Irbesartan
Irbesartan: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. For violations of liver function
- 12. With hypovolemia
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Irbesartan
ATX code: C09CA04
Active ingredient: Irbesartan (Irbesartan)
Manufacturer: Kern Pharma S. L. Spain
Description and photo update: 19.10.2018
Prices in pharmacies: from 212 rubles.
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Irbesartan is a drug used for arterial hypertension.
Release form and composition
The dosage form of Irbesartan is film-coated tablets: biconvex, round, the shell and core are almost white or white (in blisters of 3, 4, 7, 10, 14, 15, 20, 25 or 30 pcs., In a cardboard box placed 1–8 or 10 packages; in PET cans of 10, 14, 20, 28, 30, 40, 50, 60 or 100 pcs., 1 can is placed in a cardboard box).
The composition of 1 tablet includes:
- active substance: irbesartan - 75, 150 or 300 mg;
- additional components (75/150/300 mg): microcrystalline cellulose - 24/48/96 mg; lactose monohydrate (milk sugar) - 46.6 / 93.2 / 186.4 mg; colloidal silicon dioxide - 0.8 / 1.6 / 3.2 mg; croscarmellose sodium - 7.2 / 14.4 / 28.8 mg; magnesium stearate - 1.6 / 3.2 / 6.4 mg; povidone-K25 - 4.8 / 9.6 / 19.2 mg;
- shell (75/150/300 mg): titanium dioxide - 1.2 / 2.4 / 4.8 mg; macrogol-4000 - 0.6 / 1.2 / 2.4 mg; hypromellose - 2.2 / 4.4 / 8.8 mg.
Pharmacological properties
Pharmacodynamics
Irbesartan, being a selective antagonist of angiotensin II receptors (type AT1), helps to eliminate the vasoconstrictor effect of angiotensin II, to lower the plasma concentration of aldosterone in the blood (without suppressing kinase II, which destroys bradykinin), to reduce the total peripheral vascular resistance, decrease in systemic arterial pressure (BP), afterload and pressure in the pulmonary circulation. It does not affect the plasma concentration of cholesterol, triglycerides, glucose, uric acid and the excretion of uric acid.
The maximum decrease in blood pressure is achieved within 3-6 hours after oral administration of the drug, the antihypertensive effect remains for at least 24 hours. One day after administration, the decrease in blood pressure is 60–70% in comparison with the maximum decrease in diastolic / systolic pressure in response to taking the drug. When taking 150-300 mg 1 time per day, the degree of blood pressure decrease at the end of the interdose interval (ie, 24 hours after taking the drug) in the sitting or lying position by an average of 5-8 / 8-13 mm Hg. Art. (respectively) more compared to placebo. The antihypertensive response from taking the drug at a dose of 150 mg once a day does not differ from the use of this dose in 2 divided doses. The antihypertensive effect of irbesartan develops within 1-2 weeks,and the maximum therapeutic effect is achieved in 4-6 weeks from the start of treatment. After discontinuation of the drug, blood pressure gradually returns to its original value, without the development of a withdrawal syndrome. Long-term treatment is required to achieve a sustained antihypertensive effect.
The effectiveness of irbesartan does not depend on gender and age.
Patients of the Negroid race respond to monotherapy with the drug weaker.
Pharmacokinetics
Absorption: after oral administration, irbesartan is well absorbed from the gastrointestinal tract. The maximum plasma concentration in the blood is reached 1.5–2 hours after ingestion; the absolute bioavailability index is 60-80%. Food intake has no significant effect on bioavailability. Irbesartan has a dose proportional and linear pharmacokinetics in the dose range of 10–600 mg; at higher doses (2 times higher than the recommended maximum), the kinetics of the substance becomes nonlinear.
Distribution: the binding of the substance with blood plasma proteins is approximately 96%. The binding with the cellular components of the blood is insignificant. The volume of distribution is 53–93 liters. Equilibrium concentration at daily intake 1 time per day is reached after 3 days. With repeated doses, there is a limited accumulation of the substance in the blood plasma (<20%).
Metabolism: irbesartan is biotransformed by oxidation and conjugation with glucuronic acid in the liver, it is oxidized mainly by the CYP2C9 isoenzyme, the participation of the CYP3A4 isoenzyme in its metabolism is insignificant. The main metabolite, which is in the systemic circulation, is irbesartan glucuronide (approximately 6%). The substance is not metabolized by most of the isoenzymes that are usually involved in the metabolism of drugs and does not cause their induction or inhibition. Irbesartan does not inhibit / induce the CYP3A4 isoenzyme.
Excretion: renal and total clearance are 3-3.5 / 157-176 ml / min, respectively. The terminal half-life ranges from 11 to 15 hours. Irbesartan and its metabolites are excreted through the intestines with bile and kidneys. In the form of an unchanged substance, the kidneys are excreted <2% of the administered dose.
