Bisoprolol-Borimed
Producer: JSC Borisovsky Plant of Medical Supplies Republic of Belarus
Code of automatic telephone exchange: C07AB07
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active ingredient: 2,5 mg, 5 mg or 10 mg of a bisoprolol of a fumarat in 1 tablet.
Excipients: cellulose microcrystallic, dihydrophosphate calcium the dihydrate, starch corn, silicon dioxide colloid anhydrous, magnesium stearate, sodium krakhmalglikolit (type A), опадрай II (including alcohol polivinilovovy, partially hydrolyzed, talc, the macrogoal 3350 painting a pigment of white color (contains titanium E 171 dioxide)).
Pharmacological properties:
Pharmacodynamics. The selection β1-адреноблокатор. Reduces the need of a myocardium for oxygen, reduces heart rate (at rest and at loading). Has hypotensive, antiarrhytmic and anti-anginal effect. Conductivity and excitability of a myocardium oppresses, reduces atrioventricular conductivity.
At arterial hypertension the effect occurs in 2-5 days, stable action – in 1-2 months.
Pharmacokinetics. Absorption and distribution. Absorption – 80-90%, meal does not influence absorption. Cmax in a blood plasma is observed in 1-3 h.
Communication with proteins of a blood plasma – about 30%. Passes through GEB and a placental barrier in insignificant degree, in insignificant quantities it is allocated with breast milk.
Metabolism and removal. 50% of a dose are metabolized in a liver with formation of inactive metabolites. T½ is 10-12 h. About 98% are removed with urine - 50% in an invariable look, less than 2% - with bile.
Indications to use:
For a dosage of 2,5 mg. Treatment of the compensated chronic heart failure with disturbance of systolic function of a left ventricle, in addition to therapy by inhibitors of an angiotensin-converting enzyme (APF), diuretics, and also to cardiac glycosides.
For dosages of 5 and 10 mg. Arterial hypertension, coronary heart disease (stenocardia).
Route of administration and doses:
Arterial hypertension, coronary heart disease (stenocardia). The recommended dose makes 5 mg (1 tablet of Bisoprolol of 5 mg) a day. If necessary it is possible to increase a daily dose to 10 mg (1 tablet of Bisoprolol of 10 mg) a day. Increase in a dose is allowed only in some cases. The maximum daily dose – 20 mg.
The compensated chronic heart failure with disturbance of systolic function of a left ventricle. The condition of patients has to be stable in an initiation of treatment bisoprololy (the acute heart failure is eliminated). In time and after titration of a dose there can be a temporary deterioration in heart failure, hypotension or bradycardia. Tablets of a bisoprolol should be swallowed entirely with liquid in the first half of day regardless of meal
Titration. Treatment bisoprololy has to be begun with gradual increase in a dose as follows:
1st week of 1,25 mg once a day. At good tolerance the 2nd week of 2,5 mg once a day. At good tolerance the 3rd week of 3,75 mg once a day. At good tolerance within 4-7 weeks the dose is increased to 5 mg once a day. At good tolerance the dose is increased to 7,5 mg within the next 4 weeks once a day. At good tolerance the dose is increased to 10 mg as a maintenance dose constantly once a day.
During a phase of a titration careful monitoring of pulse, arterial pressure and signs of deterioration in cordial therapy is necessary.
Dose adjustment. If the maximum recommended dose badly is transferred, the gradual dose decline has to be carried out.
At temporary deterioration in heart failure, hypotension or bradycardia it is possible to consider temporary reduction or the termination of treatment bisoprolololy. At stabilization a condition of the patient in each case the titration of a dose of a bisoprololol is necessary for resuming of treatment.
Treatment termination. The dose should be reduced gradually as sharp cancellation can lead to a sharp exacerbation of a disease. The dose should be lowered gradually (by 25% a week).
