IRBEK

Irbesartan is an angiotensin receptor blocker (ARB) indicated to treat hypertension or diabetic nephropathy. 7, 8 It can also be used as part of a with hydrochlorothiazide for patients not well controlled or not expected to be well controlled on monotherapy.

Unlike angiotensin converting enzyme inhibitors, ARBs are not associated with a dry cough. 7, 8 Irbesartan was granted FDA approval on 30 September 1997. 7, 8.

Irbesartan is indicated to treat hypertension and diabetic nephropathy in hypertensive patients with type 2 diabetes, elevated serum creatinine, and proteinuria.

A with hydrochlorothiazide is indicated for hypertension in patients with uncontrolled hypertension with monotherapy or first line in patients not expected to be well controlled with monotherapy.

Irbesartan is an angiotensin receptor blocker used to treat hypertension and diabetic nephropathy. 7, 8 It has a long duration of action as it is usually taken once daily and a wide therapeutic index as doses may be as low as 150 mg daily but doses of 900 mg/day were well tolerated in healthy human subjects. 7, 8, 5.

Irbesartan is 60-80% bioavailable with a T max of 1.5-2hours. 7, 8 Taking irbesartan with food does not affect the bioavailability. 7, 8 In one study, healthy subjects were given single or multiple oral doses of 150 mg, 300 mg, 600 mg, and 900 mg of irbesartan.

A single 150 mg dose resulted in an AUC of 9.7±3.0 µg•hr/mL, a T max of 1.5 hours, a half life of 16±7 hours, and a C max of 1.9±0.4 µg/mL.

A single 300 mg dose resulted in an AUC of 20.0±5.2 µg•hr/mL, a T max of 1.5 hours, a half life of 14±7 hours, and a C max of 2.9±0.9 µg/mL.

A single 600 mg dose resulted in an AUC of 32.6±11.9 µg•hr/mL, a T max of 1.5 hours, a half life of 14±8 hours, and a C max of 4.9±1.2 µg/mL.

A single 900 mg dose resulted in an AUC of 44.8±20.0 µg•hr/mL, a T max of 1.5 hours, a half life of 17±7 hours, and a C max of 5.3±1.9 µg/mL.

Multiple 150 mg doses resulted in an AUC of 9.3±3.0 µg•hr/mL, a T max of 1.5 hours, a half life of 11±4 hours, and a C max of 2.04±0.4 µg/mL.

Multiple 300 mg doses resulted in an AUC of 19.8±5.8 µg•hr/mL, a T max of 2.0 hours, a half life of 11±5 hours, and a C max of 3.3±0.8 µg/mL.

Multiple 600 mg doses resulted in an AUC of 31.9±9.7 µg•hr/mL, a T max of 1.5 hours, a half life of 15±7 hours, and a C max of 4.4±0.7 µg/mL.

Multiple 900 mg doses resulted in an AUC of 34.2±9.3 µg•hr/mL, a T max of 1.8 hours, a half life of 14±6 hours, and a C max of 5.6±2.1 µg/mL.

The volume of distribution of irbesartan is 53-93 L. 7, 8.

Irbesaran is largely metabolized by glucuronidation and oxidation in the liver. 7, 8 The majority of metabolism occurs through the action of CYP2C9 with a negligible contribution from CYP3A4. 7, 8 Some hydroxylation also occurs in irbesartan metabolism.

Irbesartan can be glucuronidated by

UGT1A3 to the M8 metabolite, oxidized to the M3 metabolite, or hydroxylated by CYP2C9 to one of the M4, M5, or M7 metabolites. 4, 3 The M4, M5, and M7 metabolites are all hydroxylated to become the M1 metabolite, which is then oxidized to the M2 metabolite. 4, 3 The M4 metabolite can also be oxidized to the M6 metabolite before hydroxylation to the M2 metabolite. 4, 3 Finally, the minor metabolite SR is generated from irbesartan by an unknown mechanism. 4, 3 Hover over products below to view reaction partners Irbesartan SR 49498 Irbesartan derivative M4 Irbesartan derivative M6 Irbesartan derivative M2 Irbesartan derivative M1 Irbesartan derivative M2 Irbesartan derivative M5 Irbesartan derivative M1 Irbesartan derivative M2 Irbesartan derivative M7 Irbesartan derivative M1 Irbesartan derivative M2 Irbesartan derivative M3 Irbesartan derivative M8.

20% of a radiolabelled oral dose of irbesartan is recovered in urine, and the rest is recovered in the feces. 10 <2% of the dose is recovered in urine as the unchanged drug.

The terminal elimination half life of irbesartan is 11-15 hours. 7, 8.

Total plasma clearance of irbesartan is 157-176 mL/min while renal clearance is 3.0-3.5 mL/min. 7, 8.

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The oral

TDLO in humans is 30 mg/kg/6W.

Symptoms of overdose include hypotension and tachycardia or bradycardia. 7, 8 Terlipressin may be given to treat hypotension and tachycardia if conventional vasopressors fail to control blood pressure.

Irbesartan tablets are contraindicated in patients who are hypersensitive to any component of this product.

Do not coadministrate aliskiren with irbesartan tablets in patients with diabetes.

Hypersensitivity to any component of this product.

Coadministration with aliskiren in patients with diabetes.

Hypertension to 300 mg once daily Diabetic Nephropathy 300 mg once daily 2.1 General Considerations Irbesartan tablets may be administered with other antihypertensive agents and with or without food. 2.2 Hypertension The recommended initial dose of irbesartan tablets is 150 mg once daily.

The dosage can be increased to a maximum dose of 300 mg once daily as needed to control blood pressure. 2.3 Nephropathy in Type 2 Diabetic Patients The recommended dose is 300 mg once daily. 2.4 Dose Adjustment in Volume and Salt-Depleted Patients The recommended initial dose is 75 mg once daily in patients with depletion of intravascular volume or salt (e.g., patients treated vigorously with diuretics or on hemodialysis) .

Irbesartan tablets are available as white to off-white biconvex oval tablets, debossed with “HH” on one side and HH;330 on other side NDC: 70518-1690-00 NDC: 70518-1690-01 PACKAGING: 90 in 1 BOTTLE PLASTIC PACKAGING: 90 in 1 BOTTLE PLASTIC Store at 20oC-25oC (68oF-77oF); excursions permitted to 15oC-30oC (59oF-86oF) .

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