Prosp Pharma
Full Prescribing Info
Each tablet contains Irbesartan 150 mg and 300 mg.
Pharmacology: Pharmacodynamics: Irbesartan are angiotensin II receptor (type AT1) antagonists. Angiotensin II is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system. Its effects are vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Angiotensin II receptor antagonists block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues (eg, vascular smooth muscle, adrenal gland).
Pharmacokinetics: Onset of action: Peak effect : 1-2 hours.
Duration : > 24 hours.
Distribution : Vd 53-93 L.
Protein binding, plasma : 90%.
Metabolism : Hepatic, primarily CYP2C9.
Bioavailability : 60% to 80%.
Half-life elimination : Terminal : 11-15 hours.
Time to peak, serum : 1.5-2 hours.
Excretion : Feces (80%); urine (20%).
Treatment of hypertension: It may be used alone or combination with other antihypertensive agents.
Treatment of diabetic nephropathy: For the treatment with an elevated serum creatinine and proteinuria (greater than 300 mg/day) in patients with type 2 diabetes and a history of hypertension.
Dosage/Direction for Use
Hypertension: Adults: Usual dosage : 150 mg orally once daily.
Initial dosage : 150 mg once daily.
Maintenance dosage : 150 to 300 mg once daily.
Maximum dose : 300 mg/day.
Dosage titration : Patients requiring further reduction in blood pressure should be titrated to 300 mg once daily.
Children : < 6 years : Safety and efficacy have not been established.
6 to 12 years of age: Usual dosage : 75 to 150 mg/day. Initial dosage : 75 mg once daily.
13 years and older: Usual dosage : 150 to 300 mg/day. Initial dosage : 150 mg once daily.
Nephropathy in type 2 diabetes and hypertension : Usual dosage : 300 mg orally once daily.
Volume and salt-depleted patients : A lower initial dose 75 mg is recommended in patients with depletion of intravascular volume or salt (eg, patients treated vigorously with diuretics or on hemodialysis).
Renal function impairment : It is necessary for patients with volume-depleted renal impairment prior to administration. The recommended initial dose is 75 mg.
Hepatic function impairment : No significantly affected in patients with mild to moderate cirrhosis of the liver. No dosage adjustment is necessary in these patients with hepatic insufficiency.
Elderly : No dosage adjustment is necessary. No overall differences in effectiveness or safety were observed between elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out and 75 mg of initial dose is recommended.
Concomitant therapy : Irbesartan may be administered with other antihypertensive agents. A low dose of a diuretic may be added if blood pressure is not controlled by irbesartan alone. Hydrochlorothiazide has been shown to have an additive effect.
Mode of administration : Irbesartan is administered orally. It can be taken without regards to meals, with or without food.
The most likely manifestation of overdosage with an irbesartan would be hypotension, dizziness, and tachycardia. If symptomatic hypotension should occur, institute supportive treatment. Irbesartan cannot be removed by hemodialysis.
Patients who have a hypersensitivity to Irbesartan or any component of this formulation, children under 6 years of age, pregnancy, breast-feeding women.
Do not use this drug during pregnancy.
Consult the physicians if lethargy symptom or vomiting have occur.
Consult the physicians immediately if swelling of the faces, tongue, larynx, or difficulty breathing have occur when using this drug.
This drug may cause renal failure. Should be used with caution.
This drug may cause hyperkalemia. Should not be used in patients who received potassium or potassium sparing diuretics treatment.
Special Precautions
Irbesartan can cause injury and death to the developing fetus when used in the second and third trimesters. It should be discontinued as soon as possible once pregnancy is detected.
Safety and efficacy have not been established in children under 6 years. Geriatric use may increase their sensitivities.
In patients who are intravascularly volume depleted (eg, those treated with diruretics, major surgery), symptomatic hypotension may occur. The administration or start treatment should be under close medical supervision with a reduced dose. If hypotension occurs, place the patient in the supine position and, if necessary, give an IV infusion of normal saline. A treatment for transient hypotension can be continued after the blood pressure is stabilized.
Irbesartan may cause hyperkalemia, so avoid potassium supplementation unless specifically required by healthcare provider.
Use with caution in renal impairment because it may deteriorate the renal function.
Use in combination with hydrochlorothiazide is not recommended in patients with severe renal impairment.
Use in patients with unilateral or bilateral renal artery stenosis, it may increases serum creatinine or serum urea nitrogen (BUN). In some patients, these effects were reversible upon discontinuation of therapy.
In patients with severe congestive heart failure, treatment with irbesartan has been associated with oliguria or progressive azotemia, and may rarely cause acute renal failure and/ or death.
Use In Pregnancy & Lactation
Use in Pregnancy: Pregnancy category C (1st semester) or D (2nd and 3rd trisemesters). Drug can cause injury and death to the developing fetus when used in the second and third trimesters. It should be discontinued as soon as possible once pregnancy is detected.
Use in Lactation: Irbesartan were present in rat milk but it is not known if it is excreted in human breast milk. Because of the potential for adverse effects on the breast-feeding infant, caution women not taking this drug to breast-feed their infants.
Adverse Reactions
Endocrine and metabolic : Hyperkalemia.
Cardiovascular : Orthostatic hypotension (5%).
Central nervous system : Fatigue (4%), dizziness (10%).
Gastrointestinal : Diarrhea (3%), dyspepsia (2%).
Respiratory : Upper respiratory infection (9%), cough (2.8%).
Others : Angina, angioedema, arrhythmia, cardiopulmonary arrest, conjunctivitis, depression, dyspnea, ecchymosis, edema, epistaxis, gout, heart failure, hepatitis, hypotension, jaundice, libido increased, MI, orthostatic hypotension, paresthesia, sexual dysfunction, stroke, transaminases increased, urticaria.
Drug Interactions
Increased effect/Toxicity : Irbesartan may increase the levels/effects of : ACE inhibitors; amifostine; antihypertensive; carvedilol; hypotensive agents; lithium; potassium sparing diuretics; Rituximab.
The levels/effects of irbesartan may be increased by diazoxide; eplerenone; fluconazole; herbs (hypotensive properties); MAO inhibitors; pentoxifylline; phosphodiesterase 5 inhibitors; potassium salts, prostacyclin analogues; tolvaptan; trimethoprim.
Decreased effect : The levels/effects of irbesartan may be decreased by herbs (hypertensive properties); methylphenidate; non-steroidol anti-inflammatory agents; rifamycin derivatives; yohimbine.
Herb/Nutraceutical : Avoid dong quai if using for hypertension (has estrogenic activity). Avoid ephedra, yohimbe, ginseng (may worsen hypertension). Avoid garlic (may have increased antihypertensive effect).
Store below 25°C.
ATC Classification
C09CA04 - irbesartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
Tab (white, oval, biconvex, plain on both sides) 150 mg x 3 x 10's. 300 mg x 3 x 10's.
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