Irbis (Tablets) Instructions for Use

ATC Code

C09CA04 (Irbesartan)

Active Substance

Irbesartan (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Angiotensin II receptor antagonist

Pharmacotherapeutic Group

Angiotensin II receptor antagonist

Pharmacological Action

Antihypertensive agent, angiotensin II receptor antagonist. It blocks AT₁ receptors, which leads to a decrease in the biological effects of angiotensin II, including its vasoconstrictive action, stimulating effect on aldosterone release, and activation of the sympathetic nervous system. As a result, blood pressure decreases.

It reduces total peripheral vascular resistance and decreases afterload. It lowers blood pressure (with minimal change in heart rate) and pressure in the pulmonary circulation, and the blood pressure reduction is dose-dependent.

It does not affect the concentration of triglycerides, cholesterol, glucose, uric acid in blood plasma, or the excretion of uric acid in urine.

Pharmacokinetics

After oral administration, it is well absorbed from the gastrointestinal tract. The C_max of irbesartan in blood plasma is reached 1.5-2 hours after oral administration. Bioavailability is 60-80%. Concurrent food intake does not affect the bioavailability of irbesartan.

Plasma protein binding is about 96%. V_d is 53-93 L. C_ss is achieved within 3 days after starting irbesartan once daily. With repeated once-daily administration, limited accumulation of irbesartan in plasma is observed (less than 20%).

After oral administration of ¹⁴C-irbesartan, 80-85% of the radioactivity in the circulating blood is accounted for by unchanged Irbesartan.

Irbesartan is metabolized in the liver by conjugation to form a glucuronide and by oxidation. The main metabolite is Irbesartan glucuronide (about 6%).

Within the therapeutic dose range, Irbesartan exhibits linear pharmacokinetics, with a T_1/2 in the terminal phase of 11-15 hours. 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 and moderate liver cirrhosis, 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).

ICD codes

Dosage Regimen

Take Irbesartan orally once daily, consistently at the same time each day, with or without food.

The initial and maintenance dose for arterial hypertension is 150 mg.

If adequate blood pressure control is not achieved, increase the dose to the maximum recommended dose of 300 mg.

For nephropathy in patients with type 2 diabetes mellitus and hypertension, the recommended dose is 300 mg.

Initiate therapy at 150 mg and titrate to 300 mg as tolerated for optimal renoprotective effect.

In patients with volume depletion due to diuretic therapy, dietary salt restriction, vomiting, diarrhea, or hemodialysis, initiate therapy at a lower initial dose of 75 mg to mitigate risks of symptomatic hypotension.

Dosage adjustment is not typically required for elderly patients or those with mild to severe renal impairment or mild to moderate hepatic impairment.

For patients with hepatic cirrhosis, initiate with caution; no initial dose adjustment is necessary, but careful monitoring is advised.

Adverse Reactions

From the central nervous system headache, dizziness.

From the digestive system nausea, vomiting.

Other malaise, weakness.

Contraindications

Pregnancy, childhood, hypersensitivity to irbesartan.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy.

If use during lactation is necessary, the issue of discontinuing breastfeeding should be considered.

Use in Renal Impairment

Use with caution in patients with impaired renal function.

Pediatric Use

Contraindicated in childhood.

Special Precautions

Use with caution in patients with impaired renal function, after severe vomiting or diarrhea, and during concurrent therapy with potassium-sparing diuretics or potassium supplements.

In experimental studies on laboratory animals, no mutagenic, clastogenic, or carcinogenic effects of irbesartan were established.

Effect on ability to drive vehicles and operate machinery

There are no indications of the effect of irbesartan on the ability to drive vehicles or operate machinery.

Drug Interactions

With simultaneous use with potassium-sparing diuretics or potassium supplements, an increase in plasma potassium levels is possible.

With simultaneous use with hydrochlorothiazide, an additive nature of the hypotensive effect is manifested.

With simultaneous use with lithium carbonate, an increase in plasma lithium concentration is possible.

With simultaneous use, fluconazole may inhibit the metabolism of irbesartan.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.