Description
Simple
A medication used to lower the amount of cholesterol in the blood and decrease the chance of having a heart attack or stroke.
Clinical
An HMG-CoA reductase inhibitor used to lower lipid levels and reduce the risk of cardiovascular disease including myocardial infarction and stroke.
Overview
Atorvastatin (Lipitor®), is a lipid-lowering drug included in the statin class of medications. By inhibiting the endogenous production of cholesterol in the liver, statins lower abnormal cholesterol and lipid levels, and ultimately reduce the risk of cardiovascular disease. More specifically, statin medications competitively inhibit the enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) Reductase,[8] which catalyzes the conversion of HMG-CoA to mevalonic acid. This conversion is a critical metabolic reaction involved in the production of several compounds involved in lipid metabolism and transport, including cholesterol, low-density lipoprotein (LDL) (sometimes referred to as "bad cholesterol"), and very-low-density lipoprotein (VLDL). Prescribing statins is considered standard practice for patients following any cardiovascular event, and for people who are at moderate to high risk of developing cardiovascular disease. The evidence supporting statin use, coupled with minimal side effects and long term benefits, has resulted in wide use of this medication in North America.[Read more
Pharmacology
Indication
Atorvastatin is indicated for the treatment of several types of dyslipidemias, including primary hyperlipidemia and mixed dyslipidemia in adults, hypertriglyceridemia, primary dysbetalipoproteinemia, homozygous familial hypercholesterolemia, and heterozygous familial hypercholesterolemia in adolesce... Read more
Pharmacodynamic
Atorvastatin is an oral antilipemic agent that reversibly inhibits HMG-CoA reductase. It lowers total cholesterol, low-density lipoprotein-cholesterol (LDL-C), apolipoprotein B (apo B), non-high density lipoprotein-cholesterol (non-HDL-C), and triglyceride (TG) plasma concentrations while increasing... Read more
Mechanism of action
Atorvastatin is a statin medication and a competitive inhibitor of the enzyme HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) reductase, which catalyzes the conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol biosynthesis.[ Read more
Absorption
Atorvastatin presents a dose-dependent and non-linear pharmacokinetic profile.[4] It is very rapidly absorbed after oral admin... Read more
Protein binding
Atorvastatin is highly bound to plasma proteins and over 98% of the administered dose is found in a bound form.[40,41 Read more
Volume of distribution
The reported volume of distribution of atorvastatin is of 380 L.[40,41]
Clearance
The registered total plasma clearance of atorvastatin is of 625 ml/min.[5]
Half life
The half-life of atorvastatin is 14 hours while the half-life of its metabolites can reach up to 30 hours.[40,41]
Route of elimination
Atorvastatin and its metabolites are mainly eliminated in the bile without enterohepatic recirculation. The renal elimination of atorvastatin is very minimal and represents less than 1% of the eliminated dose.[40, Read more
Toxicity
The reported LD50 of oral atorvastatin in mice is higher than 5000 mg/kg.[MSDS] In cases of overdose with atorvastatin, there is reported symptoms of complicated breathing, jaundice, liver damage, dark urine, muscle pain, and seizures.[ Read more
Adverse Effects
Effect | Regions | Age Groups | Incidences | Evidence Type |
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Elevated serum transaminase | US |
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Varying Reports |
Diarrhea | US |
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Clinical Trial |
Nasopharyngitis | US |
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Clinical Trial |
Arthralgia | US |
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|
Clinical Trial |
All-cause Mortality | US |
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|
Clinical Trial |
Pain in extremity | US |
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|
Clinical Trial |
Urinary Tract Infection | US |
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|
Clinical Trial |
Myalgia | US |
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Clinical Trial |
Nausea | US |
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|
Clinical Trial |
Diabetes | US |
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|
Clinical Trial |
Dyspepsia | US |
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|
Clinical Trial |
Non-cardiovascular death | US |
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|
Clinical Trial |
Musculoskeletal Pain | US |
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|
Clinical Trial |
Muscle Spasm | US |
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Clinical Trial |
Insomnia | US |
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|
Clinical Trial |
Phayngolaryngeal pain | US |
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|
Clinical Trial |
Persistent hepatic transaminase elevations | US |
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Clinical Trial |
Elevated serum transaminase | US |
|
Varying Reports | |
Myopathy | US |
|
Varying Reports | |
Rhabdomyolisis | US |
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Varying Reports | |
Immune-mediated necrotizing myopathy | US |
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Unclassified | |
Interstitial Lung Disease | US |
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Post Marketing | |
Cognitive Impairment | US |
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Unclassified | |
Bullous rashes | US |
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Post Marketing | |
Angioneurotic Edema | US |
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Post Marketing | |
Anaphylaxis | US |
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Post Marketing | |
Rhabdomyolysis | US |
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Post Marketing | |
Toxic Epidermal Necrolysis | US |
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Post Marketing | |
Stevens-Johnson Syndrome | US |
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Post Marketing | |
Erythema multiforme | US |
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Post Marketing | |
Fatal and non-fatal hepatic failure | US |
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Post Marketing | |
Tendon Rupture | US |
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Post Marketing | |
Fatigue | US |
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Post Marketing | |
Myositis | US |
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Post Marketing | |
Pancreatitis | US |
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Post Marketing | |
Peripheral neuropathy | US |
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Post Marketing | |
Depression | US |
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Post Marketing | |
Dizziness | US |
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Post Marketing | |
Urticaria | US |
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Clinical Trial | |
Vision blurred | US |
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Clinical Trial | |
Nightmare | US |
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Clinical Trial | |
Epistaxis | US |
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Clinical Trial | |
Tinnitus | US |
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Clinical Trial | |
White blood cells urine positive | US |
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Clinical Trial | |
Eructation | US |
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Clinical Trial | |
Abdominal Discomfort | US |
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Clinical Trial | |
Hepatitis | US |
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Clinical Trial | |
Flatulence | US |
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Clinical Trial | |
Musculoskeletal Pain | US |
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Clinical Trial | |
Cholestasis | US |
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Clinical Trial |
Contraindications
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Food Interactions
Avoid grapefruit products. Grapefruit products may increase the risk for atorvastatin related adverse effects such as myopathy and rhabdomyolysis.
Take with or without food. Food decreases absorption but not to a clinically significant extent.