Bidop - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate 135.20 mg, microcrystalline cellulose 32.00 mg,magnesium stearate 0.70 mg, crospovidone 6.00 mg, pigment grade PB 22812 yellow (lactose monohydrate 87%, iron oxide yellow 13%) 1.10 mg.

1 a 10 mg tablet contains:

active substance: bisoprolol fumarate 10.00 mg;

Excipients: lactose monohydrate 130.20 mg, microcrystalline cellulose 32.00 mg, magnesium stearate 0.70 mg, crospovidone 6.00 mg, pigment grade PB-27215 beige (lactose monohydrate 60%, iron oxide yellow 38% and iron oxide red 2% ) 1.10 mg.

Description:

Tablets 5 mg: round, biconvex tablets of light yellow color with yellowish impregnations with marking В1 in the center above the risk and number 5 below risks.

Tablets 10 mg: round, biconvex tablets of light brown color with brownish impregnations, with marking В1 in the center above the risk and number 10 below risks.

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B Selective beta-blockers

C.07.A.B.07 Bisoprolol

Pharmacodynamics:

Selective beta₁-adrenoceptor 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, anti-anginal and antiarrhythmic effect. Blocking in low doses of beta₁-adrenoceptors of the heart, reduces catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect, inhibits conduction and excitability.

If the therapeutic dose is exceeded, 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-adrenoreceptors), which after 1-3 days returns to the original, and with a long-term appointment - decreases.

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 (more important for patients with initial hypersecretion of renin), restoration of sensitivity in response to lowering blood pressure (BP) and central nervous system (CNS) .With arterial hypertension, the effect occurs after 2-5 days, a stable effect is observed after 1-2 months.

Antianginal effect is caused by a decrease in myocardial oxygen demand as a result of a decrease in heart rate and a decrease in myocardial contractility, diastole lengthening, and improvement in myocardial perfusion. By increasing the end diastolic pressure in the left ventricle and increasing the tension of the ventricular muscle fibers, the need for oxygen may increase, especially in patients with chronic heart failure.

When used in average therapeutic doses, in contrast to non-selective beta-blockers, it exerts a less pronounced effect on organs containing beta₂- adrenergic receptors (pancreas, skeletal muscles, smooth musculature of peripheral arteries, bronchi and uterus) and carbohydrate metabolism; does not cause retention of sodium ions (Na+) in the body; the severity of atherogenic action does not differ from that of propranolol.

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

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 the proteins of the blood plasma - 26-33%. 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 is 10-12 hours. About 98% is excreted by the kidneys, 50% unchanged, less than 2% through the intestines (with bile).

Indications:

- Arterial hypertension;

- Ischemic heart disease: prevention of attacks of stable angina pectoris.

Contraindications:

Hypersensitivity to bisoprolol and other beta-blockers; shock (including cardiogenic); collapse; pulmonary edema; acute heart failure; chronic heart failure in the stage of decompensation, requiring inotropic therapy; AV blockade II-III degree without pacemaker; sinoatrial blockade; syndrome of weakness of the sinus node; bradycardia (heart rate less than 60 beats / min); cardiomegaly (no signs of heart failure); severe arterial hypotension (systolic blood pressure less than 100 mm Hg, 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; Raynaud's syndrome; pheochromocytoma (without simultaneous use of alpha-blockers); metabolic acidosis; age under 18 years (effectiveness and safety not established); lactose intolerance, lactase deficiency or glucose-galactose malabsorption (as lactose is included in the formulation).

Carefully:

Liver failure; chronic renal failure (CC less than 20 ml / min.); myasthenia gravis; thyrotoxicosis; diabetes; angina of Prinzmetal, AV blockade of the 1st degree; psoriasis; depression (including in the anamnesis); allergic reactions in the anamnesis; adherence to a strict diet; elderly age.

Pregnancy and lactation:

The use of Bidop ® in pregnancy is possible only if the intended benefit of therapy for the mother exceeds the potential risk of side effects in the fetus and / or the child.

There is no data on whether the bisoprolol in mother's milk. If it is necessary to use the drug during lactation, it is recommended to stop breastfeeding.

Dosing and Administration:

Inside, in the morning on an empty stomach, without chewing, once. The dose should be selected individually.

Arterial hypertension and ischemic heart disease: prevention of attacks of stable angina usually the initial dose is 5 mg once a day.

If necessary, increase the dose to 10 mg once a day. The maximum daily dose is 20 mg per day.

In patients with impaired renal function with clearance of creatinine (CC) less than 20 ml / min or with severe hepatic impairment the maximum daily dose is 10 mg. Increasing the dose in such patients should be done with extreme caution.

Dose adjustment in elderly patients not required.

