Irbesartan Canon, tablets 300 mg 14 pcs

Irbesartan lowers blood pressure (BP) with minimal change in heart rate (HR). When administered in doses up to 900 mg once daily, the BP reduction is dose-dependent. Maximum BP reduction is achieved 3-6 hours after a single oral dose and is maintained for at least 24 hours. After 24 hours, BP remains at 60-70% of the maximum diastolic and systolic BP reduction with recommended doses.

After taking 1 50-300 mg once daily, 24 hours later (i.e., at the end of the interdose interval), BP (systolic/diastolic) in the supine or sitting position decreases by 8-13/5-8 mmHg, respectively, which is significantly greater than when taking placebo.

Taking the drug in a dose of 150 mg once daily results in a hypotensive effect comparable to twice the same dose divided into two doses.

Stable antihypertensive effect develops within 1-2 weeks of therapy, and maximum therapeutic effect is reached 4-6 weeks after the start of treatment. There is no “withdrawal” syndrome on withdrawal of the drug.

The efficacy of Irbesartan Canon is independent of age and sex. Patients of non-human race respond less well to Irbesartan Canon monotherapy (as to all other drugs that affect the renin-angiotensin-aldosterone system (RAAS)).

Irbesartan has almost no effect on serum uric acid concentration or uric acid excretion by the kidneys.

Indications

– Arterial hypertension (in monotherapy and in combination with other antihypertensive drugs, for example, thiazide diuretics, beta-blockers, long-acting slow calcium channel blockers (SCBCs).

– Nephropathy in arterial hypertension and type 2 diabetes mellitus (as part of combination antihypertensive therapy).

Pharmacological effect

Irbesartan reduces blood pressure (BP) with minimal changes in heart rate (HR). When taken in doses up to 900 mg once a day, the reduction in blood pressure is dose-dependent. The maximum reduction in blood pressure is achieved 3-6 hours after a single oral dose and persists for at least 24 hours. After 24 hours, blood pressure remains at 60-70% of the maximum reduction in diastolic and systolic blood pressure when taking recommended doses.

After taking 1 50-300 mg 1 time per day after 24 hours (i.e. at the end of the interdose interval), blood pressure (systolic/diastolic) in the patient’s “lying” or “sitting” position decreases by 8-13/5-8 mmHg, respectively, which is significantly more than when taking placebo.

Taking the drug at a dose of 150 mg once a day leads to a hypotensive effect comparable to taking the same dose twice, divided into two doses.

A stable antihypertensive effect develops within 1-2 weeks of therapy, and the maximum therapeutic effect is achieved 4-6 weeks after the start of treatment. When the drug is discontinued, there is no withdrawal syndrome.

The effectiveness of Irbesartan Canon does not depend on age and gender. Patients of the Negroid race respond less poorly to monotherapy with Irbesartan Canon (as well as to all other drugs that affect the renin-angiotensin-aldosterone system (RAAS)).

Irbesartan has virtually no effect on the concentration of uric acid in the blood serum or on the excretion of uric acid by the kidneys.

Special instructions

Violation of water and electrolyte balance. Before using the drug Irbesartan Canon in patients with a decrease in blood volume (including due to diarrhea or vomiting, intensive diuretic therapy, a diet with limited salt intake), it is necessary to restore circulating blood volume and eliminate hyponatremia, because There is a risk of developing symptomatic hypotension, especially after taking the first dose.

Renovascular hypertension. The risk of severe hypotension and renal failure is potentially increased in patients with bilateral renal artery stenosis or arterial stenosis of a single functioning kidney.

Kidney failure and kidney transplantation. It is recommended to monitor serum potassium and creatinine levels in patients with renal failure. There are no clinical data regarding the use of irbesartan in patients after kidney transplantation.

Patients with arterial hypertension and type 2 diabetes mellitus with impaired renal function.

The beneficial effect noted for irbesartan in slowing the progression of renal and cardiovascular disorders has varying degrees of severity in different groups of patients: less pronounced in women and in patients who are not Caucasian.

