Bisoprolol tab n / 5mg film about 60 pieces vertex


Bisoprolol tab n / 5mg film about 60 pieces vertex


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Active substance:
1 tablet contains: bisoprolol fumarate – 2.5 mg, 5.0 mg or 10.0 mg.
Lactose monohydrate; microcrystalline cellulose; colloidal silicon dioxide; crospovidone; magnesium stearate; film coating: [hypromellose, talc, titanium dioxide, macrogol 4000 (polyethylene glycol 4000) – iron oxide yellow dye] or [yellow dry film sheath containing hypromellose – 60% talc – 20% titanium dioxide – 10.33%; macrogol 4000 (polyethylene glycol 4000) – 9%, and iron oxide yellow dye – 0.67%].
Round biconvex tablets, film-coated white or nearly white (dosage 5 mg and 10 mg) or yellow (dosage 2.5 mg). The cross-sectional core of a white or nearly white.
Product form:
Tablets, film-coated, 2.5 mg, 5 mg and 10 mg. 10, 15 or 30 tablets in blisters of PVC film and aluminum foil. 1, 2, 3, 5 or 6 contour cell packs 10 tablets, or 1, 2 or 4 blisters 15 tablets, or 1 or 2 blisters of 30 tablets together with instructions for use in a stack of cardboard.
Hypersensitivity to bisoprolol or any of the excipients (see section “Composition”.); acute heart failure, decompensated heart failure, inotropic therapy requires; cardiogenic shock; atrioventricular (AV) block II and III extent without the pacemaker; sick sinus syndrome; sinoatrial block; bradycardia (heart rate less than 60 beats / min); marked hypotension (systolic blood pressure less than 100 mm Hg..); severe bronchial asthma; expressed human peripheral blood circulation or Raynaud’s syndrome; pheochromocytoma (without simultaneous application of alpha-blockers); metabolic acidosis; age 18 years (lack of data on efficacy and safety in this age group); Lactose Intolerance, Lactase deficiency syndrome or glucose-galactose malabsorption.
Be wary conducting desensitizing therapy; Prinzmetal angina; hyperthyroidism; diabetes type I and diabetes with considerable fluctuations in blood glucose concentration; AV block I degree; severe renal failure (creatinine clearance (CC) of less than 20 ml / min); expressed human liver; psoriasis; restrictive cardiomyopathy; congenital heart defects or heart disease valve with severe hemodynamic compromise;
CHF with myocardial infarction within the last three months; severe chronic obstructive pulmonary disease (COPD); strict diet.
5 mg
Arterial hypertension; Coronary artery disease (CAD) (prevention of attacks of stable angina); chronic heart failure.
Interaction with other drugs
The effectiveness and tolerability of bisoprolol can affect concurrent use of other drugs. Such interaction may also occur in those cases when the two drugs are taken over a short period of time. The doctor should be informed about the use of other drugs, even if their application is carried out without a doctor’s prescription (ie, non-prescription drugs).
Not recommended combinations
Class I antiarrhythmics (e.g., quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone), while the use of bisoprolol can reduce AV conduction and contractility of the myocardium.
Blockers “slow” calcium channel (BCCI) verapamil type and to a lesser extent, diltiazem, while the use of bisoprolol can lead to a decrease of myocardial contractility and AV conduction disturbance. In particular, intravenous administration of verapamil in patients receiving beta-blockers may cause severe hypotension and AV conduction disturbance.
Centrally acting antihypertensives (such as clonidine, methyldopa, moxonidine, rilmenidine) can lead to slowing of the heart rate and reducing cardiac output and vasodilation in the appearance of symptoms due to the reduction of the central sympathetic tone. Abrupt withdrawal, particularly before the abolition of beta-blockers may increase the risk of “rebound” hypertension.
Combinations requiring special care
BCCI dihydropyridine derivatives (e.g. nifedipine, felodipine, amlodipine) while the application of bisoprolol can increase the risk of hypotension. In patients with heart failure can not eliminate the risk of further deterioration of the contractile function of the heart.
Class III antiarrhythmics (e.g., amiodarone), while the use of bisoprolol can exacerbate violation of AV conduction.
The action of beta-blockers for topical (e.g., eye drops for treating glaucoma) may enhance the systemic effects of bisoprolol (decrease in blood pressure, heart rate slowing).
Parasympathomimetics while the use of bisoprolol can exacerbate violation of AV conduction and increase the risk of bradycardia.
Hypoglycemic effect of insulin or hypoglycemic agents for oral administration may be enhanced. Symptoms of hypoglycemia, particularly tachycardia, may be masked or suppressed. This interaction is more likely when using non-selective beta-blockers.
