Biprol tab p / 10 mg of the film 30 pc

Description

Composition
Active substance:
1 tablet contains bisoprolol fumarate 5,000 mg / 10,000 mg.
Excipients:
Microcrystalline Cellulose 44.500 mg / 62,400 mg; ludipress LTSE (94,7-98,3% lactose monohydrate, povidone, 4.3%) 40,000 mg / 38,500 mg; Corn starch 8.000 mg / 11,000 mg; colloidal silicon dioxide 0.500 mg / 0.600 mg; crospovidone (Kollidon CL) 1,000 mg / 1,250 mg; Magnesium stearate 1.000 mg / 1,250 mg;
sheath: titanium dioxide 0.287 mg / 0.430 mg; macrogol (polyethylene glycol 4000), 0.287 mg / 0.430 mg; hypromellose 1.320 mg / 1,968 mg; talc 0.106 mg / 0.172 mg.
Description:
Round, biconvex tablets, film-coated white or almost white. On the cross-section of the kernel white or white with Valium a barely perceptible color.
Product form:
Tablets, coated membrane shell 5 mg and 10 mg.
10 tablets in blisters of PVC film and aluminum foil.
3, 5 or 10 contour cell packages together with instructions for use in paper cartons.
Contraindications
Hypersensitivity to bisoprolol, other ingredients and other beta-blockers; shock (including cardiogenic); pulmonary edema; acute heart failure or heart failure decompensation requiring inotropic of therapy; AV blockade II-III extent without the pacemaker; sinoatrial block; sick sinus syndrome; bradycardia (heart rate less than 60 beats / min); Prinzmetal angina; cardiomegaly (without heart failure); severe hypotension (systolic blood pressure less than 100 mm Hg…) especially in myocardial infarction; severe bronchial asthma and chronic obstructive pulmonary disease (COPD) in history; simultaneous reception floctafenine, sultopride, monoamine oxidase inhibitors (MAO) except MAO-B; simultaneous intravenous administration of verapamil or diltiazem; severe peripheral circulatory disorders, Raynaud’s syndrome; pheochromocytoma (without the simultaneous use of alpha blockers); metabolic acidosis; age 18 years (effectiveness and safety have been established).
Lactase deficiency, lactose intolerance, malabsorption syndrome lactose / isomaltose (a part of the lactose included drug).
Carefully
Severe hepatic insufficiency, severe renal impairment (creatinine clearance less than 20 mL / min), myasthenia gravis, thyrotoxicosis, diabetes mellitus (may mask symptoms of hypoglycemia), allergic history, AV block I degree, depression (including history), psoriasis, asthma, COPD, peripheral circulatory disorders, a strict diet.
Dosage
10 mg
Indications
Arterial hypertension.
Ischemic heart disease: prevention of attacks of stable angina.
Interaction with other drugs
Floctafenine. In case of shock or hypotension due floctafenine, beta-blockers cause reduction compensatory ¬ cardio vascular reactions (joint use is contraindicated).
Sultopride. Due to the additive effect may develop severe bradycardia (combined use is contraindicated).
MAO inhibitors. Not recommended simultaneous application (except for the MAO-B), because it is likely significant increase antihypertensive action. Break in treatment between reception and bisoprolol MAO inhibitor should not be less than 14 days.
Blockers “slow” calcium channel (diltiazem and verapamil). Avoid this combination. During the period of treatment Biprol intravenous verapamil or diltiazem and other antiarrhythmic drugs is contraindicated. Due to synergistic action may sharp decrease in blood pressure, disorders of automaticity (bradycardia, cardiac sinus) AV conduction disorders, heart failure. If necessary, such a combination of destination requires careful clinical and ECG monitoring of patients, particularly the elderly and early treatment.
Class I antiarrhythmics (e.g., quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone), while the application may reduce AV conduction and contractility of the myocardium (avoid combination with bisoprolol).
Class III antiarrhythmics (e.g., amiodarone). When coupled with a possible violation of bisoprolol contraction, automaticity and conduction due to depression of sympathetic compensatory mechanisms (avoid this combination).