Double blockade of the RAAS when combining irbesartan with ACE inhibitors or aliskiren

Double blockade of the RAAS when using a combination of Irbesartan Canon with ACE inhibitors or aliskiren is not recommended, since, compared with monotherapy, there is an increased risk of a sharp decrease in blood pressure, the development of hyperkalemia and renal dysfunction.

The use of Irbesartan Canon in combination with aliskiren is contraindicated in patients with diabetes mellitus or renal failure with GFR <60 ml/min/1.73 m2 body surface area) and is not recommended in other patients.

The use of Irbesartan Canon in combination with ACE inhibitors is contraindicated in patients with diabetic nephropathy and is not recommended in other patients.

Hyperkalemia. It is recommended to monitor potassium levels in patients simultaneously taking potassium preparations, potassium-sparing diuretics, heparin with Irbesartan Canon, especially in the presence of renal failure and/or diseases of the cardiovascular system.

Stenosis of the aortic and mitral valve, HOCM. As with any vasodilator, Irbesartan Canon should be used with caution.

Primary hyperaldosteronism. The use of the drug Irbesartan Canon for primary hyperaldosteronism is inappropriate.

Other. In patients whose vascular tone and renal function primarily depend on the activity of the RAAS (for example, patients with chronic heart failure of functional class III-IV according to the NYHA classification, concomitant kidney diseases, including renal artery stenosis), therapy with ACE inhibitors or angiotensin II receptor antagonists is accompanied by the development of arterial hypotension, azotemia, oliguria and, in rare cases, acute renal failure. As with other antihypertensive drugs, a significant decrease in blood pressure in patients with coronary artery disease and/or atherosclerotic cerebral vascular disease can lead to the development of myocardial infarction and stroke. When treating such patients, blood pressure should be strictly monitored.

Impact on the ability to drive vehicles. Wed and fur.:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions. If dizziness and weakness occur, decreased attention and slower psychomotor reactions may occur. In patients who have such adverse reactions, the decision about the possibility of engaging in any potentially hazardous activities should be made by the doctor individually.

Active ingredient

Irbesartan

Composition

1 tablet contains:

active substance:

irbesartan 300 mg;

excipients:

pregelatinized corn starch 102 mg,

croscarmellose sodium 24 mg,

lactose monohydrate 88 mg,

magnesium stearate 4 mg,

povidone K-30 20 mg,

talc 6 mg,

microcrystalline cellulose 56 mg.

Pregnancy

Pregnancy Considering that when pregnant women took ACE inhibitors in the second and third trimesters of pregnancy, damage and death to the developing fetus were observed, Irbesartan Canon, like any other drug that acts directly on the RAAS, should not be used during pregnancy.

Contraindications

– Hypersensitivity to irbesartan or to any component of the drug.

– Concomitant use with medicinal products containing aliskiren in patients with diabetes mellitus or with moderate to severe renal failure (glomerular filtration rate [GFR] <60 ml/min/1.73 m2 body surface).

– Simultaneous use with ACE inhibitors in patients with diabetic nephropathy.

– Hereditary lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

– Pregnancy.

– Lactation period.

– Age up to 18 years (efficacy and safety have not been established).

– In case of severe liver failure (functional class C or more than 9 points on the Child-Pugh scale) (lack of experience in clinical use).

With caution:

– For stenosis of the aortic or mitral valve or hypertrophic obstructive cardiomyopathy (HOCM).

– In case of hypovolemia, hyponatremia, which occurs, for example, during intensive treatment with diuretics, hemodialysis, following a diet with limited salt intake, diarrhea, vomiting (danger of excessive reduction in blood pressure, especially when taking the first dose).

– In case of bilateral renal artery stenosis, unilateral stenosis of the artery of the only functioning kidney, chronic heart failure of functional class III-IV (according to the NYHA classification) (when treating such patients with drugs that affect the RAAS, the following were observed: excessive decrease in blood pressure, oliguria and/or progressive azotemia and rarely acute renal failure and/or death, the risk of which cannot be excluded when taking irbesartan).

– With coronary heart disease and/or clinically significant cerebral atherosclerosis (with an excessive decrease in blood pressure, there is a risk of increased ischemic disorders, including the development of acute myocardial infarction and stroke).

