Carvedilol 12.5mg tab-obl 30 pc

Description

Composition
Active substance:
1 tablet contains: Carvedilol 6.25 mg, 12.5 mg and 25.0 mg ;.
Excipients:
Sucrose, magnesium stearate, potato starch, hypromellose, croscarmellose sodium, colloidal silicon dioxide, calcium hydrogenphosphate dihydrate.
Description:
Tablets white or white color with a yellowish shade, biconvex shape.
Product form:
Tablets of 6.25 mg, 12.5 mg and 25 mg.
At 7, 10, 15, 20 or 30 tablets in blisters.
2, 3, 4, 5, 8 or 10 contour of cellular packaging together with instructions for use placed in a pile of cardboard.
Contraindications
Hypersensitivity to carvedilol or other components of the formulation; chronic obstructive pulmonary disease (COPD); bronchial asthma or bronchospasm (history); IV heart failure class NYHA functional classification (decompensation requiring intravenous inotropic agents), acute heart failure; Prinzmetal angina; cardiogenic shock; bradycardia (less than 50 beats / min alone), sick sinus syndrome (including sinus block), atrioventricular (AV) block II-III extent (except in patients with an artificial pacemaker); end stage occlusive peripheral vascular disease; clinically significant abnormal liver function, metabolic acidosis; patients receiving intravenous therapy with verapamil or diltiazem, of the possibility of developing severe bradycardia (less than 40 beats / min) and arterial hypotension; marked hypotension (systolic blood pressure less than 85 mmHg..); fructose intolerance and malabsorption syndrome glucose / galactose or deficit sucrase / isomaltase; breastfeeding; age 18 years (Safety and efficacy have not been established), pheochromocytoma (without the simultaneous use of alpha-blockers).
Precautions: AV blockade degree I, diabetes mellitus, hypoglycemia, hyperthyroidism, occlusive peripheral vascular disease, pheochromocytoma (with simultaneous application of alpha-blockers), depression, myasthenia gravis, psoriasis, extensive surgery, general anesthesia, renal failure, pregnancy.
Dosage
12.5 mg
Indications
Arterial hypertension (alone or in combination with other antihypertensive agents);
Ischemic heart disease: prevention of attacks of stable angina;
Chronic heart failure (in a combination therapy).
Interaction with other drugs
During treatment with carvedilol in patients is not recommended to drink alcohol, because Ethanol can potentiate the side effects of carvedilol.
When simultaneous administration of carvedilol digoxin and digoxin concentration in the blood plasma increased by approximately 16% and may increase the AV conduction time. At the beginning of carvedilol therapy in the selection of the dose or withdrawal of the drug is recommended regular monitoring of digoxin plasma concentration.
Carvedilol may potentiate the action of insulin and hypoglycemic agents for oral administration, including sulfonylureas, with symptoms of hypoglycemia (especially tachycardia) may be masked, so diabetic patients recommended the regular control of blood glucose concentration.
Carvedilol enhances the effect of antihypertensive agents (ACE inhibitor, thiazide diuretics, vasodilators).
The simultaneous use of drugs to lower content of catecholamines (reserpine, monoamine oxidase inhibitors), increases the risk of significant decrease in blood pressure and bradycardia.
In applying carvedilol in patients undergoing kidney transplantation, who developed a chronic vascular graft rejection, it was observed a moderate increase in average minimum concentration of cyclosporine. To maintain the concentration of cyclosporine in the therapeutic range, approximately 30% of patients had to reduce the dose of cyclosporin (on average 20%), the rest of the patients the dose correction is not required. Due to the pronounced individual variations required daily dose of cyclosporin recommended careful monitoring of cyclosporin plasma concentrations after initiation of therapy of carvedilol and, if required, corresponding correction daily dose cyclosporine.
The simultaneous use of carvedilol with blockers “slow” calcium channel (dihydropyridine derivatives) may lead to severe heart failure, and severe hypotension.
Sympathomimetics having alpha and beta adrenomimeticheskim effects, while the use of carvedilol increases the risk of hypertension and severe bradycardia.