Patients with a renal failure or a liver. For patients with arterial hypertension or coronary heart disease and disturbance of functions of a liver or kidneys easy and moderate severity selection of a dose usually does not need to be done. For patients with a severe form of a renal failure (clearance of creatinine less than 20 ml/min.) and patients with a severe form of a liver failure the daily dose should not exceed 10 mg of a bisoprolol.
Patients of advanced age. Dose adjustment of drug is not required.
Features of use:
Use during pregnancy and feeding by a breast. Pregnancy. Bisoprolol has pharmacological effect which exerts adverse impact on the course of pregnancy and fetation (newborn). In general, beta adrenoblockers reduce a placental blood stream, increases risk of a growth inhibition of an embryo, pre-natal death of a fruit, premature abortion and premature births. Undesirable effects (for example a hypoglycemia and bradycardia) can be observed both at embryos, and at newborns. Bisoprolol is not recommended to apply pregnancies in time. The exception is made by cases when the advantage for mother exceeds potential risk for a fruit. It is recommended to carry out monitoring of an uteroplacental blood-groove and pre-natal growth of a fruit. At an adverse effect of a bisoprolol on the course of pregnancy and (or) fetation it is necessary to consider the possibility of purpose of alternative therapy. Besides, it is necessary to control a condition of newborns carefully. The hypoglycemia and bradycardia, as a rule, are registered during the first 3 days of a puerperal period.
Feeding by a breast. There is no information on ability of a bisoprolol to get into breast milk, and also data on safety of a bisoprolol for the babies who are on breastfeeding. In this regard breastfeeding is not recommended to be carried out against the background of therapy bisoprololy.
Children. There is no experience of use of a bisoprolol for children therefore drug cannot be recommended for treatment of children.
Features of use. Treatment bisoprololy the compensated chronic heart failure is begun with titration of a dose.
In the absence of absolute indications therapy bisoprololy should not be stopped sharply, it can lead to passing deterioration in cardiac performance. Especially it concerns patients with coronary heart disease.
The initiation of treatment bisoprololy the compensated chronic heart failure demands continuous monitoring.
There is no experience of therapeutic use of a bisoprolol by patients with heart failure with such diseases and states:
- Insulin-dependent diabetes mellitus (I type);
- Heavy renal failures;
- Heavy abnormal liver functions;
- Hemodynamically significant organic lesion of valves of heart;
- The myocardial infarction which developed within the last three months.
Bisoprolol it is necessary to apply with care at:
- A diabetes mellitus with the expressed fluctuations of level of glucose in blood; effects of a bisoprolol (for example tachycardia, heartbeat or plentiful sweating) can mask hypoglycemia symptoms;
- Strict starvation;
- The specific hyposensibilizing therapy. Like other beta adrenoblockers, бисопролол it is capable to increase sensitivity of an organism to allergens and to strengthen anaphylactic reactions. Therapy by adrenaline not always provides desirable therapeutic effect;
- To an atrioventricular block of the I degree;
- Occlusal defeat of peripheral arterial vessels. Strengthening of clinical manifestations can be observed (more often - at the beginning of therapy bisoprololy).
Patients with psoriasis and patients with anamnestic data in favor of psoriasis have to receive beta-blockers (including бисопролол) only after careful assessment of a ratio advantage / risk.
Therapy bisoprololy can mask thyrotoxicosis symptoms.
At treatment of patients with a pheochromocytoma therapy bisoprololy should not be begun before use of alpha adrenoblockers.
Blockade of beta adrenoceptors reduces probability of development of disturbances of a heart rhythm and ischemia of a myocardium during induction of anesthesia and an intubation of a trachea, and also in the postoperative period. Today it is recommended to continue a maintenance therapy by beta adrenoblockers in the preoperative period. The anesthesiologist has to know that the patient receives beta adrenoblockers as interaction of beta adrenoblockers with other medicines can lead to development of bradyarrhythmias, oppression of reflex tachycardia and suppression of reflex ability to compensate blood loss. If it is considered that therapy by beta adrenoblockers needs to be stopped in the preoperative period, then cancellation should be carried out gradually and to complete approximately in 48 hours prior to anesthesia.
