pharmacopeia
GET
/api/v1/drug/atorvastatin
2D structure
(3R,5R)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoic acid
SMILES CC(C)C1=C(C(=C(N1CC[C@H](C[C@H](CC(=O)O)O)O)C2=CC=C(C=C2)F)C3=CC=CC=C3)C(=O)NC4=CC=CC=C4
InChIKey XUKUURHRXDUEBC-KAYWLYCHSA-N

Mechanism of action

Sourced from openFDA

Atorvastatin is a selective, competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-­methylglutaryl-coenzyme A to mevalonate, a precursor of sterols, including cholesterol. In animal models, atorvastatin calcium lowers plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase and cholesterol synthesis in the liver and by increasing the number of hepatic LDL receptors on the cell surface to enhance uptake and catabolism of LDL; atorvastatin calcium also reduces LDL production and the number of LDL particles.

Hydroxymethylglutaryl-CoA Reductase

Indications

Sourced from openFDA
  • Atorvastatin calcium tablets are indicated: To reduce the risk of: Myocardial infarction (MI), stroke, revascularization procedures, and angina in adults with multiple risk factors for coronary heart disease (CHD) but without clinically evident CHD MI and stroke in adults with type 2 diabetes mellitus with multiple risk factors for CHD but without clinically evident CHD Non-fatal MI, fatal and non-fatal stroke, revascularization procedures, hospitalization for congestive heart failure, and angina in adults with clinically evident CHD As an adjunct to diet to reduce low-density lipoprotein cholesterol (LDL-C) in: Adults with primary hyperlipidemia. Adults and pediatric patients aged 10 years and older with heterozygous familial hypercholesterolemia (HeFH).ICD-10: E11.9, E78.00, E78.5, I20.9, I21.9, I50.9, I63.9

Contraindications

Sourced from openFDA
  • Acute liver failure or decompensated cirrhosis [see Warnings and Precautions (5.3) ] Hypersensitivity to atorvastatin or any excipients in atorvastatin calcium. Hypersensitivity reactions, including anaphylaxis, angioneurotic edema, erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis, have been reported [see Adverse Reactions (6.2) ].contraindicated

Dosage & administration

Sourced from openFDA

Take orally once daily with or without food ( 2.1 ). Assess LDL-C when clinically appropriate, as early as 4 weeks after initiating atorvastatin calcium tablets, and adjust dosage if necessary ( 2.1 ). Adults ( 2.2 ): Recommended starting dosage is 10 or 20 mg once daily; dosage range is 10 mg to 80 mg once daily. Patients requiring LDL-C reduction >45% may start at 40 mg once daily. Pediatric Patients Aged 10 Years of Age and Older with HeFH: Recommended starting dosage is 10 mg once daily; dosage range is 10 to 20 mg once daily ( 2.3 ). Pediatric Patients Aged 10 Years of Age and Older with HoFH: Recommended starting dosage is 10 to 20 mg once daily; dosage range is 10 to 80 mg once daily ( 2.4 ). See full prescribing information for atorvastatin calcium tablets dosage modifications due to drug interactions ( 2.5 ). 2.1 Important Dosage Information Take atorvastatin calcium tablets orally once daily at any time of the day, with or without food. Assess LDL-C when clinically appropriate, as early as 4 weeks after initiating atorvastatin calcium tablets, and adjust the dosage if necessary. 2.2 Recommended Dosage in Adult Patients The recommended starting dosage of atorvastatin calcium tablets are 10 mg to 20 mg once daily. The dosage range is 10 mg to 80 mg once daily. Patients who require reduction in LDL-C greater than 45% may be started at 40 mg once daily. 2.3 Recommended Dosage in Pediatric Patients 10 Years of Age and Older with HeFH The recommended starting dosage of atorvastatin calcium tablets are 10 mg once daily. The dosage range is 10 mg to 20 mg once daily.

