Description

Simple

A medication used to treat high blood pressure, and enlarged heart, and slow the progress of kidney problems in diabetes.

Clinical

An angiotensin receptor blocker used to treat hypertension, systolic hypertension, left ventricular hypertrophy, and delay progression of diabetic nephropathy.

Overview

Candesartan is an angiotensin-receptor blocker (ARB) that may be used alone or with other agents to treat hypertension. It is administered orally as the prodrug, candesartan cilexetil, which is rapidly converted to its active metabolite, candesartan, during absorption in the gastrointestinal tract. Candesartan lowers blood pressure by antagonizing the renin-angiotensin-aldosterone system (RAAS); it competes with angiotensin II for binding to the type-1 angiotensin II receptor (AT1) subtype and prevents the blood pressure increasing effects of angiotensin II. Unlike angiotensin-converting enzyme (ACE) inhibitors, ARBs do not have the adverse effect of dry cough. Candesartan may be used to treat hypertension, isolated systolic hypertension, left ventricular hypertrophy and diabetic nephropathy. It may also be used as an alternative agent for the treatment of heart failure, systolic dysfunction, myocardial infarction and coronary artery disease.

Pharmacology

Indication

May be used as a first line agent to treat uncomplicated hypertension, isolated systolic hypertension and left ventricular hypertrophy. May be used as a first line agent to delay progression of diabetic nephropathy. Candesartan may be also used as a second line agent in the treatment of congestive h... Read more

Pharmacodynamic

Candesartan cilexetil is an ARB prodrug that is rapidly converted to candesartan, its active metabolite, during absorption from the gastrointestinal tract. Candesartan confers blood pressure lowering effects by antagonizing the hypertensive effects of angiotensin II via the RAAS. RAAS is a homeostat... Read more

Mechanism of action

Candesartan selectively blocks the binding of angiotensin II to AT1 in many tissues including vascular smooth muscle and the adrenal glands. This inhibits the AT1-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in an overall decrease in blood pressure. Cande... Read more

Absorption

Following administration of the candesartan cilexetil prodrug, the absolute bioavailability of candesartan was estimated to be 15%. Food with a high fat content has no effect on the bioavailability of candesartan from candesartan cilexetil.

Protein binding

Candesartan is highly bound to plasma proteins (>99%) and does not penetrate red blood cells.

Volume of distribution

0.13 L/kg

Clearance

0.37 mL/min/kg

Half life

Approximately 9 hours.

Route of elimination

When candesartan is administered orally, about 26% of the dose is excreted unchanged in urine. Candesartan is mainly excreted unchanged in urine and feces (via bile).

Toxicity

No lethality was observed in acute toxicity studies in mice, rats and dogs given single oral doses of up to 2000 mg/kg of candesartan cilexetil or in rats given single oral doses of up to 2000 mg/kg of candesartan cilexetil in combination with 1000 mg/kg of hydrochlorothiazide. In mice given single... Read more

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Diabetes
      • Drugbank Id: DBCOND0022048
  • With Drugs Coadmin:
      • Name: Aliskiren
      • Drugbank Id: DB09026

Food Interactions

  • Take at the same time every day.
  • Take with or without food. The absorption is unaffected by food.

Interactions

Type in a drug name to check for interaction with Candesartan cilexetil
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Candesartan cilexetil.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Candesartan cilexetil.
1-benzylimidazole
1-benzylimidazole may decrease the antihypertensive activities of Candesartan cilexetil.
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Candesartan cilexetil.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may decrease the antihypertensive activities of Candesartan cilexetil.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Candesartan cilexetil.
4-Methoxyamphetamine
4-Methoxyamphetamine may decrease the antihypertensive activities of Candesartan cilexetil.
5-methoxy-N,N-dimethyltryptamine
5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Candesartan cilexetil.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Candesartan cilexetil.
Abatacept
The metabolism of Candesartan cilexetil can be increased when combined with Abatacept.
Abediterol
Abediterol may decrease the antihypertensive activities of Candesartan cilexetil.
Abiraterone
The metabolism of Candesartan cilexetil can be decreased when combined with Abiraterone.
Acebutolol
The risk or severity of hyperkalemia can be increased when Candesartan cilexetil is combined with Acebutolol.
Aceclofenac
The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Candesartan cilexetil is combined with Aceclofenac.
Acemetacin
The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Candesartan cilexetil is combined with Acemetacin.
Acenocoumarol
The metabolism of Acenocoumarol can be decreased when combined with Candesartan cilexetil.
Acepromazine
Acepromazine may decrease the antihypertensive activities of Candesartan cilexetil.
Acetohexamide
The metabolism of Candesartan cilexetil can be decreased when combined with Acetohexamide.
Acetyl sulfisoxazole
The metabolism of Candesartan cilexetil can be decreased when combined with Acetyl sulfisoxazole.
Acetylsalicylic acid
The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Candesartan cilexetil is combined with Acetylsalicylic acid.
5 References
  1. 1 . Pfeffer MA, Swedberg K, Granger CB, Held P, McMurray JJ, Michelson EL, Olofsson B, Ostergren J, Yusuf S, Pocock S: Effects of candesartan on mortality and morbidity in patients with chronic heart failure: the CHARM-Overall programme. Lancet. 2003 Sep 6;362(9386):759-66.PubMed: 13678868
  2. 2 . Mendis B, Page SR: Candesartan: widening indications for this angiotensin II receptor blocker? Expert Opin Pharmacother. 2009 Aug;10(12):1995-2007. doi: 10.1517/14656560903092197.PubMed: 19563275
  3. 3 . Baguet JP, Barone-Rochette G, Neuder Y: Candesartan cilexetil in the treatment of chronic heart failure. Vasc Health Risk Manag. 2009;5(1):257-64. Epub 2009 Apr 8.PubMed: 19436650
  4. 4 . Stanfield, Cindy L.;Germann, William J. (2009). Principles of Human Physiology (3rd ed.). Benjamin-Cummings Publishing Company.
  5. 5 . Bader, M. (2004). Renin-angiotensin-aldosterone system. In Encyclopedic reference of molecular pharmacology (pp. 810-814). Berlin: Springer.