Lovastatin

MEVACOR

What it isHMG-CoA reductase inhibitor; hyperlipidemia.

Why this oneFood-dependent absorption and modest potency have pushed it behind atorvastatin and rosuvastatin.

What limits itCYP3A4 inhibitors and grapefruit increase myopathy risk; the immediate-release product must be taken with food.

FDA-approved for

FDA dosing	Population	Start	Target	Max
Hypercholesterolemia / hyperlipidemia	Adults	20 mg QD with evening meal (10 mg if smaller LDL reduction needed)	10–80 mg/day, QD or divided BID	80 mg/day
Heterozygous familial hypercholesterolemia	Adolescents 10–17 yr	20 mg/day (10 mg if smaller reduction)	10–40 mg/day	40 mg/day

Titration Adjust at intervals of 4 weeks or more

Renal Severe (CLcr <30 mL/min): carefully consider before exceeding 20 mg/day

Hepatic Contraindicated in active liver disease or unexplained persistent transaminase elevations

With danazol/diltiazem/dronedarone/verapamil: start 10 mg, max 20 mg/day; with amiodarone: max 40 mg/day

Take with meals (evening meal for once-daily dosing)
Place patient on a standard cholesterol-lowering diet before and during treatment

Active liver disease or unexplained persistent serum transaminase elevations
Concomitant strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, HIV protease inhibitors, clarithromycin, erythromycin, telithromycin, nefazodone, cobicistat-containing products)
Pregnancy and lactation

Myopathy / rhabdomyolysis (higher risk with CYP3A4 inhibitors, cyclosporine, gemfibrozil, niacin)
Immune-mediated necrotizing myopathy (rare)
Liver dysfunction / persistent transaminase elevations

Pregnancy Contraindicated (Category X) — may harm the fetus; discontinue immediately if pregnancy is recognized

Lactation Contraindicated in nursing mothers

NO BOXED WARNINGS

Principal riskMyopathy; the most CYP3A4-dependent statin

Cost, est. cash$5–$150/month

Generic entry2001

Therapeutic safety burden1 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryX

Defining liabilityMyopathy/rhabdomyolysis and hepatotoxicity; interaction burden varies by agent.

CYP3A4 substrate