Verapamil, diltiazem and other antiarrhythmic agents (propranolol, amiodarone) priodnovremennom application with carvedilol can increase the risk of AV conduction disorders by oral administration. Concomitant intravenous verapamil or diltiazem with carvedilol.
With simultaneous use of carvedilol and diltiazem, marked individual cases conduction disturbances (rarely – with hemodynamic disorders). As in the case of other drugs with beta-adrenoceptor blocking properties, together with the use of carvedilol blockers “slow” calcium channel blockers verapamil and diltiazem type recommended under the control of ECG and blood pressure.
The simultaneous use of clonidine may potentiate antihypertensive and hromotropny negative effects of carvedilol.
Inhibitors of microsomal oxidation (cimetidine, ketoconazole, fluoxetine, haloperidol, verapamil, erythromycin) increase, and inductors (barbiturates, rifampicin) weaken the antihypertensive effect of carvedilol.
Nitrates and beta-blockers (e.g., in the form of eye drops) may potentiate the antihypertensive effect of carvedilol.
General anesthetics enhance the negative inotropic and hypotensive effect of carvedilol.
Ergotamine vasoconstriction increases while the use of carvedilol.
Nonsteroidal anti-inflammatory drugs reduce the antihypertensive effect of carvedilol.
Overdose
Symptoms: marked decrease in blood pressure (systolic blood pressure of 80 mm Hg or less..), Bradycardia (less than 50 beats / min), impaired lung function (including bronchospasm), heart failure, cardiogenic shock, heart failure, generalized cramps, vomiting, confusion.
Treatment: In the first hours after the overdose, induce vomiting and stomach wash. It is necessary to carry out monitoring and correction of vital signs, if necessary – in the intensive care unit.
Put the patient on his back (with raised feet) with bradycardia – atropine 0.5-2 mg intravenously, in resistant to therapy bradycardia shown staging artificial cardiac pacemaker; In marked decrease in blood pressure – norepinephrine (noradrenaline); with bronchospasm used beta-agonists for inhalation (for inefficiency – i.v.) or aminophylline intravenously.
In convulsions administered by slow intravenous diazepam or clonazepam.
Because of severe overdose with symptoms of shock possible extension of the T1 / 2 of carvedilol and elimination of the drug from the depot, it is necessary to continue maintenance therapy for quite a long time. Length of maintenance treatment depends on the severity of overdose, it must continue to stabilize the patient’s clinical condition.
pharmachologic effect
Pharmacological group:
Alpha- and beta-blocker.
Pharmacodynamics:
Carvedilol – alpha 1 blocker, beta1-, beta2-adrenoceptor has organoprotective effect. Possesses anti-proliferative properties against vascular smooth muscle cell walls, is a racemic mixture of R (+) and S (-) stereoisomers, each of which has the same alpha-adrenoceptor blocking properties. Due kardioneselektivnomu beta-adrenoceptor blocking caused by S (-) stereoisomer, carvedilol reduces blood pressure (BP) reduces the heart rate (HR) and cardiac output, reduces the pressure in the pulmonary arteries and into the right atrium. Due alpha1 adrenoceptor blockade causes peripheral vasodilation and reduction in peripheral vascular resistance (MSS). It reduces the load on the heart muscle and prevents the development of angina attacks. Patients with chronic heart failure (CHF) increases the ejection fraction of the left ventricle (LV) and reduces the severity of symptoms. Similar effects were observed in patients with impaired left ventricular function.
Carvedilol has no intrinsic sympathomimetic activity, and the like propranolol, has the property of stabilizing the membranes. The activity of the renin-angiotensin-aldosterone system (RAAS) is reduced, reducing the release of renin, so fluid retention characteristic of selective alpha-adrenergic blockers, is rare. The effect on blood pressure and heart rate was most pronounced after 1 – 2 h after dosing.
Carvedilol has no adverse effect on the lipid profile, while maintaining normal ratio lipoproteins and low density lipoproteins (HDL / LDL).
