Fluvastatin

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[edit] BRAND NAMES

[edit] STRUCTURE

Fluvastatin.jpg

[edit] MECHANISM OF ACTION

Fluvastatin is an hypolipidemic belonging to the class of drugs called Statins.

Cholesterol is made mainly in the liver. Statins work by blocking a key liver enzyme involved in this process, thereby slowing down the production of cholesterol in the liver. This encourages the liver to take extra cholesterol, LDL cholesterol in particular, out of the bloodstream, by increasing the number of hepatic LDL receptors on the cell-surface and thus, causing the LDL cholesterol level to decrease .

Fluvastatin selectively and competitively inhibits the hepatic enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. As HMG-CoA reductase is responsible for converting HMG-CoA to mevalonate, this results in a decrease in mevalonate, a precursor of cholesterol.

[edit] INDICATIONS

  • Hyperlipidemia:
    • Patients with primary hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia (elevated LDL-cholesterol and triglyceride) as an adjunct to diet to reduce elevated total-C, LDL-C, ApoB, and TG levels and to increase HDL-C
    • Boys and post-menarchal girls, 10 to 16 years of age with Heterozygous Familial Hypercholesterolemia (HeFH) to reduce elevated total-C, LDL-C and ApoB after failing an adequate trial of diet therapy
  • Secondary Prevention of Cardiovascular Disease: Cholesterol can cause coronary heart disease by narrowing the coronary arteries. This condition, called atherosclerosis, may lead to angina, a heart attack (myocardial infarction), or a stroke. Fluvastatin is indicated to slow the progression of atherosclerosis and to reduce the risk of coronary revascularization procedures (e.g. heart bypass, angioplasty) in patients WITH clinically evident coronary heart disease.

[edit] DOSAGE

  • Adult recommended starting dose: 40 mg to 80 mg (administered as one 40 mg capsule twice daily, or one 80 mg extended-release tablet (XL) once daily. For patients requiring LDL-C reduction to a goal of <25% a starting dose of 20 mg may be used.
  • Children with heterozygous familial hypercholesterolemia (ages 10 to 16, inclusive): the recommended starting dose is 20 mg once daily

Since the maximal effect of a given dose is seen within 4 weeks, periodic lipid determinations should be performed at this time and dosage adjusted according to the patient’s response to therapy and established treatment guidelines.

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to Fluvastatin
  • Active liver disease, which may include unexplained persistent elevations in hepatic transaminase levels
  • Women who may become pregnant, pregnancy and breastfeeding

[edit] WARNINGS AND PRECAUTIONS

  • Skeletal Muscle Effects: Myalgia, myopathy and, rarely, rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with HMG-CoA reductase inhibitors, including Fluvastatin. These risks can occur at any dose level, but are increased at the highest dose.
    Fluvastatin should be prescribed with caution in patients with predisposing factors for myopathy (e.g., age ≥ 65 years, inadequately treated hypothyroidism, renal impairment, personal or family history of hereditary muscular disorders, alcohol abuse).
    Concomitant use of cyclosporine,or gemfibrozil may increase the risk of myopathy. (see Interaction).
    Whilst on treatment, patients should be asked to report inexplicable muscle pain, weakness or cramps immediately, particularly if associated with malaise or fever. Creatine Kinase levels should be measured in these patients. Therapy should be discontinued if Creatine Kinase levels are markedly elevated.
  • Liver enzyme abnormalities and monitoring: As with other HMG-CoA reductase inhibitors, persistent elevations in hepatic transaminases can occur. Monitor liver enzymes prior to initiating therapy and repeat it when clinically indicated.

[edit] INTERACTIONS

Drug Interactions Associated with Increased Risk of 
Myopathy/Rhabdomyolysis
Interacting Agents 
Prescribing Recommendations 
Fluconazole Limit Fluvastatin to 20 mg twice daily
Cyclosporine Limit Fluvastatin to 20 mg twice daily
Colchicine Cases of myopathy, including rhabdomyolysis, have been reported with fluvastatin coadministered with colchicine. Caution should be exercised when prescribing fluvastatin with colchicine.
Gemfibrozil (Fibrate) concomitant administration of Fluvastatin with gemfibrozil should be avoided
Other Fibrates Fluvastatin should be administered with caution when used concomitantly with other fibrates
Niacin A reduction in Fluvastatin dosage should be considered when Niacin doses are ≥1 g/day
  • Glyburide: Concomitant administration of fluvastatin and glyburide increased glyburide exposures. Monitor blood glucose levels when fluvastatin dose is changed
  • Phenytoin: Concomitant administration of fluvastatin and phenytoin increased phenytoin exposures. Monitor plasma phenytoin levels when fluvastatin treatment is initiated or when the dosage is changed
  • Warfarin and coumarin derivates: Monitor prothrombin times when fluvastatin co-administration is initiated, discontinued, or the dosage changed

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category X (US). Fluvastatin should be administered to women of child-bearing potential only when such patients are highly unlikely to conceive and have been informed of the potential hazards. If a woman becomes pregnant while taking Fluvastatin, the drug should be discontinued and the patient advised again as to the potential hazards to the fetus.
  • Nursing mothers who require Fluvastatin treatment should be advised not to nurse their infants.

[edit] SIDE EFFECTS

Most frequent adverse reactions are: headache, dyspepsia, myalgia, abdominal pain and nausea.

See also WARNINGS AND PRECAUTIONS section

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

Lescol PI (U.S.)

[edit] REFERENCES