Side effects:

Side effects observed with the use of the drug,are classified into categories according to the frequency of their occurrence: very often ≥1 / 10; often> 1/100, ≤1 / 10; infrequently ≥ 1/1000, ≤1 / 100; rarely ≥1 / 10000, ≤ 1/1000; very rarely ≤1 / 10000, including individual messages.

From the central nervous system: infrequent - fatigue, weakness, asthenia, dizziness, headache, sleep disorders, depression, anxiety, confusion, or short-term memory loss; rarely - hallucinations, myasthenia gravis, "nightmarish" dreams, convulsions (including in the calf muscles), paresthesia in the extremities (in patients with "intermittent" lameness and Raynaud's syndrome), tremor.

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

From the side of the cardiovascular system: very often - sinus bradycardia, palpitations; often - marked decrease in blood pressure, the manifestation of angiospasm (increased peripheral circulatory disturbance, lower extremities cooling, paresthesia, Raynaud's syndrome); infrequently - orthostatic hypotension, disturbance of myocardial conductance, AV blockade (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakening of myocardial contractility,development of chronic heart failure (swelling of the ankles, feet, shortness of breath), chest pain.

From the digestive system: often - dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea; rarely - violations of the liver (dark urine, icterus sclera or skin, cholestasis), changes in taste, hepatitis.

From the respiratory system: infrequent breathing difficulties when prescribing in high doses (loss of selectivity) and / or in predisposed patients - laryngo- and bronchospasm; rarely - nasal congestion.

From the endocrine system: hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), a hypothyroid condition.

Allergic reactions: rarely - skin itching, rash, hives.

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

Laboratory indicators: rarely - increased activity of "hepatic" transaminases (increased alanine aminotransferase, aspartate aminotransferase), hyperbilirubinemia,hypertriglyceridemia; in some cases - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, and leukopenia.

Influence at fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

Other: infrequently - arthralgia; rarely - weakening of libido, decreased potency; back pain, withdrawal syndrome (increased angina attacks, increased blood pressure).

Overdose:

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

Treatment: gastric lavage and administration of adsorptive agents; symptomatic therapy: with developed AV blockade - intravenous injection of 1-2 mg of atropine, epinephrine or temporary staging of a pacemaker; with ventricular extrasystole - lidocaine (preparations IA class do not apply); with a pronounced 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,if 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 extracts of allergens 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 reducing 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 the blood plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking.

The hypotensive effect weakens nonsteroidal anti-inflammatory drugs (retention of sodium ions (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 anticoagulant effect coumarins.

Tri- and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives and hypnotics increase the inhibition of the central nervous system.

Do not use concurrently from MAO inhibitors (with the exception of MAO-B, see the section "Contraindications"), due to a significant increase in hypotensive effect,a break in treatment between the intake of MAO inhibitors (except MAO-B) 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; rifampicin shortens the half-life.

Special instructions:

Control of patients receiving Bidop ® should include a measurement of heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 months) ECG, determination of glucose concentration in the blood of patients with diabetes mellitus (1 every 4-5 months .). In elderly patients it is recommended to monitor kidney function (1 time in 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 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.

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).

In thyrotoxicosis, Bidop® can mask certain clinical signs of thyrotoxicosis (eg, 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 can be stopped only a few days after the cancellation of Bidop®.

It is possible to increase the severity of the reaction of hypersensitivity and the lack of effect from the usual doses of epinephrine (adrenaline) against the background of a weighed allergic 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 the reserves of catecholamines (including, reserpine), can enhance the action of beta-blockers, so patients who take such combinations of drugs should be under constant observation of the doctor for the detection of a marked decrease in blood pressure or bradycardia.

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

In the case of an increasing bradycardia (less than 50 beats per minute) in elderly patients, a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg) AV blockade, bronchospasm, ventricular arrhythmias, severe impairment of liver and kidney function, 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 abolished before the study of blood and urine levels of catecholamines, normetanephrine and vanillylmandelic acid; titers of antinuclear antibodies.

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

During the treatment period, dizziness is possible, especially at the beginning of therapy, and therefore care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

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

Packaging:

For 14 tablets in the blister PVC / PVDC / Al.

For 1, 2 or 4 blisters with instructions for use in a cardboard box.

Storage conditions:

In a dry, the 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:LS-000414

Date of registration:31.05.2010 / 05.10.2015

Expiration Date:Unlimited

The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary

Manufacturer: & nbsp

GEDEON RICHTER-RUS, CJSC Russia

NICHE GENERICS, Limited Ireland

Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary

Information update date: & nbsp25.01.2017

Illustrated instructions

Instructions

Bidop® (Bidop®)