Indications for use
- arterial hypertension - as a monopreparation and in combination with other drugs with antihypertensive action, for example, long-acting slow calcium channel blockers, thiazide diuretics, beta-blockers;
- nephropathy against the background of arterial hypertension and type 2 diabetes mellitus - simultaneously with other drugs with hypotensive action.
Contraindications
Absolute:
- hepatic failure in severe course (> 9 points on the Child-Pugh scale);
- lactase deficiency, galactose intolerance and glucose-galactose malabsorption syndrome;
- combined use with aliskiren and aliskiren-containing drugs in patients with diabetes mellitus or with severe / moderate renal failure (at a glomerular filtration rate <60 ml / min / 1.73 m 2);
- combined use with angiotensin-converting enzyme inhibitors in patients with diabetic nephropathy;
- pregnancy and the period of breastfeeding;
- age up to 18 years;
- individual intolerance to the components of the drug.
Relative (diseases / conditions in the presence of which the appointment of Irbesartan requires caution):
- hypertrophic obstructive cardiomyopathy;
- mitral / aortic valve stenosis;
- hyponatremia;
- hypovolemia;
- adherence to a diet with limited consumption of table salt;
- diarrhea, vomiting;
- bilateral renal artery stenosis;
- unilateral stenosis of an artery of a single kidney;
- ischemic heart disease and / or atherosclerotic vascular lesions of the brain;
- chronic heart failure III – IV functional class according to NYHA classification;
- renal failure;
- hyperkalemia;
- condition after kidney transplantation;
- hemodialysis;
- primary hyperaldosteronism;
- combination therapy with diuretics;
- combined use with non-steroidal anti-inflammatory drugs, including cyclooxygenase II inhibitors, angiotensin-converting enzyme inhibitors, or aliskiren;
- age over 75 years.
Instructions for the use of Irbesartan: method and dosage
Irbesartan is taken orally by swallowing the tablets whole with water. The drug can be used regardless of the meal time.
The initial / maintenance dose is 150 mg once a day (provides optimal blood pressure control during the day; in some cases, especially in patients on hemodialysis, or in patients over 75 years of age, the initial dose is 75 mg). If the therapeutic effect is not achieved, the dose can be doubled.
In cases of insufficient lowering of blood pressure as monotherapy, diuretics or other antihypertensive drugs can be added to Irbesartan.
With arterial hypertension and type 2 diabetes mellitus, therapy should be started with 150 mg once a day and gradually increased to 300 mg - the dose that is more preferable in the treatment of nephropathy.
Side effects
Estimation of the frequency of occurrence of adverse reactions:> 10% - very often; > 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare; if it is impossible to assess the frequency of occurrence - with an unspecified frequency.
Disorders that develop with arterial hypertension:
- reproductive system: infrequently - sexual dysfunction;
- cardiovascular system: infrequently - tachycardia, edema;
- nervous system: often - headache, dizziness; infrequently - orthostatic dizziness;
- digestive system: often - vomiting, nausea; infrequently - dyspepsia, diarrhea, heartburn;
- respiratory system: infrequently - cough;
- the body as a whole: often - increased fatigue; infrequently - chest pains.
In arterial hypertension and type 2 diabetes mellitus with impaired renal function, adverse reactions were similar to those in patients with arterial hypertension, except for orthostatic symptoms - dizziness, orthostatic dizziness and orthostatic hypotension.
Violations observed during the post-registration period of Irbesartan use:
- musculoskeletal system: with an unknown frequency - myalgia;
- nervous system: with an unknown frequency - vertigo;
- immune system: very rarely - allergic reactions (angioedema, urticaria);
- urinary system and kidneys: with an unknown frequency - impaired renal function, including the development of renal failure in patients at risk;
- hepatobiliary system: with an unknown frequency - jaundice, hepatitis, increased activity of liver enzymes and the concentration of bilirubin in the blood;
- organ of hearing: with an unknown frequency - ringing in the ears;
- nutrition and metabolism: with an unknown frequency - hyperkalemia;
- general disorders: with an unknown frequency - asthenia.
Overdose
The main symptoms: a marked decrease in blood pressure, bradycardia, tachycardia.
Therapy: in case of accidental intake of high doses of Irbesartan, induction of artificial vomiting / gastric lavage, activated charcoal, supportive (symptomatic) treatment is indicated. Hemodialysis is ineffective.
special instructions
Until now, the use of Irbesartan without the presence of concomitant diseases has rarely been accompanied by an excessive decrease in blood pressure. An excessive decrease in blood pressure, occurring with clinical symptoms, can be observed in patients with hypovolemia / hyponatremia (for example, due to intensive diuretic therapy, vomiting or diarrhea, adherence to a diet with limited salt intake), as well as in patients on hemodialysis. Hypovolemia / hyponatremia should be corrected before starting therapy.
