Fluvastatin detailed information

Fluvastatin detailed information

Clinical data
ATC code	C10AA04 (WHO)
Pharmacokinetic data
Protein binding	98%
Elimination half-life	2.5 hours
Identifiers
IUPAC name 7-[3-(4-fluorophenyl) -1-(1-methylethyl) -1H-indol-2-yl]-3, 5-dihydroxy-hept-6-enoic acid
CAS Number	93957-54-1
PubChem CID	1548972
DrugBank	APRD00346
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C24H26FNO4
Molar mass	411.466 g/mol

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Class: Antihyperlipidemic, HMG-CoA reductase inhibitor

Trade Names

Lescol - Capsules 20 mg - Capsules 40 mg

Lescol XL - Tablets, extended-release 80 mg

Pharmacology

Increases rate at which body removes cholesterol from blood and reduces production of cholesterol in body by inhibiting enzyme that catalyzes early rate-limiting step in cholesterol synthesis; increases HDL; reduces LDL, VLDL, and triglycerides.

Pharmacokinetics

Absorption

Absolute bioavailability is 9% to 50%. The relative bioavailability for the extended-release (ER) form is 9% to 66%. T max is less than 1 h. C max is 48.9 to 990 ng/mL.

Immediate-release

Administration with food at steady state increases T max and decreases C max .

ER

Administration with a high-fat meal increases bioavailability by about 50%.

Distribution

Fluvastatin is 98% protein bound. The mean Vd at steady state is about 0.35 L/kg.

Metabolism

No active metabolites are present systemically. The drug is metabolized in the liver primarily via hydroxylation; oxidation occurs via CYP2C9 isozyme systems (75%), 3A4 (about 20%), and 2C8 (about 5%).

Elimination

About 90% is excreted in feces as metabolites, and less than 2% is unchanged. The t ½ is less than 3 h.

Special Populations

Hepatic Function Impairment

AUC and C max increase 2.5-fold.

Indications and Usage

Atherosclerosis

To slow the progression of coronary atherosclerosis

Heterozygous familial hypercholesterolemia in children

Adjunct to diet to reduce total-cholesterol (C), LDL-C, and apolipoprotein (apo) B levels in adolescent boys and girls at least 1 yr post-menarche whose response to dietary restriction has not been adequate and who have the following: 1) LDL-C remains at a value of at least 190 mg/dL, or 2) LDL-C remains at a level of 160 mg/dL or more and there is a positive family history of premature CV disease, or 2 or more other CV disease risk factors are present.

Hypercholesterolemia

Reduction of elevated total-C, LDL, apo B, and triglyceride cholesterol levels, and to increase HDL levels.

Secondary prevention of coronary events

To reduce the risk of undergoing coronary revascularization procedures in patients with coronary heart disease.

Contraindications

Active liver disease or unexplained persistent elevations of LFTs; pregnancy; lactation.

Dosage and Administration

Adults

PO 20 to 80 mg daily.

General Advice

• Administer without regard to meals, but administer with food if GI upset occurs.
• Have patient swallow ER tablets whole. Tablets should not be crushed, chewed, or cut.

Storage/Stability

Store capsules and tablets at controlled room temperature (59° to 86°F). Protect from light.

Drug Interactions

Azole antifungal agents (eg, fluconazole), cyclosporine, gemfibrozil, macrolide antibiotics (eg, erythromycin), niacin

Severe myopathy or rhabdomyolysis may occur with coadministration.

Cholestyramine

Reduced absorption of fluvastatin if taken with or up to 4 h after cholestyramine.

Cimetidine, cyclosporine, fluconazole, omeprazole, ranitidine

Fluvastatin serum levels may be increased.

Diclofenac, digoxin, glyburide, hydantoins

Serum levels of these agents may be increased.

Rifampin

Fluvastatin serum levels may be reduced.

Warfarin

Anticoagulant effect of warfarin may be increased.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (9%); fatigue, insomnia (3%).

ENT

Sinusitis (4%).

GI

Dyspepsia (8%); abdominal pain, diarrhea (5%); flatulence, nausea (3%).

Genitourinary

UTI (3%).

Musculoskeletal

Myalgia (5%).

Respiratory

Bronchitis (3%).

Miscellaneous

Flu-like symptoms (7%); accidental trauma (5%).

Precautions

Monitor

Ensure that serum cholesterol and triglycerides are measured before therapy is started and not less than 4 wk of starting therapy or changing the fluvastatin dose, and then periodically thereafter.

Pregnancy

Category X .

Lactation

Excreted in breast milk; patients should not breast-feed while taking. Children Heterozygous familial hypercholesterolemia

Safety and efficacy not established in children younger than 9 years of age.

Endocrine effects

Use caution when administering HMG-CoA reductase inhibitors with drugs that affect steroid levels or activity.

LFTs

Perform LFTs before initiating therapy, at 12 wk (or after elevation in dose), and periodically thereafter.

Hepatic function impairment

Use with caution in patients who consume substantial quantities of alcohol or who have a history of liver disease. If elevated serum transaminase levels develop during treatment, repeat levels more frequently. Be prepared to reduce dose or discontinue therapy.

Secondary causes of hypercholesterolemia

Ensure that secondary causes of hypercholesterolemia (eg, poorly controlled diabetes, hypothyroidism) are excluded before starting therapy.

Skeletal muscle effects

Rhabdomyolysis with renal function impairment secondary to myoglobinuria has been reported with other drugs in this class. Temporarily withhold therapy in any patient experiencing an acute or serious condition suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis (eg, sepsis, hypotension). The risk of myopathy with other drugs in this class was found to be increased if therapy with either cyclosporine, gemfibrozil, erythromycin, or niacin is coadministered. Consider myopathy in any patient with diffuse myalgias, muscle tenderness or weakness, or marked elevations of CPK.

Patient Information

• Advise patient to take prescribed dose without regard to meals but to take with food if stomach upset occurs.
• Instruct patient to swallow ER tablet whole and not to cut, chew, or crush the tablet.
• Advise patient who is also taking a bile acid resin (eg, cholestyramine) to take the resin at least 2 h before fluvastatin.
• Advise patient to try to take each dose(s) at about the same time each day.
• Inform patient that drug helps control, but does not cure, cholesterol abnormality and instruct patient to continue taking drug as prescribed if cholesterol levels are lowered.
• Advise patient that if a dose is missed, to take it as soon as remembered but never to take more than 1 dose of medicine a day.
• Instruct patient to continue taking other cholesterol-lowering medications as prescribed by health care provider.
• Emphasize to patient importance of following other modalities on cholesterol control: dietary changes (eg, reduced saturated fat intake, increased soluble fiber intake), weight control, regular exercise, and smoking cessation.
• Advise women of childbearing potential to use effective contraception during treatment with fluvastatin, and that the drug should be discontinued immediately if pregnancy occurs.
• Instruct patient to notify health care provider if experiencing any unexplained muscle pain, tenderness, and/or weakness, or any other unusual feelings.

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