Aprovel 300mg tab 14 pc

Description

Composition
Active substance:
1 tablet contains: irbesartan – 150 mg; 1 tablet contains: -300 mg irbesartan ;.
Excipients:
1 tablet of 150 mg contains: lactose monohydrate – 51.0 mg Microcrystalline cellulose – 27.0 mg Croscarmellose sodium – 12.0 mg Hypromellose – 5.0 mg magnesium stearate – 2.5 mg of silicon dioxide – 2, 5 mg; film coating: Opadry White * – 10.0 mg Carnauba wax – less than 0.05 mg. One 300 mg tablet contains: lactose monohydrate – 102.0 mg Microcrystalline cellulose – 54.0 mg Croscarmellose sodium – 24.0 mg Hypromellose – 10.0 mg Magnesium stearate – 5.0 mg of silicon dioxide – 5, 0 mg; film coating: Opadry White * 20.0 mg Carnauba wax – less than 0.1 mg. * – Opadray® white lactose monohydrate – 36.00%, hypromellose – 28.00%, macrogol-3000 – 10.00% titanium dioxide (E 171) – 26.00%.
Description:
Tablets, film-coated, 150 mg oval Biconvex tablets, film-coated white or almost white, with an engraving in a heart on one side and of 2872 – to another.
Tablets, film-coated, 300 mg oval Biconvex tablets, film-coated white or almost white, with an engraving in a heart on one side and of 2873 – to another.
Product form:
Tablets, film-coated, 150 mg and 300 mg.
14 tablets in blister PVC / PVDC / aluminum foil. 1, 2 or 4 blister together with instructions for use in a cardboard box.
Contraindications
Hypersensitivity to irbesartan or any of the excipients Aprovel® preparation.
The simultaneous use of pharmaceutical preparations containing aliskiren in patients with diabetes or with moderate and severe renal failure (GFR [SCF]
The simultaneous use of ACE inhibitors in patients with diabetic nephropathy.
Pregnancy.
During breastfeeding.
Age 18 years (effectiveness and safety have been established).
Hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption.
In severe liver failure (functional class C 9 or more points on the Child-Pugh) (no clinical experience).
Caution: When aortic stenosis and mitral valve or hypertrophic obstructive cardiomyopathy (GOKMP). – When hypovolemia, hyponatremia, arising, for example, during intensive diuretic therapy, hemodialysis, a diet restriction of salt intake, diarrhea, vomiting (danger of excessive reduction in blood pressure). – In patients with renal function, depending on the activity of the RAAS, such as patients with hypertension with bilateral or unilateral renal artery stenosis, or patients with chronic heart failure III-IV functional class (classification NYHA) (see section “Special Instructions”.) . – In ischemic heart disease and / or clinically significant atherosclerosis of cerebral vessels (in the excessive lowering of blood pressure there is a risk of ischemic disorders gain, until the development of acute myocardial infarction and stroke). – In renal failure (potassium content required control and creatinine concentration in blood), a recent renal transplant (no clinical experience). – With simultaneous use of nonsteroidal anti-inflammatory drugs (NSAIDs), including selective inhibitors of cyclooxygenase 2 (COX-2) (increased risk of kidney damage, including the possibility of acute renal failure and increase in the potassium content in blood serum, especially in elderly patients, patients hypovolaemic [including patients receiving diuretics] or patients with impaired renal function (see “Interaction with other drugs.”) -. When used to bination with ACE inhibitors or aliskiren as compared with monotherapy with dual blockade of the RAAS, there is an increased risk of excessive reduction of blood pressure, hyperkalemia, and renal dysfunction (see. section “Special Instructions”).
Dosage
300 mg
Indications
Arterial hypertension (in monotherapy or in combination with other antihypertensives, for example, thiazide diuretics, beta-blockers, blockers “slow” calcium channel (BCCI) long-acting).
Nephropathy with hypertension and diabetes mellitus type 2 (in a combination antihypertensive therapy).