The accompanying therapy is recommended to patients of a bronchial astmoya with other chronic obstructive pathology of lungs which can be followed by clinical manifestations by bronchial spasmolytics. Sometimes at patients with bronchial asthma resistance of respiratory tracts increases. In such cases there can be a need for increase in a dose of beta2-adrenomimetik.
Lactose. Lactose is a part of this medicine. This drug should not be accepted to patients with rare hereditary intolerance of a galactose, deficit of lactase or a sprue of glucose galactose.
Ability to influence speed of response at control of motor transport or other mechanisms. In individual cases in an initiation of treatment and when replacing drug, and also at interaction with alcohol ability to drive the car or to work with mechanisms can be reduced.
Side effects:
Side effects are classified by emergence frequency: very often (> 1/10), it is frequent (> 1/100, <1/10), sometimes (> 1/1000 and <1/100), is rare (> 1/10000i <1/1000), is very rare (<1/10000).
From a nervous system. Often: dizziness, a headache (especially in an initiation of treatment, usually poorly also pass within 1-2 weeks). Sometimes: sleep disorders, depressions. Seldom hallucinations, paresthesias.
From organs of sight. Seldom: disturbance of a slezootdeleniye (to consider a gift of contact lenses). Very seldom: conjunctivitis.
From acoustic organs. Seldom: disorders of hearing.
From cardiovascular system. Very often: bradycardia (at patients with heart failure). Often: a cryesthesia or immovabilities of extremities, signs of deterioration in heart failure in an initiation of treatment (at patients with chronic heart failure). Sometimes: disturbances of atrioventricular conductivity (at patients with arterial hypertension and coronary heart disease), orthostatic hypotension.
From respiratory system. Sometimes: a bronchospasm at patients with bronchial asthma in the anamnesis and chronic obstructive respiratory diseases. Seldom: allergic rhinitis.
From digestive tract. Often: nausea, vomiting, diarrhea, lock.
From a liver. Seldom: metabolism disturbance (increase in level of triglycerides in blood), increase in activity of liver enzymes in a blood plasma (ACT, ALT), hepatitis.
From skin and a musculoskeletal system. Sometimes: muscular weakness, spasms. Seldom: hypersensitivity reactions (an itch, the increased perspiration, rashes). Very seldom: the hair loss, at treatment by blockers of beta receptors can be observed an aggravation of symptoms of patients with psoriasis in the form of psoriasis rash.
From urinogenital system. Seldom: disturbance of a potentiality.
General frustration. Often: an adynamy (at patients with chronic heart failure), fatigue (especially in an initiation of treatment, it is usually poorly expressed and passes within 1-2 weeks). Sometimes: an adynamy (at patients with arterial hypertension and coronary heart disease).
Interaction with other medicines:
Not recommended combinations
Antiarrhytmic drugs I of a class (for example quinidine, Disopyramidum, lidocaine, Phenytoinum, флекаинид, пропафенон). Strengthening of influence on time of AV conductivity and increase in a negative inotropic effect can be observed.
Blockers of calcium channels from group of verapamil and to a lesser extent - from group of diltiazem. A negative impact on contractility and AV conductivity. Administration of verapamil to the patients receiving therapy by beta adrenoblockers can be followed by development of the expressed arterial hypotension and AV of blockade.
Anti-hypertensive central acting agents (for example clonidine, Methyldopum, моксонидин, рилменидин). Simultaneous use of anti-hypertensive drugs of the central action can lower in addition a sympathetic tone of the central nervous system and, as a result, reduce the heart rate and cordial emission, and also cause a vazodilatation. The sharp termination of therapy, especially in the conditions of preliminary cancellation of beta adrenoblockers, the riskrazvitiya of effect of a ricochet can increase (arterial hypertension).
