Irbesartan Canon, 150 mg tablets 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 decrease is dose-dependent. Maximum BP decrease is achieved 3-6 hours after a single oral administration and lasts for at least 24 hours.

24 hours later, 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 (i.e., at the end of the interdose interval), BP (systolic/diastolic) in the prone or sitting position decreased by 8-13/5-8 mm Hg, respectively, which is significantly greater than placebo administration.

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-hyrogenic 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 hypotensive agents, e.g. thiazide diuretics, beta-adrenoblockers, slow calcium channel blockers (SCBs) of long action).

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

Active ingredient

Composition

1 tablet contains:

the active ingredient:

irbesartan 150 mg;

excipients:

Corn pregelatinized starch 51 mg,

croscarmellose sodium 12 mg,

lactose monohydrate 44 mg,

magnesium stearate 2 mg,

povidone K-30 10 mg,

/p>

talc 3 mg,

microcrystalline cellulose 28 mg.

How to take, the dosage

To the mouth, swallow the tablet whole with water. Take once a day, regardless of meals.

The recommended starting and maintenance dosage is usually 150 mg once daily.

Patients with decreased circulating blood volume (RBC) (including diarrhea, vomiting) with hyponatremia, during treatment with diuretics or diet with restriction of table salt intake, or being on hemodialysis, or patients older than 75 years old the recommended initial dose of Irbesartan Canon is 75 mg/day (1/2 tablet of 150 mg). If the therapeutic effect is not sufficiently pronounced, the drug dose is increased to 300 mg/day. Further increase in dose at intervals of 1-2 weeks (more than 300 mg/day) does not lead to increase in intensity of antihypertensive effect.

If there is no effect with monotherapy, a combination with another hypotensive drug, such as low-dose diuretics (hydrochlorothiazide), is possible.

In the treatment of nephropathy in patients with arterial hypertension and diabetes mellitus type 2 the recommended initial dose of Irbesartan Canon is 150 mg once daily, in case of insufficient therapeutic effect the dose can be increased (in 2 weeks intervals) to 300 mg once daily – the preferred maintenance dose for nephropathy treatment.

Use in selected patient groups

Patients with impaired renal function do not require dosing adjustments.

The starting dose of the drug in patients on hemodialysis should be 75 mg/day (1/2 tablet of 150 mg).

Hepatic impairment

Patients with mild to moderate hepatic impairment do not require dosage adjustment. There is no clinical experience with use in patients with severe hepatic impairment.

Patients with hypovolemia

In patients with severe hypovolemia and/or hyponatremia, such as patients receiving intensive diuretic therapy or those on hemodialysis, hypovolemia and hyponatremia must be corrected before initiating the drug.

Patients in the elderly

It is recommended that patients over 75 years of age begin treatment with a dose of 75 mg (1/2 tablet of 150 mg).

Interaction

Based on in vitro studies, no interaction of irbesartan with drugs metabolized by the CYP1A1, CYP1A2, CYP2A6, CYP2B6, CYP2E1 or CYP3A4 isoenzymes is expected. Irbesartan is primarily metabolized by the CYP2C9 isoenzyme and, to a lesser extent, undergoes glucuronidation. No significant pharmacokinetic and pharmacodynamic interactions have been observed when irbesartan is coadministered with warfarin, a drug metabolized by the CYP2C9 isoenzyme. The effects of CYP2C9 isoenzyme inducers, such as rifampicin, on the pharmacokinetics of irbesartan have not been studied. Irbesartan does not alter the pharmacokinetics of digoxin and simvastatin.

Special Instructions

Disorders of water-electrolyte balance. Before Irbesartan Canon administration in patients with decreased BOD (including due to diarrhea or vomiting, intensive therapy with diuretics, diet with restriction of table salt intake) it is necessary to restore circulating blood volume, eliminate hyponatremia, because there is a risk of symptomatic arterial hypotension, especially after the first dose.

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

Kidney failure and renal transplantation. Monitoring of serum potassium and creatinine in patients with renal insufficiency is recommended. There are no clinical data regarding the use of irbesartan in patients after renal transplantation.

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

The beneficial effects noted for irbesartan in slowing the progression of renal and cardiovascular events vary among patient groups, being less pronounced in women and in patients who are not Caucasian.

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

Dual RAS blockade in combination with ACE inhibitors or aliskiren is not recommended because compared to monotherapy there is an increased risk of BP depression, hyperkalemia and renal dysfunction.

The use of Irbesartan Canon in combination with aliskiren is contraindicated in patients with diabetes mellitus or renal insufficiency with a 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 content in patients concomitantly taking potassium preparations, potassium-saving diuretics, heparin, especially in the presence of renal failure and/or cardiovascular diseases with the drug Irbesartan Canon.

Aortic and mitral valve stenosis, GOCMP. As with any vasodilators, Irbesartan Canon should be used with caution.

Primary hyperaldosteronism. The use of Irbesartan Canon in primary hyperaldosteronism is inadvisable.

Other. In patients whose vascular tone and renal function is mainly dependent on the activity of RAAS (e.g. patients with chronic heart failure of III-IV functional class according to NYHA classification, concomitant renal diseases, including renal artery stenosis), therapy with ACE inhibitors or angiotensin II receptor antagonists is accompanied with the development of arterial hypotension, azotemia, oliguria and, rarely, acute renal failure. As with other hypotensive drugs, a significant decrease in BP in patients with CHD and/or atherosclerotic cerebral vascular lesions may lead to myocardial infarction, stroke. BP should be strictly monitored while treating such patients.

