lovastatin

lovastatin /lo·va·stat·in/ (lo´vah-stat″in) an antihyperlipidemic agent that acts by inhibiting cholesterol synthesis, used in the treatment of hypercholesterolemia and other forms of dyslipidemia and to lower the risks associated with atherosclerosis and coronary heart disease.

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lo·va·stat·in (lv-sttn)

n.

A statin drug isolated from a strain of Aspergillus terreus, used to treat hyperlipidemia.

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lovastatin

(lō´vstat´n),
n brand name: Mevacor;
drug class: cholesterol-lowering agent;
action: inhibits HMG-CoA reductase enzyme, which reduces cholesterol synthesis;
uses: adjunct in primary hypercholesterolemia, mixed hyperlipidemia.

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lovastatin

Apo-Lovastatin (CA), Dom-Lovastatin (CA), Gen-Lovastatin (CA), Mevacor, Novo-Lovastatin (CA), PMS-Lovastatin (CA)

Pharmacologic class: HMG-CoA reductase inhibitor

Therapeutic class: Antihyperlipidemic

Pregnancy risk category X

Action

Inhibits HMG-CoA reductase, an enzyme crucial to cholesterol synthesis. Decreases total cholesterol and low-density lipoprotein (LDL) levels and increases high-density lipoprotein level.

Availability

Tablets: 10 mg, 20 mg, 40 mg

Tablets (extended-release): 10 mg, 20 mg, 40 mg, 60 mg

⊘Indications and dosages

➣ To reduce LDL, total cholesterol, triglyceride, and apolipoprotein B levels

Adults: Initially, 20 mg P.O. daily. May be increased, as needed, at 4-week intervals to a maximum of 80 mg/day as a single dose or in divided doses. Or 20 mg P.O. (extended-release) daily. May be increased, as needed, at 4-week intervals to a maximum daily dosage of 60 mg.

Dosage adjustment

• Severe renal insufficiency

Off-label uses

• High-risk patients with diabetic dyslipidemia, familial dysbetalipoproteinemia, familial combined hyperlipidemia, or nephrotic hyperlipidemia

Contraindications

• Hypersensitivity to drug, its components, or angiotensin-converting enzyme inhibitors
• Active hepatic disease or unexplained persistent hepatic enzyme elevation
• Concurrent gemfibrozil or azole antifungal therapy
• Females of childbearing age
• Pregnancy or breastfeeding

Precautions

Use cautiously in:
• cerebral arteriosclerosis, heart disease, renal impairment, severe acute infection, severe hypotension or hypertension, uncontrolled seizures, myopathy, visual disturbances, major surgery, trauma, alcoholism
• severe metabolic, endocrine, or electrolyte problems
• children.

Administration

• Give daily dose with evening meal.
• Increase dosage at intervals of 4 weeks or longer, as ordered.
• Don't give with grapefruit juice (may increase drug blood level).
☞ Discontinue if alanine aminotransferase (ALT) or aspartate aminotransferase (AST) level exceeds three times the upper limit of normal.
• Be aware that drug may be used to treat heterozygous familial hypercholesterolemia in boys and postmenarchal girls ages 10 and older who have high LDL and cholesterol levels despite adequate trial of diet therapy.

Route	Onset	Peak	Duration
P.O.	Unknown	2 hr	Unknown
P.O.(extended)	Unknown	Unknown	Unknown

Adverse reactions

CNS: headache, dizziness, asthenia

EENT: blurred vision, eye irritation

GI: nausea, vomiting, constipation, diarrhea, abdominal pain or cramps, dyspepsia, flatulence

Hepatic: hepatotoxicity

Musculoskeletal: myalgia, cramps, rhabdomyolysis

Skin: pruritus, rash, photosensitivity

Other: hypersensitivity reaction

Interactions

Drug-drug. Antifungals, cyclosporine, erythromycin, folic acid derivatives, gemfibrozil, niacin, other HMG-CoA inhibitors: increased risk of myopathy and rhabdomyolysis

Bile acid sequestrants: decreased lovastatin blood level

Isradipine: increased lovastatin clearance

Warfarin: increased prothrombin time, bleeding

Drug-diagnostic tests. ALT, AST: increased levels

Drug-food. Grapefruit juice: increased lovastatin blood level

Drug-herbs. Red yeast rice: increased risk of adverse reactions

Chaparral, comfrey, germander, jin bu huan, kava, pennyroyal, St. John's wort: increased risk of hepatotoxicity

Patient monitoring

• Obtain liver function tests before starting therapy, 6 and 12 weeks after therapy begins or dosage is increased, and periodically thereafter.

Patient teaching

• Tell patient to take immediate-release tablets with evening meal or extended-release tablets at bedtime.
• Instruct patient not to break, crush, or chew extended-release tablets.
• Emphasize importance of cholesterol-lowering diet and other therapies, such as exercise and weight control.
☞ Instruct patient to report unexplained muscle pain, tenderness, or weakness, as well as signs or symptoms of hepatotoxicity (fever, malaise, abdominal pain, yellowing of skin or eyes, clay-colored stools, or tea-colored urine).
☞ Advise patient to contact prescriber immediately if she is breastfeeding or suspects pregnancy.
• Tell patient not to use herbs without consulting prescriber.
• Inform patient that drug may cause photosensitivity. Caution him to avoid excessive sun or heat lamp light.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and herbs mentioned above.

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lovastatin

Mevacor^® Cardiology A lipid-lowering agent used to manage hypercholesterolemia and other dyslipidemias including primary mixed and primary moderate hyperlipidemias, diabetic dyslipidemia and hyperlipidemia of nephrotic syndrome in healthy volunteers, ↓ LDL-C by 35%, apoB by 25%, VLDL-C and IDL-C by 30-40%, ↑ HDL-C by 7% Lab ↓ Total cholesterol, ↓ LDL-C, ↓ TGs, ↑ HDL-C. See Statin. Cf Cholesterol-lowering drugs, Gemfibrozil, HMG CoA reductase inhibitors.