Espirit tab p / 50 mg of the film 30 pc

$20.80

Espirit tab p / 50 mg of the film 30 pc

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Description

Composition
Active substance:
1 tablet (50 mg) contains: eplerenone – 50.00 mg.
Coating: Opadry II 33G32578 (yellow) – 8,00 mg: Hypromellose-6sR (E464) – 3.20 mg; titanium dioxide (E171) – 1.82 mg; lactose monohydrate – 1.68 mg; macrogol-3350 – 0.64 mg; Triacetin – 0.48 mg; iron oxide yellow dye (E172) – 0.18 mg.
Excipients:
1 tablet (50 mg) contains: lactose monohydrate – 77.34 mg; microcrystalline cellulose – 30.76 mg; hypromellose-15sR – 2.50 mg; Sodium lauryl sulfate – 1.70 mg; croscarmellose sodium – 6.00 mg; magnesium stearate – 1.70 mg.
Description:
Round, biconvex tablets, film-coated yellow, with the mark on one side. Color pills on a break from white to almost white.
Product form:
Tablets, film-coated, 25 mg and 50 mg.
10 tablets in a blister made of PVC film and aluminum foil. 3 or blisters 9 together with instructions for use placed in a pile of cardboard.
Contraindications
• hypersensitivity to eplerenone or other components of the formulation; • clinically significant hyperkalemia; • the content of potassium in blood serum at the beginning of treatment more than 5.0 mmol / l; • moderate or severe renal failure (creatinine clearance (CC) of less than 30 ml / min in patients with chronic heart failure class II NYHA functional classification); • severe hepatic insufficiency (more than 9 points on a scale Child-Pugh); • simultaneous reception of potassium-sparing diuretics, potassium preparations or strong inhibitors isoenzyme CYP3A4, such as itraconazole, ketoconazole, ritonavir, nelfinavir, clarithromycin, telithromycin and nefazodone; • creatinine concentration in blood plasma of> 2.0 mg / dL (or> 177 mg / dL) in men or> 1.8 mg / dL (or> 159 mmol / l) in women; • lack of lactase, lactose intolerance, glucose-galactose malabsorption; • experience of the drug in children under the age of 18 years is not, so his appointment to patients in this age group is not recommended.
Precautions • Type 2 diabetes and microalbuminuria; • the simultaneous use of eplerenone and angiotensin converting enzyme (ACE) inhibitors or angiotensin II receptor antagonists (ARAII); preparations containing lithium; cyclosporine or tacrolimus; digoxin and warfarin doses close to the maximum therapeutic, strong inducers of CYP3A4 isoenzyme; • elderly age; • renal dysfunction (creatinine clearance less than 50 mL / min);
You should not use the triple combination of an ACE inhibitor and ARAII with eplerenone.
Dosage
50 mg
Indications
• Myocardial infarction: in addition to standard therapy to reduce the risk of cardiovascular mortality and morbidity in patients with stable left ventricular dysfunction (ejection fraction less than 40%) and clinical signs of heart failure after myocardial infarction. • Congestive heart failure: in addition to standard therapy to reduce cardiovascular mortality and morbidity in patients with chronic heart failure functional class II of NYHA classification with reduced left ventricular ejection fraction (
Interaction with other drugs
pharmacodynamic interactions
Potassium-sparing diuretics and potassium supplements: taking into account the increased risk of hyperkalemia, eplerenone should not be administered to patients receiving potassium-sparing diuretics and potassium supplements. Potassium-sparing diuretics may enhance the effects of antihypertensives and other diuretics.
Preparations containing lithium: lithium eplerenone interaction with drugs have not been studied.
However, patients treated with preparations of lithium in combination with diuretics and inhibitors
ACE cases increasing concentration and lithium intoxication described. If such a combination is necessary, it is advisable to monitor the lithium content in the blood plasma.
Cyclosporin, tacrolimus: Cyclosporin and tacrolimus can cause renal failure and increase the risk of hyperkalemia. It should avoid the simultaneous use of eplerenone and cyclosporin or tacrolimus. If during treatment with eplerenone require administration of cyclosporine or tacrolimus, it is recommended to regularly monitor the content of potassium in the blood serum and kidney function.
