Atorvastatin
The most prescribed high-intensity statin, HMG-CoA reductase inhibitor. AHA/ACC and ESC lipid guideline anchor since 1996. Gold standard for primary and secondary ASCVD prevention.
WHAT IS ATORVASTATIN?
Detailed overview
Atorvastatin is a synthetic, lipophilic HMG-CoA reductase inhibitor developed by Pfizer (Lipitor, FDA 1996). It inhibits the rate-limiting step of cholesterol synthesis in the liver, upregulating hepatocyte LDL receptors and lowering plasma LDL cholesterol. The TNT (Treating to New Targets, LaRosa 2005 NEJM), CARDS (Colhoun 2004 Lancet) and SPARCL (Amarenco 2006 NEJM) trials demonstrated cardiovascular (MI, stroke) and cerebrovascular outcome benefit. The Cholesterol Treatment Trialists' (CTT) meta-analysis (Baigent 2010 Lancet PMID 21067804) showed each 1 mmol/L LDL reduction yields ~22% relative risk reduction for major vascular events. High-intensity dose (40-80 mg) targets ≥50% LDL reduction for guideline-driven primary (LDL ≥4.9 mmol/L) or secondary (ASCVD history) prevention.
ATC code
C10AA05
Prescription
Prescription only (Rx)
Mechanism
HMG-CoA reductase inhibitor (statin)
Half-life
14 h (active metabolites 20-30 h)
LDL reduction (40-80 mg)
50-60% (high-intensity)
Data console
Lab data
Safety
Side effects, stop signs, contraindications
Side effects · 7
- Muscle pain, myalgia and weakness (statin-associated muscle symptoms, SAMS), typically symmetric and proximal; dose-dependent, more common at 80 mg.
- Rare but serious: rhabdomyolysis (CK >10x ULN + myoglobinuria) that can cause acute kidney injury; risk increased when combined with CYP3A4 inhibitors or fibrates.
- Elevation of liver transaminases (ALT/AST), usually reversible and dose-dependent; persistent rise >3x ULN warrants dose reduction or discontinuation.
- Slightly increased risk of new-onset type 2 diabetes (about 9–12% relative), mainly in prediabetic patients; cardiovascular benefit outweighs this.
- Gastrointestinal complaints: nausea, diarrhea, constipation, abdominal discomfort, dyspepsia.
- Headache, nasopharyngitis, joint pain (arthralgia) and pain in extremities, among the common, generally mild adverse effects.
- Very rare: immune-mediated necrotizing myopathy (anti-HMGCR antibodies), which can persist after stopping the statin and requires immunosuppression.
Contraindications · 4
- Active liver disease or persistent unexplained ALT elevation (>3x ULN)
- Pregnancy and lactation (lipid synthesis needed for embryonic development)
- Concomitant strong CYP3A4 inhibitor use (clarithromycin, itraconazole, ritonavir)
- Active rhabdomyolysis or CK elevation > 10x ULN
Related Pharmaceuticals
Same therapeutic category
Studies
Related research and clinical findings
Intensive lipid lowering with atorvastatin in patients with stable coronary disease (TNT)
LaRosa JC, Grundy SM, Waters DD et al.
Primary prevention of cardiovascular disease with atorvastatin in type 2 diabetes (CARDS)
Colhoun HM, Betteridge DJ, Durrington PN et al.
High-dose atorvastatin after stroke or transient ischemic attack (SPARCL)
Amarenco P, Bogousslavsky J, Callahan A 3rd et al.
Efficacy and safety of cholesterol-lowering treatment: prospective meta-analysis (CTT)
Baigent C, Blackwell L, Emberson J et al.
Early, intensive statin treatment reduces 'hard' cardiovascular outcomes after acute coronary syndrome.
Schwartz GG, Fayyad R, Szarek M, DeMicco D, Olsson AG
Prevention of coronary and stroke events with atorvastatin (ASCOT-LLA)
Sever PS, Dahlöf B, Poulter NR et al.
2018 AHA/ACC/Multisociety guideline on the management of blood cholesterol
Grundy SM, Stone NJ, Bailey AL et al.
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Have a question about Atorvastatin?
Educational drug info from official sources (PubMed, FDA, EMA). Does NOT replace medical consultation or the SmPC. Talk to your doctor!
The information here is for educational and scientific purposes only. Medication use requires medical consultation and a prescription. The indications, dose ranges, and side effects listed here do NOT replace the official Summary of Product Characteristics (SmPC) or consultation with a physician. Do not start or stop any medication on your own. In an emergency, call your local emergency number.