Bisoprolol-Prana - instructions for use, doses, side effects, contraindications

Tablets with a dosage of 5 mg - light yellow color, tablets with a dosage of 10 mg - light orange color. On the cross-section, two layers are visible, the inner layer is white or almost white.

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B Selective beta-blockers

C.07.A.B.07 Bisoprolol

Pharmacodynamics:

Selective β₁- adrenoblocker, without its own sympathomimetic activity, does not possess membrane-stabilizing action. Reduces the activity of renin plasma, reduces the need for myocardium in oxygen, reduces the heart rate (heart rate) (at rest and with exercise).Has antihypertensive, antiarrhythmic and antianginal action. Blocking in low doses β₁-adrenoceptors of the heart, reduces catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular current of calcium ions (Ca²⁺), has a negative chrono-, dromo-, batmo- and inotropic effect, reduces atrioventricular conductivity and excitability.

If the therapeutic dose is exceeded, β₂-adrenoblocking action.

The total peripheral vascular resistance at the beginning of the drug application, in the first 24 hours, increases (as a result of the reciprocal increase in the activity of a-adrenergic receptors and elimination of stimulation of β₂adrenoreceptors), returns to the initial one after 1-3 days, and decreases with prolonged use.

The hypotensive effect is associated with a decrease in the minute volume of blood, sympathetic stimulation of peripheral vessels, restoration of sensitivity in response to lowering blood pressure (BP) and affecting the central nervous system (CNS). With arterial hypertension, the effect occurs after 2-5 days, a stable effect is observed after 1-2 months.

The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in the heart rate (heart rate) and a decrease in myocardial contractility, diastole lengthening, and improved myocardial perfusion. By increasing the end-diastolic pressure in the left ventricle and increased tensile ventricular muscle fibers may be increased oxygen demand, especially in patients with chronic heart failure (CHF).

When used at average therapeutic doses, in contrast to non-selective β-blockers, it exerts a less pronounced effect on organs containing β₂-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and carbohydrate metabolism; does not cause retention of sodium ions (Na⁺) in organism; the severity of atherogenic action does not differ from that of propranolol.

Pharmacokinetics:

Absorption - 80-90%, food intake does not affect absorption. The maximum concentration in blood plasma is observed after 1-3 h, the connection with plasma proteins is about 30%. Permeability through the blood-brain barrier and the placental barrier is low.

50% of the dose is metabolized in the liver with the formation of inactive metabolites, half-life (T_1/2) 10-12 hours. About 98% is excreted by the kidneys, of which 50% is excreted unchanged; less than 2% - through the intestines with bile.

Indications:

- Ahyperthermia;

- ischemic heart disease: prevention of angina attacks voltage.

Contraindications:

Hypersensitivity to the drug components and other β-blockers, shock (including cardiogenic), collapse, pulmonary edema, acute heart failure, chronic heart failure in decompensation, atrioventricular (AV) blockade II-III degree, sinoatrial block, sinus node weakness syndrome, pronounced bradycardia, prinzmetal angina, cardiomegaly (no signs of heart failure), arterial hypotension (systolic blood pressure less than 100 mmHg, especially with myocardial infarction); severe forms of bronchial asthma and chronic obstructive pulmonary disease (COPD) in history; simultaneous administration of monoamine oxidase inhibitors (MAO) (with the exception of MAO-B), late stages of peripheral circulation disorders, Raynaud's disease, pheochromocytoma (without simultaneous use αadrenoblockers), metabolic acidosis, age under 18 years (efficacy and safety not established).

Carefully:

Hepatic failure, chronic renal failure insufficiency, myasthenia gravis, thyrotoxicosis, diabetes mellitus, AV blockade of the I degree, depression (including in the anamnesis), psoriasis, allergic reactions (in the anamnesis), elderly age.

Pregnancy and lactation:

Use during pregnancy is possible if the benefit to the mother exceeds the risk of side effects in the fetus and the baby.

There is no data on the isolation of bisoprolol in breast milk. Therefore, if you need to use the drug BISOPROLOL-PRANA during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Inside, in the morning on an empty stomach, without chewing, once.

Arterial hypertension and ischemic heart disease: prevention of angina attacks

It is recommended to take 5 mg once. If necessary, increase the dose to 10 mg once a day. The maximum daily dose is 20 mg.