Nonsteroidal anti-inflammatory drugs (NSAIDs): NSAIDs treatment can lead to acute kidney failure due to the direct suppression of glomerular filtration, especially in patients at risk (elderly patients and / or patients with dehydration). When the joint application of these means before and during treatment is necessary to ensure adequate water regime and monitor renal function.
Trimethoprim: the simultaneous use of trimethoprim with eplerenone increases the risk of hyperkalemia. It is recommended to monitor the content of potassium in the blood serum and renal function, particularly in patients with renal insufficiency and in elderly patients.
ACE inhibitors and angiotensin II receptor antagonists: The use of eplerenone with ACE inhibitors or angiotensin II receptor antagonists should regularly monitor the content of serum potassium. Such combination may result in increased risk of hyperkalemia, especially in patients with impaired renal function, including in elderly patients.
You should not use the triple combination of an ACE inhibitor and ARAII with eplerenone.
Alpha 1-blockers (prazosin, alfuzosin), while the use alpha 1 blockers with eplerenone may intensify antihypertensive effect and / or increase the risk of orthostatic hypotension, and therefore, it is recommended to monitor blood pressure when changing body position.
Tricyclic antidepressants, neuroleptics, amifostine, baclofen: while the use of these funds with eplerenone may increase the antihypertensive effect and increased risk of orthostatic hypotension.
Glucocorticosteroids, tetracosactide: the simultaneous use of these means with eplerenone can lead to sodium retention and liquid.
pharmacokinetic interactions
in vitro studies indicate that eplerenone does not inhibit isozymes CYP1A2, CYP2C19, CYP2C9, CYP2D6 and CYP3A4. Eplerenone is not a substrate or inhibitor of glycoprotein P.
Digoxin: AUC digoxin while the use of eplerenone is increased by 16% (90% CI: 4-30%). Caution should be exercised if digoxin is used in doses close to the maximum therapeutic.
Warfarin: no clinically significant pharmacokinetic interactions with warfarin have been identified.
Care must be taken when warfarin is used in doses close to the maximum therapeutic.
Substrates isoenzyme CYP3A4: in special research signs eplerenone pharmacokinetic interactions with substrates isoenzyme CYP3A4, e.g., midazolam and cisapride, have been identified.
Inhibitors of CYP3A4
Strong inhibitors isoenzyme CYP3A4: the application of eplerenone with means inhibiting the isozyme CYP3A4, possibly significant pharmacokinetic interaction. Strong inhibitor of CYP3A4 (ketoconazole 200 mg twice a day) caused an increase in AUC of eplerenone by 441%.
The simultaneous use of eplerenone with potent inhibitors isoenzyme CYP3A4, such as ketoconazole, itraconazole, ritonavir, nelfinavir, clarithromycin, telithromycin and nefazadon contraindicated (see. The section “Contra ‘).
Weak to moderate inhibitors isoenzyme CYP3A4: simultaneous application of erythromycin, saquinavir, amiodarone, diltiazem, verapamil and fluconazole was accompanied by a significant pharmacokinetic interaction (magnification AUC ranged from 98% to 187%). With the simultaneous use of these means with eplerenone dose of the latter should not exceed 25 mg (see. The section “Method of administration and dose”).
Inductors isoenzyme CYP3A4: simultaneous administration of drugs containing St. John’s wort (strong inducer of CYP3A4) with eplerenone AUC last caused a decrease of 30%. When applying a strong inducers of CYP3A4, such as rifampicin, perhaps more pronounced decrease AUC eplerenone. Given the possible reduction in the efficiency of eplerenone simultaneous application of strong inducers of CYP3A4 (rifampicin, carbamazepine, phenytoin, phenobarbital, preparations containing St. John’s wort) is not recommended.
Antacids: Based on clinical pharmacokinetic studies significant interactions with antacids eplerenone at their simultaneous use is not assumed.
Overdose
Overdose of eplerenone in humans has not been described. The most likely manifestations of overdose may be pronounced reduction in blood pressure and hyperkalemia.