General anesthetics
Able to increase the risk cardiodepressive action, resulting in hypotension (see. Section “Special Instructions”).
cardiac glycosides
While the use of bisoprolol can lead to an increase of the pulse time, and thus, to the development of bradycardia.
Nonsteroidal anti-inflammatory drugs (NSAIDs)
May reduce the antihypertensive effect of bisoprolol.
The simultaneous use of bisoprolol formulation with beta-agonists (e.g., isoprenaline, dobutamine) may reduce the effect of both drugs.
Bisoprolol combination with agonists affecting the alpha- and beta-adrenoceptors (for example, norepinephrine, epinephrine) may enhance vasoconstrictor effects of these agents arising with alpha-adrenoceptors, leading to increased blood pressure. Such interactions are more likely to occur when using non-selective beta-blockers.
When combined with bisoprolol norepinephrine and epinephrine may experience worsening of intermittent claudication.
Antihypertensives, like other means with possible antihypertensive effect (e.g., tricyclic antidepressants, barbiturates, phenothiazines) may enhance the antihypertensive effect of bisoprolol.
The allergens used for immunotherapy, or allergen extracts for skin tests increase the risk of anaphylactic reactions.
The clearance of lidocaine and xanthine (except theophylline) may be reduced due to the possible increase of their plasma concentrations, especially in patients with initially increased clearance of theophylline under the influence of smoking.
Tricyclic and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives and hypnotics enhance central nervous system depression.
Diuretics, sympatholytic, hydralazine and other antihypertensive drugs may lead to an excessive reduction in blood pressure.
The action of non-depolarizing muscle relaxants and anticoagulant effect of coumarin during treatment with bisoprolol may lengthen.
While the use of bisoprolol can increase the risk of bradycardia.
MAO inhibitors (MAO inhibitors with the exception of B)
May enhance the antihypertensive effect of beta-blockers. Concomitant use can also lead to the development of hypertensive crisis. The interval between administration of bisoprolol MAO inhibitors and should be at least 14 days.
Possibly slight decrease in half-life of bisoprolol because rifampicin induction of hepatic isoenzymes of cytochrome P450. Typically, a dose adjustment is required.
ergotamine derivatives
Non-hydrogenated ergot alkaloids increase the risk of peripheral circulatory disorders. Ergotamine increases the risk of peripheral circulatory disorders.
Sulfasalazine increases the concentration of bisoprolol in blood plasma.
Arrhythmias, ventricular premature beats, AV block, bradycardia, marked reduction of blood pressure, worsening the flow of CHF (rise of edema, slowing of the heart rate or bradycardia, decrease blood pressure), shortness of breath, bronchoconstriction, acute heart failure, hypoglycemia, cyanosis nails of fingers or hands, dizziness, fainting, seizures.
Sensitivity to single high dose bisoprolol reception varies greatly among individual patients and probably patients with CHF have a high sensitivity.
In the event of an overdose, it is first necessary to stop taking the drug, to gastric lavage, appoint adsorbing drugs and start supporting symptomatically.
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.
In marked decrease in blood pressure: intravenous plasma-substituting solutions and vazopressivnyh preparations.
When AV blockade: patients should be under constant supervision and receive treatment of beta-agonists such as epinephrine. If necessary – setting an artificial pacemaker.
During exacerbation flow CHF: intravenous diuretics, drugs with a positive inotropic effect, and vasodilators.
When bronchospasm: the appointment of bronchodilators including beta2-agonists and / or aminophylline.
When hypoglycemia: intravenous glucagon or intravenous administration of dextrose (glucose).
Hemodialysis is ineffective.
pharmachologic effect
Pharmacological group:
Beta1-selective blocker.
Bisoprolol – selective beta1-blocker without its own sympathomimetic activity, has no membrane stabilizing action. Reduces plasma renin activity, reduces myocardial oxygen demand, reduce heart rate (HR) (at rest and during exercise). It has antihypertensive, antiarrhythmic and antianginal effects. Blocking in low doses beta1-adrenergic receptors of the heart, reduce stimulated formation of cyclic denozinmonofosfata catecholamine (cAMP) from adenosine triphosphate reduces intracellular calcium ion current has a negative chronotropic, dromo-, BATM and inotropic action (inhibits conduction and excitability slows atrioventricular (AV ) conductivity).
With increasing doses of the above therapeutic exerts beta2-adrenoceptor blocking effect.
Total peripheral vascular resistance at the beginning of the application of the preparation (within 24 hours) somewhat increases (as a result of reciprocal increase in the activity of alpha-adrenoreceptors) after 1-3 days returns to the initial and long-term use – is reduced.
