BIDOP

Active material: Bisoprolol
When ATH: C07AB07
CCF: Beta₁-adrenoblokator
ICD-10 codes (testimony): I10, i20
When CSF: 01.01.01.02
Manufacturer: NICHE GENERICS Limited (Great Britain)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills, coated light yellow colour with yellow inclusions, round, lenticular, labeled “IN 1” centered over the mark and digit “5” lower risks.

Excipients: lactose monohydrate, microcrystalline cellulose, magnesium stearate, krospovydon, PB dye 27812 yellow (lactose monohydrate, iron oxide yellow), PB dye 27215 Beige (lactose monohydrate, iron oxide red, iron oxide yellow).

14 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (2) – packs cardboard.
14 PC. – blisters (4) – packs cardboard.

Pills, coated light brown with brown specks, round, lenticular, labeled “IN 1” centered over the mark and digit “10” lower risks.

Excipients: lactose monohydrate, microcrystalline cellulose, magnesium stearate, krospovydon, PB dye 27812 yellow (lactose monohydrate, iron oxide yellow), PB dye 27215 Beige (lactose monohydrate, iron oxide red, iron oxide yellow).

14 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (2) – packs cardboard.
14 PC. – blisters (4) – packs cardboard.

Pharmacological action

Selective beta₁-blocker without intrinsic sympathomimetic activity, It does not have the membrane-stabilizing action. It reduces plasma renin activity, reducing myocardial oxygen demand, reduces heart rate (at rest and during exercise). It has hypotensive, antiarrhythmic and antianginal. Blocking in low doses β₁-adrenergic receptors of the heart, reduces the formation of catecholamines stimulated cAMP from ATP, reduces intracellular calcium ion current, It has a negative chrono, dromo-, ʙatmo- and inotropic effect, oppressing conductivity and anxiety, reduces myocardial contractility.

With increasing doses of beta has₂-adrenoceptor blocking action.

At the beginning of the drug, first 24 no, PR increases (as a result of reciprocal increase in the activity of α-adrenergic stimulation and removal of β₂-adrenoreceptorov), through 1-3 h 20 ROUND returned to the original, and if long-term treatment is reduced.

The hypotensive effect is associated with a decrease in cardiac output, sympathetic stimulation of peripheral vessels, decreased activity of the renin-angiotensin system (It is more important for patients with initial hypersecretion of renin), restoring sensitivity of aortic arch baroreceptors (not going to enhance their activity in response to the decline of HELL and the impact on the central nervous system. In arterial hypertension effect develops through 2-5 days, stable operation – through 1-2 Months.

Antianginal effect is due to a decrease in myocardial oxygen demand as a result of deceleration in heart rate and decrease contractility, lengthening of diastole, improving myocardial perfusion. At the expense of increasing end-diastolic pressure in the left ventricle and increased tensile ventricular muscle fibers can increase oxygen demand, especially in patients with chronic heart failure.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP, hypertension), decrease speed of spontaneous excitation of the sine and jektopicheskogo pacemakers and slowing AV conduction (mainly in the antegrade and, less, in retrograde directions through the AV node) and on additional routes.

When used in high therapeutic doses, Unlike non-selective beta-blockers, It has a less pronounced effect on the organs, содержащие b₂-adrenoreceptory (pancreas, skeletal muscle, smooth muscle peripheral arteries, bronchial and uterine) and carbohydrate metabolism, It does not cause a delay of sodium ions in the body; the severity of atherogenic actions no different from the actions of propranolol.

When used in high doses (200 mg, and more) has a blocking effect on both beta-adrenoceptor subtype, mainly, in the bronchi and smooth muscles receptacles.

Pharmacokinetics

Absorption

Absorption – 80-90%, meal no effect on absorption. C_max in the blood plasma through 2-4 no.

Distribution

The binding to plasma proteins – 26-33%.

The permeability of the BBB and placental barrier – low, the secretion of breast milk – low.

Metabolism and excretion

It is metabolized in the liver.

T_1/2 – 9-12 no. Report the news – 50% in unchanged form, less 2% the bile.

Testimony

- Arterial hypertension;

- Prevention of angina attacks.

Dosage regimen

Assign inside dose 2.5-5 mg 1 time / day, morning, fasting. If necessary, increase the dose to 10 mg 1 time / day. The maximum daily dose – 20 mg / day.

