Losartan


Description

Losartan is an angiotensin II receptor blocker (ARB) used to treat hypertension.[3] Angiotensin-converting enzyme (ACE) inhibitors are used...

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Pharmacology

Indication

Losartan is indicated to treat hypertension in patients older than 6 years, reduce the risk of strok... Read more

Pharmacodynamic

Losartan is an HMG-CoA inhibitor used to treat hypertension, diabetic nephropathy, and to reduce the... Read more

Mechanism of action

Losartan reversibly and competitively prevents angiotensin II binding to the AT1 receptor... Read more

Absorption

Losartan is approximately 33% orally bioavailable.[ Read more

Protein binding

Losartan is 98.6-98.8% protein bound and the active metabolite (E-3174) is 99.7% protein bound in se... Read more

Volume of distribution

The volume of distribution of losartan is 34.4±17.9L and 10.3±1.1L for the active metabolite (E-3174... Read more

Clearance

Losartan has a total plasma clearance of 600mL/min and a renal clearance of 75mL/min.[ Read more

Half life

The terminal elimination half life of losartan is 1.5-2.5 hours while the active metabolite has a ha... Read more

Route of elimination

A single oral dose of losartan leads to 4% recovery in the urine as unchanged losartan, 6% in the ur... Read more

Toxicity

The oral TDLO in mice is 1000mg/kg and in rats is 2000mg/kg.[ Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Upper Respiratory Infection US
  • adult
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Atrial Fibrillation US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Syncope US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Dyspnea US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Cerebrovascular Accident US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Vertigo US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Migraine US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Palpitations US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Tinnitus US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Pruritus US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Urticaria US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Photosensitivity US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Rash US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Constipation US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Abdominal Pain US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Vomiting US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Somnolence US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Sleep Disorders US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Paresthesia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Nasal Congestion US
    • adult
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Back Pain US
    • adult
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Anemia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Depression US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Arthralgia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Myalgia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Edema US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Impotence US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Dysgeusia US
    Post Marketing
    Erythroderma US
    Post Marketing
    Hyponatremia US
    Post Marketing
    Rhabdomyolysis US
    Post Marketing
    Thrombocytopenia US
    Post Marketing
    Malaise US
    Post Marketing
    Hepatitis US
    Post Marketing
    Anaphylactic reactions US
    Post Marketing
    Henoch-Schönlein Purpura US
    Post Marketing
    Vasculitis US
    Post Marketing
    Angioedema US
    Post Marketing

    Contraindications

    • Hypersensitivity:
      • true
    • Regions: US
    • Route:
      • Oral
    • Regions: US
    • With Drugs Coadmin:
        • Name: Aliskiren
        • Drugbank Id: DB09026

    Food Interactions

    • Take without regard to meals. Take at same time each day. Food delays absorption, but does not affect the extent of absorption.

    Interactions

    Type in a drug name to check for interaction with Losartan

    The serum concentration of (R)-warfarin can be increased when it is combined with Losartan.
    The serum concentration of (S)-Warfarin can be increased when it is combined with Losartan.
    1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid may decrease the antihypertensive activities of Losartan.
    1-benzylimidazole may decrease the antihypertensive activities of Losartan.
    2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Losartan.
    2,5-Dimethoxy-4-ethylthioamphetamine may decrease the antihypertensive activities of Losartan.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Losartan.
    4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Losartan.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Losartan.
    4-Methoxyamphetamine may decrease the antihypertensive activities of Losartan.
    The metabolism of 5-androstenedione can be decreased when combined with Losartan.
    5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Losartan.
    The metabolism of Losartan can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Losartan.
    The metabolism of 7-ethyl-10-hydroxycamptothecin can be decreased when combined with Losartan.
    7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Losartan.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Losartan.
    The metabolism of Losartan can be increased when combined with Abatacept.
    Abediterol may decrease the antihypertensive activities of Losartan.
    The serum concentration of Abemaciclib can be increased when it is combined with Losartan.

    References

    • 1 . Sica DA, Gehr TW, Ghosh S: Clinical pharmacokinetics of losartan. Clin Pharmacokinet. 2005;44(8):797-814. [PubMed: 16029066]
    • 2 . Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed: 19515014]
    • 3 . FDA Approved Drug Products: Losartan Oral Tablets [Link]
    • 4 . FDA Approved Drug Products: Losartan and Hydrochlorothiazide Oral Tablets [Link]
    • 5 . Cayman Chemicals: Losartan Potassium MSDS [Link]

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