fluvastatin sodium

fluvastatin sodium

(floo´vstat´n sōdēm),
n brand name: Lescol;
drug class: cholesterol-lowering agent;
action: inhibits HMG-CoA reductase enzyme, which reduces cholesterol synthesis;
uses: adjunct in primary hypocholesterolemia (types IIa and IIb).

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fluvastatin sodium

Lescol, Lescol XL

Pharmacologic class: HMG-CoA reductase inhibitor

Therapeutic class: Antihyperlipidemic

Pregnancy risk category X

Action

Competitively inhibits HMG-CoA reductase, an enzyme needed to synthesize cholesterol. This inhibition reduces cholesterol concentration in hepatic cells, which in turn increases synthesis of low-density lipoprotein (LDL) receptors, enhances LDL uptake, and ultimately reduces plasma cholesterol concentration.

Availability

Capsules: 20 mg, 40 mg

Tablets (extended-release): 80 mg

⊘Indications and dosages

➣ Adjunctive therapy to reduce LDL cholesterol (LDL-C), total cholesterol, triglyceride, and apolipoprotein B levels

Adults: For LDL-C reduction of less than 25%, initial dosage is 20 mg daily at bedtime. For reduction of at least 25%, initial dosage is 40 mg P.O. (capsules) daily at bedtime; may increase if necessary to 40 mg (capsules) P.O. b.i.d. or 80 mg (extended-release tablet) P.O. daily in evening. Maximum dosage is 80 mg/day.

➣ Secondary prevention of cardiovascular events in patients with coronary heart disease who have undergone percutaneous intervention procedures

Adults: 40 mg (capsule) P.O. b.i.d.

Contraindications

• Hypersensitivity to drug
• Active hepatic disease
• Severe renal impairment
• Pregnancy or breastfeeding

Precautions

Use cautiously in:
• hypotension, mild to moderate renal impairment, severe metabolic disorders, visual disturbances, alcoholism
• patients receiving concurrent azole antifungals
• females of childbearing age
• children younger than age 18 (safety not established).

Administration

• Know that before starting drug, patient should be on standard cholesterol-lowering diet and weight-control and physical exercise programs, if appropriate.
• Give with or without food.
• Be aware that drug works better when taken in evening.
• If patient is also receiving bile-acid resin, give fluvastatin at bedtime at least 4 hours after resin.

Route	Onset	Peak	Duration
P.O.	1-2 wk	4-6 wk	Unknown
P.O. (extended)	2 wk	4 wk	Unknown

Adverse reactions

CNS: amnesia, malaise, drowsiness, weakness, emotional lability, facial paralysis, syncope, headache, poor coordination, hyperkinesia, paresthesia, peripheral neuropathy

CV: orthostatic hypotension, palpitations, phlebitis, arrhythmias

EENT: amblyopia, altered refraction, eye hemorrhage, glaucoma, dry eyes, hearing loss, tinnitus, epistaxis, sinusitis, pharyngitis

GI: nausea, vomiting, diarrhea, constipation, dyspepsia, flatulence, abdominal pain or cramps, gastroenteritis, colitis, stomach ulceration, dysphagia, esophagitis, stomatitis, melena, tenesmus, rectal hemorrhage, pancreatitis

GU: urinary frequency, urinary retention, nocturia, dysuria, hematuria, cystitis, decreased libido, epididymitis, erectile dysfunction, renal calculi, nephritis

Hematologic: anemia, thrombocytopenia

Hepatic: jaundice, hepatitis

Metabolic: hyperglycemia, hypoglycemia

Musculoskeletal: joint pain, back pain, leg cramps, gout, bursitis, myasthenia gravis, myositis, torticollis

Respiratory: dyspnea, pneumonia, bronchitis

Skin: acne, alopecia, contact dermatitis, eczema, diaphoresis, rash, urticaria, skin ulcers, seborrhea, photosensitivity

Other: gingival hemorrhage, appetite changes, weight gain, fever, facial or generalized edema, flulike symptoms, infection, allergic reaction

Interactions

Drug-drug. Antacids, cholestyramine, colestipol: decreased fluvastatin blood level

Antifungals, cyclosporine, erythromycin, niacin, other HMG-CoA inhibitors: increased risk of myopathy

Cimetidine, omeprazole, ranitidine: increased fluvastatin blood level

Digoxin: increased digoxin blood level

Phenytoin: increased blood levels of both drugs

Rifampin: increased fluvastatin metabolism, decreased blood level

Drug-diagnostic tests. Alanine aminotransferase, aspartate aminotransferase, creatine kinase (CK): increased levels

Drug-herbs. Comfrey, germander, jin bu huan, pennyroyal, skullcap, valerian: increased risk of hepatotoxicity

Red yeast rice: increased risk of adverse reactions

Drug-behaviors. Alcohol use: increased risk of hepatotoxicity

Patient monitoring

• Watch for allergic reaction to drug.
• Assess for myositis. If patient has muscle pain, monitor CK level.
• Monitor lipid levels and liver function test results.
• Watch for bleeding tendencies.
• In patients receiving phenytoin, monitor closely when fluvastatin therapy begins or fluvastatin dosage is changed.

Patient teaching

• Instruct patient to take in evening for best effect.
• Advise patient to maintain standard cholesterol-lowering diet and weight-control and physical exercise programs, as appropriate.
☞ Instruct patient to immediately report unusual bleeding or bruising, irregular heart beat, muscle aches or pains, yellowing of eyes or skin, or unusual tiredness.
• Teach patient how to recognize and report signs and symptoms of allergic response.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, alertness, and vision.
• Inform male patient that drug may cause erectile dysfunction and abnormal ejaculation.
• Tell patient that full effect of drug may take up to 4 weeks.
• Tell patient to move slowly when rising, to avoid dizziness from sudden blood pressure decrease.
• Tell patient that he'll undergo regular blood testing during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.