Warnings & precautions

Sourced from openFDA

Myopathy and Rhabdomyolysis: Risk factors include age 65 years or greater, uncontrolled hypothyroidism, renal impairment, concomitant use with certain other drugs, and higher atorvastatin calcium dosage. Discontinue atorvastatin calcium if markedly elevated CK levels occur or myopathy is diagnosed or suspected. Temporarily discontinue atorvastatin calcium in patients experiencing an acute or serious condition at high risk of developing renal failure secondary to rhabdomyolysis. Inform patients of the risk of myopathy and rhabdomyolysis when starting or increasing atorvastatin calcium dosage. Instruct patients to promptly report unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever ( 2.5 , 5.1 , 7.1 , 8.5 , 8.6 ). Immune-Mediated Necrotizing Myopathy (IMNM): Rare reports of IMNM, an autoimmune myopathy, have been reported with statin use. Discontinue atorvastatin calcium if IMNM is suspected ( 5.2 ). Hepatic Dysfunction: Increases in serum transaminases have occurred, some persistent. Rare reports of fatal and non-fatal hepatic failure have occurred. Consider testing liver enzymes before initiating therapy and as clinically indicated thereafter. If serious hepatic injury with clinical symptoms and/or hyperbilirubinemia or jaundice occurs, promptly discontinue atorvastatin calcium ( 5.3 ). 5.1 Myopathy and Rhabdomyolysis Atorvastatin calcium may cause myopathy (muscle pain, tenderness, or weakness associated with elevated creatine kinase [CK]) and rhabdomyolysis.

Adverse reactions

Sourced from openFDA

The following important adverse reactions are described below and elsewhere in the labeling: Myopathy and Rhabdomyolysis [see Warnings and Precautions (5.1) ] Immune-Mediated Necrotizing Myopathy [see Warnings and Precautions (5.2) ] Hepatic Dysfunction [see Warnings and Precautions (5.3) ] Increases in HbA1c and Fasting Serum Glucose Levels [see Warnings and Precautions (5.4) ] Most common adverse reactions (incidence ≥5%) are nasopharyngitis, arthralgia, diarrhea, pain in extremity, and urinary tract infection ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Novadoz Pharmaceuticals LLC at 1-855-668-2369 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, the adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. In the atorvastatin calcium placebo-controlled clinical trial database of 16,066 patients (8755 atorvastatin calcium vs. 7311 placebo; age range 10 to 93 years, 39% women, 91% White, 3% Black, 2% Asian, 4% other) with a median treatment duration of 53 weeks, the most common adverse reactions in patients treated with atorvastatin calcium that led to treatment discontinuation and occurred at a rate greater than placebo were: myalgia (0.7%), diarrhea (0.5%), nausea (0.4%), alanine aminotransferase increase (0.4%), and hepatic enzyme increase (0.4%).

Use in specific populations

Sourced from openFDA

Pregnancy: May cause fetal harm. ( 8.1 ). Lactation: Breastfeeding not recommended during treatment with atorvastatin calcium ( 8.2 ). 8.1 Pregnancy Risk Summary Discontinue atorvastatin when pregnancy is recognized. Alternatively, consider the ongoing therapeutic needs of the individual patient. atorvastatin decreases synthesis of cholesterol and possibly other biologically active substances derived from cholesterol; therefore, atorvastatin may cause fetal harm when administered to pregnant patients based on the mechanism of action [see Clinical Pharmacology (12.1) ] . In addition, treatment of hyperlipidemia is not generally necessary during pregnancy. Atherosclerosis is a chronic process and the discontinuation of lipid-lowering drugs during pregnancy should have little impact on the outcome of long-term therapy of primary hyperlipidemia for most patients. Available data from case series and prospective and retrospective observational cohort studies over decades of use with statins in pregnant women have not identified a drug-associated risk of major congenital malformations. Published data from prospective and retrospective observational cohort studies with atorvastatin use in pregnant women are insufficient to determine if there is a drug-associated risk of miscarriage (see Data) .