During the use of Irbesartan, deterioration of renal function is possible (if there is a predisposition).
In patients with functional impairment of the kidneys, it is recommended to periodically monitor the potassium content and serum creatinine concentration in the blood.
During the period of therapy, hyperkalemia may develop, especially in the presence of heart disease and / or renal failure. Such patients are advised to monitor serum potassium in the blood.
For aortic / mitral stenosis or hypertrophic obstructive cardiomyopathy, Irbesartan should be used with caution.
The use of the drug in patients with primary hyperaldosteronism is inappropriate.
Influence on the ability to drive vehicles and complex mechanisms
The ability to drive vehicles while using Irbesartan has not been studied. Patients should consider the likelihood of an individual response to therapy, including the development of dizziness and weakness.
Application during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation.
If pregnancy is detected during treatment, Irbesartan should be canceled immediately.
Pediatric use
According to the instructions, Irbesartan is not prescribed to children and adolescents under the age of 18, which is due to the lack of clinical data that would confirm the safety and effectiveness of therapy in this group of patients.
For violations of liver function
Irbesartan is not prescribed for severe liver dysfunction (> 9 points on the Child-Pugh scale) (due to the lack of clinical experience of its use).
With hypovolemia
In the presence of violations of the water-electrolyte balance, before taking Irbesartan, it is necessary to restore the volume of circulating blood / eliminate hyponatremia.
The initial dose for patients on hemodialysis is 75 mg per day.
Use in the elderly
For patients over 75 years of age, it is recommended to start therapy with a dose of 75 mg per day.
Drug interactions
With the combined use of Irbesartan with certain drugs / substances, the following effects may develop:
- medicines containing aliskiren: the combination is contraindicated in patients with diabetes mellitus or with moderate / severe renal failure, in other patients it is not recommended;
- angiotensin-converting enzyme inhibitors: the combination is contraindicated in patients with diabetic nephropathy, in other patients it is not recommended;
- diuretics (previous therapy in high doses): dehydration of the body and an increase in the likelihood of arterial hypotension at the beginning of the use of Irbesartan;
- diuretics and other antihypertensive drugs: increased antihypertensive action (it is possible to carry out combined therapy with β-blockers, long-acting slow calcium channel blockers and thiazide diuretics);
- lithium preparations: a reversible increase in the serum concentration of lithium in the blood or its toxicity (if necessary, combined use requires careful monitoring of the concentration of lithium);
- potassium preparations, aqueous electrolyte solutions with potassium content, potassium-sparing diuretics, drugs that can increase the potassium content in the blood, including heparin: an increase in the serum potassium content in the blood;
- non-steroidal anti-inflammatory drugs: weakening of the antihypertensive effect of irbesartan; an increase in the likelihood of developing functional renal impairment, including the risk of acute renal failure, and an increase in serum potassium, especially with already impaired renal function (the combination requires caution, especially in elderly patients and with hypovolemia; it is necessary to restore the volume of circulating blood, during the entire period of combination therapy, as well as periodically after its completion, monitor renal function).
Analogs
The analogues of Irbesartan are: Aprovel, Firmasta, Ibertan, Irsar, etc.
Terms and conditions of storage
Store at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Irbesartan
According to reviews, Irbesartan is one of the available drugs for the long-term treatment of mild / moderate hypertension. It is also noted to be effective in severe hypertension (when using a daily dose of 300 mg) and an increase in blood pressure at night. The drug, as a rule, is well tolerated and leads to the development of side effects (mainly in the form of weakness and dizziness) only in rare cases.
There are also reviews about the effectiveness of Irbesartan against the background of diabetes mellitus and diabetic nephropathy.
Price for Irbesartan in pharmacies
The approximate price for Irbesartan (28 pcs. In a package): dosage 150 mg - 440 rubles, dosage 300 mg - in the range from 260 to 520 rubles.
Irbesartan: prices in online pharmacies
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Drug name Price Pharmacy |
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Irbesartan 150 mg film-coated tablets 14 pcs. 212 r Buy |
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Irbesartan Canon 150 mg tablets 14 pcs. 224 r Buy |
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Irbesartan 300 mg film-coated tablets 14 pcs. 269 r Buy |
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Irbesartan Canon 300 mg tablets 14 pcs. RUB 319 Buy |
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Irbesartan 150 mg film-coated tablets 28 pcs. 369 r Buy |
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Irbesartan Canon 150 mg tablets 28 pcs. 399 RUB Buy |
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Irbesartan 300 mg film-coated tablets 28 pcs. 507 r Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
