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.[39,40 Read more

Volume of distribution

The reported volume of distribution of atorvastatin is of 380 L.[39,40]

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.[39,40]

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.[39, 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
Elevated serum transaminase US
  • Kind: experimental
    • Percent: 62%
  • Varying Reports
    Diarrhea US
    • adolescent
    • adult
    • pediatric
  • Kind: experimental
    • Percent: 5-14%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Nasopharyngitis US
    • adolescent
    • adult
    • pediatric
  • Kind: experimental
    • Percent: 4-13%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Arthralgia US
    • adolescent
    • adult
    • pediatric
  • Kind: experimental
    • Percent: 4-12%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    All-cause Mortality US
    • adult
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Pain in extremity US
    • adolescent
    • adult
    • pediatric
  • Kind: experimental
    • Percent: 3-9%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Urinary Tract Infection US
    • adolescent
    • adult
    • pediatric
  • Kind: experimental
    • Percent: 4-8%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Myalgia US
    • adolescent
    • adult
    • pediatric
  • Kind: experimental
    • Percent: 3-8%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Nausea US
    • adolescent
    • adult
    • pediatric
  • Kind: experimental
    • Percent: 4-7%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Diabetes US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Dyspepsia US
    • adolescent
    • adult
    • pediatric
  • Kind: experimental
    • Percent: 3-6%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Non-cardiovascular death US
    • adult
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Musculoskeletal Pain US
    • adolescent
    • adult
    • pediatric
  • Kind: experimental
    • Percent: 2-5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Muscle Spasm US
    • adolescent
    • adult
    • pediatric
  • Kind: experimental
    • Percent: 2-5%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Insomnia US
    • adolescent
    • adult
    • pediatric
  • Kind: experimental
    • Percent: 1-5%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Phayngolaryngeal pain US
    • adolescent
    • adult
    • pediatric
  • Kind: experimental
    • Percent: 1-4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Persistent hepatic transaminase elevations US
    • adult
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Elevated serum transaminase US
    Varying Reports
    Myopathy US
    Varying Reports
    Rhabdomyolisis US
    Varying Reports
    Immune-mediated necrotizing myopathy US
    Unclassified
    Interstitial Lung Disease US
    Post Marketing
    Cognitive Impairment US
    Unclassified
    Bullous rashes US
    Post Marketing
    Angioneurotic Edema US
    Post Marketing
    Anaphylaxis US
    Post Marketing
    Rhabdomyolysis US
    Post Marketing
    Toxic Epidermal Necrolysis US
    Post Marketing
    Stevens-Johnson Syndrome US
    Post Marketing
    Erythema multiforme US
    Post Marketing
    Fatal and non-fatal hepatic failure US
    Post Marketing
    Tendon Rupture US
    Post Marketing
    Fatigue US
    Post Marketing
    Myositis US
    Post Marketing
    Pancreatitis US
    Post Marketing
    Peripheral neuropathy US
    Post Marketing
    Depression US
    Post Marketing
    Dizziness US
    Post Marketing
    Urticaria US
    • adolescent
    • adult
    • pediatric
    Clinical Trial
    Vision blurred US
    • adolescent
    • adult
    • pediatric
    Clinical Trial
    Nightmare US
    • adolescent
    • adult
    • pediatric
    Clinical Trial
    Epistaxis US
    • adolescent
    • adult
    • pediatric
    Clinical Trial
    Tinnitus US
    • adolescent
    • adult
    • pediatric
    Clinical Trial
    White blood cells urine positive US
    • adolescent
    • adult
    • pediatric
    Clinical Trial
    Eructation US
    • adolescent
    • adult
    • pediatric
    Clinical Trial
    Abdominal Discomfort US
    • adolescent
    • adult
    • pediatric
    Clinical Trial
    Hepatitis US
    • adolescent
    • adult
    • pediatric
    Clinical Trial
    Flatulence US
    • adolescent
    • adult
    • pediatric
    Clinical Trial
    Musculoskeletal Pain US
    • adolescent
    • adult
    • pediatric
    Clinical Trial
    Cholestasis US
    • adolescent
    • adult
    • pediatric
    Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Dose Form:
      • Tablet
    • Hypersensitivity:
      • true
    • Regions: US
    • Regions: US
    • Patient Conditions:
        • Name: Nursing mothers
        • Drugbank Id: DBCOND0107390
    • Regions: US
    • Patient Conditions:
        • Name: Pregnancy
        • Drugbank Id: DBCOND0018394
    • Regions: US
    • Patient Conditions:
        • Name: Active liver disease
        • Drugbank Id: DBCOND0107507
        • Modification Of:
          • Condition Status: active
          • Base:
            • Name: Liver Disease
            • Drugbank Id: DBCOND0028338

    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.