Centrally acting antihypertensive agents (clonidine, apraclonidine, alpha – methyldopa, guanfantsin, moxonidine, rilmenidine). In a joint application increased risk of severe bradycardia, sinus node stops, the AV conduction, a sharp decline in blood pressure, heart failure (synergistic effect). Avoid this combination. If necessary, use requires careful clinical and electrocardiographic monitoring, particularly in elderly patients and at the beginning of treatment. A significant rise in blood pressure during sharp cancellation centrally acting antihypertensive agent.
Cardiac glycosides. Decreased heart rate, conduction disturbances.
Beta-blockers for topical (e.g., eye drops for treating glaucoma) may enhance the systemic effects of bisoprolol (blood pressure reduction, slowing the heart rate).
Calcium channel blockers (e.g., nifedipine). Perhaps an excessive reduction in blood pressure.
Parasympathomimetics. In a joint application the risk of bradycardia.
Mefloquine. The combined use of bisoprolol increased risk of bradycardia (additive effect).
Phenytoin intravenous administration, drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity cardiodepressive steps and probability of lowering blood pressure.
The simultaneous use of beta-agonists (e.g., isoprenaline, dobutamine) may reduce the effect of both drugs.
Bisoprolol combination with agonists affecting the alfa- and beta-adrenergic receptors (such as norepinephrine, epinephrine), may enhance the vasoconstrictor action of these agents, with the resulting alpha- adrenoceptor, resulting in increased blood pressure. Such interactions are more likely to occur when using non-selective beta-blockers.
Bisoprolol can change the effectiveness of insulin and hypoglycemic agents for oral administration, to mask the symptoms of developing hypoglycemia (tachycardia, hypertension).
Bisoprolol reduces the clearance of lidocaine and xanthine (except dyphylline) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking.
Antihypertensive effects of impaired non-steroidal anti-inflammatory drugs (delay sodium and kidney blockade of prostaglandin synthesis) and glucocorticoids, estrogens (delay sodium ions).
Diuretics, sympatholytic, hydralazine, and other antihypertensive drugs. The risk of excessive blood pressure lowering.
Bisoprolol prolongs the action of non-depolarizing muscle relaxants and anticoagulant effect of coumarin.
Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics drugs – when combined with bisoprolol amplification depression of the central nervous system.
Non-hydrogenated ergot alkaloids increase the risk of peripheral circulatory disorders.
Ergotamine increases the risk of peripheral circulatory disorders.
Sulfasalazine increases the concentration in plasma bisoprolol.
Rifampicin reduces the half-life of bisoprolol.
The allergens used for immunotherapy, or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol.
Iodine-containing radiopaque diagnostic agents for intravenous administration increases the risk of anaphylactic reactions.
Overdose
Symptoms: arrhythmia, ventricular arrythmia, bradycardia, AV block, marked decrease in blood pressure, congestive heart failure, hypoglycemia, acrocyanosis, shortness of breath, bronchoconstriction, dizziness, fainting, convulsions.
Treatment: gastric lavage, the appointment of absorbent, symptomatic therapy. In severe bradycardia – intravenous administration of atropine. If the effect is insufficient, you can enter with caution agent with positive chronotropic effect. Sometimes it may require temporary staging an artificial pacemaker.
At which developed AV blockade – intravenous administration 1-2 mg atropine, epinephrine or setting a temporary pacemaker.
When ventricular arrhythmia – lidocaine (IA class of drugs does not apply). In marked decrease in the patient’s blood pressure should be transferred to the Trendelenburg position; if no signs of pulmonary edema – intravenous plasma-substituting solutions in their inefficiency – administration of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and eliminate expressed lowering blood pressure).
When hypoglycemia can be shown intravenous solution of dextrose (glucose). In heart failure – cardiac glycosides, diuretics. In convulsions – diazepam intravenously. When bronchospasm – inhaled beta2- agonists.
pharmachologic effect
Pharmacological group:
Beta1-selective blocker.
Pharmacodynamics:
Selective beta1-adrenergic blocker, without own sympathomimetic activity, has no membrane stabilizing effect. It has antihypertensive, antiarrhythmic and antianginal effects.