– In case of renal failure (requires monitoring of potassium levels and creatinine concentrations in the blood), recent kidney transplantation (lack of experience in clinical use).

– In case of severe liver failure (functional class C or more than 9 points on the Child-Pugh scale) (lack of experience in clinical use).

– With simultaneous use of non-steroidal anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase 2 (COX-2) inhibitors (increased risk of renal dysfunction, including the possibility of developing acute renal failure and an increase in serum potassium, especially in patients with already impaired renal function).

– When used in combination with ACE inhibitors or aliskiren, since, compared with monotherapy with dual blockade of the RAAS, there is an increased risk of developing an excessive decrease in blood pressure, hyperkalemia and renal dysfunction.

– Patients over 75 years of age.

Side Effects

The following adverse events are presented in accordance with the following gradations of the frequency of their occurrence (according to the World Health Organization (WHO) classification): very often (≥ 1/10); often (≥ 1/100, < 1/10); uncommon (≥ 1/1000, < 1/100); rare (≥ 1/10000, < 1/1000); very rare (<1/10000, including isolated reports); unknown frequency (it is not possible to determine the frequency of occurrence of an adverse event based on available data).

The safety of irbesartan was studied in clinical studies in approximately 5000 patients, including 1300 patients with hypertension who took the drug for more than 6 months and 400 patients who took the drug for one year or more. Adverse events in patients taking irbesartan were usually moderate and transient, and their frequency was not related to the dose taken. The incidence of adverse events did not depend on gender, age or race.
In placebo-controlled studies in which 1965 patients took irbesartan (for an average of 1-3 months), discontinuation of treatment due to the development of any clinical or laboratory adverse events was required in 3.3% of patients taking irbesartan and in 4.5% of patients taking placebo (the differences were statistically significant).

Adverse events observed in placebo-controlled clinical trials with the use of irbesartan in arterial hypertension, probably or possibly related to its use, or without an established relationship with the drug.

The incidence of the following adverse events when taking irbesartan was not statistically significantly different from that when taking placebo.

Nervous system disorders

Common: dizziness, headache.

Uncommon: orthostatic dizziness.

Heart disorders

Uncommon: edema, tachycardia.

Respiratory, thoracic and mediastinal disorders

Uncommon: cough.

Gastrointestinal disorders

Common: nausea/vomiting.

Uncommon: diarrhea, dyspepsia/heartburn.

Disorders of the genital organs and breast

Uncommon: sexual dysfunction.

General violations

Common: increased fatigue.

Uncommon: chest pain.

Laboratory and instrumental data

During controlled clinical studies in patients with arterial hypertension, no clinically significant changes in laboratory parameters were observed. No special monitoring of laboratory parameters is required for patients with arterial hypertension taking irbesartan.

Adverse events observed in controlled clinical studies when using irbesartan in patients with nephropathy due to arterial hypertension and type 2 diabetes mellitus (clinical studies IDNT and IRMA 2).

Adverse events were similar to those in patients with hypertension, with the exception of orthostatic symptoms (dizziness (10.2%) (placebo 6%), orthostatic dizziness (5.4%) (placebo 2.7%), and orthostatic hypotension (5.4%) (placebo 3.2%).

Treatment discontinuation rates due to orthostatic symptoms with irbesartan compared with placebo were 0.3% versus 0.5% for dizziness, 0.2% versus 0.0% for orthostatic dizziness, and 0.0% versus 0.0% for orthostatic hypotension, respectively.

Laboratory abnormalities. Hyperkalemia.

In the 1DNT clinical trial, the percentage of patients with hyperkalemia (>6 mEq/L) was 18.6% in the irbesartan group, compared with 6.0% in the placebo group. In the IRMA 2 clinical trial, the percentage of patients with hyperkalemia (> 6 mEq/L) was 1.0% in the irbesartan group, and no hyperkalemia was observed in the placebo group.

In the IDNT clinical trial, treatment discontinuation rates due to hyperkalemia with irbesartan and placebo were 2.1% and 0.36%, respectively. In the IRMA clinical trial, treatment discontinuation rates due to hyperkalemia with irbesartan and placebo were 0.5% and 0%, respectively.

