lovastatin

REMS

Primary hypercholesterolemia and mixed dyslipidemias..
Primary prevention of coronary heart disease (myocardial infarction, unstable angina, and coronary revascularization) in asymptomatic patients with increased total and low-density lipoprotein (LDL) cholesterol and decreased high-density lipoprotein (HDL) cholesterol.
Slows the progression of coronary atherosclerosis in patients with coronary artery disease.

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:

Lowering of total and LDL cholesterol and triglycerides. Slightly increases HDL cholesterol.
Slows the progression of coronary atherosclerosis with resultant decrease in coronary heart disease-related events.

Pharmacokinetics ⬆ ⬇

Absorption: Poorly and variably absorbed after oral administration.

Distribution: Crosses the blood-brain barrier and placenta.

Metabolism/Excretion: Extensively metabolized by the liver, most during first pass; excreted in bile and feces. 10% excreted unchanged by the kidneys.

Half-Life: 3 hr.

Time/Action Profile ⬆ ⬇

(cholesterol-lowering effect)

ROUTE	ONSET	PEAK	DURATION
PO, PO-ER	2 wk	4–6 wk	6 wk‡

‡After discontinuation.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Active liver disease or unexplained persistent elevations in AST and ALT;
Concurrent use with strong CYP3A4 inhibitors (e.g. itraconazole, ketoconazole, posaconazole, voriconazole, protease inhibitors, erythromycin, clarithromycin, nefazodone, and cobicistat-containing products);
Lactation: Lactation.

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;
Pedi: Children 10 yr (safety not established).

Adv. Reactions/Side Effects ⬆ ⬇

Derm: rash, pruritus

EENT: blurred vision

Endo: hyperglycemia

GI: abdominal cramps, constipation, diarrhea, flatus, heartburn, nausea, ↑liver enzymes, altered taste, drug-induced hepatitis, dyspepsia, pancreatitis

GU: erectile dysfunction

MS: arthralgia, immune-mediated necrotizing myopathy, myopathy, myositis, RHABDOMYOLYSIS

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

Misc: hypersensitivity reactions

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A4 inhibitors, including ketoconazole, itraconazole, posaconazole, voriconazoleprotease inhibitors, clarithromycin, erythromycin, nefazodone, and cobicistat-containing products↑ risk of myopathy; concurrent use contraindicated
Cholesterol-lowering effect may be ↑ with cholestyramine andcolestipol, but bioavailability may be ↓.
Risk of myopathy is ↑ by concurrent amiodaronecyclosporine,gemfibrozil, diltiazem, verapamil, danazol, and large doses of niacin (concurrent use with gemfibrozil or cyclosporine should be avoided; use ↓ doses with danazol, amiodarone, diltiazem, or verapamil).
May ↑ effects of warfarin.

Drug-Natural Products:

St. John's wort may ↓ levels and effectiveness.

Grapefruit juice ↑blood levels and the risk of rhabdomyolysis.
Food enhances blood levels of lovastatin.

Route/Dosage ⬆ ⬇

PO (Adults ): 20 mg once daily with evening meal. May be ↑ at 4-wk intervals to a maximum of 80 mg/day (immediate-release) or 60 mg/day (extended-release); Concurrent danazol, verapamil, or diltiazem therapy: Initiate at 10 mg/day; do not exceed 20 mg/day; Concurrent amiodarone therapy: Dose should not exceed 40 mg/day; .
PO (Children 10–17 yr): Familial heterozygous hypercholesterolemia: 10–40 mg/day; adjusted at 4 wk intervals.

Renal Impairment

PO (Adults ): CCr <30 mL/min: dosage should not exceed 20 mg/day unless carefully titrated.

Availability ⬆ ⬇

(Generic available)

Tablets: 10 mg; 20 mg; 40 mg
Extended-release tablets: 20 mg; 40 mg; 60 mg

Assessment ⬆ ⬇

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

Lab Test Considerations:

Evaluate serum cholesterol and triglyceride levels before initiating, after 4–6 wk of therapy, and periodically thereafter.
- Monitor liver function tests prior to initiation of therapy and as clinically indicated. If symptoms of serious liver injury, hyperbilirubinemia, or jaundice occur, discontinue lovastatin and do not restart. May also cause ↑ alkaline phosphatase and bilirubin levels.
- If patient develops muscle tenderness during therapy, monitor CK levels. If CK levels are >10 times the upper limit of normal or myopathy occurs, therapy should be discontinued.

Implementation ⬆ ⬇

PO: Administer with food. Administration on an empty stomach decreases absorption by approximately 30%. Initial once-daily dose is administered with the evening meal. DNC: Swallow extended-release tablets whole; do not crush, break or chew.
- Avoid grapefruit and grapefruit juice during therapy; may increase risk of toxicity.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed, not to skip doses or double up on missed doses. Advise patient to avoid drinking more that 200 mL/day of grapefruit juice during therapy. Medication helps control but does not cure elevated serum cholesterol levels.
Advise patient that this medication 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 unexplained muscle pain, tenderness, or weakness occurs, especially if accompanied by fever or malaise.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Advise patient to wear sunscreen and protective clothing to prevent photosensitivity reactions (rare).
Advise patient to notify health care professional of medication regimen before treatment or surgery.
Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraception during therapy and to notify health care professional promptly if pregnancy is planned or suspected or if breastfeeding. Discontinue lovastatin as soon as pregnancy is recognized. Avoid breastfeeding during therapy.
Emphasize the importance of follow-up exams to determine effectiveness and to monitor for side effects.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