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

Excipients: cellulose microcrystalline 21.10 mg, mannitol 148,50 mg; sodium croscarmellose 1.80 mg, magnesium stearate 3.60 mg, hypromellose 2.19 mg, titanium dioxide 0.88 mg, macrogol 6000 0.53 mg.

1 tablet of 10 mg contains:

active substance: bisoprolol fumarate 10 mg;

Excipients: cellulose microcrystalline 20.00 mg, mannitol 144,60 mg; sodium croscarmellose 1.80 mg, magnesium stearate 3.60 mg, hypromellose 2.19 mg, titanium dioxide 0.88 mg, macrogol 6000 0.53 mg.

Description:

Round, convex, film-coated tablets are white, with risk on the one hand, side risks and engraving "B 5" (for tablets 5 mg) or "B 10" (for tablets 10 mg) on the other side.

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-adrenoceptors of the heart, reduces the 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, and slows the atrioventricular conductivity.

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 somewhat (as a result of the reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of beta stimulation₂-adrenoreceptors), which returns to the initial one after 1-3 days, and decreases with long-term administration.

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.

In contrast to nonselective beta-blockers, when administered at average therapeutic doses, it has 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 delay Na+ in the body; the severity of atherogenic action does not differ from that of propranolol.

When used in large doses has a blocking effect on both subtypes of beta-adrenergic receptors.

Pharmacokinetics:

Absorption - 80-90%, food intake does not affect absorption. The maximum concentration in blood plasma is observed after 1-3 h, the connection with blood plasma proteins is about 35%. Permeability through the blood-brain barrier and placental barrier, secretion with breast milk - low. 50% of the dose is metabolized in the liver with the formation of inactive metabolites, the half-life is 9-12 hours. About 98% is excreted by the kidneys, 50% is unchanged, less than 2% with bile.

Indications:

- Ahyperthermia;

- ischemic heart disease (prevention of angina attacks);

Contraindications:

Hypersensitivity to bisoprolol or to any of the components of the drug, other beta-blockers, shock (including cardiogenic), collapse, pulmonary edema, acute heart failure, chronic heart failure in decompensation, atrioventricular block (AV) blockade II-III Art. (without a pacemaker), sinoatrial blockade,syndrome of weakness of the sinus node, pronounced bradycardia (heart rate less than 50 beats / min), angina of Prinzmetal, cardiomegaly (without signs of heart failure), arterial hypotension (systolic blood pressure less than 100 mm Hg, especially with myocardial infarction); The bronchial asthma and chronic obstructive pulmonary disease in the anamnesis; 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:

Take inside, in the morning on an empty stomach, without chewing, 2.5-5 mg once.Usually the initial dose is 5 mg 1 time per day. If necessary, increase the dose to 10 mg once a day. The maximum dose for adults is 20 mg / day.

Treatment of arterial hypertension and angina: treatment of patients with impaired hepatic or renal function of mild or moderate degree usually does not require dose adjustment.

In patients with marked renal impairment (creatinine clearance less than 20 ml / min) or with severe impairment of liver function, the maximum daily dose is 10 mg.

Dose adjustments in elderly patients are not required.

Side effects:

From the central nervous system: increased fatigue, weakness, dizziness, headache, drowsiness or insomnia, nightmares, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenia, myasthenia gravis, paresthesia in the extremities (in patients with "intermittent" lameness and Raynaud's syndrome ), a tremor.

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

From the side of the cardiovascular system: sinus bradycardia, palpitation, conduction disturbance of the myocardium, violation AV conductivity (up to the full development of cross-blockade and heart failure), arrhythmia, weakening of the myocardial contractility, the development of (worsening) of chronic heart failure (swelling of ankles, feet, shortness of breath), reduced blood pressure, orthostatic hypotension, a manifestation of vasoconstriction (increased peripheral circulatory disorders, chill lower extremities, Raynaud's syndrome), chest pain.

Co side of the gastrointestinal tract: 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), a hypothyroid condition.

Allergic reactions: itching, rash, hives.

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

Laboratory indicators: thrombocytopenia (unusual hemorrhages and hemorrhages), agranulocytosis, leukopenia, changes in the activity of liver enzymes (increased ALT, ACT), the level of bilirubin, triglycerides.

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

From the musculoskeletal system: muscle weakness, cramps in the calf muscles.

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

Overdose:

Symptoms: arrhythmia, ventricular extrasystole, pronounced bradycardia, AV blockade, decreased blood pressure, chronic heart failure, cyanosis of the fingernails or palms, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.

Treatment: gastric lavage and administration of absorbent drugs; symptomatic therapy: with developed AV blockade - intravenous (intravenous) administration 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 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 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 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.

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

Cardiac glycosides, methyldopa, reserpine and guanfacine, slow calcium channel blockers (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or worsening 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, antipsychotics (antipsychotics), antipsychotics ethanol, sedative and hypnotic drugs increase the inhibition 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.

Special instructions:

Do not interrupt treatment drastically and do not change the recommended dosage without first consulting a physician.

Control of patients taking Cordinorm should include monitoring of heart rate and blood pressure (at the beginning of treatment - every day, then once every 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).

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, 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 Cordinorm may 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. In contrast to nonselective beta-blockers, it does not substantially increase insulin-induced hypoglycemia and does not delay the recovery of glucose in the blood to normal levels.

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

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 has taken the drug before the surgery, 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 stores (for example, 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 diagnosis of arterial hypotension or bradycardia.

Patients with bronchospastic diseases can be prescribed cardioselective adrenoblockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs, but strict monitoring of dosage should be carried out. Overdosing is dangerous by the development of bronchospasm.

In the case of an increased bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mm Hg) in elderly patients, 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 caused by the use of beta-blockers.

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 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:

For 10 tablets in blisters of PVC / PVDC / aluminum foil or 100 tablets per container of PE.

For 3.6, 9 blisters or 1 container, put in a cardboard box with instructions for use.

Storage conditions:

At a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001043/08

Date of registration:26.02.2008 / 10.01.2018

Expiration Date:Unlimited

The owner of the registration certificate:AKTAVIS GROUP, AO AKTAVIS GROUP, AO Iceland

Manufacturer: & nbsp

CATALENT GERMANY SCHORNDORF, GmbH Germany

Representation: & nbspAktavis, Open Company Aktavis, Open Company

Information update date: & nbsp04.02.2018

Illustrated instructions

Instructions

Cordinorm (Cordinorm)