Lovastatin

Statin, Lipid-lowering agent

Lovastatin

Altoprev (ER), Mevacor (discontinued US); mostly generic

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Summary

Classes

Statin, Lipid-lowering agent

Pharmacy

Starting dose

20 mg PO once daily with the evening meal; titrate to 40-80 mg/d

Preparations

10, 20, 40 mg tablets; 20, 40, 60 mg ER tablets

US FDA Max

80 mg/d (40 mg/d if combined with diltiazem, verapamil, danazol; lower limits with various interactions)

Pharmacology

Routes

Oral

Onset

LDL lowering at 2 weeks, max by 4 weeks

Duration

24 hours

Half-life

~2-4 hours (parent and active β-hydroxy acid metabolite); pharmacodynamic effect 24 hours via target turnover

Bioavailability

<5% (extensive hepatic first-pass; food enhances absorption of IR, hence the evening-meal dosing)

Pregnancy

Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021.^{[citation needed]}

Legal status

Rx-only in US

Purported mechanism

Lovastatin is an inactive lactone prodrug hydrolyzed to its active β-hydroxy acid, a competitive HMG-CoA reductase inhibitor.▲0▼ Originally derived from Aspergillus terreus; the first statin approved for clinical use (1987). CYP3A4 substrate with extensive drug-interaction profile similar to simvastatin's. SLCO1B1 polymorphism affects exposure; CPIC guidance is most actionable for simvastatin.