The antihypertensive effect is associated with a decrease in cardiac output, sympathetic stimulation of peripheral blood vessels, reduction in the activity of the sympathoadrenal system (important for patients with initial hypersecretion renin) sensitivity reduction in response to the lowering of blood pressure (BP) and the influence on the central nervous system (CNS) . When hypertension effect occurs within 2-5 days, stable operation – in 1-2 months.
Antianginal effect due to a decrease in myocardial oxygen demand as a result of shortening of heart rate, a slight reduction in contractility, lengthening of diastole, improving myocardial perfusion.
Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased sympathetic nervous system activity, increased cAMP levels, 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 AV node) and additional routes.
When applied in high therapeutic doses, unlike nonselective beta-blockers, 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, does not cause delays of sodium ions in the body.
The maximum effect of the drug is achieved within 3-4 hours after ingestion. Even when assigning bisoprolol once daily its therapeutic effect lasts for 24 hours, due to the 10-12 hour half-life (T1 / 2) from the blood plasma. Generally, the maximum blood pressure reduction achieved within 2 weeks after starting treatment.
Bisoprolol almost completely (over 90%) is absorbed from the gastrointestinal tract. Its bioavailability is due to low metabolization at “primary” through the liver (at about 10%) is approximately 90% after oral administration. Food intake does not affect absorption. Bisoprolol demonstrates linear kinetics, and its plasma concentration is proportional to the dose in the range of 5 to 20 mg. The maximum plasma concentration is achieved in 2-3 hours.
Bisoprolol is distributed widely enough. The volume of distribution of 3.5 l / kg. Communication with the plasma protein reaches about 35%; capture blood cells was observed. The permeability of the blood-brain barrier and the placental barrier – is low.
Metabolized by oxidative way without subsequent conjugation. All metabolites have a strong polarity and excreted by the kidneys. The main metabolites found in blood plasma and urine, does not exhibit pharmacological activity. Data obtained from experiments with microsomes in vitro human liver show that bisoprolol is metabolized primarily via CYP3A4 isoenzyme (about 95%), a CYP2D6 isozyme plays only a small role.
Clearance bisoprolol determined by the equilibrium between its excretion via the kidneys in the form of unchanged substance (about 50%) and in the liver by oxidation (about 50%) to metabolites that then also the kidneys. Total clearance was 15.6 ± 3.2 l / h, and the renal clearance is 9.6 ± 1.6 L / h. T1 / 2 of 10-12 hours.
Pharmacokinetics in special patient groups
Patients with impaired liver function and kidney
Since excretion takes place in the kidneys and liver alike, patients with impaired liver function or renal insufficiency dose adjustment is required.
Elderly patients
The pharmacokinetics of bisoprolol is linear and independent of age.
Patients with chronic heart failure (CHF)
In patients with chronic heart failure bisoprolol plasma level above, and T1 / 2 is increased to 17 hours compared with healthy volunteers.
There is no information on the pharmacokinetics of bisoprolol in patients with chronic heart failure and simultaneous impaired liver or kidney function.
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.
During pregnancy, bisoprolol should be encouraged only if the benefit to the mother outweighs the risk of side effects in the fetus.
Typically, beta-blockers reduce blood flow to the placenta and affect fetal development. It is necessary to closely monitor the blood flow in the placenta and uterus, as well as to monitor the growth and development of the child, and, in case of occurrence of adverse events in relation to pregnancy and / or fetus, taking alternative therapies.
It is necessary to carefully examine the newborn after delivery. In the first three days of life may have symptoms of hypoglycemia and bradycardia.
the allocation of data bisoprolol passes into breast milk is not. Therefore, the drug bisoprolol is not recommended for women during lactation.
If necessary, use during lactation, breast-feeding should be discontinued.
Conditions of supply of pharmacies
side effects
Class ifikatsiya frequency of side effects according to the recommendations of the World Health Organization (WHO): very common> 1/10; often by> 1/100 to 1/1000 to 1/10000 to
Disorders of the nervous system: often – dizziness *, headache *, asthenia (patients with chronic heart failure), fatigue, sleep disturbances, depression, anxiety; infrequently – asthenia (patients with hypertension or angina), drowsiness or insomnia, depression; rarely – hallucinations, “nightmarish” dream, confusion, or short-term memory loss, myasthenia gravis, tremor, muscle cramps. Usually, these effects are mild and are usually within 1-2 weeks after starting treatment.
Violations by the organ of vision: rarely – visual disturbances, reduced secretion of lacrimal fluid; very rare – dryness and soreness of the eyes, conjunctivitis.