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption Atorvastatin is rapidly absorbed after oral administration; maximum plasma concentrations occur within 1 to 2 hours. Extent of absorption increases in proportion to atorvastatin dose.

Overdosage

Sourced from openFDA

No specific antidotes for atorvastatin are known. Contact Poison Control (1-800-222-1222) for latest recommendations. Due to extensive drug binding to plasma proteins, hemodialysis is not expected to significantly enhance atorvastatin clearance.

Approval history

Sourced from openFDA
  • Dec 17, 1996NDANDA020702Upjohn
  • Jan 30, 2004NDANDA021540Pharmacia
  • Nov 30, 2011ANDAANDA076477Sun Pharm Inds Ltd
  • May 29, 2012ANDAANDA090548Apotex Inc
  • May 29, 2012ANDAANDA091226Mylan Pharms Inc
  • Jul 17, 2012ANDAANDA091650Dr Reddys Labs Ltd
  • Jul 17, 2012ANDAANDA202357Dr Reddys Labs Ltd
  • Nov 29, 2013ANDAANDA200465Mylan

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
246,648 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fatigue14,1835.8%
  2. 2Drug Ineffective13,1695.3%
  3. 3Nausea12,7555.2%
  4. 4Dyspnoea11,3594.6%
  5. 5Diarrhoea11,3414.6%
  6. 6Type 2 Diabetes Mellitus11,2724.6%
  7. 7Pain10,2794.2%
  8. 8Dizziness10,0184.1%
  9. 9Myalgia9,9624.0%
  10. 10Headache9,9514.0%
  11. 11Asthenia9,0523.7%
  12. 12Arthralgia8,6843.5%
  13. 13Pain In Extremity8,3153.4%
  14. 14Fall8,0393.3%
  15. 15Death7,6693.1%

Literature

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Recent PubMed references pinned to Atorvastatin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 1,172 ClinicalTrials.gov registrations naming Atorvastatin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Atorvastatin. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Frequently asked questions

How does Atorvastatin work?
Atorvastatin is a selective, competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-­methylglutaryl-coenzyme A to mevalonate, a precursor of sterols, including cholesterol. In animal models, atorvastatin calcium lowers plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase and cholesterol synthesis in the liver and by increasing the number of hepatic LDL receptors on the cell surface to enhance uptake and catabolism of LDL; atorvastatin calcium also reduces LDL production and the number of LDL particles.
What is Atorvastatin used for?
According to FDA labeling, Atorvastatin carries indications including: Atorvastatin calcium tablets are indicated: To reduce the risk of: Myocardial infarction (MI), stroke, revascularization procedures, and angina in adults with multiple risk factors for coronary heart disease (CHD) but without clinically evident CHD MI and stroke in adults with type 2 diabetes mellitus with multiple risk factors for CHD but without clinically evident CHD Non-fatal MI, fatal and non-fatal stroke, revascularization procedures, hospitalization for congestive heart failure, and angina in adults with clinically evident CHD As an adjunct to diet to reduce low-density lipoprotein cholesterol (LDL-C) in: Adults with primary hyperlipidemia. Adults and pediatric patients aged 10 years and older with heterozygous familial hypercholesterolemia (HeFH).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Atorvastatin?
Atorvastatin is classified as HMG CoA reductase inhibitors, HMG-CoA Reductase Inhibitor, Hydroxymethylglutaryl-CoA Reductase Inhibitors, Decreased Cholesterol Synthesis.
What are the brand names for Atorvastatin?
Atorvastatin is marketed under brand names including Atorvaliq, Caduet, Lipitor.
What are the contraindications for Atorvastatin?
Atorvastatin labeling lists contraindications including: Acute liver failure or decompensated cirrhosis [see Warnings and Precautions (5.3) ] Hypersensitivity to atorvastatin or any excipients in atorvastatin calcium. Hypersensitivity reactions, including anaphylaxis, angioneurotic edema, erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis, have been reported [see Adverse Reactions (6.2) ].. Always consult the full prescribing information and a clinician.
Note. Data for atorvastatin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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