KORBIS

Active material: Bisoprolol
When ATH: C07AB07
CCF: Beta₁-adrenoblokator
ICD-10 codes (testimony): I10, i20
When CSF: 01.01.01.02
Manufacturer: UNICHEM Laboratories Ltd. (India)

DOSAGE FORM, COMPOSITION AND PACKAGING

Pills, coated light yellow, round, with Valium on one side.

Excipients: calcium hydrogen phosphate, anhydrous, microcrystalline cellulose, colloidal silicon dioxide, pre-gelatinized starch, magnesium stearate, iron oxide yellow, Titanium dioxide, triacetine, gipromelloza, ethyl cellulose.

10 PC. – strips of aluminum foil (3) – packs cardboard.

Pills, coated light pink, round, lenticular.

Excipients: calcium hydrogen phosphate, anhydrous, microcrystalline cellulose, colloidal silicon dioxide, pre-gelatinized starch, magnesium stearate, iron oxide red, Titanium dioxide, triacetine, gipromelloza, ethyl cellulose.

10 PC. – strips of aluminum foil (3) – packs cardboard.

Pharmacological action

Selective beta₁-adrenoblokator, without its own sympathomimetic activity, It does not have the membrane-stabilizing action. It reduces plasma renin activity, reducing myocardial oxygen demand, It reduces the heart rate at rest and during exercise. It has hypotensive, antiarrhythmic and antianginal.

Blocking in low doses Beta₁-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. PR in the first 24 h of the drug increases (as a result of reciprocal increase in the activity of α-adrenergic stimulation and removal of β₂-adrenoreceptorov), through 1-3 d returns to the original, and prolonged the appointment of reduced.

The antihypertensive action is due to a decrease in cardiac output, sympathetic stimulation of peripheral vessels, decreased activity of the renin-angiotensin system (It is of great importance for patients with initial hypersecretion renin), restoration of sensitivity in response to a decrease in blood pressure and the influence of the central nervous system. When hypertension effect after 2-5 days, stable operation through 1-2 of the month.

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.

Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP, hypertension), decrease in the rate of spontaneous excitation of the sinus and ectopic pacemakers and slowing of AV- (mainly in the antegrade and, less, in retrograde direction 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 (incl. 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. Intensity of atherogenic action is different from that of propranolol. When used in large doses (≥200 mg) It exerts a blocking effect on both subtypes of β-adrenoceptor, mainly, bronchial and vascular smooth muscle.

Pharmacokinetics

Absorption and distribution

The absorption of the drug from the gastrointestinal tract 80-90 %, meal no effect on absorption. C_max in the blood plasma through 1-3 no, binding to plasma proteins – about 30%. The permeability of the BBB and placental barrier – low, selection with breast milk – poor.

Metabolism and excretion

It is metabolized in the liver, T_1/2 sostavlyaet10-12 h. It appears unchanged in the urine – 50%, the bile – <2%.

Testimony

- Arterial hypertension;

- CHD;

- Prevention of angina attacks.

Dosage regimen

The drug is taken orally 2.5-5 mg dose, in the morning on an empty stomach, without chewing.

If necessary, increase the dose to 10 mg 1 time / day. The maximum daily dose is 20 mg.

In patients impaired renal function in QA<20 ml / min or severe hepatic impairment The maximum daily dose is 10 mg.

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, palpitations, 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 and feet, 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.

From the laboratory parameters: increase in ALT and / or ACT, bilirubin, triglycerides.

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

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

On the part of the reproductive system: the weakening of the libido, reduced potency.

On the part of the musculoskeletal system: backache, arthralgia.

From the hematopoietic system: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia.

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

Allergic reactions: itching, rash, hives.

Effect on the fetus: intrauterine growth, gipoglikemiâ, bradycardia.

Other: withdrawal (increasing angina attacks, increased blood pressure).