For patients with impaired renal function at least QC 20 ml / min or severe hepatic impairment the maximum daily dose – 10 mg.

The tablets are not liquid.

Side effect

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

From the senses: blurred vision, reduced secretion of tear fluid, dryness and soreness of eyes, conjunctivitis.

Cardio – vascular system: sinusovaya bradycardia, heartbeat, conduction disturbances infarction, AV блокада (until the development of a full cross-blockade and heart failure), Arrhythmia, weakening of myocardial contractility, development (aggravation) chronic heart failure (swelling of the ankles, stop; breathlessness), decrease in blood pressure, orthostatic hypotension, manifestation of vasospasm (increased peripheral circulatory disorders, 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, abnormal liver function (dark urine, yellow skin or sclera, cholestasis), changes in taste, hepatitis.

The respiratory system: nasal congestion, difficulty breathing when administered at high doses (loss of selectivity) and / or in predisposed patients – laringo- and bronchospasm.

On the part of the endocrine system: giperglikemiâ (in patients with non-insulin dependent diabetes mellitus), gipoglikemiâ (patients, receiving insulin), hypothyroid state.

Allergic reactions: itching, rash, hives.

Dermatological reactions: increased sweating, dermahemia, rash, psoriasiform skin reactions, exacerbation of psoriasis symptoms.

From the laboratory parameters: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, changes in liver enzymes (improvement ACT, GOLD), bilirubin, triglycerides.

Other: backache, arthralgia, the weakening of the libido, reduced potency, withdrawal (increasing angina attacks, increased blood pressure).

Contraindications

- Shock (including cardiogenic);

- Collapse;

- Pulmonary edema;

- Acute heart failure;

- Chronic heart failure decompensation (incl. cardiogenic shock);

-AV-blokada II degree;

- Sinoatrialynaya blockade;

- SSS;

- Vыrazhennaya bradycardia;

- Prinzmetal angina;

- Kardiomegalija (without signs of heart failure);

- Hypotension (systolic blood pressure less than 100 mmHg., especially in myocardial infarction);

- Asthma and COPD history;

- Simultaneous MAO inhibitors (except MAO type B);

- Late stages of peripheral circulatory disorders;

- Raynaud's disease;

- Pheochromocytoma (without the simultaneous use of alpha-blockers);

- Metabolic acidosis;

- Up to 18 years (efficacy and safety have not been established);

-hypersensitivity to bisoprololu and other beta-adrenoblokatoram.

FROM caution should be applied when liver failure, chronic renal failure, myasthenia, thyrotoxicosis, diabetes, AV blockade degree I, psoriaze, depression (incl. history), in elderly patients.

Pregnancy and lactation

Use of the drug during pregnancy and lactation is possible only if, projected benefits for a mother than the potential risk to the fetus and child.

Bidop^® affects on the fetus: causing intrauterine growth delay, gipoglikemiû, ʙradikardiju.

Cautions

Control of patients, host Bisoprolol, It should include measurement of blood pressure and heart rate (at the beginning of treatment – daily, then 1 once every 3-4 Months), conduct an electrocardiogram, determination of blood glucose in patients with diabetes (1 once every 4-5 Months). In elderly patients, it is recommended to monitor renal function (1 once every 4-5 Months).

It should teach the patient methods of calculating heart rate and instruct on the need of medical advice in heart rate less than 50 u. / min.

Before treatment is recommended study of respiratory function in patients with a history of bronchopulmonary history.

Approximately 20% patients with angina Beta-blockers are ineffective. Main reasons – severe coronary atherosclerosis with a low threshold of ischemia (HR less 100 u. / min) and increased end-diastolic volume of the left ventricle, violates the subendocardial blood flow.

Smokers the effectiveness of beta-adrenoblokatorov below.

Sick, use contact lenses, We should take into account, that against the background of treatment may decrease the production of tear fluid.

When used in patients with a risk of paradoxical feohromotsytoma hypertension (if not previously achieved effective alpha adrenoblockade).

If you can knock out Bisoprolol tireotoxicose certain clinical signs of hyperthyroidism (eg, taxikardiju). Sudden removal in patients with thyrotoxicosis is contraindicated, as able to exacerbate symptoms.

