Atorvastatin

ATC code

C10AA05

Therapeutic class

Statin (HMG-CoA reductase inhibitor) · HMG-CoA reductase inhibitor

Forms

oral tablet

Brand names

Lipitor (US) · Tahor (FR) · Zarator (ES) · Atorvastatina Cinfa (ES)

Overall confidence

medium

Regulatory sources consulted

AEMPS CIMA FT 69534 (https://cima.aemps.es/cima/dochtml/ft/69534/FT_69534.html)
PubMed PMID:37934798 ↗
Flockhart Table
KDIGO 2024 Clinical Practice Guideline for the Management of Dyslipidemia in Chronic Kidney Disease
AEMPS CIMA · nº registro 69534 ↗
RxNorm rxcui 83367 ↗

Approved indications

Hypercholesterolemia: Treatment of primary hypercholesterolemia or mixed dyslipidemia, as an adjunct to diet, when response to diet and other non-pharmacological measures is inadequate. Treatment of homozygous familial hypercholesterolemia as an adjunct to diet and other lipid-lowering treatments.
Prevention of cardiovascular disease: Prevention of cardiovascular events in adult patients considered at high risk for a first cardiovascular event, as an adjunct to correction of other risk factors.

Contraindications

Absolute

Hypersensitivity to the active substance or to any of the excipients.
Active liver disease or unexplained persistent elevations of serum transaminases exceeding three times the upper limit of normal.
Pregnancy, lactation and in women of childbearing potential not using appropriate contraceptive measures.

Clinical warnings

Major warning · Hepatic effects: Liver function tests are recommended before treatment initiation and periodically thereafter. If transaminase levels exceed 3 times the ULN, the dose should be reduced or the drug withdrawn. — AEMPS CIMA
Major warning · Myopathy/Rhabdomyolysis: Risk of muscle toxicity. Patients should be advised to promptly report any unexplained muscle pain, tenderness, or weakness. The risk is increased with higher doses and with concomitant use of certain drugs (e.g., CYP3A4 inhibitors, fibrates). — AEMPS CIMA

Drug interactions

HighItraconazoleJ02AC02
Mechanism: Strong inhibition of atorvastatin metabolism via CYP3A4, which significantly increases its plasma concentration and the risk of myopathy.
Recommendation: Avoid concomitant use. If unavoidable, the dose of atorvastatin should not exceed 20 mg/day and close clinical monitoring is recommended.
AEMPS CIMA
HighGemfibrozilC10AB04
Mechanism: Inhibition of atorvastatin glucuronidation and possible inhibition of OATP1B1, increasing atorvastatin exposure and the risk of myopathy/rhabdomyolysis.
Recommendation: Concomitant use is contraindicated.
AEMPS CIMA

Adverse events

Common (≥1%)

nasopharyngitis · hyperglycemia · headache · myalgia · diarrhea · nausea · arthralgia · blood creatine phosphokinase increased

Rare but serious

rhabdomyolysis · hepatotoxicity · pancreatitis · interstitial lung disease · anaphylactic reactions

Pregnancy and lactation

FDA category: X

Atorvastatin is contraindicated during pregnancy and lactation. Women of childbearing potential must use effective contraceptive methods during treatment.

Recent literature (PubMed)

[Efficacy and safety of atorvastatin in major cardiovascular events: Meta-analysis].
Villegas-Quintero VE, et al. · Rev Med Inst Mex Seguro Soc · 2023 · Relevance 5/5
Metaanálisis de 6 ECAs (29,333 pacientes) que evaluó el impacto de altas dosis de atorvastatina (80 mg) en la prevención secundaria de eventos cardiovasculares mayores (MACE). Se encontró una reducción del riesgo relativo del 20% (RR 0.80) para MACE con atorvastatina 80 mg en comparación con otras terapias. Los eventos adversos fueron similares a dosis más bajas.