Contraindications

- Shock (incl. cardiogenic);

- Collapse;

- Pulmonary edema;

- Acute heart failure;

- Chronic heart failure decompensation;

— AV-blockade II and III degrees;

- Sinoatrialynaya blockade;

- SSS;

- Vыrazhennaya bradycardia;

- Prinzmetal angina;

- Kardiomegalija (without signs of heart failure);

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

- Asthma and COPD history;

- Simultaneous use of 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;

- Childhood and adolescence up 18 years (efficacy and safety have not been established);

- Hypersensitivity to the drug;

- Hypersensitivity to other beta-blockers.

FROM caution use in patients with hepatic insufficiency, chronic renal failure, myasthenia, thyrotoxicosis, diabetes, AV-blockade I degree, depression (incl. history), psoriaze, in elderly patients.

Pregnancy and lactation

Use of the drug during pregnancy and lactation is possible only if, when the intended benefits to the mother outweighs the potential risk to the fetus.

Cautions

Patients, receiving bisoprolol, requires clinical monitoring: measurement of heart rate and blood pressure (at the beginning of treatment – daily, then 1 once every 3-4 of the month), conduct an electrocardiogram, determination of blood glucose in patients with diabetes mellitus (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 prevent the need to consult a doctor if the heart rate of less than 50 u. / min.

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

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 (reduce the dose by 25% in 3-4 day). It should stop the drug before the study content in the blood and urine catecholamines, normetanephrine and vanillylmandelic acid; antinuclear antibodies.

Effects on ability to drive vehicles and management mechanisms

In 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, AV 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. With AV-blockade which developed in / 1-2 mg atropine, epinephrine, or staging a temporary pacemaker. If ventricular arrhythmia – lidokain (1a-class drugs do not apply). By reducing blood pressure – the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema, – I / O solutions plazmozameschayuschie, the ineffectiveness of administration of epinephrine, dopamine, doʙutamina (to maintain chronotropic and inotropic effects and eliminate significant decrease in blood pressure). In heart failure – cardiac glycosides, Diuretic, glucagon. In convulsions – in / diazepam. When bronchospasm – beta₂-adrenostimulyatorov inhalation.

Drug Interactions

In an application with allergens Corbis, used for immunotherapy, or extracts of allergens for skin tests and increased risk of severe systemic allergic reactions or anaphylaxis in patients, receiving bisoprolol.

In an application with Corbis iodine radiopaque drugs for i / v administration increases the risk of anaphylactic reactions.

In an application with phenytoin Corbis (at / in the introduction), drugs for inhalation general anesthesia (derivatives of hydrocarbons) increased severity cardiodepressive action and the probability of reduction of blood pressure.

In an application Corbis insulin and oral hypoglycemic drugs, changed their effectiveness, masked the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

In an application with Corbis reduced clearance of lidocaine and xanthine (except difillina) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of tobacco smoking.

With simultaneous use of anti-hypertensive effect of NSAIDs weaken Corbis (delay of sodium ions and the blockade of prostaglandin synthesis by the kidneys), SCS and estrogens (delay of sodium ions).

In an application with cardiac glycosides Corbis, methyldopa, reserpine and guanfacine, blockers slow calcium channels (verapamil, diltiazem), amiodoron and other antiarrhythmic drugs increase the risk of developing or worsening of bradycardia, AV-blockade, heart failure and congestive heart failure.

In an application with Corbis nifedipine may lead to a significant reduction in blood pressure.

While the use of diuretics Corbis, klonidin, simpatolitiki, hydralazine, and other antihypertensive drugs may cause an excessive decrease of blood pressure.

In an application Corbis prolongs the action of non-depolarizing muscle relaxants and anticoagulant effect of coumarin.

In an application with Corbis tricyclic and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics drugs increase CNS depression.

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

While the use of non-hydrogenated Corbis ergot alkaloids increase the risk of peripheral circulatory disorders.

Sulfasalazine increases the concentration of bisoprolol plasma. Рифампицин укорачивает T_1/2 bisoprolol.

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. Do not use beyond the expiration date, on the package.