fluvastatin

REMS

Reduction in low-density lipoprotein cholesterol (LDL-C) (as adjunct to diet).
Reduction in coronary revascularization and slowed progression of coronary atherosclerosis in patients with clinically evident coronary heart disease.
Reduction in LDL-C in heterozygous familial hypercholesterolemia (HeFH) in patients who require 80 mg of fluvastatin daily (as adjunct to diet) (sustained release only).

Action ⬆ ⬇

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

Therapeutic effects:

Reduction in LDL-C.
Reduction in coronary revascularization procedures and slowed progression of coronary atherosclerosis in patients with clinical evident coronary heart disease.

Pharmacokinetics ⬆ ⬇

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

Distribution: Well distributed to tissues.

Protein Binding: >98%.

Metabolism/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

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Lactation: Lactation;
Active liver disease or unexplained persistent elevations in AST and ALT.

Use Cautiously in:

History of liver disease;
Alcoholism;
Renal impairment;
OB: Use statin therapy during pregnancy only if potential maternal benefit justifies potential fetal risk (if needed, consider using a more water-soluble agent [pravastatin or rosuvastatin] that is less likely to cross the placenta);
Rep: Women of reproductive potential.

Adv. Reactions/Side Effects ⬆ ⬇

CV: chest pain, peripheral edema

Derm: photosensitivity, pruritus, rash

EENT: pharyngitis, rhinitis

Endo: hyperglycemia

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

MS: arthritis, back pain, immune-mediated necrotizing myopathy, myopathy, RHABDOMYOLYSIS

Neuro: amnesia, confusion, dizziness, fatigue, headache, insomnia, memory loss

Resp: bronchitis, cough, sinusitis

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

Gemfibrozil, erythromycin, colchicine, cyclosporine, azole antifungals, or large doses of niacin may ↑ risk of myopathy; avoid concurrent use with gemfibrozil; ↓ dose when used with cyclosporine or fluconazole.
Cholestyramine orcolestipol↓ absorption and effectiveness.
Cimetidine, omeprazole, and alcohol may ↑ levels and risk of toxicity.
May ↑ levels and risk of toxicity of glyburide
May ↓ levels and effectiveness of rifampin.
May slightly ↑ digoxin levels.
May ↑ risk of bleeding with warfarin.

Route/Dosage ⬆ ⬇

PO (Adults ): 20–40 mg (immediate release) once daily at bedtime. May ↑ to 40 mg twice daily (immediate release) or 80 mg once daily (extended release); Concurrent use of fluconazole or cyclosporine: Dose should not exceed 20 mg twice daily.
PO (Children ≥10 yr with HeFH): 20 mg (immediate release) once daily at bedtime. In 6 wk, may ↑ to 40 mg twice daily (immediate release) or 80 mg once daily (extended release).

Availability ⬆ ⬇

(Generic available)

Capsules: 20 mg; 40 mg
Extended-release tablets: 80 mg

Assessment ⬆ ⬇

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

Lab Test Considerations:

Monitor serum cholesterol and triglyceride levels before, at 4 wk after initiating therapy or ↑ dose, and periodically during therapy.
Monitor liver function tests, including AST and ALT, before initiating therapy and if signs of liver injury (fatigue, anorexia, right upper abdominal discomfort, dark urine or jaundice) occur. May also cause ↑ alkaline phosphatase and bilirubin levels.
If patient develops muscle tenderness during therapy, monitor CK levels. If CK levels are markedly ↑ or myopathy occurs, discontinue fluvastatin. Monitor for signs and symptoms of immune-mediated necrotizing myopathy (proximal muscle weakness and ↑ CK), persisting despite discontinuation of statin therapy. Perform muscle biopsy to diagnose; shows necrotizing myopathy without significant inflammation. Treat with immunosuppressive agents.

Implementation ⬆ ⬇

PO: Administer once daily at bedtime. May be administered without regard to food.
- DNC: Do not crush, break, or chew extended-release tablets or open capsules. Do not take two 40-mg tablets at one time.
- If administered in conjunction with bile acid sequestrants (cholestyramine, colestipol), administer fluvastatin at least 4 hr after bile acid sequestrant.

Patient/Family Teaching ⬆ ⬇

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 ↑ 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 signs of liver injury or 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.
Rep: Instruct females of reproductive potential to use effective contraception during therapy, to notify health care professional promptly if pregnancy is planned or suspected, and to avoid breastfeeding during therapy. Use statin therapy during pregnancy only if potential maternal benefit justifies potential fetal risk (if needed, consider using a more water-soluble agent [pravastatin or rosuvastatin] that is less likely to cross the placenta).
Emphasize the importance of follow-up exams to determine effectiveness and to monitor for side effects.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