Index of drugs

Treatment of primary hypertension. Treatment of kidney disease in patients with hypertension and type 2 diabetes as part of antihypertensive therapeutic management.

1 tabl powl. contains 75 mg, 150 mg or 300 mg irbesartan.

Angiotensin II receptor antagonist (AT type₁). Irbesartan blocks all actions of angiotensin II, regardless of the source or route of its synthesis. Selective antagonism towards AT₁ causes an increase in the concentration of renin and angiotensin II in the blood and a decrease in aldosterone. Irbesartan, in therapeutic doses, does not significantly affect the level of potassium in the blood. It is also not an ACE inhibitor, thanks to which it does not increase the effects of bradykinin-dependent effects. It does not require metabolic activation for its activity. Irbesartan is well absorbed after oral administration (absolute bioavailability is about 60-80%), reaching C_max after 1.5-2 h. Simultaneous food intake does not significantly affect the bioavailability of irbesartan. About 96% is bound to plasma proteins. It is metabolized in the liver by conjugation with glucuronic acid and oxidation (mediated by CYP2C9). Irbesartan and its metabolites are excreted in both bile (80%) and urine (20%). Final T_0,5 is 11-15 hours.

Hypersensitivity to irbesartan or to any of the excipients. II and III trimester of pregnancy. Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (glomerular filtration rate, GFR <60 ml / min / 1.73 m²).

Do not use the preparation in patients with primary hyperaldosteronism. There is no experience regarding the use of irbesartan in patients with severe hepatic impairment or in patients with recent kidney transplantation. In patients with impaired renal function, periodic monitoring of potassium and creatinine in the blood is recommended. In patients with bilateral renal artery stenosis or stenosis of the artery to the sole active kidney, there is an increased risk of severe hypotension and renal failure with irbesartan. In patients whose vascular tone and renal function are dependent on the activity of the renin-angiotensin-aldosterone system (eg patients with severe congestive heart failure or kidney disease, including renal artery stenosis), irbesartan may precipitate a sudden fall in blood pressure blood, azotemia, oliguria, or in rare cases - acute renal failure. Because of the risk of hypotension, use caution in patients with a decreased intravascular volume and / or sodium depletion due to intense dehydrating treatment, reduced salt supply in the diet, diarrhea or vomiting - these deficiencies should be corrected before irbesartan is used. As with other antihypertensive agents, excessive hypotension in patients with ischemic cardiomyopathy or ischemic heart disease can lead to a heart attack or stroke. Particularly cautiously use in patients with aortic or mitral valve stenosis or hypertrophic cardiomyopathy with narrowing of the left ventricle outflow pathway. In patients at risk for hyperkalemia, especially with impaired renal function, overt proteinuria due to diabetic kidney disease and / or heart failure, close monitoring of potassium levels in blood is recommended. Irbesartan is less effective in lowering blood pressure in black patients than in other breeds. In patients with hypertension, type 2 diabetes and advanced renal disease, the effects of irbesartan, both in relation to renal and cardiovascular incidents, may be less effective in women and non-white patients.The concomitant use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren increases the risk of hypotension, hyperkalaemia and renal dysfunction (including acute renal failure) - therefore, dual blocking of the RAA system is not recommended by concomitant use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren. If the use of a dual RAA blockade is absolutely necessary, it should only be carried out under the supervision of a specialist, and the vital parameters of the patient, such as kidney function, electrolyte concentration and blood pressure should be closely monitored. In patients with diabetic nephropathy, ACE inhibitors and angiotensin II receptor antagonists should not be used concurrently. Co-administration of irbesartan and lithium is not recommended. Irbesartan is not recommended for use in children and adolescents due to insufficient data on safety and efficacy (the drug was tested in the population of children aged 6 to 16 years, but the current data is insufficient to extend its use to this population).

The use of the preparation in the first trimester of pregnancy is not recommended (there is a risk of teratogenic effect). Use in the second and third trimester of pregnancy is contraindicated. Irbesartan used in the second and third trimester of pregnancy is toxic to fetal development (deterioration of renal function, oligohydramnios, delayed ossification of the skull) and newborn (renal failure, hypotension, hyperkalemia) - when exposure to the drug occurred from the second trimester of pregnancy, it is recommended an ultrasound examination of the fetus skull and kidneys; children whose mothers took the drug during pregnancy should be closely monitored for hypotension. The drug is not recommended during breast-feeding.

Very common: hyperkalemia. Common: increase in creatine kinase, decrease in hemoglobin, dizziness, orthostatic dizziness, nausea, vomiting, musculoskeletal pain, orthostatic hypotension, fatigue. Uncommon: tachycardia, cough, diarrhea, indigestion, heartburn, redness of the face, chest pain, sexual dysfunction. In addition, you may experience: headache, tinnitus, disturbed taste, kidney problems (including cases of kidney failure in patients with risk factors), leukocytoclastic vasculitis, arthralgia, myalgia (in some cases associated with increased creatine kinase activity) , painful muscle cramps, hypersensitivity reactions (rash, urticaria, angioneurotic edema), hepatitis, abnormal liver function.

Orally. The usual recommended initial and maintenance dose is 150 mg once a day. A single daily dose of 150 mg enables a better daily control of blood pressure than at a dose of 75 mg. In patients who do not achieve adequate control after a single daily dose of 150 mg, the dose may be increased to 300 mg or another antihypertensive agent may be used. In particular, the additional use of a diuretic, such as hydrochlorothiazide, has shown additive activity with irbesartan. In patients with hypertension and type 2 diabetes, treatment should be initiated with 150 mg irbesartan once a day and gradually increase to 300 mg once a day, ie to the recommended maintenance dose for the treatment of co-existing renal disease. If necessary, another antihypertensive drug may be used to obtain normal blood pressure.Special groups of patients. No dosage adjustment is necessary in patients with mild to moderate hepatic impairment and in patients with impaired renal function. A lower starting dose (75 mg) should be considered in patients undergoing hemodialysis. Elderly patients do not usually need to adjust their dosage, although in patients> 75 years of age, starting 75 mg should be considered.
The tablets can be taken with or without food, with water.