In all cases, the regimen and dosage are chosen by the doctor for each patient individually, in particular, taking into account the values of heart rate and the therapeutic response.

In patients with impaired renal function with creatinine clearance (CC) less than 20 ml / min, or with severe impairment of liver function, the maximum daily dose is 10 mg.

Dose adjustments in elderly patients are not required.

Side effects:

From the central and peripheral nervous system: increased fatigue, weakness, dizziness, headache, sleep disorders, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenia, myasthenia gravis, paresthesia in the extremities (in patients with intermittent claudication and Raynaud's syndrome), tremors, convulsions (including gastrocnemius muscles).

From the side of the organ of vision: impaired vision, decreased secretion of tear fluid, dryness and soreness of the eyes, conjunctivitis.

From the side of the cardiovascular system: sinus bradycardia, heart beat, conduction disturbances of the myocardium, AV blockade (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakening of myocardial contractility, development (aggravation) of CHF (swelling of the ankles, stop, dyspnea), lowering of blood pressure, orthostatic hypotension, manifestation of angiospasm peripheral circulatory disorders, cooling of the lower extremities, Raynaud's syndrome), chest pain.

From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, impaired liver function (dark urine, icteric sclera or skin, cholestasis), changes in taste.

From the respiratory system: nasal congestion, difficulty breathing when given in high doses (loss of selectivity) and / or in predisposed patients - laryngo- and bronchospasm.

From the endocrine system: hyperglycemia (in patients with insulin-dependent diabetes), hypoglycemia (in patients receiving insulin), hypothyroidism.

Allergic reactions: itching, rash, hives.

From the skin: increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions, exacerbation of psoriasis symptoms, alopecia.

Laboratory indicators: thrombocytopenia (unusual hemorrhages and hemorrhages), agranulocytosis, leukopenia, changes in the activity of liver enzymes (increased alanine aminotransferase (ALT), aspartate aminotransferase (ACT), the level of bilirubin, triglycerides.

Influence on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

Other: pain in the back, arthralgia, weakening of libido, decreased potency, withdrawal syndrome (increased angina attacks, increased blood pressure).

Overdose:

Symptoms: arrhythmia, ventricular extrasystole, pronounced bradycardia, AV blockade, marked decrease in blood pressure, chronic heart failure, cyanosis of finger nails or palms, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.

Treatment: gastric lavage and the appointment of absorbents; symptomatic therapy:

with developed AV blockade - intravenous injection of 1-2 mg of atropine, epinephrine or temporary setting of a pacemaker;

with ventricular extrasystole - lidocaine (preparations of the IA class do not apply);

with a decrease in blood pressure - the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema - intravenous injection of plasma-substituting solutions, with inefficiency - the introduction of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and eliminate the pronounced decrease in blood pressure);

with heart failure - cardiac glycosides, diuretics, glucagon;

with convulsions - intravenously diazepam;

at bronchospasm - β₂-adrenostimulators inhalation.

Interaction:

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 agents for intravenous administration increase the risk of developing anaphylactic reactions.

Phenytoin with intravenous administration, means for inhalation anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.

Changes the efficiency insulin and hypoglycemic agents for oral administration, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

Reduces ground clearance lidocaine and xanthine (except theophylline) and increases their concentration in blood plasma, especially in patients with initially elevated clearance theophylline under the influence of smoking.

The hypotensive effect weakens nonsteroidal anti-inflammatory drugs (NSAIDs) (sodium ion retention (Na⁺) and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids and estrogens (ion retardation Na⁺).

Cardiac glycosides, methyldopa, reserpine and guanfacine, blockers of "slow" calcium channels (verapamil, diltiazem), amiodarone and other antiarrhythmics increase the risk of developing or worsening bradycardia, AV blockade, cardiac arrest and heart failure. Nifedipine can lead to a significant decrease in blood pressure.

Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs may lead to an excessive decrease in blood pressure.

Lengthens the action Nondepolarizing muscle relaxants and increases the anticoagulant effect coumarins.

Tri- and tetracyclic antidepressants, antipsychotics (antipsychotics), antipsychotics ethanol, sedatives and hypnotics increase the CNS depression.