Blocking in low doses beta1-adrenergic receptors of the heart, stimulated by catecholamines reduces the formation of cyclic AMP from ATP, reduces intracellular calcium ion current has a negative chronotropic, dromo-, BATM inotropic effect and reduces the atrioventricular (AV) conduction and excitability. When exceeding the therapeutic dose has beta2-adrenoceptor blocking effect. Total peripheral vascular resistance at the beginning of the application of the preparation (within 24 hours) is increased (as a result of reciprocal increase in the activity of alpha-adrenoceptor stimulation and removal of beta2-adrenoceptor), which is 1-3 days returns to the original, and prolonged decreases appointment.
Antihypertensive action associated with a decrease in cardiac output, sympathetic stimulation of peripheral blood vessels, reduction in activity of the renin-angiotensin-aldosterone system (important for patients with initial hypersecretion renin) baroreceptors aortic arch sensitivity reduction (not going to increase their activity in response to a decrease in blood pressure) and the influence of the central nervous system. When hypertension effect develops after 2-5 days, stable operation – through 1-2 months.
Antianginal effect due to a decrease in myocardial oxygen demand as a result of shortening of the heart rate and reduce myocardial contractility, lengthening of diastole, improving myocardial perfusion. By increasing the end-diastolic pressure in the left ventricle and increased tensile ventricular muscle fibers can increase myocardial oxygen demand, especially in patients with chronic heart failure (CHF).
Antiarrhythmic effect due to elimination of arrhythmogenic factors (tachycardia, increased sympathetic nervous system activity, increasing the content of cyclic AMP, hypertension), decrease the rate of spontaneous excitation of the sinus and ectopic pacemaker and deceleration AV conducting (preferably antegrade and to a lesser extent, in the retrograde direction ) through the atrioventricular node and additional routes.
When applied in high therapeutic doses, unlike nonselective beta-blockers, it has a less pronounced effect on organs containing beta 2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchial and uterine) and carbohydrate metabolism; It does not cause a delay of sodium ions in the body.
Pharmacokinetics:
Suction. Absorption – 80-90%, food intake does not affect absorption of the drug. The maximum plasma concentration observed after 1-3 hours. Bioavailability – about 90%. Communication with plasma proteins – about 30%.
Distribution. The volume of distribution of 3.5 l / kg. The permeability of the blood-brain and placental barriers – low.
Metabolism. It is metabolized in the liver with the participation isozymes CYP3A4 (95%) and CYP2D6. The effect of “first pass” through the liver, slight (about 10%). Biotransformation of bisoprolol is not accelerated in patients with hyperthyroidism.
Withdrawal. Total clearance was 15.6 ± 3.2 l / h, renal clearance – 9.6 ± 1.6 l / h. Balanced bisoprolol clearance determined by the equilibrium between its excretion via the kidneys in unchanged form (about 50%) and in the liver by oxidation (about 50%) to inactive metabolites that then also the kidneys; less than 2% is excreted through the intestines (in bile). It does not accumulate in the body. The half-life of 9-12 hours.
The dependence of the pharmacokinetics of bisoprolol dose is linear.
The pharmacokinetics of bisoprolol is stable, does not depend on the age and sex of the patient.
Pharmacokinetics in special clinical situations
Renal insufficiency. In case of severe renal failure (creatinine clearance less than 20 mL / min) and in patients with anuria half-life may be increased more than 2 times.
Liver failure. In case of severe liver failure marked increase in half-life period of up to 13-15 hours.
Chronic heart failure. In patients with chronic heart failure (III functional class NYHA classification), the concentration of bisoprolol in blood plasma is higher than in healthy volunteers, and the elimination half-life increased to 17 hours.
Pregnancy and breast-feeding
Bisoprolol has no direct cytotoxic, mutagenic and teratogenic effects, but it has pharmacological effects that may cause harmful effects on pregnancy and / or the fetus or newborn.
Typically, beta-blockers reduce placental perfusion, leading to slower growth of the fetus, fetal death, premature delivery or miscarriage. In the fetus and newborn child may have abnormal reactions such as intrauterine growth retardation, hypoglycemia, bradycardia.
