Description
Release form
Film-coated tablets.
Packing
30 pcs.
Pharmacological action
Selective beta1-blocker without internal sympathomimetic activity and membrane-stabilizing properties. By blocking in low doses the 1-adrenergic receptors of the heart, bisoprolol reduces the formation of cAMP stimulated by catecholamines from ATP, and reduces the intracellular flow of calcium ions. It has a negative chrono-, dromo-, batmo- and inotropic effect, inhibits conduction and excitability, slows down AV-conduction, reduces myocardial oxygen demand. Reduces heart rate at rest and during exercise. Reduces blood plasma renin activity. It has hypotensive, antiarrhythmic and antianginal effects.
With increasing doses, bisoprolol has a beta2-blocking effect.
At the beginning of the drug administration (in the first 24 hours), as a result of a reciprocal increase in the activity of -adrenoreceptors and the elimination of stimulation of 2-adrenoreceptors, OPSS slightly increases. After 1-3 days, OPSS returns to its original level, and with prolonged use it decreases.
The hypotensive effect of bisoprolol is due to a decrease in IOC, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (of great importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure and effects on the central nervous system. 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 decreased heart rate and reduced contractility, lengthening of diastole, and improved myocardial perfusion. By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, it can increase the need for oxygen, especially in patients with chronic heart failure.
Antiarrhythmic effect due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased content of cAMP, arterial hypertension), as well as a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown in AV conduction (mainly in the antegrade and, to a lesser extent, retrograde directions through the AV node) and along additional paths.
Unlike non-selective beta-blockers, when prescribed at moderate therapeutic doses, bisoprolol has a less pronounced effect on organs containing 2-adrenergic receptors (pancreas, skeletal muscle, smooth muscles of peripheral arteries, bronchi and uterus) and does not cause carbohydrate metabolism sodium retention in the body. The severity of the atherogenic effect does not differ from the action of propranolol.
When used in large doses, it has a blocking effect on both subtypes of -adrenoreceptors.
Indications
Arterial hypertension
ischemic heart disease (prevention of angina attacks).
Contraindications
Hypersensitivity to bisoprolol or to any of the components of Cordinorm, other beta-blockers of
shock (including cardiogenic)
collapse
pulmonary edema
acute heart failure
chronic heart failure decompensation stage
AV block 2 ² 3 degrees (without pacemaker)
sinoatrial block
sinus syndrome srdlrdkrd cardiomyopathy sardlrdkrd cardiac heart failure)
arterial hypotension (SBP
asthma and COPD with a history of
concurrent administration of MAO inhibitors (except MAO-B)
late stage impaired I
peripheral circulatory Raynaud
pheochromocytoma (without the simultaneous use of alpha-blockers)
metabolic acidosis
age of 18 years (effectiveness and safety have been established). cardiogenic)
collapse
pulmonary edema
acute heart failure
chronic heart failure decompensation stage
AV block 2 ² 3 degrees (without pacemaker)
sinoatrial block
sinus syndrome srdlrdkrd cardiomyopathy sardlrdkrd cardiac heart failure)
arterial hypotension (SBP
asthma and COPD with a history of
concurrent administration of MAO inhibitors (except MAO-B)
late stage impaired I
peripheral circulatory Raynaud
pheochromocytoma (without the simultaneous use of alpha-blockers)
metabolic acidosis
age of 18 years (effectiveness and safety have been established).
Use during pregnancy and lactation
Use of Cordinorm during pregnancy and breastfeeding is possible if the benefit to the mother outweighs the risk of side effects in the fetus and the baby.
Special instructions
The patient should be aware that treatment should not be abruptly interrupted or the recommended dose should be changed without first consulting a doctor.
Monitoring of patients taking Cordinorm should include monitoring for heart rate and blood pressure (at the beginning of treatment daily, then 1 time every 3-4 months), an ECG, determination of blood glucose in patients with diabetes mellitus (1 time every 4-5 months ) In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months).
The patient should be trained in the method of calculating heart rate and instructed on the need for medical advice for heart rate less than 50 beats / min.
Before starting treatment in patients with a burdened bronchopulmonary history, it is recommended to study the function of external respiration.
In approximately 20% of patients with angina pectoris, beta-blockers are ineffective. The main reasons for this are severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 beats / min) and an increased final diastolic volume of the left ventricle, which violates the subendocardial blood flow.
When smoking, the effectiveness of beta-blockers is lower.
Patients using contact lenses should consider that tear fluid production may be reduced during treatment.
When using Cordinorm in patients with pheochromocytoma, there is a risk of developing paradoxical hypertension (unless effective alpha-adrenoblockade is previously achieved).
In patients with thyrotoxicosis, Cordinorm may mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated, since it can enhance the symptoms.
In diabetes mellitus, the effect of bisoprolol may mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, Cordinorm practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal levels.
With simultaneous treatment with clonidine, its administration can be stopped only a few days after the cancellation of Cordinorm.
It is possible to increase the severity of the hypersensitivity reaction and the lack of effect of the usual doses of epinephrine (adrenaline) against the background of a burdened allergic history. If it is necessary to carry out planned surgical treatment, drug withdrawal is carried out 48 hours before the start of general anesthesia. If the patient took the drug before surgery, he should choose a drug for general anesthesia with a minimally negative inotropic effect.
Reciprocal vagus nerve activation can be eliminated iv by administration of atropine (1-2 mg).
Medicines that reduce catecholamine stores (for example, reserpine) can enhance the effect of beta-blockers, so patients taking these combinations of drugs should be under constant medical supervision to detect arterial hypotension or bradycardia.
