- Overview
- Properties
- Genetics
- Related Genes
- Pathways
- Related Drugs
- Related Diseases
- Downloads/LinkOuts
Overview
| Generic Names: | Candesartan cilexetil |
|---|---|
| Trade Names: | Amias; Atacand; Blopress; Ratacand |
| Brand Mixtures: | Atacand Plus (Candesartan Cilexetil + Hydrochlorothiazide) |
| PharmGKB Accession Id: | PA448765 |
Description
Candesartan, a specific angiotensin II antagonist, is used alone or with other antihypertensive agents to treat hypertension. Candesartan competes with angiotensin II for binding at the AT1 receptor subtype. As angiotensin II is a vasoconstrictor which also stimulates the synthesis and release of aldosterone, blockage of its effects results in a decreases in systemic vascular resistance. (source: Drug Bank)
Indication
For the treatment of hypertension. (source: Drug Bank)
ATC Therapeutic Category
- C09CA:Angiotensin II antagonists, plain
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Candesartan competes with angiotensin II for binding at the AT<sub>1</sub> receptor subtype. As angiotensin II is a vasoconstrictor which also stimulates the synthesis and release of aldosterone, blockage of its effects results in a decreases in systemic vascular resistance. (source: Drug Bank)
Pharmacology
Candesartan, a specific angiotensin II antagonist, is used alone or with other antihypertensive agents to treat hypertension. Unlike the angiotensin receptor antagonist losartan, Candesartan does not have an active metabolite or possess uricosuric effects. (source: Drug Bank)
Food Interactions
Administer on a regular basis, at about the same time each day.
Take without regard to meals.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
During absorption from the gastrointestinal tract, the prodrug candesartan cilexetil undergoes rapid and complete ester hydrolysis 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 occurs by O -deethylation to form an inactive metabolite. (source: Drug Bank)
Protein Binding
Candesartan is highly bound to plasma proteins (>99%) and does not penetrate red blood cells. (source: Drug Bank)
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. (source: Drug Bank)
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. (source: Drug Bank)
Isomeric SMILES Code:
CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)O (source: Drug Bank)
Curated Annotations (
)
-
rs5030062
at chr3:187936874
in
KNG1
This study investigated aldosterone response to two antihypertensive drugs with the result that the existence of one or more variants in the KNG1gene influences interindividual variation in aldosterone response. The SNPs rs5030062 and rs698078 were significantly associated in European-American responders to the diuretic (p=0.05 and p=0.01) and European-American responders to the angiotensin receptor blocker (p=0.04 and p=0.02).- Related Drugs:
- Antihypertensives, candesartan, hydrochlorothiazide
- Evidence:
-
PMID:19584173
-
rs698078
at chr3:187941921
in
KNG1
This study investigated aldosterone response to two antihypertensive drugs with the result that the existence of one or more variants in the KNG1gene influences interindividual variation in aldosterone response. The SNPs rs5030062 and rs698078 were significantly associated in European-American responders to the diuretic (p=0.05 and p=0.01) and European-American responders to the angiotensin receptor blocker (p=0.04 and p=0.02).- Related Drugs:
- Antihypertensives, candesartan, hydrochlorothiazide
- Evidence:
-
PMID:19584173
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
CYP11B2 |
|
Publications |
|
|
KNG1 |
|
Publications, Variants |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| AGTR1 |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| amiloride |
|
Increased risk of hyperkaliemia (source: Drug Bank) |
| drospirenone |
|
Increased risk of hyperkaliemia (source: Drug Bank) |
| lithium |
|
The ARB increases serum levels of lithium (source: Drug Bank) |
| potassium |
|
Increased risk of hyperkaliemia (source: Drug Bank) |
| spironolactone |
|
Increased risk of hyperkaliemia (source: Drug Bank) |
| triamterene |
|
Increased risk of hyperkaliemia (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Hypertension |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
LinkOuts
Common Searches
Search PubMed
Search Medline Plus
Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.