Do not use concurrently from MAO inhibitors due to a significant increase in antihypertensive effect, a break in treatment between the intake of MAO inhibitors and bisoprolol should be at least 14 days.

Unhydrated alkaloids of ergot increase the risk of peripheral circulatory disorders.

Ergotamine increases the risk of peripheral circulatory disorders; sulfasalazine increases the concentration of bisoprolol in the blood plasma; rifampicin reduces T_1/2.

Special instructions:

Control of patients taking BISOPROLOL-PRANA should include a measurement of heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 months), ECG, blood glucose in patients with diabetes mellitus (1 time in 4 -5 months). In elderly patients it is recommended to follow the function of the kidneys (once every 4-5 months).

It is necessary to teach the patient how to calculate heart rate and instruct about the need for medical consultation at a heart rate of less than 50 beats per minute.

Before the start of treatment, it is recommended to perform an external respiration function in patients with a history of bronchopulmonary anamnesis. Approximately 20% patients with angina pectoris-adrenoblockers are ineffective. The main causes are: marked coronary atherosclerosis with low ischemia threshold (heart rate less than 100 beats per minute) and an increased end-diastolic volume of the left ventricle, which breaks the subendocardial blood flow.

Smokers have efficacy β-adrenoconcretors below.

Patients who use contact lenses should take into account that, on the background of treatment, tear fluid production can be reduced.

When used in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (unless an effective α-adrenoblockade has been previously achieved).

With thyrotoxicosis bisoprolol can mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can strengthen symptoms.

In diabetes mellitus can mask tachycardia caused by hypoglycemia. In contrast to non-selective β-blockers, there is almost no increase in insulin-induced hypoglycemia and does not delay the restoration of the glucose concentration in the blood to normal levels.

With the simultaneous administration of clonidine, his reception may be discontinued only a few days after the withdrawal of the drug BISOPROLOL-PRANA.

It is possible to increase the severity of the reaction of hypersensitivity and the lack of effect from the usual doses of epinephrine against the background of a burdened allergological anamnesis.

If it is necessary to conduct routine surgical treatment, the drug can be withdrawn 48 hours before the start of the general anesthesia. If the patient has taken the drug before surgery, he should choose a drug for general anesthesia with a minimum negative inotropic effect.

Reciprocal activation of the vagus nerve can be eliminated by intravenous administration of atropine (1-2 mg).

Drugs that reduce catecholamine stocks (including reserpine), can enhance the action of β-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect a marked decrease in blood pressure or bradycardia.

Patients with bronchospastic diseases can be prescribed cardioselective β-blockers in case of intolerance and / or inefficiency of other antihypertensive agents. Overdosing is dangerous by the development of bronchospasm.

In the case of an increase in bradycardia (less than 50 beats per minute) in elderly patients, a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg) AV blockade, it is necessary to reduce the dose or stop treatment.

It is recommended to stop therapy with the development of depression.

You can not abruptly interrupt treatment because of the danger of developing the syndrome of "withdrawal" (severe arrhythmias and myocardial infarction). Abolition is carried out gradually, reducing the dose for 2 weeks or more (reduce the dose by 25% in 3-4 days).

It should be canceled before the study of the content in the blood and urine of catecholamines, normetanephrine and vanillin-mandelic acid, titers of antinuclear antibodies.

Effect on the ability to drive transp. cf. and fur:

The question of the possibility of practicing potentially dangerous activities requiring increased attention and speed of psychomotor reactions should be addressed only after assessing the patient's individual response to the drug (especially at the beginning of treatment, due to the possibility of developing dizziness).

Form release / dosage:Tablets, film-coated, 5 and 10 mg.

Packaging:

10 tablets per contour cell pack.

50, 60, 70, 80, 90, 100 tablets in a polymer bank.

Each bank or 1, 2, 3, 4 contour mesh packages together with instructions for use are placed in a pack of cardboard.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006031/10

Date of registration:28.06.2010

Expiration Date:Unlimited

The owner of the registration certificate:PRANAFARM, LLC PRANAFARM, LLC Russia

Manufacturer: & nbsp

PRANAFARM, LLC Russia

Information update date: & nbsp14.02.2017

Illustrated instructions

Instructions

Bisoprolol-Prana (Bisoprolol-Prana)