Interaction with other drugs
Based on data from studies in vitro, is expected irbesartan interactions with drugs metabolized via isozymes CYP1A1, CYP1A2, CYP2A6, CYP2B6, CYP2E1 or CYP3A4. Irbesartan is mainly metabolized via isoenzyme CYR2S9 and, to a lesser extent, it undergoes glucuronidation. No significant pharmacokinetic and pharmacodynamic interactions in the combined use of irbesartan with warfarin, a drug is metabolized via isoenzyme CYP2C9. Irbesartan does not alter the pharmacokinetics of digoxin and simvastatin. In a joint application with hydrochlorothiazide irbesartan or irbesartan pharmacokinetics nifedipine does not change. With drugs, the drug combination comprising aliskiren Aprovel® with medicinal preparations containing aliskiren, contraindicated in patients with diabetes or with moderate to severe renal failure (GFR
Overdose
Experience with the drug in adult patients at doses up to 900 mg / day for weeks did not reveal any toxicity. No further specific information regarding the treatment of overdose Aprovel® drug. It should set a permanent monitoring of the patient and, if necessary, to carry out 12 symptomatic and supportive therapy. In case of overdose it is recommended to induce vomiting, and / or to gastric lavage. Irbesartan is not excreted via hemodialysis.
pharmachologic effect
Pharmacological group:
Angiotensin II receptor antagonist.
Pharmacodynamics:
Irbesartan is a selective antagonist of angiotensin II receptor (type AT1). Irbesartan does not require metabolic activation for the acquisition of the pharmacological activity. Angiotensin II is an important component of the renin-angiotensin-aldosterone system (RAAS) and is involved in the pathogenesis of hypertension, as well as sodium homeostasis. Irbesartan blocks all physiologically significant effects of angiotensin II, regardless of the source or path of its synthesis, including, it is strongly expressed aldosteronosekretiruyuschy and vasoconstrictor effects are realized through type receptors AT1, disposed on the surface of vascular smooth muscle cells in the adrenal cortex. It has no agonist activity to the AT1 receptor and has much larger (more than 8500-fold) affinity for the AT1 receptor than AT2- receptor (not related to the regulation of the cardiovascular system). Irbesartan does not inhibit enzymes RAAS (such as renin, angiotensin converting enzyme [ACE]) and has no effect on other hormone receptors or ion channels involved in the regulation of blood pressure (BP) and sodium homeostasis. Blocking AT1-receptor irbesartan interrupts the feedback loop in the renin-angiotensin system, leading to an increase in plasma concentrations of renin and angiotensin II. Upon receiving the recommended doses of irbesartan plasma aldosterone concentration reduced without causing significant influence on the serum potassium level (its average value is larger
The effectiveness of irbesartan is not dependent on age or gender. As with other drugs that affect RASF, antihypertensive effect of irbesartan in patients blacks significantly less pronounced, however, when applying irbesartan simultaneously with low dose of hydrochlorothiazide (e.g. 12.5 mg per day) antihypertensive response in patients blacks close performance to that of Caucasian patients. After the abolition of irbesartan blood pressure returned to baseline gradually. Syndrome “cancel” is not observed. In a multicenter, randomized, controlled active agent (amlodipine) and placebo IDNT double-blind clinical study conducted in 1715 patients with hypertension and Type 2 diabetes (proteinuria> 900 mg / day, and serum creatinine concentration in the range 1.0 – 3.0 mg / dl) have been shown 20% (p = 0,024) reduction (compared to placebo) and 23% (p = 0,006) reduction (compared with amlodipine) relative risk of first occurrence of any of the following states: doubling of serum creatinine concentrations, isolator Itie stage renal disease or death from any cause (for achieving a comparable reduction in blood pressure when applying irbesartan and amlodipine). In a multicenter, randomized, placebo-controlled, double-blind clinical trial to study the effects of irbesartan microalbuminuria in patients with hypertension and Type 2 diabetes (IRMA 2), held at 590 patients with hypertension and Type 2 diabetes with microalbuminuria (20 – 200 mcg / min, 30-300 mg / day) and normal renal function (serum creatinine concentration
Pharmacokinetics:
Absorption
After ingestion irbesartan is rapidly and completely absorbed, its absolute bioavailability is about 60-80%. Simultaneous food intake does not significantly influence the bioavailability of irbesartan. After ingestion maximum plasma concentration (Cmax) of irbesartan achieved after 1.5-2 hours.
Distribution
Communication with the plasma proteins is approximately 96%. Binding to cellular components of blood slightly. The volume of distribution of 93 l 53-.
