fluvastatin

REMS

Reduction in low-density lipoprotein cholesterol (LDL-C) (as adjunct to diet).
Reduction incoronary 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 which is 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: Enters breast milk; remainder of distribution unknown.

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, rash/pruritus

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, pharyngitis, rhinitis, sinusitis

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

Concurrent use with gemfibrozil, erythromycin, colchicine, cyclosporine, azole antifungals, or large doses of niacin may ↑ risk of myopathy (concurrent use with gemfibrozil should be avoided; use ↓ doses with cyclosporine, and fluconazole).
Concurrent ingestion with cholestyramine orcolestipol↓ absorption of fluvastatin.
Blood levels are ↑ by cimetidine, omeprazole, and concurrent ingestion of alcohol.
May ↑ glyburide levels
Concurrent use with rifampin↓ blood levels.
May slightly ↑ serum digoxin levels.
May ↑ risk of bleeding with warfarin.

Route/Dosage ⬆ ⬇

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); 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 increasing 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 creatine kinase (CK) levels. If CK levels are markedly ↑ or myopathy occurs, discontinue fluvastatin. Monitor for signs and symptoms of immune-mediated necrotizing myopathy (IMNM) (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.
- Avoid grapefruit and grapefruit juice during therapy; may increase risk of toxicity.

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 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 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: May cause fetal harm. Serum cholesterol and triglycerides increase during normal pregnancy, and cholesterol is essential for fetal development. Instruct females of reproductive potential to use effective contraception during therapy and to notify health care professional immediately if pregnancy is planned or suspected, and to avoid breastfeeding during therapy.
Emphasize the importance of follow-up exams to determine effectiveness and to monitor for side effects.

Evaluation/Desired Outcomes ⬆ ⬇

Decrease in LDL and total cholesterol levels.
Increase in HDL cholesterol levels.
Decrease in serum triglyceride levels.

US Brand Names ⬆ ⬇

~~Lescol,~~ Lescol XL

Code ⬆

NDC Code

0078- Novartis Pharmaceuticals Corporation
- 0078-0354- Lescol XL
  - 0078-0354-05- 100 TABLET, EXTENDED RELEASE in 1 BOTTLE (0078-0354-05)

0078- Novartis Pharmaceuticals Corporation
- 0078-0354- Lescol XL
  - 0078-0354-15- 30 TABLET, EXTENDED RELEASE in 1 BOTTLE (0078-0354-15)

0093- Teva Pharmaceuticals USA, Inc.
- 0093-7442- Fluvastatin
  - 0093-7442-01- 100 CAPSULE in 1 BOTTLE (0093-7442-01)

0093- Teva Pharmaceuticals USA, Inc.
- 0093-7442- Fluvastatin
  - 0093-7442-56- 30 CAPSULE in 1 BOTTLE (0093-7442-56)

0093- Teva Pharmaceuticals USA, Inc.
- 0093-7443- Fluvastatin
  - 0093-7443-01- 100 CAPSULE in 1 BOTTLE (0093-7443-01)

0093- Teva Pharmaceuticals USA, Inc.
- 0093-7443- Fluvastatin
  - 0093-7443-56- 30 CAPSULE in 1 BOTTLE (0093-7443-56)

0093- Teva Pharmaceuticals USA, Inc.
- 0093-7446- Fluvastatin Sodium
  - 0093-7446-01- 100 TABLET, FILM COATED, EXTENDED RELEASE in 1 BOTTLE (0093-7446-01)

0093- Teva Pharmaceuticals USA, Inc.
- 0093-7446- Fluvastatin Sodium
  - 0093-7446-56- 30 TABLET, FILM COATED, EXTENDED RELEASE in 1 BOTTLE (0093-7446-56)

0378- Mylan Pharmaceuticals Inc.
- 0378-8020- Fluvastatin Sodium
  - 0378-8020-77- 90 CAPSULE in 1 BOTTLE, PLASTIC (0378-8020-77)

0378- Mylan Pharmaceuticals Inc.
- 0378-8020- Fluvastatin Sodium
  - 0378-8020-93- 30 CAPSULE in 1 BOTTLE, PLASTIC (0378-8020-93)

0378- Mylan Pharmaceuticals Inc.
- 0378-8021- Fluvastatin Sodium
  - 0378-8021-77- 90 CAPSULE in 1 BOTTLE, PLASTIC (0378-8021-77)

0378- Mylan Pharmaceuticals Inc.
- 0378-8021- Fluvastatin Sodium
  - 0378-8021-93- 30 CAPSULE in 1 BOTTLE, PLASTIC (0378-8021-93)

0781- Sandoz Inc
- 0781-8017- FLUVASTATIN SODIUM ER
  - 0781-8017-01- 100 TABLET, EXTENDED RELEASE in 1 BOTTLE (0781-8017-01)

0781- Sandoz Inc
- 0781-8017- FLUVASTATIN SODIUM ER
  - 0781-8017-31- 30 TABLET, EXTENDED RELEASE in 1 BOTTLE (0781-8017-31)

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