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

Excipients: calcium hydrophosphate 40.0 mg, cellulose microcrystalline 84.9 mg (for a dosage of 5 mg) and 79.8 (for a dosage of 10 mg), silicon dioxide colloidal 0.30 mg, pregelatinized starch 19.0 mg, magnesium stearate 0.70 mg;

film sheath: iron oxide yellow (for a dosage of 5 mg) 0.01 mg, iron oxide red (for a dosage of 10 mg) 0.01 mg, titanium dioxide 0.70 mg, triacetin 0.40 mg, hypromellose 2.0 mg, ethyl cellulose 0.01 mg.

Description:

Tablets 5 mg: round tablets, covered with a film shell of light yellow color, biconvex form, with a risk on one side.

Tablets 10 mg: round tablets, covered with a film shell of light pink color, biconvex form.

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 in the blood plasma, reduces the need for myocardium in oxygen, reduces the frequency of cardiac contractions (heart rate) (at rest and with exercise). Has antihypertensive, antiarrhythmic and antianginal action. 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-, dromobathic and inotropic effect, inhibits conductivity and excitability, reduces myocardial contractility.

With an increase in the dose of 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), which returns to the initial one after 1-3 days, and decreases with long-term administration.

Antihypertensive effect is associated with a decrease in the minute volume of blood, sympathetic stimulation of peripheral vessels, a decrease in the activity of renin-angiotensin-aldosterone system (is of great importance for patients with initial hypersecretion of renin), restoration of sensitivity in answer to decrease in blood pressure (BP) and influence on the central nervous system (CNS). With arterial hypertension, the effect occurs after 2-5 days, a stable effect - after 1-2 months.

Antianginal effect 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. 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.

Pharmacokinetics:

Absorption from the gastrointestinal tract - 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 is about 30%. The permeability of the blood-brain barrier and the placental barrier - low secretion breast milk - low.

Metabolized in the liver, half-life of 10-12 hours. 98% are excreted by the kidneys, 50% of them are unchanged, less than 2% - through the intestine.

In elderly patients and patients with cirrhosis of the liver, the elimination half-life increases.

Indications:

- Arterial hypertension;

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

Contraindications:

Hypersensitivity to the components of the drug,shock (including cardiogenic), collapse, pulmonary edema, acute heart failure, chronic heart failure in the stage of decompensation, requiring inotropic therapy, AV, blockade of II-III degree (without artificial pacemaker), sinoatrial block, sinus node weakness syndrome , pronounced bradycardia (pulse at rest less than 50 beats per minute), angina of prinzmetal, cardiomegaly (without signs of heart failure), severe arterial hypotension (systolic blood pressure less than 100 mm Hg, especially with infar those with myocardial infarction), severe bronchial asthma and chronic obstructive pulmonary disease in the anamnesis, simultaneous administration of monoamine oxidase inhibitors (MAO) (except MAO-B), severe peripheral circulation disorders, Raynaud's syndrome, pheochromocytoma (without simultaneous use of alpha-blockers), metabolic acidosis , age under 18 years (efficacy and safety not established), the period of breastfeeding, the concomitant use of floktaphenin and sultopride.

Carefully:

Hepatic insufficiency, bronchospasm in the anamnesis,peripheral circulatory disorders (especially at the beginning of therapy), general anesthesia, chronic heart failure, pheochromocytoma (with simultaneous use with alpha-blockers), renal failure (creatinine clearance less than 20 ml / min), myasthenia gravis, thyrotoxicosis, type 1 diabetes mellitus and sugar Diabetes with significant fluctuations in the concentration of glucose in the blood plasma, atrioventricular blockade I degree, depression (including in anamnesis), strict diet, carrying out desensitizing therapy, psoriasis, and advanced 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.

If it is necessary to use breastfeeding should be discontinued, since bisoprolol It is secreted with breast milk.

Dosing and Administration:

Inside, in the morning on an empty stomach, without chewing, 2.5-5 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 impaired liver function, the initial dose should not exceed 2.5 mg per day, the maximum daily dose - 10 mg.