Treatment: If severe reduction in blood pressure is necessary to assign a maintenance treatment.
In the case of hyperkalemia is a standard therapy.
Eplerenone is not removed in hemodialysis. It was found that eplerenone is actively associated with the activated carbon.
pharmachologic effect
Pharmacological group:
Potassium-sparing diuretic agent.
Pharmacodynamics:
Eplerenone has a high selectivity to a human mineralocorticoid receptor unlike glucocorticoid, progesterone and androgen receptors, and inhibits the binding of the mineralocorticoid aldosterone – key hormone renin-aldosterone system (RAAS), which is involved in the regulation of blood pressure (BP) and the pathogenesis cardiovascular diseases.
Eplerenone is a persistent increase in the activity of renin in blood plasma and aldosterone in the blood serum. Subsequently, renin secretion is suppressed aldosterone through a feedback mechanism. This increase in renin activity or concentration of circulating aldosterone does not affect the effects of eplerenone.
Significant effect of eplerenone on heart rate (HR), duration of QRS interval, PR or QT is not found in healthy volunteers.
Pharmacokinetics:
Absorption and distribution
The absolute bioavailability is 69% eplerenone after ingestion of 100 mg of eplerenone inside a pill. The maximum concentration (Cmax) in plasma reached in about 2 hours after ingestion. Cmax and area under the curve “concentration-time» (AUC) is linearly dependent on the dose range from 10 to 100 mg, and nonlinear – in a dose of 100 mg. The equilibrium state is reached within 2 days. Food intake does not affect absorption.
Eplerenone approximately 50% bound to plasma proteins, mainly from the group of alpha 1 acid glycoprotein. The calculated volume of distribution at steady state is 50 (± 7) l. Eplerenone does not bind to red blood cells.
Metabolism and excretion
Metabolism eplerenone is performed mainly under the action of the isoenzyme CYP3A4. Active metabolites of eplerenone have not been identified in plasma.
In an unmodified form through the kidneys and intestines output less than 5% of the dose of eplerenone. After a single oral administration of eplerenone labeled about 32% of the dose excreted through the intestines and about 67% – by the kidneys. The half-life of eplerenone is approximately 3-5 hours, a clearance of plasma – about 10 l / h.
Special patient groups
Age, gender and race: The pharmacokinetics of eplerenone at a dose of 100 mg once a day has been studied in elderly patients (over 65 years) – men and women. Pharmacokinetic parameters of eplerenone in men and women were not significantly different. In the equilibrium state in elderly patients Cmax and AUC values ​​were respectively 22% and 45% higher than in younger patients (18-45 years).
Renal insufficiency: pharmacokinetics of eplerenone were studied in patients with renal failure and of varying severity in patients on hemodialysis.
Compared with patients in the control group of patients with severe renal failure showed an increase of the equilibrium AUC and Cmax by 38% and 24% respectively, and in patients undergoing hemodialysis, – they are 26% and 3% reduction. Correlation between clearance of eplerenone from the blood plasma, and creatinine clearance were found. Eplerenone is not removed in hemodialysis.
Hepatic impairment: the pharmacokinetics of eplerenone at a dose of 400 mg was compared in patients with moderate hepatic impairment (7-9 points on a scale Child-Pugh) and healthy volunteers.
Equilibrium Cmax and AUC of eplerenone were increased by 3.6% and 42%, respectively.
In patients with severe hepatic insufficiency eplerenone has not been investigated, therefore its use in these patients is contraindicated.
Heart failure: pharmacokinetics of eplerenone 50 mg were studied in patients with heart failure (II-IV functional class NYHA classification). Equilibrium AUC and Cmax in patients with heart failure were, respectively, 38% and 30% higher than in healthy volunteers, matched for age, weight and gender. Clearance of eplerenone in patients with heart failure is similar to that in healthy elderly people.
Pregnancy and breast-feeding
Information on the use of the drug in pregnant women do not. Espirit drug should be used with caution and only in those cases where the expected benefit to the mother is significantly greater than the potential risk to the fetus / baby.
Information on the allocation of eplerenone after ingestion of breast milk does not. Possible unwanted effects of eplerenone on newborns are breastfed are unknown, so it is advisable or to stop breastfeeding, or stop the drug, depending on its importance to the mother.
Conditions of supply of pharmacies
Prescription.
side effects
The following undesirable effects are presented in accordance with the following gradations their frequency of occurrence in accordance c World Health Organization classification: very common (> 10%); often (> 1%, 0.1%, 0.01%,
Infectious diseases: rare – pyelonephritis, gynecomastia.
Blood disorders and lymphatic system: Infrequent – eosinophilia.
Violations by the endocrine system: rarely – hypothyroidism.
Violations by the Metabolism and nutrition: often – hyperkalemia, hypercholesterolemia, hypertriglyceridemia, dehydration; infrequently – hyponatremia.
Mental disorders: rarely – insomnia.
Disorders of the nervous system: often – dizziness, fainting; rarely – headache, hypoesthesia.
Violations of the heart: often – myocardial infarction; rarely – atrial fibrillation, left ventricular failure, tachycardia.
Violations of the vessels Frequently – marked decrease in blood pressure (BP); rarely – orthostatic hypotension, thrombosis of the lower extremity arteries.
Violations of the respiratory system, thorax and mediastinum: often – cough; infrequently – pharyngitis.
Disorders of the gastrointestinal tract: often – diarrhea, nausea, constipation; infrequently – flatulence, vomiting.
Violations of the liver and biliary tract: rarely – cholecystitis.
Violations of the skin and subcutaneous tissue disorders: often – itching; Infrequent – increased sweating, skin rash; frequency is unknown – angioedema.
Violations by musculoskeletal and connective tissue disorders: often – cramps in the calf muscles of the legs, musculoskeletal pain; infrequently – back pain.
Violations by the kidneys and urinary tract: often – impaired renal function.
General disorders and at the injection site: rare – fatigue, malaise.
Laboratory and instrumental data: infrequently – increasing the concentration of residual urea nitrogen, creatinine, decreased expression of the receptor of epidermal growth factor, increasing the concentration of serum glucose.
special instructions
hyperkalemia
In drug treatment, Espirit may develop hyperkalemia, which is due to its mechanism of action. At the beginning of treatment and when changing dose all patients should control the content of potassium in serum. Subsequently periodic monitoring the potassium content is recommended for patients with an increased risk of hyperkalemia, for example, elderly patients, patients with renal insufficiency and diabetes. Given the increased risk of hyperkalemia, potassium drugs appointment after the start of treatment is not recommended Espirit. Reducing the dose Espirit formulation leads to a decrease in potassium in serum. In one study, the addition of hydrochlorothiazide to eplerenone prevented the increase in potassium in serum.
Renal function
In patients with impaired renal function, including diabetic microalbuminuria, it is recommended to regularly monitor the content of potassium in the blood serum. The risk of hyperkalemia is increased with a decrease in kidney function. Although the number of patients with type 2 diabetes and microalbuminuria in the studies were limited, however, in this small sample was an increase in the frequency of hyperkalemia. Therefore, such patients should be treated with caution. Eplerenone is not removed in hemodialysis.
Use of the drug Espirit contraindicated in severe renal failure (see. The section “Contra ‘).
Abnormal liver function
Patients with mild to moderate hepatic impairment (5-6 and 7-9 on a scale ChayldPyu) increasing the content of potassium in the serum of more than 5.5 mmol / l were detected. These patients should be monitored electrolytes content. In patients with severe hepatic impairment has not been studied eplerenone function, so its use is contraindicated (see. Section “Contraindications”).
Inducers of CYP3A4
Одновременное применение препарата Эспиро с сильными индукторами изофермента CYP3A4 не рекомендуется (см. раздел «Взаимодействие с другими лекарственными препаратами»).
Циклоспорин, такролимус, препараты, содержащие литий
Во время лечения препаратом Эспиро следует избегать назначения этих средств (см. раздел «Взаимодействие с другими лекарственными препаратами»).