Diabetes can mask tachycardia, induced hypoglycemia. In contrast, non-selective beta blockers hardly increase insulin-induced hypoglycemia or delay recovery of the concentration of glucose in the blood to normal levels.

At the same time taking clonidine its reception can be terminated only after a few days after discontinuation of bisoprolol.

Perhaps the increased severity of hypersensitivity reactions and the lack of effect of conventional doses of epinephrine with aggravated allergic history.

In the case of the need for a planned surgical treatment is carried out for the abolition of the drug 48 h before general anesthesia. If the patient has taken the drug before surgery, he should choose a drug for general anesthesia with minimal negative inotropic effects.

Reciprocal activation of the vagus nerve can eliminate I / atropine (1-2 mg).

Drugs, reducing stocks catecholamines (incl. reserpine), may enhance the action of beta-blockers, so patients, taking such drug combinations, We should be under constant medical supervision to identify pronounced reduction in blood pressure or bradycardia.

Patients with diseases bronhospasticheskimi cardioselective blockers can be administered in case of intolerance and / or ineffectiveness of other antihypertensive drugs. Overdose danger of developing bronchospasm.

In the case of elderly patients increasing bradycardia (less 50 u. / min), pronounced reduction in blood pressure (systolic BP below 100 mmHg.), AV blockade, bronchospasm, ventricular arrhythmias, Serious liver and kidneys need to reduce the dose or stop treatment.

It is recommended to discontinue therapy in the development of depression.

Do not abruptly discontinue the treatment because of the risk of severe arrhythmias and myocardial infarction. The abolition of a gradually, reducing the dose for 2 weeks or more (reduce the dose by 25% in 3-4 day). Should be lifted before the test content in the blood and urine Catecholamines, normetanephrine and vanilinmindalnoy acid; antinuclear antibodies.

Effects on ability to drive vehicles and management mechanisms

During the period of treatment must be careful when driving and occupation of other potentially hazardous activities, require high concentration and speed of psychomotor reactions.

Overdose

Symptoms: arrhythmia, ventricular premature beats, vыrazhennaya bradycardia, OF блокада, decrease in blood pressure, congestive heart failure, cyanosis of nails of fingers or hands, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.

Treatment: gastric lavage and appointment of adsorbing drugs; simptomaticheskaya therapy: When Advanced AV-blockade-in/ 1-2 mg atropine, epinephrine, or staging a temporary pacemaker; when ventricular arrhythmia – lidokain (class A drugs I do not apply); with a decrease in blood pressure – the patient must be in the position of Trendelenburg; if there are no signs of pulmonary edema, – I / O solutions plazmozameschayuschie, the ineffectiveness – administration of epinephrine, dopamine, doʙutamina (to maintain chronotropic and inotropic effects and eliminate significant decrease in blood pressure); Heart failure – cardiac glycosides, Diuretic, glucagon; cramps-in/diazepam; with bronchospasm – beta₂-adrenostimulyatorov inhalation.

Drug Interactions

Allergens, used for immunotherapy, or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients, receiving bisoprolol.

Iodized rentgencontrastnye medicines for on/in the introduction increases the risk of anaphylactic reactions.

Phenytoin in in / in the introduction, drugs for inhalation general anesthesia (hydrocarbon derivatives) cardiodepressive increase the severity of the action and the probability of reduction of blood pressure.

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

Lowers klirens lidocaine and xantinov (except difillina) and increases their concentration in the plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking.

Antihypertensive effect of weakening the NSAID (delay of sodium ions and the blockade of prostaglandin synthesis by the kidneys), SCS and estrogens (delay of sodium ions).

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

Diuretic, klonidin, simpatolitiki, hydralazine, and other antihypertensive drugs may cause an excessive decrease of blood pressure.

Extends the effect nedepoliarizuth miorelaksantov and antikoagulyannetary kumarinov effect.

Three- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics drugs increase CNS depression.

Not recommended simultaneous application with MAO inhibitors due to a significant increase in the hypotensive action, a break in treatment between the reception of MAO inhibitors and bisoprolol must not be less than 14 days.

Non-hydrogenated ergot alkaloids increase the risk of peripheral circulatory disorders.

Ergotamine increases the risk of peripheral circulatory disorders; sulfasalazine Bisoprolol improves concentration in plasma; rifampicin shorter T_1/2.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children, dry, dark place at a temperature no higher than 25 ° C. Shelf life – 3 year.