Fluvastatin

What is Fluvastatin?

• Fluvastatin (Lescol; Lescol XL) is an HMG-CoA reductase inhibitor (statin) that lower cholesterol in your blood.

Fluvastatin

Fluvastatin Enantiomers Structural Formulae

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Fluvastatin2DCSD

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Fluvastatin bounded to HMG-CoA reductase

What are the uses of this medicine?

Fluvastatin (Lescol; Lescol XL) is used as an adjunctive therapy to diet to:

• Reduce elevated total cholesterol (Total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), and triglyceride (TG) , and to increase high-density lipoprotein cholesterol (HDL-C) in adult patients with primary hypercholesterolemia and mixed dyslipidemia.
• Reduce elevated TC, LDL-C, and Apo B levels in boys and post-menarchal girls, 10 to 16 years of age, with heterozygous familial hypercholesterolemia after failing an adequate trial of diet therapy.
• Reduce the risk of undergoing revascularization procedures in patients with clinically evident CHD.
• Slow the progression of atherosclerosis in patients with CHD.

• Fluvastatin capsules are a prescription medicine called "statins" that lower cholesterol in your blood. They lower the "bad" cholesterol and triglycerides in your blood. They can raise your "good" cholesterol as well.
• Fluvastatin capsules are for people whose cholesterol does not come down enough with exercise and a low-fat diet alone.

Fluvastatin capsules may be used in patients with heart disease (coronary artery disease) to:

• lower the chances of heart problems which would require procedures to help restore blood flow to the heart.
• slow the buildup of too much cholesterol in the arteries of the heart.
• Treatment with fluvastatin capsules has not been shown to prevent heart attacks or stroke.

Limitations of Use:

• Fluvastatin capsules have not been studied in conditions where the major abnormality is elevation of chylomicrons, VLDL, or IDL (i.e., hyperlipoproteinemia Types I, III, IV, or V).

How does this medicine work?

• The sodium salt of a synthetic lipid-lowering agent with potential antineoplastic activity.
• Fluvastatin competitively inhibits hepatic 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis.
• This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses through the suppression of MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells.
• Through the inhibition of mevalonate synthesis, statins, like fluvastatin, have been shown to inhibit the production of dolichol, geranylpyrophosphate (GPP) and farnesylpyrophosphate (FPP) and the isoprenylation of the intracellular G-proteins Ras and Rho, which may result in antiangiogenic, apoptotic, and antimetastatic effects in susceptible tumor cell populations.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are pregnant or think you may be pregnant, or are planning to become pregnant.
• are breast-feeding.
• have liver problems.
• are allergic to fluvastatin capsules or any of their ingredients.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• anticoagulants ('blood thinners') such as warfarin
• cimetidine (Tagamet)
• colchicine (Colcrys)
• cyclosporine (Neoral, Sandimmune)
• diclofenac (Cataflam, Voltaren)
• digoxin (Lanoxin)
• erythromycin (E.E.S., E-Mycin, Erythrocin)
• fluconazole (Diflucan), glyburide (DiaBeta, Glynase, Micronase)
• ketoconazole (Nizoral)
• omeprazole (Prilosec)
• other cholesterol-lowering medications such as cholestyramine (Questran), fenofibrate (Tricor), gemfibrozil (Lopid), and niacin (nicotinic acid, Niacor, Niaspan)
• phenytoin (Dilantin)
• ranitidine (Zantac)
• rifampin (Rifadin, Rimactane)
• spironolactone (Aldactone)

Is this medicine FDA approved?

• Fluvastatin was approved for use in the United States in 1993 and remains a commonly prescribed drug with more than one million prescriptions filled yearly.

How should this medicine be used?

Recommended dosage:

• Dose range: 20 mg to 80 mg/day.

Adult Patients With Hypercholesterolemia (Heterozygous Familial and Nonfamilial) and Mixed Dyslipidemia:

• Adult patients can be started on fluvastatin capsules.
• The recommended starting dose for fluvastatin capsules is one 40 mg capsule in the evening, or one fluvastatin capsule, 40 mg twice daily.
• Do not take two fluvastatin capsules, 40 mg at one time.

Pediatric Patients (10 to 16 Years of Age) With Heterozygous Familial Hypercholesterolemia:

• The recommended starting dose is one fluvastatin capsule, 20 mg.
• Dose adjustments, up to a maximum daily dose administered as fluvastatin capsules, 40 mg twice daily should be made at 6 week intervals.

Use With Cyclosporine:

• Do not exceed a dose of 20 mg b.i.d. fluvastatin capsules in patients taking cyclosporine.

Use With Fluconazole:

• Do not exceed a dose of 20 mg b.i.d. fluvastatin capsules in patients taking fluconazole.

Administration:

• Fluvastatin comes as a capsule and an extended-release tablet to take by mouth.
• Take fluvastatin capsules exactly as prescribed. Do not change your dose or stop fluvastatin capsules without talking to your doctor. Your doctor may do blood tests to check your cholesterol levels during treatment with fluvastatin capsules. Your dose of fluvastatin capsules may be changed based on these blood test results.
• Take fluvastatin capsules at the same time every evening. When fluvastatin capsules are taken twice daily, the capsules may be taken once in the morning and once in the evening.
• Fluvastatin capsules can be taken with or without food.
• Do not open fluvastatin capsules.
• Your doctor should start you on a low-fat and low-cholesterol diet before giving you fluvastatin capsules.
• Stay on this low-fat and low-cholesterol diet while taking fluvastatin capsules.
• If you miss a dose of fluvastatin capsules, take it as soon as you remember.
• Do not take fluvastatin capsules if it has been more than 12 hours since your last dose.
• Wait and take the next dose at your regular time.
• Do not take 2 doses of fluvastatin capsules at the same time.
• Swallow the extended-release tablets whole; do not split, chew, or crush them.
• Your doctor may start you on a low dose of fluvastatin and gradually increase your dose, not more than once every 4 weeks.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As a capsule and an extended-release (long-acting) tablet

This medicine is available in fallowing brand namesː

• Lescol
• Lescol XL

What side effects can this medication cause?