Violations by the organ of hearing and labyrinth: rarely – ringing in the ears, hearing loss, ear pain.
Violations of the heart: often – bradycardia; often – the aggravation of heart failure symptoms (in patients with heart failure); infrequently – a violation of AV conduction, decompensation of heart failure; rarely – syndrome “cancel” (increasing angina attacks, increased blood pressure).
Violations by vessels: often – marked reduction of blood pressure (especially in patients with CHF), a manifestation of vasospasm (strengthening of peripheral blood circulation, cooling of the lower extremities, paresthesia); rarely – orthostatic hypotension, peripheral edema.
Gastrointestinal: often – nausea, vomiting, diarrhea, constipation, dryness of the oral mucosa, stomach pain; very rare – changing taste.
Нарушения со стороны печени и желчевыводящих путей: редко – гепатит.
Нарушения со стороны дыхательной системы, органов грудной клетки и средостения: нечасто – бронхоспазм у пациентов с бронхиальной астмой или обструкцией дыхательных путей в анамнезе, боль в груди; редко – заложенность носа.
Нарушения со стороны иммунной системы: редко – кожный зуд, кожная сыпь, крапивница, аллергический ринит.
Нарушения со стороны кожи и подкожных тканей: редко – реакции повышенной чувствительности, такие как кожный зуд, сыпь, гиперемия кожи, усиление потоотделения, экзантема, псориазоподобные кожные реакции; очень редко – обострение симптомов псориаза, алопеция.
Нарушения со стороны мышечной, скелетной и соединительной ткани: нечасто – артралгия, боль в спине.
Лабораторные и инструментальные данные: редко – повышение активности «печеночных» трансаминаз (аланинаминотрансферазы, аспартатаминотрансферазы), повышение концентрации билирубина, гипер- триглицеридемия; в отдельных случаях – тромбоцитопения, лейкопения, агранулоцитоз.
Нарушения со стороны репродуктивной системы и молочных желез: редко – нарушение потенции, ослабление либидо. * У пациентов с артериальной гипертензией или стенокардией особенно часто данные симптомы появляются в начале курса лечения. Обычно эти симптомы носят легкий характер и проходят, как правило, в течение 1-2 недель после начала лечения.
special instructions
Не прерывайте лечение препаратом Бисопролол резко и не меняйте рекомендованную дозу без предварительной консультации с врачом, так как это может привести к временному ухудшению деятельности сердца. Лечение не следует прерывать внезапно, особенно у пациентов с ИБС. Если прекращение лечения необходимо, то дозу следует снижать постепенно.
На начальных этапах лечения препаратом Бисопролол пациенты нуждаются в постоянном наблюдении.
Препарат следует применять с осторожностью в следующих случаях: -тяжелые формы ХОБЛ и нетяжелые формы бронхиальной астмы; -сахарный диабет со значительными колебаниями концентрации глюкозы в крови: симптомы выраженного снижения концентрации глюкозы (гипогликемии), такие как тахикардия, сердцебиение или повышенная потливость, могут маскироваться; -строгая диета; – проведение десенсибилизирующей терапии; – AV блокада I степени; – Prinzmetal angina; – нарушение периферического артериального кровообращения легкой и умеренной степени (в начале терапии может возникнуть усиление симптомов); – псориаз (в том числе в анамнезе).
Дыхательная система: при бронхиальной астме или ХОБЛ показано одновременное применение бронходилатирующих средств. У пациентов с бронхиальной астмой возможно повышение резистентности дыхательных путей, что потребует более высокой дозы бета2-адреномиметиков. Пациентам с ХОБЛ бисопролол, назначаемый в комплексной терапии с целью лечения сердечной недостаточности, следует назначать, начиная с наименьшей возможной дозы, и у пациентов тщательно наблюдать за появлением новых симптомов (например, одышки, непереносимости физических нагрузок, кашля).
Аллергические реакции: бета-адреноблокаторы, включая препарат Бисопролол, могут повышать чувствительность к аллергенам и тяжесть анафилактических реакций из-за ослабления адренергической компенсаторной регуляции под действием бета-адреноблокаторов. Терапия эпинефрином (адреналином) не всегда дает ожидаемый терапевтический эффект.
Общая анестезия: при проведении общей анестезии следует учитывать риск возникновения блокады бета-адренорецепторов. Если необходимо прекратить терапию препаратом Бисопролол перед хирургическим вмешательством, это следует делать постепенно и завершать за 48 часов до проведения общей анестезии. Следует предупредить врача-анестезиолога о том, что Вы принимаете препарат Бисопролол.
Феохромоцитома: у пациентов с опухолью надпочечников (феохромоцитомой) препарат Бисопролол может быть назначен только на фоне применения альфа-адреноблокаторов.