Metabolism
After oral or intravenous administration of 14C-irbesartan 80-85% of the radioactivity in the circulating blood plasma, it is necessary to unmodified irbesartan. Irbesartan is metabolized by the liver by oxidation and conjugation with glucuronic acid. The major metabolite being in the systemic circulation, is irbesartan glucuronide (approximately 6%). Oxidation of irbesartan is carried out mainly through the cytochrome P450 isoenzyme CYP2C9, CYP3A4 isozyme involved in the metabolism of irbesartan is negligible. Irbesartan is not metabolized by most isoenzymes that are commonly involved in drug metabolism (isozymes CYP1A1, CYP1A2, CYP2A6, CYP2B6 CYP2D6 or SYP2E1), and does not cause their inhibition or induction. Irbesartan does not induce or inhibit isoenzyme CYP3A4.
breeding
Irbesartan and its metabolites are excreted as through the intestine (in the bile) and kidneys. After oral or intravenous administration of 14C-irbesartan about 20% of the radioactivity found in urine, and the rest – in the feces. Less than 2% of the administered dose excreted by the kidneys in unchanged form of irbesartan. Irbesartan terminal half-life (T1 / 2) was 11-15 hours. The total clearance of intravenously administered irbesartan is 157-176 ml / min, and its renal clearance of 3-3.5 ml / min. When once-daily for one day reception irbesartan equilibrium plasma concentration (CSS) is reached after 3 days, while it is observed limited accumulation in plasma (less than 20%).
Special patient groups
Influence of gender on the pharmacokinetics of irbesartan
Women (compared with men) had somewhat higher plasma concentrations of irbesartan. However, the gender-related differences in half-life and accumulation of irbesartan is not detected. Irbesartan dose adjustment is not required in women. There were no gender-related differences in the effects of irbesartan.
The pharmacokinetics of irbesartan in elderly patients
The values ​​of AUC (area under the curve “concentration-time”) and Cmax of irbesartan in elderly patients (65-80 years) with clinically normal renal function and liver were about 20-50% higher than in younger patients (18 -40 years). Terminal half-life have been comparable. There was no age-related differences in the effects of irbesartan.
The pharmacokinetics of irbesartan with abnormal liver function
In patients with mild (functional class A or 5-6 points on a scale Child-Pugh) and moderate (functional class B, or 7-9 points on the scale of Child-Pugh) hepatic impairment due to cirrhosis, the pharmacokinetic parameters of irbesartan are not significantly altered.
The pharmacokinetics of irbesartan with impaired renal function
In patients with impaired renal function or patients undergoing hemodialysis, pharmacokinetics of irbesartan are not significantly altered. Irbesartan is not excreted via hemodialysis. The influence of race on the pharmacokinetics of irbesartan in the volunteers without hypertension AUC and T1 / 2 of irbesartan in blacks were about 20-25% higher than that of Caucasians; Cmax of irbesartan have been virtually identical to that in Caucasians.
Pregnancy and breast-feeding
Pregnancy
Experience in the use of the drug during pregnancy Aprovel® offline. Given the fact that upon receipt of ACE inhibitors pregnant women in the second and third trimesters of pregnancy were observed damage and death of the developing fetus, irbesartan, like any other drug which acts directly on the RAAS can not be used during pregnancy (I, II, III trimesters ). When the diagnosis of pregnancy during treatment with Aprovel® should, as soon as possible, stop taking it.
Breastfeeding
It is not known whether irbesartan is excreted or its metabolites in breast milk. During breastfeeding Aprovel® receiving the drug is contraindicated. Therefore, after the evaluation of the expected benefit ratio of the drug to the mother and the potential risk for the baby, you should stop or breastfeeding, or taking Aprovel® drug.
Conditions of supply of pharmacies
Prescription.
side effects
The following adverse events are presented in the description complies with the following gradations their frequency of occurrence (according to the classification (WHO World Organization of)): very common (> 1/10); common (> 1/100,
special instructions
Excessive blood pressure reduction – patients with hypovolemia preparation Application Aprovel® hitherto rarely accompanied by an excessive decrease of blood pressure in hypertensive patients without concomitant illnesses. As with ACE inhibitors, excessive reduction in blood pressure is accompanied by clinical symptoms may develop in patients with hyponatremia / hypovolemia (e.g., as a result of intensive diuretic therapy, diarrhea or vomiting, dieting with restriction of salt intake), as well as in patients on hemodialysis. Before the start of the drug Aprovel® necessary to correct hypovolaemia, and / or hyponatremia. Patients with kidney function depending on the activity of the RAAS As a consequence of inhibiting the RAAS can expect a deterioration in renal function in susceptible patients have this. Patients with renal function dependent on the activity of the RAAS (patients with hypertension and renal artery stenosis of one or both kidneys, patients with chronic heart failure III and IV functional class [on NYHA classification]), treatment drugs which act on the RAAS associated with oliguria and / or progressive azotemia and rarely with acute renal failure and / or death. We can not exclude the possibility of this effect in the application of angiotensin II receptor antagonists, including irbesartan.