The most common side effects of this medicine include:

• headache, upset stomach and stomach pain, diarrhea, flu-like symptoms, muscle pain, sinus infection, tiredness, or trouble sleeping. These side effects are usually mild and may go away.

• The following additional side effects have been reported with fluvastatin capsules: memory loss, and confusion.

Fluvastatin may develop serious side effects, including:

• muscle problems
• liver problems

What special precautions should I follow?

• Rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with fluvastatin capsules and other drugs in this class. Risks increase with advanced age (≥ 65), uncontrolled hypothyroidism, renal impairment, and combination use with cyclosporine ,or gemfibrozil. Advise patients to promptly report to their physician unexplained and/or persistent muscle pain, tenderness, or weakness and discontinue fluvastatin if myopathy is diagnosed or suspected.
• Patients should be advised to report promptly any symptoms of myopathy. Fluvastatin capsules therapy should be discontinued if myopathy is diagnosed or suspected.
• There have been rare reports of Immune-Mediated Necrotizing Myopathy (IMNM), an autoimmune myopathy, associated with statin use. IMNM is characterized by: proximal muscle weakness and elevated serum creatine kinase, which persist despite discontinuation of statin treatment; positive anti-HMG CoA reductase antibody; muscle biopsy showing necrotizing myopathy; and improvement with immunosuppressive agents.
• Increases in serum transaminases (aspartate aminotransferase [AST]/serum glutamic-oxaloacetic transaminase, or alanine aminotransferase [ALT]/serum glutamic-pyruvic transaminase) have been reported with HMG-CoA reductase inhibitors, including fluvastatin sodium. Persistent elevations in hepatic transaminases can occur. Check liver enzyme tests before initiating therapy and as clinically indicated thereafter.
• Increases in HbA1c and fasting serum glucose levels have been reported with HMG-CoA reductase inhibitors, including fluvastatin sodium. Patients treated with fluvastatin sodium who develop clinical evidence of endocrine dysfunction should be evaluated appropriately. Caution should be exercised if a statin or other agent used to lower cholesterol levels is administered to patients receiving other drugs (e.g., ketoconazole, spironolactone, cimetidine) that may decrease the levels of endogenous steroid hormones.
• Women who are breastfeeding should not use fluvastatin capsules. Patients who have a lipid disorder and are breastfeeding should be advised to discuss the options with their healthcare professional.
• It is associated with mild, asymptomatic and self-limited serum aminotransferase elevations during therapy and rarely with clinically apparent acute liver injury.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• increased serum CPK values
• hepatic enzyme elevations
• convulsions
• gastroenteritis/vomiting/diarrhea

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• If an overdose occurs, it should be treated symptomatically with laboratory monitoring and supportive measures should be instituted as required.
• The dialyzability of fluvastatin sodium and of its metabolites in humans is not known at present.

Can this medicine be used in pregnancy?

• Pregnancy Category X.
• Fluvastatin sodium is contraindicated in women who are or may become pregnant.

Can this medicine be used in children?

• The safety and efficacy of fluvastatin sodium in children and adolescent patients 9 to 16 years of age with heterozygous familial hypercholesterolemia have been evaluated.

What are the active and inactive ingredients in this medicine?

• Active Ingredient: fluvastatin sodium (hydrated form)
• Inactive Ingredients: black iron oxide, colloidal silicon dioxide, crospovidone, gelatin, lactose monohydrate, magnesium stearate, propylene glycol, red iron oxide, shellac, titanium dioxide, and yellow iron oxide. The imprinting ink may contain potassium hydroxide.

Who manufactures and distributes this medicine?

Manufactured In Israel By:

• Teva Pharmaceutical Ind. Ltd.
• Kfar Saba, Israel

Manufactured For:

• Teva Pharmaceuticals USA, Inc.
• Parsippany, NJ

What should I know about storage and disposal of this medication?

• Store fluvastatin capsules at room temperature, 20° to 25°C (68° to 77°F). Protect from light.
• Do not keep medicine that is out of date or that you no longer need.
• Keep fluvastatin capsules out of the reach of children.
• Be sure that if you throw medicines away, they are out of the reach of children.

Lipid lowering medications

• Bile Acid Resins/Sequestrants

• • Cholestyramine
  • Colesevelam
  • Colestipol

• Fibrates
  • Clofibrate
  • Fenofibrate
  • Gemfibrozil

• Monoclonal Antibodies - Anti-PCSK9
  • Alirocumab
  • Evolocumab

• Niacin (Nicotinic Acid)

• • Omega-3 Fatty Acids,
  • Icosapent Ethyl
  • Omega-3 Acid Ethyl Esters
  • Omega-3 Carboxylic Acids

• Statins
  • Atorvastatin
  • Fluvastatin
  • Lovastatin
  • Pitavastatin
  • Pravastatin
  • Rosuvastatin
  • Simvastatin

• Miscellaneous
  • Ezetimibe
  • Lomitapide
  • Mipomersen

• Dailymed label info on Fluvastatin
• FDA Fluvastatin

Fluvastatin Resources
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