Irbesartan

Irbesartan is an AT1 receptor blocker (sartan) with studies on protecting the kidneys in type 2 diabetes. It is used to treat high blood pressure and diabetic nephropathy.

Irbesartan is available as a generic and under the brand name Aprovel®. It is taken once daily and is well tolerated.

Irbesartan blocks the AT1 receptor:

Mechanism of action:

• Selective and long-lasting AT1 blockade
• Prevents the action of angiotensin II
• Dilation of blood vessels and lowering of blood pressure
• No activation by liver enzymes required (not a prodrug)

Kidney protection:

• Lowers the pressure in the renal glomerulus
• Reduces protein excretion (proteinuria)
• Slows the progression of diabetic kidney disease
• Demonstrated in the IDNT and IRMA-2 studies

Irbesartan is suitable for:

• Adults with high blood pressure
• Kidney disease in people with high blood pressure and type 2 diabetes

Especially recommended for:

• Diabetic nephropathy with proteinuria
• People with type 2 diabetes and high blood pressure

Not suitable for:

• Pregnancy and breastfeeding
• Severely impaired liver function (no clinical experience)
• Use together with aliskiren in diabetes or impaired kidney function (GFR below 60 ml/min/1.73 m²)

High blood pressure:

• Starting dose: 150 mg once daily
• Usual dose: 150-300 mg once daily
• Maximum dose: 300 mg daily

Diabetic nephropathy:

• Target dose: 300 mg once daily

Available strengths:

• 75 mg, 150 mg, 300 mg tablets

How to take:

• Once daily, always at the same time of day
• Regardless of meals
• Take with water

Notes:

• Regular blood pressure and lab checks
• Have your kidney values and potassium monitored
• Do not stop abruptly
• Drink enough fluids

Irbesartan must not be taken in case of:

• Hypersensitivity to irbesartan
• Pregnancy in the 2nd and 3rd trimester
• Use together with aliskiren in diabetes or impaired kidney function (GFR below 60 ml/min/1.73 m²)

Caution in case of:

• Kidney impairment
• Renal artery stenosis
• Hyperkalemia
• Dehydration
• Aortic stenosis

Pregnancy and breastfeeding: Irbesartan is not recommended in the 1st trimester of pregnancy and is contraindicated in the 2nd and 3rd trimesters. It can cause serious harm to the unborn child. Treatment should not be started during pregnancy. If pregnancy is detected, treatment must be stopped immediately and, if necessary, another therapy started. Irbesartan is not recommended during breastfeeding.

Very common (>10%):

• Hyperkalemia (in people with diabetes and high blood pressure)

Common (1-10%):

• Dizziness
• Orthostatic hypotension
• Fatigue

Uncommon (0.1-1%):

• Headache
• Nausea
• Gastrointestinal complaints
• Muscle pain
• Chest pain

Rare:

• Angioedema
• Liver function disorders
• Skin reactions

General: A well-tolerated medication.

Contraindicated:

• Aliskiren in diabetes or kidney impairment

Caution with:

• Potassium-sparing diuretics → hyperkalemia
• NSAIDs → reduced effect
• Lithium → increased levels
• Other antihypertensives → enhanced lowering of blood pressure

Note: Irbesartan is broken down in the liver mainly by the enzyme CYP2C9 and to a lesser extent by glucuronidation.