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

core: croscarmellose sodium (impellosis) 2.2 mg, 4.4 mg; povidone (medium molecular weight polyvinylpyrrolidone) 6.0 mg, 12.0 mg; starch pregelatinized (starch 1500) 4.0 mg, 8.0 mg; silicon dioxide colloid (aerosil) 1.54 mg, 3.08 mg; talc 2.0 mg, 4.0 mg; cellulose microcrystalline 30.4 mg, 60.8 mg; lactose (milk sugar) 47.86 mg, 95.72 mg; magnesium stearate 1.0 mg, 2.0 mg;

shell: Opadrai II (polyvinyl alcohol, partially hydrolyzed 1.2 mg, 2.4 mg, titanium dioxide 0.67998 mg, 1.35996 mg, talc 0.444 mg, 0.888 mg, macrogol (polyethylene glycol 3350) 0.606 mg, 1.212 mg, iron dye oxide (II) yellow 0.07002 mg, 0.14004 mg).

Description:

Tablets, covered with a film shell from beige-yellow to beige, round, biconvex. Tablets on a break of white or almost white color.

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B Selective beta-blockers

C.07.A.B.07 Bisoprolol

Pharmacodynamics:

Selective beta₁- 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 of beta₁-adrenoreceptors of the heart, reduces catecholamine-stimulated cAMP formation from ATP, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect, inhibits conduction and excitability, reduces atrioventricular conductivity.

When the dose is increased above the therapeutic dose, beta₂-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 alpha-adrenergic receptors and the elimination of beta stimulation₂- adrenergic receptors), which after 1-3 days returns to the original, and with a long-term administration decreases.

The hypotensive effect is associated with a decrease in the minute volume of blood, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (important for patients with initial hypersecretion of renin), 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 - after 1-2 months.

The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in heart rate and a decrease in contractility, diastole lengthening, and improvement in myocardial perfusion. By increasing the end diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles can increase the need for oxygen, especially in patients with chronic heart failure.

Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased sympathetic nervous system activity, increased cAMP levels, hypertension), decrease of the spontaneous excitation rate sinus and ectopic pacemaker and deceleration atrioventricular (AV) of carrying out (mainly in antegrade and, to a lesser extent, in retrograde directions through AV node) and on additional paths.

When used in average therapeutic doses, in contrast to non-selective beta-blockers, it exerts a less pronounced effect on organs containing beta₂-adrenoceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchial and uterine) and carbohydrate metabolism, does not cause delays 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 the blood plasma is observed after 1-3 h, the connection with blood plasma proteins about 30%. The permeability of the blood-brain barrier and the placental barrier - low secretion breast milk - low.

50% of the dose is metabolized in the liver with the formation of inactive metabolites, a half-life of 10-12 hours. About 98% is excreted by the kidneys - 50% in unchanged form, less than 2% with bile.

Indications:

- Ahyperthermia;

- ischemic heart disease: prevention of angina attacks.

Contraindications:

Increased sensitivity to the drug and other beta-blockers, shock (including cardiogenic) collapse, pulmonary edema, congestive heart failure, chronic heart failure decompensation, atrioventricular (AV) blockade II-III st., sinoatrial blockade, weakness syndrome sinus node, 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 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 of alpha-blockers), metabolic acidosis, age under 18 years (efficacy and safety not established).

Carefully:

Hepatic failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, diabetes mellitus, atrioventricular blockade of the I degree, depression (including in the history), psoriasis, advanced age.

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

Dosing and Administration:

Inside, in the morning on an empty stomach, without chewing, 5 mg once. If necessary, increase the dose to 10 mg once a day. The maximum daily dose is 20 mg / day.

In patients with impaired renal function with creatinine clearance less than 20 ml / min or with severe hepatic impairment the maximum daily dose is 10 mg.

Dose adjustment in elderly patients not required.

Side effects:

From the central 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), tremor.