Patients with hypertension (AH) and kidney diseases carvedilol decreases renal vascular resistance, with no significant change in glomerular filtration rate, renal plasma flow and the excretion of electrolytes. Peripheral blood flow is maintained, therefore cooling the hands and feet, often noted when taking beta-blockers, is rare.
Pharmacokinetics:
Carvedilol is rapidly absorbed after oral administration.
The maximum concentration of carvedilol in the blood plasma (Cmax) is achieved within 1 h. The absolute bioavailability of carvedilol is about 25-30% for the R-form and 15% for S-shape.
Carvedilol has high lipophilicity. Approximately 98-99% of its bound to plasma proteins. The volume of distribution of about 2 liters / kg and increased in patients with cirrhosis of the liver by reducing the effect of “first pass” through the liver.
Carvedilol is metabolized primarily in the liver by oxidation and conjugation to form several metabolites. When metabolized “first pass” through the liver.
Metabolism of carvedilol by oxidation is stereoselective. R (+) isomer is metabolized mainly via isoenzymes CYP2D6 and CYP1A2, and S (-) isomer of – mostly via isozyme CYP2D9 and, to a lesser extent via isozyme CYP2D6. Other cytochrome P450 isozymes involved in the metabolism of carvedilol, are isozymes CYP3A4, CYP2E1, CYP2C19.
Demethylation and hydroxylation of phenol ring formed metabolite 3 which have less pronounced vasodilating properties than carvedilol.
The half-life (T1 / 2) is about 6 hours, plasma clearance – about 500-700 ml / min. Carvedilol is displayed mainly in the bile and partly through the intestines kidneys as metabolites.
Age of the patient does not have a statistically significant effect on the pharmacokinetics of carvedilol.
Patients with cirrhosis bioavailability of carvedilol is increased by 80% due to the decrease of expression of metabolism at “first pass” through the liver.
Carvedilol crosses the placental barrier and into breast milk. Carvedilol is almost removed from the plasma by hemodialysis.
Pregnancy and breast-feeding
Data on the use of carvedilol drug during pregnancy is limited.
Beta-blockers reduce placental blood flow, have an adverse impact on the development of the embryo, may cause hypotension, bradycardia and hypoglycaemia in the fetus.
The drug carvedilol should not be used during pregnancy unless absolutely necessary, if the potential benefit to the mother justifies the risk to the fetus.
Since carvedilol is excreted in breast milk during therapy with carvedilol breastfeeding should be discontinued.
Conditions of supply of pharmacies
Prescription.
side effects
The frequency of side effects emerged when taking carvedilol, classified according to World Health Organization recommendations: very often – at least 10%; often – at least 1% but less than 10%; infrequently – at least 0.1% but less than 1%; rarely – at least 0.01% but less than 0.1%; very rarely – less than 0.01%, including isolated reports.
The frequency of some side effects such as dizziness, marked reduction in blood pressure, bradycardia and visual impairment, dose-dependent. These effects are more likely to develop in patients with CHF. The most common side effects of carvedilol – dizziness, orthostatic hypotension, or without it, which occurs in approximately 6% of patients.
With the development of serious side effects of treatment with the drug should be discontinued.
From the nervous system: often – dizziness, headache (especially at the beginning of treatment); rarely – sleep disturbances, mood changes and thinking, paresthesia, myasthenia gravis, loss of consciousness.
Cardio-vascular system; very often – orthostatic hypotension; often – bradycardia; rarely – worsening of heart failure flow (especially when the dose is increased), cold hands and feet, decreased blood pressure, fainting; rarely – conduction disorders, palpitations, worsening angina pectoris, occlusion of peripheral circulation, “intermittent” claudication, peripheral edema.
From the digestive system: often – nausea, abdominal pain (up to 2%), diarrhea, dryness of the oral mucosa; rare – loss of appetite, vomiting, flatulence, constipation; very rarely – dryness of the oral mucosa, increased activity “liver” transaminase (alanine aminotransferase (ALT), aspartate aminotransferase (AST), gamma glutamyltransferase).
