgia, myopathy, rhabdomyolysis
Respiratory: exertional dyspnea, bronchitis
Other: flulike symptoms, tooth disorder, accidental trauma, peripheral edema, allergic reaction
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
• 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.
• 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.
n brand name: Lescol;
drug class: cholesterol-lowering agent;
action: inhibits HMG-CoA reductase enzyme, which reduces cholesterol synthesis;
uses: adjunct in primary hypocholesterolemia (types IIa and IIb).