Biprol should not be used during pregnancy. Application is possible that if the benefit to the mother outweighs the risk of side effects in the fetus and / or the child. In the case when treatment with Biprol seen as necessary, should monitor blood flow in the placenta and uterus, as well as to observe the growth and development of the fetus. In case of occurrence of adverse events in relation to pregnancy and / or fetus, you must apply alternative therapies.
It is necessary to carefully examine the newborn after delivery. Symptoms of hypoglycaemia and bradycardia occur, usually within the first 3 days of life.
Information about the penetration of bisoprolol in human milk is not, so the drug is not recommended Biprol women during lactation.
If necessary, use during lactation, breast-feeding should be discontinued.
Conditions of supply of pharmacies
Prescription.
side effects
Frequency following side effects listed in accordance with the WHO classifications: very often – more than 10%; often – more than 1% and less than 10%; infrequently – more than 0.1% or less
1%; rarely – more than 0.01% and less than 0.1%; very rarely – less than 0.01%, including some cases.
From the central and peripheral nervous system: often – fatigue, asthenia, dizziness, headache. Typically, these events are developing at the beginning of treatment, usually expressed slightly and held for 1-2 weeks; infrequently – sleep disturbances, depression; rarely – nightmares, hallucinations, loss of consciousness.
Cardio-vascular system: very often – bradycardia, palpitations; often – pronounced reduction in blood pressure (especially in patients with heart failure), the manifestations of vasoconstriction (increased peripheral circulatory disorders, cold sensation in the extremities (paraesthesia); rarely – a violation of AV conduction (up to the full development of cross-blockade and heart failure), arrhythmia, worsening flow of CHF with the development of peripheral edema (swelling of ankles, feet) and dyspnea, postural hypotension, chest pain.
From the digestive system: often – nausea, vomiting, diarrhea, abdominal pain,
constipation, dryness of the oral mucosa; rarely – hepatitis, increased activity of “liver” transaminases (ALT, AST), increased bilirubin.
The respiratory system: rarely – laryngo and bronchospasm in patients with asthma or obstructive airways disease; seldom –
allergic rhinitis, nasal congestion.
On the part of the musculoskeletal system: rarely – muscle weakness, cramps in the calf muscles, arthralgia.
From the sensory organs: rarely – visual disturbances, reduced lacrimation (to consider when wearing contact lenses), hearing loss, change in taste;
very rare – dryness and soreness of the eyes, conjunctivitis.
For the skin: rarely – increased sweating, psoriasiform skin reactions; very rare – alopecia, exacerbation of psoriasis flow.
From endocrine system: rarely – hypoglycemia.
From the urogenital system: rarely – a violation of potency, libido weakening.
Со стороны иммунной системы: редко — появление антинуклеарных антител с необычной клинической симптоматикой волчаночноподобного синдрома, которые исчезают после окончания лечения.
Аллергические реакции: редко — гиперемия кожи, кожный зуд, кожная сыпь, крапивница.
Лабораторные показатели: редко — гипертриглицеридемия; очень редко — тромбоцитопения, агранулоцитоз, лейкопения.
Прочие: редко — синдром «отмены» (усиление приступов стенокардии, повышение артериального давления).
special instructions
Лечение препаратом обычно является долговременным.
Перед началом лечения рекомендуется проведение исследования функции внешнего дыхания у пациентов с отягощенным бронхолегочным анамнезом. Пациентам с бронхоспастическими заболеваниями можно назначать бисопролол в случае непереносимости и/или неэффективности других гипотензивных лекарственных средств, при этом следует строго следить за дозой препарата. Overdose risk of developing bronchoconstriction.
Наблюдение за пациентами, принимающими бисопролол, должно включать контроль частоты сердечных сокращений, артериального давления (в начале лечения — ежедневно, затем 1 раз в 3-4 месяца), электрокардиограммы, концентрации глюкозы в плазме крови у пациентов с сахарным диабетом (1 раз в 4-5 месяцев). У пожилых пациентов рекомендуется контролировать функцию почек (1 раз в 4-5 месяцев). Следует обучить пациента методике подсчета частоты сердечных сокращений и проинструктировать о необходимости врачебной консультации при снижении ее менее 60 уд/мин.
