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, and 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 oxygen demand of the myocardium as a result of a decrease in heart rate and a decrease in contractility, lengthening of the diastole, 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 is 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 antegrade and, to a lesser extent, in retrograde directions via the AV node) and along additional paths.
Unlike non-selective beta-blockers, when prescribed in moderate therapeutic doses, bisoprolol has a less pronounced effect on organs, containing 2-adrenergic receptors (pancreas, skeletal muscle, smooth muscles of the peripheral arteries, bronchi and uterus) and for carbohydrate metabolism, does not cause 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).
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 patients taking Cordinorm, should include monitoring of heart rate and blood pressure (at the beginning of treatment – daily, then 1 time in 3-4 months), ECG, determination of blood glucose in patients with diabetes mellitus (1 time in 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 bpm.
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 the case of elderly patients with increasing bradycardia (less than 50 beats / min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV block bronchospasm, ventricular arrhythmias, severe violations of the liver and kidneys, 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 should be discontinued before examining the blood and urine levels of catecholamines, normetanephrine, vanillin amindolic acid, and antinuclear antibody titers.
Influence on the ability to drive vehicles and control mechanisms
During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities, requiring increased concentration of attention and speed of psychomotor reactions.
Composition
1 tablet contains 10 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
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 From the side of the central nervous system: increased fatigue, weakness, dizziness, headache, drowsiness or insomnia, nightmares, depression, anxiety, confusion or short-term loss of memory, 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, impaired AV conduction (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakened myocardial contractility, development (worsening) of chronic heart failure (ankle swelling) , stop shortness of breath), 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 digestive system: dry mouth, nausea, vomiting, abdominal pain, constipation or diarrhea, impaired liver function (dark urine, yellowness of the sclera or skin, cholestasis), change in liver enzyme activity (increased ALT, ACT), bilirubin content triglycerides, taste changes. From the respiratory system: nasal congestion, difficulty breathing when prescribed in high doses (due to 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: pruritus, rash, urticaria. Dermatological reactions: increased sweating, flushing of the skin, exanthema, psoriasis-like skin reactions, exacerbation of symptoms of psoriasis, alopecia. From the hemopoietic system: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia. From the musculoskeletal system: muscle weakness, cramps in the calf muscles, back pain, arthralgia. From the reproductive system: weakening libido and decreased potency. Other: withdrawal syndrome (increased angina attacks, increased blood pressure). Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia. 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 used together with bisoprolol increase the risk of developing or worsening bradycardia, AV blockade, heart failure 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. Overdose Symptoms: arrhythmia, ventricular extrasystole, pronounced bradycardia, AV blockade, decrease in blood pressure, chronic heart failure, cyanosis of finger nails or palms, difficulty breathing, bronchospasm, headache. Treatment: gastric lavage and the appointment of adsorbing drugs symptomatic therapy: in the developed AV blockade – the introduction of 1-2 mg of atropine, epinephrine (adrenaline) or the setting of a temporary pacemaker for ventricular extrasystole – the introduction of lidocaineA when reducing blood pressure – the patient should be in the position of Trendelenburg if there are no signs of pulmonary edema, plasma replacement solutions should be introduced into / in the case of inefficiency – epinephrine (adrenaline), dopamine, dobutamine (for maintenance of chronotropic and inotropic action and elimination of the expressed decrease in blood pressure) at heart failure – introduction of cardiac glycosides, diuretics, glucagon at convulsions – in / in introduction of diazepam at bronchospasm – inhalation beta-2. Storage Conditions The product should be stored out of the reach of children at a temperature not exceeding 30 ° C. Shelf life 2 years. Deystvuyushtee substance bisoprolol Terms and conditions prescription dosage form tablets Possible product names CORDINORM 0.01 N30 TABLE P / O CORDINORM 0.01 N30 TABLE P / FILM / SHELL Cordinorm 10mg Tab. p / pl / rev X30 (R) Cordinorm 10mg Tab. p / pl / rev X30 (R) /! Until 07.13g / Cordinorm 10mg Tab. captivity. P / o X30do 05.10g. / Katalent Germani Schorndorf GmbH, Germany