Renal impairment and kidney transplant
In applying Aprovel® drug in patients with renal insufficiency recommended periodic control potassium, and creatinine concentration in blood serum. No clinical data on the use of the drug Aprovel® in patients who have recently had a kidney transplant. Patients with hypertension and Type 2 diabetes with impaired renal function Aprovel® Suitable drug action against progression of renal and cardiovascular disorders had varying degrees of severity in different groups of patients, it was less pronounced in women and in patients non- Caucasian race. IDNT In a clinical study in patients with hypertension and Type 2 diabetes with proteinuria (> 900 mg / day), in a subgroup of patients at high risk of renal artery stenosis, none of the patients who took the drug Aprovel® not observed early acute upconcentration serum creatinine associated with renal artery stenosis. Dual blockade of the RAAS by combining Aprovel® preparation with ACE inhibitors or dual blockade of the RAAS aliskiren with the combination drug Aprovel® with ACE inhibitors or aliskiren is not recommended, as compared with monotherapy, there is an increased risk of a sharp reduction in blood pressure, disorders of hyperkalemia and renal function. Use of the drug in combination with Aprovel® aliskiren is contraindicated in patients with diabetes or renal failure GFR
Как и при применении других вазодилататоров, при приеме препарата Апровель® пациентами с аортальным или митральным стенозом или с гипертрофической обструктивной кардиомиопатией необходимо соблюдать осторожность. Первичный гиперальдостеронизм Пациенты с первичным гиперальдостеронизмом обычно не реагируют на гипотензивные препараты, действующие через ингибирование РААС. Поэтому применение препарата Апровель® в таких случаях нецелесообразно. Пациенты с ишемической болезнью сердца и/или клинически значимым атеросклерозом сосудов головного мозга Как и при применении других гипотензивных препаратов, значительное снижение АД у пациентов с ишемической болезнью сердца и/или выраженным атеросклерозом сосудов головного мозга может привести к развитию инфаркта миокарда или инсульта. Лечение таких пациентов должно осуществляться под строгим контролем АД.
Impact on the ability to drive or engage in other potentially hazardous activities
Влияние препарата Апровель® на способность управлять транспортными средствами или заниматься другими потенциально опасными видами деятельности, требующими повышенного внимания и высокой скорости психомоторных реакций, не изучалось. Однако, исходя из его фармакодинамических свойств, препарат Апровель® не должен влиять на способность управлять транспортными средствами и заниматься другими потенциально опасными видами деятельности (работа на высоте, работа авиадиспетчера, работа с механизмами и т. п.). Но, в случае возникновения головокружения и слабости, возможно снижение внимания и замедление психомоторных реакций. У пациентов, имеющих такие нежелательные реакции, решение о возможности занятия любыми потенциально опасными видами деятельности должно приниматься врачом индивидуально.
Storage conditions
Store at a temperature not higher than 30 C.
Keep out of the reach of children.
Dosing and Administration
Препарат следует принимать внутрь, вне зависимости от времени приема пищи.
Tablet is swallowed whole with water. Обычно начальная доза препарата Апровель® составляет 150 мг один раз в сутки. Пациенты, у которых для достижения целевых значений АД требуется его дополнительное снижение, доза может быть увеличена до 300 мг один раз в сутки. В случае недостаточного снижения АД при монотерапии препаратом Апровель® к лечению могут быть добавлены диуретики (например, гидрохлоротиазид 12,5 мг в сутки) или другие гипотензивные средства (например, бета-адреноблокаторы или БМКК длительного действия). У пациентов с нефропатией при артериальной гипертензии и сахарном диабете 2 типа предпочтительной поддерживающей дозой является доза 300 мг один раз в сутки.
Применение у отдельных групп пациентов
Дети и подростки
На настоящий момент безопасность и эффективность препарата у пациентов детского и подросткового возраста не установлена.
Elderly patients
Обычно у пациентов пожилого возраста снижения дозы не требуется. У пациентов, которые принимали препарат Апровель® в клинических исследованиях, в целом не наблюдалось различий эффективности и безопасности между пациентами в возрасте 65 лет и старше и пациентами более молодого возраста.
Patients with hepatic insufficiency
Обычно у пациентов с нарушением функции печени (лёгкой и умеренной степени тяжести) снижения дозы не требуется. Опыт применения препарата у пациентов с тяжелой печеночной недостаточностью отсутствует.
Patients with renal insufficiency
Обычно у пациентов почечной недостаточностью (независимо от ее степени тяжести) снижения дозы не требуется.
Пациенты с гиповолемией
У пациентов с выраженной гиповолемией и/или гипонатриемией, таких как пациенты, получающие интенсивную диуретическую терапию, или находящиеся на гемодиализе, гиповолемия и гипонатриемия должны быть скорректированы до начала применения препарата Апровель®.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist