Description

Simple

A medication used to treat high blood pressure and kidney problems in diabetes, and to reduce the risk of having a stroke.

Clinical

An angiotensin receptor blocker used to treat hypertension and diabetic nephropathy, and is used to reduce the risk of stroke.

Overview

Losartan is an angiotensin II receptor blocker (ARB) used to treat hypertension.[3] Angiotensin-converting enzyme (ACE) inhibitors are used for a similar indication but are associated with a cough.[3] When patients with ACE inhibitor associated coughs are switched to ARBs like losartan, they have an incidence of cough similar to placebo or [hydrochlorothiazide].[3] Losartan is available as losartan potassium oral tablets as well as a combination tablet of losartan potassium and hydrochlorothiazide.[3,4] Patients taking losartan should have their renal function and potassium levels monitored.[3] Losartan was granted FDA approval on 14 April 1995.[3]

Pharmacology

Indication

Losartan is indicated to treat hypertension in patients older than 6 years, reduce the risk of stroke in patients with hypertension and left ventricular hypertrophy (though this benefit may not extend to patients with African heritage), and to treat diabetic nephropathy with elevated serum creatinin... Read more

Pharmacodynamic

Losartan is an angiotensin II receptor blocker used to treat hypertension, diabetic nephropathy, and to reduce the risk of stroke.[1,... Read more

Mechanism of action

Losartan reversibly and competitively prevents angiotensin II binding to the AT1 receptor in tissues like vascular smooth muscle and the adrenal gland.[3, Read more

Absorption

Losartan is approximately 33% orally bioavailable.[1, Read more

Protein binding

Losartan is 98.6-98.8% protein bound and the active metabolite (E-3174) is 99.7% protein bound in serum.[1]

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).[1]

Clearance

Losartan has a total plasma clearance of 600mL/min and a renal clearance of 75mL/min.[1] E-3174, the active metabolite, has a total p... Read more

Half life

The terminal elimination half life of losartan is 1.5-2.5 hours while the active metabolite has a half life of 6-9 hours.[1]

Route of elimination

A single oral dose of losartan leads to 4% recovery in the urine as unchanged losartan, 6% in the urine as the active metabolite.[3, Read more

Toxicity

The oral TDLO in mice is 1000mg/kg and in rats is 2000mg/kg.[3, Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Coughing US
  • Kind: experimental
    • Percent: 17
  • Kind: comparator
    • Percent: 69
  • Kind: comparator
    • Percent: 25
  • Clinical Trial
    Coughing US
  • Kind: experimental
    • Percent: 29
  • Kind: comparator
    • Percent: 35
  • Kind: comparator
    • Percent: 62
  • Clinical Trial
    Discontinuation of treatment US
  • Kind: experimental
    • Percent: 19
  • Kind: placebo
    • Percent: 24
  • Clinical Trial
    Upper Respiratory Infection US
  • Kind: experimental
    • Percent: 8
  • Kind: placebo
    • Percent: 7
  • Clinical Trial
    Upper Respiratory Tract Infection US
  • Kind: experimental
    • Percent: 6.1
  • Kind: placebo
    • Percent: 4.6
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 5.7
  • Kind: placebo
    • Percent: 2.9
  • Clinical Trial
    Discontinuation of therapy US
  • Kind: experimental
    • Percent: 2.3
  • Kind: placebo
    • Percent: 3.7
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Back Pain, Unspecified US
  • Kind: experimental
    • Percent: 2.1
  • Kind: placebo
    • Percent: 0.6
  • Clinical Trial
    Back Pain US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Nasal Congestion US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Liver function abnormalities US
    Clinical Trial
    Weakness US
    Clinical Trial
    Fever US
    Clinical Trial
    Malaise US
    Clinical Trial
    Edema and swelling US
    Clinical Trial
    Chest Pain US
    Clinical Trial
    Impotence US
    Clinical Trial
    Renal Failure US
    Clinical Trial
    Interstitial nephritis US
    Clinical Trial
    Renal Dysfunction US
    Clinical Trial
    Glycosuria US
    Clinical Trial
    Arthralgia US
    Clinical Trial
    Myalgia US
    Clinical Trial
    Muscle Spasm US
    Clinical Trial
    Muscle Cramps US
    Clinical Trial
    Cutaneous Lupus Erythematosus US
    Clinical Trial
    Photosensitivity US
    Clinical Trial
    Urticaria US
    Clinical Trial
    Toxic Epidermal Necrolysis US
    Clinical Trial
    Purpura US
    Clinical Trial
    Pruritus US
    Clinical Trial
    Rash US
    Clinical Trial
    Intrahepatic cholestatic jaundice US
    Clinical Trial
    Jaundice US
    Clinical Trial
    Sialoadenitis US
    Clinical Trial
    Pancreatitis US
    Clinical Trial
    Vomiting US
    Clinical Trial
    Nausea US
    Clinical Trial
    Constipation US
    Clinical Trial
    Diarrhea US
    Clinical Trial
    Cramping US
    Clinical Trial
    Gastric irritation US
    Clinical Trial
    Abdominal Pain US
    Clinical Trial
    Dyspepsia US
    Clinical Trial
    Pulmonary Edema US
    Clinical Trial
    Pneumonitis US
    Clinical Trial
    Respiratory Distress US
    Clinical Trial
    Sinus disorder US
    Clinical Trial
    Pharyngitis US
    Clinical Trial

    Contraindications

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

    Food Interactions

    Take at the same time every day.

    Take with or without food. Food delays absorption, but does not affect the extent of absorption.