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 HMG-CoA inhibitor 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

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
Type a drug name in the box above to get started
  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The serum concentration of (R)-warfarin can be increased when it is combined with Losartan.
(S)-Warfarin
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
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid may decrease the antihypertensive activities of Losartan.
1-benzylimidazole
1-benzylimidazole may decrease the antihypertensive activities of Losartan.
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Losartan.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may decrease the antihypertensive activities of Losartan.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Losartan.
4-hydroxycoumarin
The metabolism of 4-hydroxycoumarin can be decreased when combined with Losartan.
4-Methoxyamphetamine
4-Methoxyamphetamine may decrease the antihypertensive activities of Losartan.
5-methoxy-N,N-dimethyltryptamine
5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Losartan.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Losartan.
9-aminocamptothecin
The metabolism of 9-aminocamptothecin can be decreased when combined with Losartan.
Abatacept
The metabolism of Losartan can be increased when combined with Abatacept.
Abediterol
Abediterol may decrease the antihypertensive activities of Losartan.
Abemaciclib
The serum concentration of Abemaciclib can be increased when it is combined with Losartan.
Abexinostat
The risk or severity of QTc prolongation can be increased when Losartan is combined with Abexinostat.
Abiraterone
The metabolism of Losartan can be decreased when combined with Abiraterone.
Acebutolol
The serum concentration of Acebutolol can be increased when it is combined with Losartan.
Aceclofenac
The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Losartan is combined with Aceclofenac.
Acemetacin
The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Losartan is combined with Acemetacin.
5 References
  1. 1 . Sica DA, Gehr TW, Ghosh S: Clinical pharmacokinetics of losartan. Clin Pharmacokinet. 2005;44(8):797-814.PubMed: 16029066
  2. 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. 3 . FDA Approved Drug Products: Losartan Oral Tablets Link
  4. 4 . FDA Approved Drug Products: Losartan and Hydrochlorothiazide Oral Tablets Link
  5. 5 . Cayman Chemicals: Losartan Potassium MSDS Link