Patients with bronchospastic diseases can be prescribed cardioselective adrenergic blockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs, but the dose should be strictly monitored. An overdose is dangerous for the development of bronchospasm. In case of increasing bradycardia (less than 50 beats / min) in elderly patients, arterial hypotension (systolic blood pressure below 100 mm Hg), AV block, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunctions, it is necessary to reduce the dose or stop treatment.
It is recommended that therapy be discontinued in the event of development of depression caused by beta-blockers.
Do not abruptly interrupt treatment because of the danger of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose for 2 weeks or more (reduce the dose by 25% in 3-4 days).
The drug Cordinorm should be discontinued before examining the blood and urine levels of catecholamines, normetanephrine, vanillyl mindic acid, and antinuclear antibody titers.
Effect on the ability to drive vehicles and control mechanisms
During treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.
Composition
1 tablet contains 5 mg bisoprolol fumarate.
Excipients: microcrystalline cellulose – 21.1 mg, mannitol – 148.5 mg, croscarmellose sodium – 1.8 mg, magnesium stearate – 3.6 mg, hypromellose – 2.19 mg, titanium dioxide – 0.88 mg, macrogol 6000 – 0.53 mg.
Dosage and administration of
The drug is taken orally, in the morning, on an empty stomach. The tablets should be swallowed whole without chewing.
A single dose is 2.5-5 mg. Typically, the initial dose is 5 mg 1 time / day. If necessary, increase the dose to 10 mg 1 time / day. The maximum daily dose for adults is 20 mg.
Treatment of patients with impaired liver or kidney function of mild or moderate degree usually does not require dose adjustment. In patients with severe renal impairment (CC <20 ml / min) or liver, the maximum daily dose is 10 mg. In elderly patients, dose adjustment is not required. Side effects of the From the nervous system: increased fatigue, weakness, dizziness, headache, drowsiness or insomnia, nightmare dreams, 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 sensory organs: impaired vision, decreased secretion of lacrimal fluid, dry and sore eyes, conjunctivitis. From the cardiovascular system: sinus bradycardia, palpitations, impaired myocardial conduction, AV block (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakened myocardial contractility, development (worsening) of chronic heart failure, decreased blood pressure, orthostatic hypotension , the manifestation of angiospasm (increased impairment of peripheral circulation, cooling of the lower extremities, Raynaud’s syndrome), chest pain. From the gastrointestinal tract: dry oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, impaired liver function (dark urine, yellowness of sclera or skin, cholestasis), changes in taste. From the respiratory system: nasal congestion, difficulty breathing when prescribed in high doses (loss of selectivity) and / or in predisposed patients – laryngo- and bronchospasm. From the endocrine system: hyperglycemia (in patients with non-insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid state. Allergic reactions: itching, rash, urticaria. From the skin: increased sweating, flushing of the skin, exanthema, psoriasis-like skin reactions, exacerbation of the symptoms of psoriasis, alopecia. Laboratory indicators: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, changes in enzyme activity, bilirubin and triglycerides. Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia. From the musculoskeletal system: muscle weakness, cramps in the calf muscles. Other: back pain, arthralgia, rarely decreased libido – decreased potency, withdrawal syndrome (increased angina attacks, increased blood pressure). Drug Interactions In patients receiving bisoprolol, allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis. Iodine-containing radiopaque drugs for iv administration increase the risk of anaphylactic reactions. Phenytoin with iv administration and drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of the cardiodepressive effect and the likelihood of a decrease in blood pressure. When used together, bisoprolol changes the effectiveness of insulin and oral hypoglycemic agents, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure). With simultaneous use, bisoprolol reduces the clearance of lidocaine and xanthines (except diphillin) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking. The antihypertensive effect of the drug when used together weaken NSAIDs (due to delayed sodium ions and blockade of prostaglandin synthesis by the kidneys), GCS and estrogens (due to delayed sodium ions). Cardiac glycosides, methyldopa, reserpine and guanfacine, slow calcium channel blockers (verapamil, diltiazem), Amiodarone and other antiarrhythmic drugs when combined with bisoprolol increase the risk of developing or exacerbating bradycardia, AV blockade, cardiac arrest and heart failure. With the simultaneous use of nifedipine can lead to a significant decrease in blood pressure. Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs with simultaneous use can lead to an excessive decrease in blood pressure. Cordinorm prolongs the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins. Tricyclic and tetracyclic antidepressants, antipsychotics (antipsychotics), ethanol, sedatives and hypnotics increase the inhibitory effect of bisoprolol on the central nervous system. The simultaneous use with MAO inhibitors is not recommended due to a significant increase in the antihypertensive effect, the break in treatment between taking MAO inhibitors and bisoprolol should be at least 14 days. Non-hydrogenated ergot alkaloids when used together increase the risk of peripheral circulation disorders. Ergotamine when used together increases the risk of developing peripheral circulatory disorders. Sulfasalazine increases the concentration of bisoprolol in plasma. Rifampicin, while used, shortens T1 / 2 of bisoprolol. Storage Conditions The product should be stored out of the reach of children at a temperature not exceeding 30 ° C. Shelf life 2 years. Active substance bisoprolol Terms and conditions prescription dosage form tablets Possible product names CORDINORM 0.005 N30 TABLE P / O CORDINORM 0.005 N30 TABLE P / FILM / SHELL Cordinorm 5mg Tab. p / pl / rev X30 (R) Kordinorm tab p / o 5mg x 30 CORDINORM TAB. P.P.O. 5MG No. 30 Katalent Germani Schorndorf GmbH, Germany