Dose adjustments in elderly patients are not required.

2.5 mg corresponds to ¹/₂ 5 mg tablets.

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, tear fluid, dry and sore eyes, conjunctivitis, hearing impairment, ringing in the ears, pain in the ears.

From the cardiovascular system: sinus bradycardia, sensation cardiac arrhythmias, myocardial conduction disturbance, AV blockade (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakened myocardial contractility, development of chronic heart failure (swelling of the ankles, feet, dyspnea), pronounced blood pressure lowering, orthostatic hypotension, manifestation angiospasm (increased peripheral circulatory disturbance, coldness of the lower limbs, 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, cough.

From the endocrine system: hyperglycemia (in patients with type 2 diabetes), hypoglycemia (in patients receiving insulin), hypothyroid status.

Allergic reactions: allergic rhinitis, skin itching, rash, hives.

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

From the musculoskeletal system: pain in the back, arthralgia.

Laboratory indicators: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, changes in hepatic transaminase activity (ALT, ACT), bilirubin concentration, triglycerides.

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

Other: weakening of libido, decreased potency, withdrawal syndrome (increased angina attacks, increased blood pressure).

Overdose:

Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV blockade, hypoglycemia, marked decrease in blood pressure, acute 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 the development of AV blockade - intravenous injection of 1-2 mg of atropine, epinephrine or the setting of a temporary 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 - intravenously plasma-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; with hypoglycemia - intravenous dextrose; with convulsions - intravenous injection 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 developing an anaphylactic reaction.

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.

When used with antiarrhythmic drugs I (quinidine, hydroquinidine, disopyramide) and III class (amiodarone) increases (mutually) the probability of a violation of automatism, conduction and contractility of the heart.

When used simultaneously with sympathomimetics (epinephrine, norepinephrine), the effect of bisoprolol may decrease.

With simultaneous application with beta-adrenomimetics, a significant reduction in their effect is possible.

When used simultaneously with beta-blockers for topical application (eye drops), there is a potential danger of an additive effect with the development of hypotension and / or a significant bradycardia.

When combined with mefloquine, bradycardia may develop.

Contraindicated in combination with floktaphenin, sultopride.

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

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

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

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

If the combined therapy of bisoprolol with clonidine is canceled, then after stopping the use of clonidine treatment with bisoprolol should continue for several more days, providing medical supervision of the patient's condition.

The combined use of nifedipine and bisoprolol 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.

Three - 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 (with the exception of MAO B 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.

Special instructions:

Control of patients taking Corbis,should include a measurement of heart rate and blood pressure (at the beginning of treatment - every day, then 1 time in 3-4 months), ECG, determination of glucose concentration in blood plasma in diabetic patients (1 time in 4-5 months).

In elderly patients it is recommended to monitor the kidney function (1 time in 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 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 / min) 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 tear production can be reduced against the background of treatment.When used in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension,if not previously achieved an effective alpha-adrenoblockade.

With thyrotoxicosis bisoprolol can mask his clinical symptoms (tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated, since it is possible to increase its 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, its administration can be stopped only a few days after the withdrawal of bisoprolol.

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

If older bradycardia is detected in elderly patients (less than 50 beats / min), a 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.

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 withdrawn before the study of blood and urine content catecholamines, normetanephrine and vanillin-mandelic acid; titers of antinuclear antibodies.

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:

10 tablets per strip of aluminum foil.

On 3 strips together with the instruction on application place in a pack a cardboard.

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 later than the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001526

Date of registration:02.05.2011

The owner of the registration certificate:Unikem Laboratories Ltd.Unikem Laboratories Ltd. India

Manufacturer: & nbsp

UNICHEM Laboratories, Ltd. India

Representation: & nbspUNICEM LABORATORIES LTD. UNICEM LABORATORIES LTD. India

Information update date: & nbsp26.11.2015

Illustrated instructions

Instructions

Corbis (Corbis)