Гипертиреоз: при лечении препаратом Бисопролол симптомы гиперфункции (гипертиреоза) щитовидной железы могут маскироваться.
Effects on ability to drive vehicles and mechanisms
Препарат Бисопролол не влияет на способность управлять транспортными средствами согласно результатам исследования пациентов с ИБС. Однако вследствие индивидуальных реакций способность управлять автотранспортом или работать с технически сложными механизмами может быть нарушена. На это следует обратить особое внимание в начале лечения, после изменения дозы, а также при одновременном употреблении алкоголя.
Storage conditions
Store in a dark place at a temperature not higher than 25 C.
Keep out of the reach of children.
Dosing and Administration
Внутрь, утром, не разжевывая, один раз в сутки с небольшим количеством жидкости, независимо от приема пищи. Tablets should not be chewed or triturate.
Дозу препарата во всех случаях подбирает врач каждому пациенту индивидуально с учетом состояния пациента, эффективности лечения и ЧСС.
Лечение артериальной гипертензии и ИБС (профилактика приступов стабильной стенокардии)
Рекомендуется начать прием с 1 таблетки 5 мг один раз в сутки. В некоторых случаях начальная доза может составлять 2,5 мг один раз в сутки. При необходимости дозу увеличивают до 10 мг один раз в сутки. Максимальная суточная доза – 20 мг.
Лечение ХСН
Стандартная схема лечения ХСН включает применение ингибиторов ангиотензинпревращающего фермента (АПФ) или агонистов рецепторов ангиотензина II (в случае непереносимости ингибиторов АПФ), бета-адреноблокаторов, диуретиков и, факультативно, сердечных гликозидов. Start treating heart failure drug bisoprolol requires a mandatory holding a special titration phase and regular medical supervision.
Предварительным условием для лечения препаратом Бисопролол является стабильная ХСН без признаков обострения.
CHF drug bisoprolol treatment starts in accordance with the following scheme titration. При этом может потребоваться индивидуальная адаптация в зависимости от того, насколько хорошо пациент переносит назначенную дозу, то есть дозу можно увеличивать только в том случае, если предыдущая схема хорошо переносилась.
Для обеспечения нижеприведенного режима дозирования препарата при ХСН возможно применение бисопролола других производителей в лекарственной форме таблетки по 2,5 мг с риской (для получения дозировок 1,25 мг и 3,75 мг).
Рекомендуемая начальная доза составляет 1,25 мг один раз в сутки. В зависимости от индивидуальной переносимости дозу следует постепенно повышать до 2,5 мг, 3,75 мг, 5 мг, 7,5 мг и 10 мг один раз в сутки. Каждое последующее увеличение дозы должно осуществляться не менее, чем через две недели.
If an increase in the dose of the drug is poorly tolerated by the patient, may reduce the dose.
Максимальная рекомендованная доза при ХСН составляет 10 мг препарата Бисопролол один раз в сутки.
Во время титрования дозы рекомендуется регулярный контроль АД, ЧСС и степени выраженности симптомов ХСН. Worsening symptoms of heart failure may flow from the first day of the drug.
If the patient does not tolerate the maximum recommended dose may gradually decrease the dose.
Во время титрования или после него могут возникнуть временное ухудшение течения ХСН, артериальная гипотензия или брадикардия. In this case it is recommended first of all to carry out correction of drug doses of concomitant therapy. You may also need a temporary reduction in the dose of bisoprolol or its cancellation.
After stabilization of the patient should be a re-titration of the dosage or further treatment.
duration of treatment
Лечение препаратом Бисопролол обычно является долговременным. Продолжительность терапии определяет врач.
Пациенты с нарушением функции почек или печени
При нарушениях функции печени или почек легкой или умеренной степени обычно не требуется корректировать дозу.
У пациентов с тяжелыми нарушениями функции почек (КК менее 20 мл/мин) или с тяжелыми нарушениями функции печени максимальная суточная доза составляет 10 мг.
Увеличение дозы у таких пациентов должно осуществляться с особой осторожностью.
elderly patients
No dose adjustment in elderly patients is not required.
Прочие категории пациентов
К настоящему времени недостаточно данных относительно применения препарата Бисопролол у пациентов с ХСН, сопряженной с сахарным диабетом 1 типа, тяжелыми нарушениями функции почек и/или печени, рестриктивной кардиомиопатией, врожденными пороками сердца или пороком сердца с выраженными гемодинамическими нарушениями. Также до сих пор не было получено достаточных данных относительно пациентов с ХСН с инфарктом миокарда в течение последних трех месяцев.
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


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