Simvastatin
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Simvastatin
Zocor
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Summary
Classes
Common uses
Hyperlipidemia0, Cardiovascular risk reduction0
Pharmacy
Starting dose
10-20 mg PO once daily in the evening (40 mg starting allowed for high CV risk)
Preparations
5, 10, 20, 40, 80 mg tablets; 4 mg/mL oral suspension
US FDA Max
40 mg/d standard; 80 mg/d restricted to patients tolerating 80 mg for ≥12 months without myopathy (post-SEARCH 2011 FDA restriction)
Pharmacology
Routes
Oral
Onset
LDL lowering at 2 weeks, max by 4 weeks
Duration
24 hours (evening dosing aligns with overnight HMG-CoA reductase peak)
Half-life
~2 hours (parent and active β-hydroxy acid metabolite); pharmacodynamic effect lasts 24 hours via target turnover[2]
Bioavailability
<5% (extensive hepatic first-pass; statin pharmacology is hepatocellular, not systemic)[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
Simvastatin is an inactive lactone prodrug hydrolyzed to its active β-hydroxy acid, a competitive HMG-CoA reductase inhibitor.0 CYP3A4 substrate; clinically extensive drug interactions with macrolides, azoles, calcium channel blockers, and grapefruit. SLCO1B1 polymorphism (rs4149056) markedly raises plasma exposure and myopathy risk; CPIC genotype-guided dosing has the highest level of evidence for simvastatin specifically[1].
References
edit- ↑ 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, Zocor (simvastatin), Merck, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/019766s108lbl.pdf