Atorvastatin
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Atorvastatin
Lipitor
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Summary
Classes
Common uses
Hyperlipidemia0, Cardiovascular risk reduction0, Atherosclerosis0
Pharmacy
Starting dose
10-20 mg PO once daily
Preparations
10 mg, 20 mg, 40 mg, 80 mg tablets
US FDA Max
80 mg/d
Pharmacology
Routes
Oral
Onset
LDL lowering at 2 weeks, max by 4 weeks; cardiovascular benefit months to years
Duration
24-48 hours per dose
Half-life
14 hours (parent); 20-30 hours including active ortho- and para-hydroxylated metabolites[1]
Bioavailability
~14% (extensive hepatic first-pass)[1]
Pregnancy
Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021. Use individualized; lactation generally avoided.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in hepatic cholesterol biosynthesis. Atorvastatin lowers serum LDL primarily by upregulating hepatic LDL receptors in response to reduced intracellular cholesterol.0 Pleiotropic anti-inflammatory and plaque-stabilizing effects are well-established at the population level[1]. CYP3A4 substrate; SLCO1B1 polymorphism increases plasma concentrations and myopathy risk[2].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Lipitor (atorvastatin calcium), Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/020702s076lbl.pdf
- ↑ CPIC Guideline for SLCO1B1, ABCG2, and CYP2C9 and Statin-Associated Musculoskeletal Symptoms, 2022. https://cpicpgx.org/guidelines/cpic-guideline-for-simvastatin-and-slco1b1/