From the senses: common – a decrease in lacrimation and eye irritation (pay attention when using contact lenses); very rarely – visual disturbances, eye irritation.
Metabolism: often – body weight increase, hypercholesterolemia, patients with pre-existing diabetes – hyperglycemia or hypoglycemia; rarely – increased triglyceride levels.
On the part of the musculoskeletal system: rarely – pain in the muscles, bones and spine.
From the hematopoietic system and lymphatic system: rarely – thrombocytopenia; very rarely – leukopenia.
The respiratory system: rarely – dyspnea, bronchospasm (in predisposed patients), nasal congestion.
From the urinary system: rarely – a violation of urination; very rarely – severe renal dysfunction.
For the skin: very rarely – worsening of psoriasis flow, alopecia, exfoliative dermatitis.
Other: often – general weakness; infrequently – hypersensitivity reactions (pruritus, rash, hives), decreased potency; very rarely – “tides” of blood to the skin, sneezing, flu-like symptoms.
There have been rare cases of urinary incontinence in women, reversible after discontinuation of the drug.
special instructions
The drug is recommended to take carvedilol for the treatment of heart failure in addition to standard CHF therapy with diuretics, ACE inhibitors, cardiac glycosides, or only after the selection of a dose of a diuretic. It can also be used in patients intolerant of ACE inhibitors.
At the beginning of therapy with carvedilol or after increasing the dose can sometimes develop orthostatic hypotension and dizziness, possible fainting, especially in patients with heart failure, elderly patients and at the same time taking other antihypertensive drugs or diuretics. These effects can be prevented by applying a low initial dose Karveldilol with a gradual increase to a maintenance dose, and taking the drug at meal times. Patients need to explain how you can avoid orthostatic hypotension (gently up from the “lying” or “sitting”, you need to sit or lie in the development of dizziness).
Patients with heart failure may take the drug carvedilol, only if their condition is successfully controlled by medication group of cardiac glycosides and / or diuretics. If during treatment for heart failure is getting worse, you need to increase the dose of diuretic, and the dose of the drug carvedilol reduced or temporarily suspend its application.
With beta-adrenoceptor blocking properties, carvedilol may mask symptoms of hypoglycemia in patients with diabetes, as well as symptoms of hyperthyroidism in patients with thyroid disease, reducing symptoms tachycardia. Patients with heart failure may increase or decrease in blood glucose concentration.
In general anesthesia in patients receiving carvedilol, narcotic analgesics must be used with minimal inotropic effect, or pre (slowly!) Cancel drug.
In some cases, carvedilol may cause liver function disorders. With the development of liver failure carvedilol drug should be discontinued. Generally, after withdrawal of the drug to normal liver function.
In COPD carvedilol may worsen bronchial obstruction in patients with COPD therefore should not be applied.
Carvedilol may worsen the clinical picture of peripheral arteriopathy, psoriasis, cause anaphylactic reactions, enhance the body’s response during allergoproby, provoking the appearance of pain in patients with Prinzmetal’s angina.
Пациенты с феохромоцитомой могут принимать карведилол только после того, как начата терапия альфа-адреноблокаторами.
При резком прекращении терапии препаратом Карведилол может развиться повышенное потоотделение, тахикардия, одышка и ухудшение течения стенокардии. Наиболее подвержены риску возникновения этих реакций пациенты со стенокардией, у которых может развиться инфаркт миокарда. При отмене препарата Карведилол дозу уменьшают постепенно, в течение 1-2 недель.
Если после прекращения терапии прошло более 2 недель, возобновлять приём препарата рекомендуется с низких доз.
Пациентам, носящим контактные линзы, следует учитывать, что препарат может вызывать уменьшение слезоотделения.
В случае урежения ЧСС до 50 уд/мин препарат следует отменить.
Препарат Карведилол не рекомендуется принимать пациентам моложе 18 лет, т.к. эффективность и безопасность препарата Карведилол у этой группы пациентов не установлена.