Adverse events observed during post-marketing use of irbesartan.

Immune system disorders

Very rare: As with all angiotensin II receptor antagonists, very rare cases of allergic reactions such as urticaria, angioedema have been reported.

The following adverse events have been identified with the use of irbesartan since its introduction to the market.

Metabolic and nutritional disorders

Unknown frequency: hyperkalemia.

Nervous system disorders

Unknown frequency: vertigo.

Disorders of the liver and biliary tract

Unknown frequency: increased activity of liver enzymes and bilirubin concentration in the blood, hepatitis, jaundice.

Hearing disorders

Unknown frequency: tinnitus.

Musculoskeletal and connective tissue disorders

Unknown frequency: myalgia.

Renal and urinary tract disorders

Unknown frequency: impaired renal function, including cases of renal failure in patients at risk (see section “Special Instructions”).

General violations

Unknown frequency: asthenia.

If severe side effects develop, treatment should be discontinued.

Interaction

Based on in vitro data, irbesartan is not expected to interact with drugs metabolized by CYP1A1, CYP1A2, CYP2A6, CYP2B6, CYP2E1 or CYP3A4. Irbesartan is mainly metabolized by the CYP2C9 isoenzyme and, to a lesser extent, undergoes glucuronidation. No significant pharmacokinetic and pharmacodynamic interactions were observed when irbesartan was co-administered with warfarin, a drug metabolized by the CYP2C9 isoenzyme. The effects of inducers of the CYP2C9 isoenzyme, such as rifampicin, on the pharmacokinetics of irbesartan have not been studied. Irbesartan does not change the pharmacokinetics of digoxin and simvastatin.

With medicinal products containing aliskiren

The combination of irbesartan with medicinal products containing aliskiren is contraindicated in patients with diabetes mellitus or with moderate to severe renal impairment (GFR < 60 ml/min/1.73 m2 body surface area) and is not recommended in other patients.

With ACE inhibitors

The use of irbesartan in combination with ACE inhibitors is contraindicated in patients with diabetic nephropathy and is not recommended in other patients.

Other antihypertensive drugs and diuretics may enhance the antihypertensive effect of irbesartan. Irbesartan can be used in combination with drugs such as beta-blockers, long-acting slow calcium channel blockers and thiazide diuretics.

Previous therapy with diuretics in high doses may lead to dehydration and an increased risk of arterial hypotension at the beginning of therapy with Irbesartan Canon.

The simultaneous use of irbesartan with potassium preparations and potassium-sparing diuretics, as well as heparin, can increase the potassium content in the blood serum.

With the simultaneous use of irbesartan with lithium preparations, a reversible increase in the content of lithium in the blood serum and an increase in its toxicity are potentially possible. Therefore, it is recommended to regularly monitor the concentration of lithium in the blood serum.

When used simultaneously with non-steroidal anti-inflammatory drugs (NSAIDs) (including selective cyclooxygenase 2 inhibitors, acetylsalicylic acid (more than 3 g/day) and non-selective NSAIDs), the antihypertensive effect may be reduced. In case of simultaneous use with NSAIDs, there is a potential increase in the risk of renal dysfunction, including the development of acute renal failure and hyperkalemia (especially in patients with already impaired renal function). This combination should be used with caution, especially in elderly patients. Before starting combination therapy, patients need to restore their blood volume, as well as monitor kidney function before starting therapy and periodically during combination therapy.

Hydrochlorothiazide and nifedipine do not affect the pharmacokinetic parameters of irbesartan.

Overdose

Experience with the use of the drug in adult patients in doses up to 900 mg/day for 8 weeks did not reveal any toxicity.

Symptoms: marked decrease in blood pressure, tachycardia, rarely – bradycardia.

Treatment: gastric lavage, taking activated carbon. Conducting symptomatic and supportive therapy under constant monitoring of the patient. Hemodialysis is ineffective.

Storage conditions

At a temperature not exceeding 25 °C in the manufacturer’s packaging.

Keep out of the reach of children.

Shelf life

2 years.
Do not use after expiration date.

Manufacturer

Kanonpharma production CJSC, Russia