Irbesartan Canon (Tablets) Instructions for Use

Marketing Authorization Holder

Canonpharma Production, CJS (Russia)

ATC Code

C09CA04 (Irbesartan)

Active Substance

Irbesartan (Rec.INN WHO registered)

Dosage Forms

	Irbesartan Canon	Tablets 150 mg: 7, 10, 14, 15, 20, 28, 30, 40, 56 or 60 pcs.
		Tablets 300 mg: 7, 10, 14, 15, 20, 28, 30, 40, 56 or 60 pcs.

Dosage Form, Packaging, and Composition

Tablets white or almost white, round, biconvex, with a score; slight marbling is allowed.

Excipients: corn starch pregelatinized – 51 mg, croscarmellose sodium – 12 mg, lactose monohydrate – 44 mg, magnesium stearate – 2 mg, povidone K30 – 10 mg, talc – 3 mg, microcrystalline cellulose – 28 mg.

7 pcs. – contour cell packaging (1) – cardboard packs.
7 pcs. – contour cell packaging (2) – cardboard packs.
7 pcs. – contour cell packaging (4) – cardboard packs.
7 pcs. – contour cell packaging (8) – cardboard packs.
10 pcs. – contour cell packaging (1) – cardboard packs.
10 pcs. – contour cell packaging (2) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (6) – cardboard packs.
14 pcs. – contour cell packaging (1) – cardboard packs.
14 pcs. – contour cell packaging (2) – cardboard packs.
14 pcs. – contour cell packaging (4) – cardboard packs.
15 pcs. – contour cell packaging (1) – cardboard packs.
15 pcs. – contour cell packaging (2) – cardboard packs.
15 pcs. – contour cell packaging (4) – cardboard packs.

Tablets white or almost white, round, biconvex, with a score; slight marbling is allowed.

Excipients: corn starch pregelatinized – 102 mg, croscarmellose sodium – 24 mg, lactose monohydrate – 88 mg, magnesium stearate – 4 mg, povidone K30 – 20 mg, talc – 6 mg, microcrystalline cellulose – 56 mg.

7 pcs. – contour cell packaging (1) – cardboard packs.
7 pcs. – contour cell packaging (2) – cardboard packs.
7 pcs. – contour cell packaging (4) – cardboard packs.
7 pcs. – contour cell packaging (8) – cardboard packs.
10 pcs. – contour cell packaging (1) – cardboard packs.
10 pcs. – contour cell packaging (2) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (6) – cardboard packs.
14 pcs. – contour cell packaging (1) – cardboard packs.
14 pcs. – contour cell packaging (2) – cardboard packs.
14 pcs. – contour cell packaging (4) – cardboard packs.
15 pcs. – contour cell packaging (1) – cardboard packs.
15 pcs. – contour cell packaging (2) – cardboard packs.
15 pcs. – contour cell packaging (4) – cardboard packs.

Clinical-Pharmacological Group

Angiotensin II receptor antagonist

Pharmacotherapeutic Group

Agents acting on the renin-angiotensin system, angiotensin II receptor antagonists (ARBs)

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 vasoconstrictor 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, decreases afterload. It reduces blood pressure (with minimal change in heart rate) and pressure in the pulmonary circulation, and the decrease in blood pressure 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. 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 reached within 3 days after starting irbesartan once daily. With repeated once-daily administration, limited accumulation of irbesartan in plasma is noted (less than 20%).

After oral administration of ¹⁴C-irbesartan, 80-85% of the radioactivity in 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%).

In the therapeutic dose range, Irbesartan is characterized by linear pharmacokinetics, with T_1/2 in the terminal phase being 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, 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 the tablets orally once daily, preferably at the same time each day, with or without food.

For arterial hypertension, initiate therapy with a dose of 150 mg.

If blood pressure control is inadequate, increase the dose to the maximum recommended dose of 300 mg.

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

In patients with a risk of excessive hypotension, such as those on a hypochloremic diet, receiving high-dose diuretics, with prior vomiting or diarrhea, or on hemodialysis, consider initiating therapy with a lower initial dose.

For patients with mild to severe renal impairment or with mild to moderate hepatic impairment, no initial dosage adjustment is typically required; titrate dose based on clinical response.

The tablets are scored and can be divided for dose titration if a 150 mg strength is unavailable.

The antihypertensive effect is substantially present within 1-2 weeks, with maximal reduction generally occurring after 4-6 weeks of treatment.

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 preparations.

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 a car and operate machinery.

Drug Interactions

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

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

With simultaneous use with lithium carbonate, an increase in the concentration of lithium in blood plasma 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.