Влияние на способность управлять автомобилем и другими сложными механизмами
Необходимо соблюдать осторожность при управлении автотранспортом и занятиями потенциально опасными видами деятельности, требующими повышенной концентрации внимания и скорости психомоторных реакций, в связи с тем, что возможно развитие головокружения.
Storage conditions
In a dry, dark place at a temperature not higher than 25 C.
Keep out of the reach of children.
Dosing and Administration
Inside, after eating, squeezed water.
The dose is adjusted individually. Лечение необходимо начинать с низких доз, постепенно повышая до достижения оптимального клинического эффекта. После первого приёма препарата Карведилол и после каждого увеличения дозы, для исключения возможной артериальной гипотензии, рекомендуется измерять АД через 1 ч после приёма препарата.
Терапию препаратом Карведилол необходимо прекращать постепенно, снижая дозу в течение 1-2 недель.
Если после прекращения терапии прошло более 2 недель, возобновлять приём препарата рекомендуется, опять начиная с низкой дозы.
Arterial hypertension
Начальная доза – по 12,5 мг 1 раз в сутки утром в течение первых 2-х дней, затем по 25 мг 1 раз в сутки. В дальнейшем при необходимости дозу можно увеличивать с интервалами не менее 2 недель, доводя до максимальной суточной дозы 50 мг в сутки (разделенной на 2 приема).
Ишемическая болезнь сердца: профилактика приступов стабильной стенокардии
Начальная доза – по 12,5 мг 2 раза в день в течение первых 2-х дней, затем по 25 мг два раза (утром и вечером) в день.
Chronic heart failure
Дозу подбирают индивидуально, необходимо тщательное наблюдение врача. Следует наблюдать за состоянием пациента в течение первых 2-3 часов после первого приема препарата или после первого увеличения дозы. Доза и применение других средств, таких как дигоксин, диуретики и ингибиторы ангиотензипревращающего фермента (АПФ), должны быть скорректированы до начала терапии препаратом Карведилол. Пациенты должны принимать таблетки во время еды (для уменьшения риска ортостатической гипотензии).
Рекомендованная начальная доза – 3,125 мг (возможно применение препарата карведилол в другой лекарственной форме: таблетки по 3,125 мг) 2 раза в сутки. Если эта доза хорошо переносится, её можно постепенно, с интервалом в 2 недели, увеличить до 6,25 мг 2 раза в сутки, затем до 12,5 мг 2 раза в сутки, потом до 25 мг 2 раза в сутки. Пациенты принимают максимально переносимую дозу. Максимально рекомендуемая доза для пациентов с массой тела до 85 кг – по 25 мг 2 раза в день и для пациентов с массой тела более 85 кг – по 50 мг 2 раза в день.
Пациентам с ХСН с целью предотвращения ортостатической гипотензии рекомендуется принимать препарат во время еды.
Перед каждым увеличением дозы врач должен осмотреть пациента для выявления возможного нарастания симптомов течения ХСН или вазодилатации. При преходящем нарастании симптомов ХСН или задержке жидкости в организме следует увеличить дозу диуретиков, хотя иногда требуется уменьшение дозы препарата Карведилол или временная его отмена. Дозу препарата Карведилол не следует увеличивать, пока симптомы усиливающейся сердечной недостаточности или артериальной гипотензии не стабилизируются.
Если лечение препаратом Карведилол прерывают более чем на 1 неделю, то его применение возобновляют в меньшей дозе, а затем увеличивают в соответствии с приведенными выше рекомендациями. Если лечение препаратом Карведилолом было приостановлено более чем на 2 недели, то возобновлять терапию следует с дозы 3,125 мг 2 раза в сутки, затем – подбирая дозу в соответствии с приведенными выше рекомендациями.
elderly patients
correction dose is not required.
Patients with impaired renal function
Существующие данные по фармакокинетике у пациентов с различной степенью нарушения функции почек (включая почечную недостаточность) позволяют полагать, что при умеренной и тяжелой почечной недостаточности коррекции дозы препарата Карведилол не требуется.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist