Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antihypertensive agent, angiotensin II receptor antagonist. It blocks AT 1 -receptors, which leads to a decrease in the biological effects of angiotensin II, incl.vasoconstrictive action, stimulating effect on the release of aldosterone and activation of the sympathetic nervous system. As a consequence, blood pressure decreases.
Reduces OPSS, reduces afterload. Reduces blood pressure (with a minimum change in heart rate) and pressure in a small circle of blood circulation, and the decrease in blood pressure is dose-dependent.
Does not affect the concentration of triglycerides, the content of cholesterol, glucose, uric acid in the blood plasma or uric acid in the urine.
PHARMACOKINETICS
After oral administration, it is well absorbed from the digestive tract. C max irbesartan in the blood plasma is achieved after 1.5-2 h after ingestion. Bioavailability is 60-80%. Simultaneous food intake does not affect the bioavailability of irbesartan.
Binding to plasma proteins is about 96%. V d - 53-93 liters. C ss is achieved within 3 days after the initiation of irbesartan 1 time / day. With repeated administration of 1 time / day there is a limited accumulation of irbesartan in plasma (less than 20%).
After ingestion of 14 C-irbesartan, 80-85% of the radioactivity in the circulating blood occurs in unchanged irbesartan.
Irbesartan is metabolized in the liver by conjugation to form glucuronide and by oxidation. The main metabolite is irbesartan glucuronide (about 6%).
In the therapeutic dose range, irbesartan is characterized by linear pharmacokinetics, with T 1/2 in the terminal phase being 11-15 hours. The total clearance and renal clearance are 157-176 ml / min and 3-3.5 ml / min, respectively. Irbesartan and its metabolites are excreted in bile and urine.
In patients with impaired renal function, cirrhosis of moderate severity, the pharmacokinetic parameters of irbesartan do not change significantly.
INDICATIONS
Arterial hypertension.
Nephropathy in patients with arterial hypertension and type 2 diabetes mellitus (as part of combined antihypertensive therapy).
DOSING MODE
The initial dose is 150 mg, if necessary, increase the dose to 300 mg. In a number of cases (a hypochloride diet, treatment with certain diuretics, previous vomiting or diarrhea, hemodialysis), a lower initial dose is used.
Irbesartan is taken orally 1 time / day, preferably at the same time of day.
SIDE EFFECT
From the side of the central nervous system: headache, dizziness.
From the digestive system: nausea, vomiting.
Other: malaise, weakness.
CONTRAINDICATIONS
Pregnancy, children's age, hypersensitivity to irbesartan.
PREGNANCY AND LACTATION
Contraindicated in pregnancy.
If it is necessary to use during the lactation period, the question of stopping breastfeeding should be solved.
APPLICATION FOR FUNCTIONS OF THE LIVER
Use with caution in patients with impaired renal function ,.
APPLICATION FOR CHILDREN
Contraindicated in childhood.
SPECIAL INSTRUCTIONS
They are used with caution in patients with impaired renal function, after severe vomiting or diarrhea, and against simultaneous therapy with potassium-sparing diuretics or potassium preparations.
In experimental studies on laboratory animals, mutagenic, clastogenic and carcinogenic effects of irbesartan have not been established.
Impact on the ability to drive vehicles and manage mechanisms
There are no indications of the influence of irbesartan on the ability to drive vehicles and control mechanisms.
DRUG INTERACTION
With simultaneous application with potassium-sparing diuretics, potassium preparations, an increase in the potassium content in the blood plasma is possible.
When used simultaneously with hydrochlorothiazide, the additive nature of the hypotensive effect is manifested.
With simultaneous application of lithium carbonate, an increase in the concentration of lithium in the blood plasma is possible.
With simultaneous application of fluconazole can inhibit the metabolism of irbesartan.
