Index of drugs

Treatment of primary hypertension. Treatment of co-existing kidney disease in patients with hypertension and type 2 diabetes as part of the antihypertensive therapeutic procedure.

1 tabl powl. contains 150 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 at the angiotensin II receptors results in increased blood levels of renin and angiotensin II and a decrease in aldosterone. Irbesartan, in therapeutic doses, does not significantly affect the level of potassium in the blood. It does not inhibit the action of ACE (kininase II), the enzyme responsible for the formation of angiotensin II and the breakdown of bradykinin into inactive metabolites. It does not require metabolic activation for its activity. Irbesartan is well absorbed after oral administration (absolute bioavailability is about 60-80%). 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 other ingredients. 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).

Patients with decreased intravascular volume and / or sodium depletion, caused by intense dehydrating treatment, reduced salt supply in the diet, diarrhea or vomiting, may exhibit symptomatic hypotension, especially after the first dose. Such conditions should be evened out before applying the preparation. In patients with bilateral renal artery stenosis or artery stenosis of the only active kidney there is an increased risk of severe hypotension and renal failure. When irbesartan is used in patients with impaired renal function, periodic monitoring of potassium and creatinine in the blood is recommended. 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 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. 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. Co-administration of irbesartan and lithium is not recommended. Particularly cautiously use in patients with aortic or mitral valve stenosis or hypertrophic cardiomyopathy with narrowing of the left ventricle outflow pathway. Do not use the preparation in patients with primary hyperaldosteronism. In patients whose vascular tone and renal function depend mainly on the activity of the renin-angiotensin-aldosterone system (e.g., patients with severe congestive heart failure or kidney disease, including renal artery stenosis), irbesartan may precipitate a rapid reduction in blood pressure of arterial blood, azotemia, oliguria, or in rare cases - acute renal failure. As with other antihypertensive agents, excessive hypotension in patients with ischemic cardiomyopathy or other forms of atherosclerosis may lead to heart attacks or strokes. Irbesartan is less effective in lowering blood pressure in black patients than in other breeds.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. 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 from 6 to 16 years of age, but the data are 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 (renal failure, oligohydramnios, delayed ossification of the skull) and newborn (renal failure, hypotension, hyperkalemia) - if exposure to the drug occurred from the second trimester of pregnancy, it is recommended performing an ultrasound examination of the fetus skull and kidneys; newborns whose mothers took the drug during pregnancy should be closely monitored due to the possibility of hypotension. The drug is not recommended during breast-feeding.

Common: increased creatine kinase in plasma, dizziness, nausea, vomiting, orthostatic hypotension, fatigue. Uncommon: tachycardia, cough, diarrhea, indigestion, heartburn, flushing, chest pain, sexual dysfunction. In addition, you may experience: headache, tinnitus, dysgeusia, renal dysfunction (including cases of renal failure in patients with risk factors), leukocytoclastic vasculitis, arthralgia, muscle pain (in some cases associated with increased creatine kinase activity) , muscle spasms, hypersensitivity reactions (rash, urticaria, angioneurotic edema), hepatitis, abnormal liver function. In patients with hypertension and type 2 diabetes mellitus with co-existing chronic renal failure and overt proteinuria, the following adverse reactions have also been reported - very common: hyperkalemia; often: orthostatic dizziness, orthostatic hypotension, musculoskeletal pain, decrease in hemoglobin. In patients with hypertension and diabetes with microalbuminuria and normal renal function, orthostatic dizziness and orthostatic hypotension have been reported uncommonly.

Orally. The usually 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. When starting treatment, however, a 75 mg dose may be considered. 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 the formulation. In patients with hypertension and type 2 diabetes, treatment should be started with 150 mg once a day and gradually increased to 300 mg once a day, the recommended maintenance dose for the treatment of co-existing renal disease. The demonstration of the beneficial effect of the preparation on renal function in patients with hypertension and type 2 diabetes is based on clinical trials in which irbesartan was used in combination with other antihypertensive agents, 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, washed down with water.