Correlation Engine 2.0
Clear Search sequence regions
Bookmark Forward

QuickView for Candesartan (compound)


PubChem
Name: candesartan
PubChem Compound ID: 2541
Molecular formula: C24H20N6O3
Molecular weight: 440.454 g/mol
Synonyms:
CV 11974; Candesartan; Blopress; CHEBI:3347; 139481-59-7; 2-ethoxy-1-({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl)-1H-benzimidazole-7-carboxylic acid; Candesartan (USAN); 2-Ethoxy-1-(p-(o-1H-tetrazol-5-ylphenyl)benzyl)-7-benzimidazolecarboxylic acid; D00522; Candesartan [USAN:INN].
show more »
DrugBank
Identification
Name: candesartan
Name (isomeric): DB00796
Drug Type: small molecule
Synonyms:
Candesartan cilexetil
Brand: Amias, Blopress, Atacand, Ratacand
Brand name mixture: Atacand Plus(Candesartan Cilexetil + Hydrochlorothiazide)
Category: Angiotensin II Type 1 Receptor Blockers, Angiotensin II Receptor Antagonists, Antihypertensive Agents
CAS number: 139481-59-7
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 heart failure, systolic dysfunction, myocardial infarction and coronary artery disease in those intolerant of ACE inhibitors.
Pharmacology:
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 homeostatic mechanism for regulating hemodynamics, water an...
show 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. Candesartan is greater than 10,000 times more selective...
show 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 affect 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.
Biotransformation: The prodrug candesartan cilexetil undergoes rapid and complete ester hydrolysis in the intestinal wall to form the active drug, candesartan. Elimination of candesartan is primarily as unchanged drug in the urine and, by the biliary route, in the feces. Minor hepatic metabolism of candesartan (<20%)occurs by O-deethylation via cytochrome P450 2C9 to form an inactive metabolite. Candesartan undergoes N-glucuronidation in the tetrazole ring by uridine diphosphate glucuronosyltransferase 1A3 (UGT1A3). O-glucuronidation may also occur. 75% of candesartan is excreted as unchanged drug in urine and feces.
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).
Half Life: Approximately 9 hours.
Clearance: 0.37 mL/min/kg
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 oral doses of the primary metabolite, candesartan, the minimum lethal dose was greater than 1000 mg/kg but less than 2000 mg/kg.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Administer on a regular basis, at about the same time each day.
Take without regard to meals.
Drug interaction:
TrandolaprilThe angiotensin II receptor blocker, Candesartan, may increase the adverse effects of Trandolapril.
LithiumThe ARB increases serum levels of lithium
TobramycinIncreased risk of nephrotoxicity
SpironolactoneIncreased risk of hyperkalemia
PotassiumIncreased risk of hyperkalemia
show more »

Targets


Enzymes


Transporters