- Overview
- Properties
- Genetics
- Related Genes
- Pathways
- Related Drugs
- Related Diseases
- Downloads/LinkOuts
Overview
| Generic Names: | irbesartan |
|---|---|
| Trade Names: | Avalide; Avapro; Irbesarran; Irbesartan [Usan:Inn]; Lrbesartan |
| Brand Mixtures: | Avalide 150/12.5 mg (Hydrochlorothiazide + Irbesartan); Avalide 300/12.5 mg (Hydrochlorothiazide + Irbesartan) |
| PharmGKB Accession Id: | PA450084 |
Description
Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. (source: Drug Bank)
Indication
For the treatment of hypertension, and for the treatment of diabetic nephropathy with an elevated serum creatinine and proteinuria (>300 mg/day) in patients with type 2 diabetes and hypertension. (source: Drug Bank)
ATC Therapeutic Category
- C09CA:Angiotensin II antagonists, plain
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Irbesartan is a nonpeptide angiotensin II antagonist that selectively blocks the binding of angiotensin II to the AT<sub>1</sub> receptor. In the renin-angiotensin system, angiotensin I is converted by angiotensin-converting enzyme (ACE) to form angiotensin II. Angiotensin II stimulates the adrenal cortex to synthesize and secrete aldosterone, which decreases the excretion of sodium and increases the excretion of potassium. Angiotensin II also acts as a vasoconstrictor in vascular smooth muscle. Irbesartan, by blocking the binding of angiotensin II to the AT<sub>1</sub> receptor, promotes vasodilation and decreases the effects of aldosterone. The negative feedback regulation of angiotensin II on renin secretion also is inhibited, but the resulting rise in plasma renin concentrations and consequent rise in angiotensin II plasma concentrations do not counteract the blood pressure–lowering effect that occurs. (source: Drug Bank)
Pharmacology
Irbesartan is a specific competitive antagonist of AT<sub>1</sub> receptors with a much greater affinity (more than 8500-fold) for the AT<sub>1</sub> receptor than for the AT<sub>2</sub> receptor and no agonist activity. (source: Drug Bank)
Food Interactions
Take without regard to meals. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic. Irbesartan is metabolized via glucuronide conjugation and oxidation. In vitro studies of irbesartan oxidation by cytochrome P450 isoenzymes indicated irbesartan was oxidized primarily by 2C9; metabolism by 3A4 was negligible. (source: Drug Bank)
Protein Binding
90% bound to serum proteins (primarily albumin and a1-acid glycoprotein) with negligible binding to cellular components of blood. (source: Drug Bank)
Absorption
Rapid and complete with an average absolute bioavailability of 60-80%. Food has no affect on bioavailability. (source: Drug Bank)
Toxicity
Hypotension and tachycardia; bradycardia might also occur from overdose, LD<sub>50</sub>=mg/kg(orally in rat) (source: Drug Bank)
Isomeric SMILES Code:
CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5 (source: Drug Bank)
Curated Annotations (
)
-
rs1367117
at chr2:21117405
in
APOB
The APOB:711C>T, C allele was associated with reduction of blood pressure in response to irbesartan treatment but not atenolol treatment.- Variant Name:
- APOB:711C>T,
- Related Drugs:
- atenolol, irbesartan
- Related Diseases:
- Hypertension
- Evidence:
-
PMID:15453913
-
rs688
at chr19:11088602
in
LDLR
The C-allele of LDLR: 16730C>T was predictive of change in systolic blood pressure in response to atenolol.- Variant Name:
- LDLR: 16730C>T,
- Related Drugs:
- atenolol, irbesartan
- Related Diseases:
- Hypertension
- Evidence:
-
PMID:15453913
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
ACE |
|
Publications |
|
APOB |
|
Variants |
|
|
CYP2C9 |
|
Publications |
|
|
LDLR |
|
Variants |
|
|
TGFB1 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| AGTR1 |
|
(source: Drug Bank) |
| AGT |
|
(source: Drug Bank) |
| JUN |
|
(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, Variants |
|
|
Marfan Syndrome |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.