During treatment, caution should be exercised when driving motor vehicles and engaging in other potentially dangerous activities requiring increased concentration and rapid psychomotor reactions. In case of dizziness and weakness, there may be decreased attention and slow psychomotor reactions. In patients who have such adverse reactions, the decision about the possibility of engaging in any potentially dangerous activities should be made by the physician individually.

Contraindications

– Hypersensitivity to irbesartan or any component of the drug.

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

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

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

– Pregnancy.

– Period of lactation.

– Age under 18 years (effectiveness and safety not established).

– In severe hepatic failure (functional class C or greater than 9 points on the Child-Pugh scale) (no experience with clinical use).

– In aortic or mitral valve stenosis or hypertrophic obstructive cardiomyopathy (HCMP).

– In hypovolemia, hyponatremia, occurring, for example, with intensive treatment with diuretics, hemodialysis, diet with restriction of table salt intake, diarrhea, vomiting (risk of excessive BP reduction, especially with the first dose).

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

– In coronary heart disease and/or clinically significant cerebral vascular atherosclerosis (with excessive BP reduction there is a risk of increased ischemic disturbances, up to the development of acute myocardial infarction and stroke).

– In renal failure (requires monitoring of potassium and creatinine concentration in the blood), recent kidney transplantation (no experience in clinical use).

– In severe hepatic impairment (functional class C or greater than 9 points on the Child-Pugh scale) (no experience with clinical use).

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

– When used in combination with ACE inhibitors or aliskiren, as compared to monotherapy with dual RAAS blockade, there is an increased risk of developing excessive BP reduction, hyperkalemia, and impaired renal function.

Patients over 75 years of age.

Side effects

The adverse events listed below are presented according to the following frequency gradations (according to the World Health Organization (WHO) classification): Very common (≥ 1/10); common (≥ 1/100, < 1/10); infrequent (≥ 1/1000, < 1/100); rare (≥ 1/10000, < 1/1000); very rare (< 1/10000, including individual reports); unknown frequency (the incidence of the adverse event could not be determined from available data).

The safety of irbesartan has been studied in clinical trials in approximately 5,000 patients, including 1,300 patients with arterial hypertension who have taken the drug for more than 6 months and 400 patients who have taken 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 was independent of gender, age, and race.
In placebo-controlled studies in which 1,965 patients took irbesartan (averaged over 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 (differences were statistically significant).

Indesirable events observed in placebo-controlled clinical trials of irbesartan for arterial hypertension were probably or possibly related to its administration, or without an established relationship with drug administration.

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

Nervous system disorders

Often: dizziness, headache.

Infrequent: orthostatic dizziness.

Cardiac disorders

Infrequent: edema, tachycardia.

Respiratory system, thorax and mediastinum disorders

Infrequent: cough.

Gastrointestinal disorders

Often: nausea/vomiting.

Infrequent: diarrhea, dyspepsia/irritation.

Gender and mammary gland disorders

Infrequent: sexual dysfunction.

General disorders

Often: increased fatigue.

Infrequent: pain in the chest.

Laboratory and instrumental data

There were no clinically significant changes in laboratory parameters during controlled clinical studies in patients with arterial hypertension. No specific monitoring of laboratory parameters is required for patients with arterial hypertension taking irbesartan.

The adverse events observed in controlled clinical trials with irbesartan in patients with nephropathy in arterial hypertension and type 2 diabetes mellitus (IDNT and IRMA 2 clinical trials).

The adverse events were similar to those in patients with arterial hypertension except for orthostatic symptoms (dizziness (10.2%) (with placebo 6%), orthostatic vertigo (5.4%) (with placebo 2.7%), and orthostatic hypotension (5.4%) (with placebo 3.2%).

The percentage of treatment discontinuation due to orthostatic symptoms when taking irbesartan, compared with placebo, was 0.3% versus 0.5% for vertigo, 0.2% versus 0.0% for orthostatic vertigo, 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, the discontinuation rate due to hyperkalemia with irbesartan and placebo was 2.1% and 0.36%, respectively. In the IRMA clinical trial, the discontinuation rate due to hyperkalemia with irbesartan and placebo was 0.5% and 0%, respectively.

The adverse events observed with the 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 adverse events listed below have been observed with irbesartan since its market introduction.

Metabolic and nutritional disorders

Unknown frequency: hyperkalemia.

Nervous system disorders

Unknown frequency: vertigo.

Liver and biliary tract disorders

Unknown frequency: increased activity of “hepatic” enzymes and blood bilirubin concentration, hepatitis, jaundice.

Hearing disorders

Unknown frequency: ringing in the ears.

Musculoskeletal and connective tissue disorders

Unknown frequency: myalgia.

Kidney and urinary tract disorders

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

General disorders

Unknown frequency: Asthenia.

In case of development of severe side effects, treatment should be discontinued.

Overdose

The experience of using the drug in adult patients in doses up to 900 mg/day for 8 weeks showed no toxicity.

Symptoms: marked BP decrease, tachycardia, rarely bradycardia.

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

Pregnancy use

Similarities