Combinations which should be applied with care
Blockers of calcium channels of dihydropyridinic type (for example фелодипин and амлодипин). It is impossible to exclude that the combined use can increase risk of arterial hypotension and decrease in pumping function of a ventricle at patients with heart failure.
Antiarrhytmic drugs III of a class (for example Amiodaronum). Strengthening of influence on AV conductivity time can be observed.
Parasshlpatomimetiki. Simultaneous use can increase time of AV conductivity and increase risk of development of bradycardia.
The beta adrenoblockers intended for topical administration (for example eye drops for treatment of glaucoma). Potentiation of system effects of a bisoprolol is possible.
Insulin and peroral sugar the reducing drugs. Strengthening of hypoglycemic effect. Blockade of beta adrenoceptors can mask hypoglycemia symptoms.
Anesthetics. Oppression of reflex tachycardia and to increase in risk of arterial hypotension.
Foxglove drugs. Increase in time of atrioventricular conductivity, reduction of heart rate.
Non-steroidal anti-inflammatory drugs (NPVP). Can suppress hypotensive effects of a bisoprolol.
Beta sympathomimetics (for example изопреналин, Dobutaminum). The combination with bisoprololy can suppress effects of both drugs.
The sympathomimetics operating both on beta and on alpha adrenoceptors (for example noradrenaline, adrenaline). The combination with bisoprololy can strengthen an alpha adrenoceptor - mediated vasoconstrictive influence of these drugs that leads to growth of level of arterial pressure and an exacerbation of the alternating lameness. Similar interaction is more probable at use of non-selective beta adrenoblockers.
Simultaneous use of the anti-hypertensive drugs or other drugs reducing arterial pressure (for example tricyclic antidepressants, barbiturates, fenotiazin), can increase risk of development of arterial hypotension.
Contraindications:
- Hypersensitivity to a bisoprolol or to any of drug excipients;
- an acute heart failure or chronic heart failure in a condition of a decompensation when intravenous inotropic therapy is required;
- an atrioventricular block of II or III degrees (in the absence of an artificial pacemaker);
- syndrome of weakness of a sinus node;
- sinuatrial blockade;
- symptomatic bradycardia (ChSS less than 60 beats per minute);
- arterial hypotension (systolic the ABP is lower than 100 mm hg);
- severe form of bronchial asthma or chronic obstructive disease of lungs;
- severe forms of occlusal disturbance of peripheric circulation, Raynaud's disease;
- uncured pheochromocytoma;
Overdose:
Symptoms: arrhythmia, ventricular premature ventricular contraction, the expressed bradycardia, AV blockade, the expressed decrease in the ABP, chronic heart failure, cyanosis of nails of fingers or palms, breath difficulty, a bronchospasm, dizziness, unconscious states, spasms.
Treatment: gastric lavage and purpose of adsorbents; symptomatic therapy: at the developed AV to blockade - in/in introduction of 1-2 mg of atropine, Epinephrinum or statement of a temporary pacemaker; at ventricular premature ventricular contraction - lidocaine (the drugs IA of a class are not used); at decrease in the ABP - the patient has to be in the provision of Trendelenburga; if there are no fluid lungs signs - in/in plasma substituting solutions, at inefficiency - introduction of Epinephrinum, dopamine, Dobutaminum; at heart failure - cardiac glycosides, diuretics, a glucagon; at spasms - in/in diazepam; at a bronchospasm beta адреностимуляторы it is inhalation. Hypoglycemia: intravenous administration of glucose. Bisoprolol is badly brought from an organism at dialysis.
Storage conditions:
In the place protected from light and moisture at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after the termination of a period of validity.
Issue conditions:
According to the recipe
Packaging:
On 10 tablets in a blister strip packaging, in packaging No. 10×3, No. 10×5, No. 10×6.