Примерно у 20% пациентов со стенокардией бета-адреноблокаторы неэффективны. Основные причины — тяжелый коронарный атеросклероз с низким порогом ишемии (частота сердечных сокращений менее 100 уд/мин) и повышение конечного диастолического объема левого желудочка, нарушающее субэндокардиальный кровоток. The “smoking” the effectiveness of beta-blockers lower.
Пациенты, пользующиеся контактными линзами, должны учитывать, что на фоне лечения возможно уменьшение продукции слезной жидкости.
При использовании у пациентов с феохромоцитомой имеется риск развития парадоксальной артериальной гипертензии (если предварительно не была достигнута эффективная альфа-адреноблокада).
При тиреотоксикозе бисопролол может маскировать определенные клинические признаки тиреотоксикоза (например, тахикардию). Резкая отмена у пациентов с тиреотоксикозом противопоказана, поскольку способна усилить симптоматику.
In diabetes may mask tachycardia caused by hypoglycemia. В отличие от неселективных бета-адреноблокаторов, практически не усиливает вызванную инсулином гипогликемию и не задерживает восстановление концентрации глюкозы в крови до нормального уровня.
При одновременном применении клонидина его прием может быть прекращен только через несколько дней после отмены бисопролола.
May increase the severity of hypersensitivity reactions and the lack of effect of conventional doses of epinephrine with aggravated allergic history.
В случае необходимости проведения планового хирургического вмешательства отмену препарата проводят за 48 часов до начала общей анестезии. Если пациент принял препарат перед хирургическим вмешательством, ему следует подобрать лекарственное средство для общей анестезии с минимальным отрицательным инотропным действием.
Reciprocal activation of the vagus nerve can be eliminated intravenous atropine (2.1 mg).
Лекарственные средства, снижающие запасы катехоламинов (например, резерпин), могут усилить действие бета-адреноблокаторов, поэтому пациенты, принимающие такие сочетания лекарственных средств, должны находиться под постоянным наблюдением врача на предмет выявления артериальной гипотензии или брадикардии.
В случае появления у пациентов пожилого возраста нарастающей брадикардии (менее 60 уд/мин), артериальной гипотензии (систолическое артериальное давление ниже 100 мм рт. ст. ), AV блокады, бронхоспазма, желудочковых аритмий, тяжелых нарушений функции печени и почек необходимо уменьшить дозу или прекратить лечение.
Нельзя резко прерывать лечение бисопрололом из-за опасности развития тяжелых аритмий и инфаркта миокарда. Отмену проводят постепенно, снижая дозу в течение 2 недель и более (дозу снижают на 25% в 3-4 дня).
Рекомендуется прекратить терапию (с постепенным снижением дозы) при развитии депрессии, вызванной приемом препарата. Препарат следует отменить перед исследованием содержания в крови и моче катехоламинов, норметанефрина и ванилинминдальной кислоты, титра антинуклеарных антител.
В период лечения необходимо соблюдать осторожность при управлении транспортными средствами и выполнении других потенциально опасных видов деятельности, требующих повышенной концентрации внимания и быстроты психомоторных реакций.
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
Препарат Бипрол принимают внутрь, утром, 1 раз в сутки с небольшим количеством жидкости, до завтрака, во время или после него. Tablets should not be chewed or triturate. Во всех случаях режим приема и дозу подбирает врач каждому пациенту индивидуально, в частности, учитывая частоту сердечных сокращений и состояние пациента.
При артериальной гипертензии и ишемической болезни сердца препарат назначают по 5 мг 1 раз в сутки. If necessary to increase the dose of 10 mg 1 time per day. При лечении артериальной гипертензии и стенокардии максимальная суточная доза составляет 20 мг 1 раз в сутки.
Для пациентов с выраженным нарушением функции почек (клиренс креатинина менее 20 мл/мин) или с выраженным нарушением функции печени максимальная суточная доза составляет 10 мг 1 раз в сутки. Увеличение дозы у таких пациентов необходимо проводить с особой осторожностью.
У пациентов пожилого возраста коррекции дозы 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