P - Contraindicated in pregnancy
L - Contraindicated in lactation
Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. Irbesartan was developed by Sanofi Research (now part of sanofi-aventis). It is jointly marketed by sanofi-aventis and Bristol-Myers Squibb under the trade names Aprovel, Karvea, and Avapro.
Irbesartan is an angiotensin II type I receptor antagonist and therefore blocks the vasoconstricting and aldosterone-secreting effects of angiotensin II.
Absorption
Rapidly absorbed from the GIT (oral); peak plasma concentrations are achieved after 1.5-2 hours.
Distribution
Protein-binding around 96%
Metabolism
Some hepatic metabolism via cytochrome P450 isoenzyme CYP2C9 to inactive metabolites.
Excretion
Via bile and urine (as unchanged drug and metabolites); via urine (20% of IV dose, <2% as unchanged). 11-15 hours (elimination half-life).
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Diarrhoea, dizziness, fatigue, headache, hyperkalaemia. Dyspepsia, oedema, myalgia, insomnia, nasal congestion, 1st dose orthostatic hypotension, rash, pharyngitis, urticaria, angioedema, anxiety/nervousness, tachycardia.
Renal Function
Use with caution in patients whose renal function may depend on the activity of the renin-angiotensin-aldosterone system (eg, patients with severe CHF); use may be associated with oliguria, progressive azotemia, acute renal failure, and death.
Hypotension
Initiation of antihypertensive therapy may cause symptomatic hypotension in patients with intravascular volume or sodium-depletion.
Child <6 years. Unilateral or bilateral renal artery stenosis; vol or Na depletion; aortic or mitral valve stenosis, hypertrophic cardiomyopathy.
Potassium or potassium-sparing diuretics may increase risk of hyperkalaemia. NSAIDs may reduce antihypertensive response. Excretion of lithium may be reduced, monitor lithium concentrations.
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Oral
Hypertension
Adult: 150 mg once daily, increased to 300 mg once daily if necessary. For patients with intravascular volume depletion: Initially, 75 mg once daily.
Child: 6-16 years: 75 mg once daily increased to 150 mg if necessary.
Elderly: >75 years: Initially 75 mg once daily.
Renal impairment: Haemodialysis: Initially, 75 mg once daily.
Oral
Diabetic nephropathy in Type 2 diabetes mellitus
Adult: 150 mg once daily, increased to 300 mg once daily if necessary.
May be taken with or without food.
Contraindicated in pregnancy
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
In 2nd & 3rd trimesters.
Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Contraindicated in lactation
Safety and efficacy not established in children younger than 6 years of age.
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Hypersensitivity; pregnancy and lactation
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