Lovastatin
Lovastatin
Altoprev (ER), Mevacor (discontinued US); mostly generic
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Summary
Classes
Common uses
Hyperlipidemia0, Cardiovascular risk reduction0
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[2]
Bioavailability
<5% (extensive hepatic first-pass; food enhances absorption of IR, hence the evening-meal dosing)[2]
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[1].
References
- ↑ CPIC Guideline for SLCO1B1, ABCG2, and CYP2C9 and Statin-Associated Musculoskeletal Symptoms, 2022. https://cpicpgx.org/guidelines/cpic-guideline-for-simvastatin-and-slco1b1/
- ↑ 2.0 2.1 FDA Prescribing Information, Altoprev (lovastatin ER), Shionogi, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021316s016lbl.pdf