Лактоза
Таблетки содержат лактозу, поэтому их не следует назначать пациентам с редкими наследственными заболеваниями, такими как непереносимость лактозы, недостаточность лактазы и синдром мальабсорбции глюкозы-галактозы.
The effect on the ability to operate vehicles, machinery
Влияние препарата Эспиро на способность управлять автотранспортом или пользоваться сложной техникой не изучалось. Однако, учитывая возможность препарата вызывать головокружение и обморочные состояния, следует соблюдать осторожность при управлении автотранспортными средствами или пользовании сложной техникой на фоне приема препарата Эспиро.
Storage conditions
At temperatures above 25 ° C.
Keep out of the reach of children.
Dosing and Administration
Inside.
Прием пищи не влияет на всасывание препарата Эспиро.
myocardial infarction
Лечение следует начинать с дозы 25 мг один раз в сутки и увеличивать ее до 50 мг один раз в сутки через 4 недели с учетом содержания калия в сыворотке крови (см. таблицу №1). Рекомендуемая поддерживающая доза препарата Эспиро составляет 50 мг один раз в сутки.
Хроническая сердечная недостаточность II функционального класса по классификации NYHA
Лечение следует начинать с дозы 25 мг один раз в сутки и увеличивать ее до 50 мг один раз в сутки через 4 недели с учетом содержания калия в сыворотке крови.
Максимальная суточная доза составляет 50 мг.
После временного прекращения приема препарата Эспиро в связи с повышением содержания калия в сыворотке крови до и более 6,0 ммоль/л, терапию препаратом Эспиро можно возобновить в дозе 25 мг через день, когда содержание калия в сыворотке крови составит
Общие рекомендации
Содержание калия в сыворотке крови следует определять до назначения препарата Эспиро, в течение первой недели и через 1 месяц после начала терапии или при изменении дозы препарата.
В дальнейшем также необходимо периодически контролировать содержание калия в сыворотке крови.
elderly patients
Коррекции начальной дозы у пожилых пациентов не требуется. В связи с возрастным снижением функции почек у пожилых пациентов повышается риск развития гиперкалиемии, особенно при наличии сопутствующих заболеваний, способствующих увеличению концентраций эплеренона в сыворотке крови, в частности при нарушении функции печени от легкой до умеренной степени тяжести.
Рекомендуется периодически определять содержание калия в сыворотке крови.
Renal function
Коррекции начальной дозы у пациентов с легкими нарушениями функции почек не требуется.
Степень гиперкалиемии увеличивается при ухудшении функции почек. Рекомендуется периодически определять содержание калия в сыворотке крови.
Эплеренон не удаляется при гемодиализе. У пациентов с тяжелой недостаточностью функции почек (КК
У пациентов с хронической сердечной недостаточностью II функционального класса по классификации NYHA и нарушением функции почек средней степени тяжести (КК 30-60 мл/мин) следует начинать терапию с дозы 25 мг через день с последующей коррекцией дозы в зависимости от содержания калия в сыворотке крови.
Опыта применения препарата Эспиро у пациентов с сердечной недостаточностью после перенесенного инфаркта миокарда и КК
У пациентов с КК
Abnormal liver function
Коррекции начальной дозы у пациентов с нарушением функции печени от легкой до умеренной степени тяжести не требуется. Учитывая увеличение концентрации эплеренона у таких пациентов, рекомендуется регулярно контролировать содержание калия в сыворотке крови, особенно у пожилых пациентов.
Применение препарата Эспиро у пациентов с тяжелыми нарушениями функции печени противопоказано (см. раздел «Противопоказания»).
Сопутствующая терапия
При одновременном применении препаратов, оказывающих слабое или умеренно выраженное ингибирующее действие на изофермент CYP3A4, например, эритромицина, саквинавира, амиодарона, дилтиазема, верапамила и флуконазола лечение препаратом Эспиро можно начать с дозы 25 мг один раз в сутки, при этом доза последнего не должна превышать 25 мг один раз в сутки (см. раздел «Взаимодействие с другими лекарственными препаратами»).
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist

Additional information

Weight0.100 kg
Manufacturer

QUINACRINE

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