Pronunciation
FLOO-va-stat-in [Pronunciation]

Trade Name(s)

• Lescol

• Lescol XL

Pregnancy Category
Category X

Ther. class.
lipid-lowering agents

Pharm. class.
hmg coa reductase inhibitors

• Adjunctive management of primary hypercholesterolemia and mixed dyslipidemia.

• Secondary prevention of coronary revascularization in patients with clinically evident coronary heart disease.

• Slows the progression of coronary atherosclerosis in patients with coronary artery disease.

Inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, an enzyme which is responsible for catalyzing an early step in the synthesis of cholesterol.

Therapeutic Effect(s):

• Lowering of total and LDL cholesterol and triglycerides. Slightly increases HDL cholesterol.

• Slows the progression of coronary atherosclerosis with resultant decrease in incidence of coronary heart disease-related events.

Absorption: 98% absorbed after oral administration but undergoes extensive first-pass hepatic metabolism resulting in 24% bioavailability.

Distribution: Enters breast milk; remainder of distribution unknown.

Protein Binding: >98%.

Metabolism and Excretion: After extensive hepatic metabolism, 5% is excreted in urine, 90% in feces.

Half-life: 1.2 hr.

TIME/ACTION PROFILE (cholesterol-lowering effect)

ROUTE	ONSET	PEAK	DURATION
PO	1–2 wk	4–6 wk	unknown

Contraindicated in:

• Hypersensitivity;

• OB: Lactation: Pregnancy and lactation;

• Active liver disease or unexplained persistent elevations in AST and ALT.

Use Cautiously in:

• History of liver disease;

• Alcoholism;

• Renal impairment;

• Safety not established.

CNS: headache, dizziness, insomnia, fatigue.

Resp: bronchitis, cough, pharyngitis, rhinitis, sinusitis.

CV: chest pain, peripheral edema.

GI: nausea, vomiting, abdominal pain/cramps, constipation, flatulence, dyspepsia, ↑ liver enzymes.

Derm: photosensitivity, rash/pruritus.

MS: RHABDOMYOLYSIS, arthritis, myopathy, back pain, arthropathy.

Misc: allergic reactions including anaphylaxis.

*CAPITALS indicates life-threatening.
*italic indicates most frequent.

Drug-Drug

• Fluvastatin is metabolized by the CYP 2C9 metabolic pathway.

• Concurrent use with gemfibrozil , erythromycin , cyclosporine , azole antifungal agents , or niacin (nicotinic acid) may ↑ risk of myopathy (concurrent use with gemfibrozil should be avoided, temporarily ↓ dose or discontinue if systemic azole antifungals are required).

• Concurrent ingestion with cholestyramine or colestipol ↓ absorption of fluvastatin.

• Blood levels are ↑ by cimetidine , ranitidine , omeprazole , and concurrent ingestion of alcohol .

• Concurrent use with rifampin ↓ blood levels.

• May slightly ↑ serum digoxin levels.

• May ↑ risk of bleeding with warfarin .

Drug-Food
Grapefruit juice ↑ blood levels and the risk of rhabdomyolysis.

• PO (Adults): 20–40 mg (immediate-release) once daily at bedtime. May be ↑ to 40 mg twice daily (immediate-release) or 80 mg once daily (extended-release)..

• Capsules: 20 mg, 40 mg

• Extended-release tablets: 80 mg

• Obtain a diet history, especially in regard to fat consumption.

Lab Test Considerations

• Serum cholesterol and triglyceride levels should be evaluated before, at 4 wk after initiating therapy or increasing dose, and periodically during therapy.

• Monitor liver function tests, including AST, before, every 6 wk during the first 3 mo after initiating therapy or increasing dose, every 8 wk during the remainder of the first year, and then every 6 mo. If AST levels ↑ to three times normal, discontinue fluvastatin. May also cause ↑ alkaline phosphatase and bilirubin levels.

• If patient develops muscle tenderness during therapy, monitor CPK levels. If CPK levels are markedly ↑ or myopathy occurs, discontinue fluvastatin.

• Deficient knowledge , related to medication regimen (Patient/Family Teaching)

• Noncompliance (Patient/Family Teaching)

PO: Administer once daily at bedtime. May be administered without regard to food.

» Do not crush, break, or chew extended-release tablets.

» If administered in conjunction with bile acid sequestrants (cholestyramine, colestipol), administer fluvastatin at least 4 hr after bile acid sequestrant.

» Avoid grapefruit and grapefruit juice during therapy; may increase risk of toxicity.

• Instruct patient to take medication as directed. Take missed doses as soon as remembered; if more than 12 hr since last dose, wait and take the next dose at the regular time. Do not double doses. Advise patient to read Patient Information sheet prior to therapy and with each Rx refill. Fluvastatin helps control but does not cure elevated serum cholesterol levels.

• Advise patient that fluvastatin should be used in conjunction with diet restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking.

• Instruct patient to notify health care professional if unexplained muscle pain, tenderness, or weakness occurs, especially if accompanied by fever, malaise, nausea, vomiting, tiredness, dark-colored urine, yellow skin or eyes, or stomach pain.

• Advise patient to use sunscreen and wear protective clothing to prevent photosensitivity reactions.

• Advise patient to notify health care professional of medication regimen before treatment or surgery.

• Instruct female patients to notify health care professional immediately if pregnancy is planned or suspected, or if breastfeeding.

• Emphasize the importance of follow-up exams to determine effectiveness and to monitor for side effects.

• Decrease in LDL and total cholesterol levels.

• Increase in HDL cholesterol levels.

• Decrease in serum triglyceride levels.