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

From the cardiovascular system: sinus bradycardia, palpitation, conduction disturbance of the myocardium, AV(up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakening of myocardial contractility, development (aggravation) of chronic heart failure (swelling of the ankles, stop, dyspnea), lowering of blood pressure, orthostatic hypotension,manifestation of angiospasm (increased peripheral circulatory disturbance, coldness 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 mellitus), hypoglycemia (in patients receiving insulin), hypothyroid status.

Allergic reactions: itching, rash, hives.

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

Laboratory indicators: thrombocytopenia (unusual hemorrhages and hemorrhages), agranulocytosis, leukopenia, changes in the activity of liver enzymes (increased ALT, ACT), bilirubin level, 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 administration of absorbent drugs; symptomatic therapy: with developed AV blockade - intravenous injection of 1-2 mg of atropine, epinephrine or the setting of a temporary pacemaker; with ventricular extrasystole - lidocaine (preparations 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, - intravenously plasmo-substituting solutions, with ineffectiveness - 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; with bronchospasm - beta₂-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 drugs for intravenous administration increase the risk of anaphylactic reactions.

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

Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

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

Hypotensive effect weakens non-steroidal anti-inflammatory drugs (delay Na⁺ and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids and estrogens (ion retention Na⁺).

Cardiac glycosides, methyldopa, reserpine and guanfacine, blockers of "slow" calcium channels (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or exacerbating bradycardia, AV-blockade, cardiac arrest and heart failure.

Nifedipine can lead to a significant reduction in blood pressure.

Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to excessive blood pressure lowering.

Lengthens the effect of nondepolarizing muscle relaxants and anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedative and hypnotic drugs increase oppression of the central nervous system.

It is not recommended simultaneous use with 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 ergot alkaloids increase the risk of peripheral circulatory disorders.

Ergotamine increases the risk of peripheral circulatory disorders; sulfasalazine increases the concentration of bisoprolol in plasma; rifampicin shortens the half-life period.

Special instructions:

Control of patients receiving Bisoprolol, should include a measurement of heart rate and blood pressure (at the beginning of treatment - every day, then once in 3-4 months), ECG, blood glucose in diabetic patients (once every 4-5 months). In elderly patients it is recommended to follow the function of the kidneys (once every 4-5 months).

You should teach the patient how to calculate heart rate and instruct you 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 in 20% of patients with angina pectoris beta-adrenoblockers are ineffective. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 beats per minute) and an increased end-diastolic volume of the left ventricle, which breaks the subendocardial blood flow.

In "smokers" the effectiveness of beta-blockers is lower.

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 alpha-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. Unlike nonselective beta-blockers, it does not actually increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal levels.

With the simultaneous administration of clonidine, his reception may be terminated only a few days after the cancellation of Bisoprolol.

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 took the drug before the operation, he should choose a medicine 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 beta-blockers, so patients who take such combinations of drugs should be under constant medical supervision to detect a pronounced lowering of blood pressure or bradycardia.

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

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

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

Do not abruptly interrupt treatment because of the risk of developing 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 blood and urine content of catecholamines, normetanephrine and vanillylmandelic acid, antinuclear antibody titers.

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 5 mg and 10 mg.

Packaging:

For 10 or 30 tablets in a contour cell package.

For 30 tablets in cans of polymeric, or vials of polymeric.

Each jar or vial, 3, 5 or 10 out-of-round cell packs of 10 tablets, or 2, 3 or 4 contour packs of 30 tablets together with the instructions for use are placed in a cardboard box.

Storage conditions:

Store in a dry, protected from light place, at a temperature not exceeding 25 FROM.

Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LSR-005035/08

Date of registration:30.06.2008 / 19.02.2016

Expiration Date:Unlimited

The owner of the registration certificate:NORTH STAR, CJSC NORTH STAR, CJSC Russia

Manufacturer: & nbsp

NORTH STAR, CJSC Russia

Representation: & nbspNORTH STAR CJSC NORTH STAR CJSC Russia

Information update date: & nbsp14.02.2017

Illustrated instructions

Instructions

Bisoprolol-SZ (Bisoprolol-SZ)