Atorvastatin


Description

Atorvastatin, also known as the brand name product Lipitor, is a lipid-lowering drug belonging to the statin class of medications. By inhibiting the endogenous production of cholesterol within the liver, statins lower abnormal cholesterol and lipid l...

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Pharmacology

Indication

Atorvastatin is approved for the treatment of several types of dyslipidemias including:

- Primary...
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Pharmacodynamic

Atorvastatin is an oral antilipemic agent which reversibly inhibits HMG-CoA reductase. It is used to... Read more

Mechanism of action

Atorvastatin is a statin medication and a competitive inhibitor of the enzyme HMG-CoA (3-hydroxy-3-m... Read more

Absorption

Atorvastatin presents a dose-dependent and non-linear pharmacokinetic profile.[ Read more

Protein binding

Atorvastatin is highly bound to plasma proteins and over 98% of the administered dose is found in a... Read more

Volume of distribution

The reported volume of distribution of atorvastatin is of 380 L.[ Read more

Clearance

The registered total plasma clearance of atorvastatin is of 625 ml/min.[ Read more

Half life

The half-life of atorvastatin is 14 hours while the half-life of its metabolites can reach up to 30... Read more

Route of elimination

Atorvastatin and its metabolites are mainly eliminated in the bile without enterohepatic recirculati... Read more

Toxicity

The reported LD50 of oral atorvastatin in mice is higher than 5000 mg/kg.[MSDS] In cases of overdose... 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 alcohol.
    • Avoid drastic changes in dietary habit.
    • Avoid taking grapefruit or grapefruit juice throughout treatment. Grapefruit can significantly increase serum levels of this product.
    • Food may decrease maximum plasma levels and area under the curve, but this is clinically inconsequential according to the manufacturer.
    • Take with low fat meal.

    Interactions

    Type in a drug name to check for interaction with Atorvastatin

    The metabolism of (R)-warfarin can be decreased when combined with Atorvastatin.
    The metabolism of (S)-Warfarin can be decreased when combined with Atorvastatin.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Atorvastatin.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Atorvastatin.
    The metabolism of 4-Methoxyamphetamine can be decreased when combined with Atorvastatin.
    The metabolism of 5-androstenedione can be decreased when combined with Atorvastatin.
    The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Atorvastatin.
    The risk or severity of adverse effects can be increased when 6-Deoxyerythronolide B is combined with Atorvastatin.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Atorvastatin.
    The metabolism of Atorvastatin can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Atorvastatin.
    The risk or severity of myopathy can be increased when Abafungin is combined with Atorvastatin.
    The metabolism of Atorvastatin can be increased when combined with Abatacept.
    The serum concentration of Abemaciclib can be increased when it is combined with Atorvastatin.
    The metabolism of Atorvastatin can be decreased when combined with Abiraterone.
    The metabolism of Atorvastatin can be decreased when combined with Acalabrutinib.
    The serum concentration of Acebutolol can be increased when it is combined with Atorvastatin.
    The metabolism of Acenocoumarol can be decreased when combined with Atorvastatin.
    The metabolism of Atorvastatin can be decreased when combined with Acetaminophen.
    The metabolism of Atorvastatin can be decreased when combined with Acetazolamide.

    References

    • 1 . Qiu S, Zhuo W, Sun C, Su Z, Yan A, Shen L: Effects of atorvastatin on chronic subdural hematoma: A systematic review. Medicine (Baltimore). 2017 Jun;96(26):e7290. doi: 10.1097/MD.0000000000007290. [PubMed: 28658127]
    • 2 . McIver LA, Siddique MS: Atorvastatin . [PubMed: 28613530]
    • 3 . Ye YC, Zhao XL, Zhang SY: Use of atorvastatin in lipid disorders and cardiovascular disease in Chinese patients. Chin Med J (Engl). 2015 Jan 20;128(2):259-66. doi: 10.4103/0366-6999.149226. [PubMed: 25591572]
    • 4 . Ray SK, Rege NN: Atorvastatin: in the management of hyperlipidaemia. J Postgrad Med. 2000 Jul-Sep;46(3):242-3. [PubMed: 11298482]
    • 5 . Lennernas H: Clinical pharmacokinetics of atorvastatin. Clin Pharmacokinet. 2003;42(13):1141-60. [PubMed: 14531725]
    • 6 . Lins RL, Matthys KE, Verpooten GA, Peeters PC, Dratwa M, Stolear JC, Lameire NH: Pharmacokinetics of atorvastatin and its metabolites after single and multiple dosing in hypercholesterolaemic haemodialysis patients. Nephrol Dial Transplant. 2003 May;18(5):967-76. [PubMed: 12686673]
    • 7 . Zhao W, Zhao SP: Different effects of statins on induction of diabetes mellitus: an experimental study. Drug Des Devel Ther. 2015 Nov 24;9:6211-23. doi: 10.2147/DDDT.S87979. eCollection 2015. [PubMed: 26648697]
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