Cordinorm pills 5 mg 90 pcs
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Active ingredients
Bisoprolol
Release form
Pills
Composition
Bisoprolol fumarate 5 mg adjuvants: 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.
Pharmacological effect
Selective beta1-adrenergic blocker without internal sympathomimetic activity and membrane stabilizing properties. By blocking the β1-adrenoreceptors of the heart in low doses, bisoprolol reduces catecholamine-stimulated cAMP formation from ATP and reduces the intracellular flow of calcium ions. It has a negative chrono-, dromo-, batmo-and inotropic effect, inhibits conductivity and excitability, slows down AV conduction, reduces myocardial need for oxygen. Reduces heart rate at rest and under load. Reduces the activity of plasma renin. It has a hypotensive, antiarrhythmic and antianginal effect. When the dose is increased, bisoprolol has a beta2-adrenoceptor blocking effect. At the beginning of the drug use (in the first 24 hours), as a result of the reciprocal increase in α-adrenoreceptor activity and the elimination of stimulation of β2-adrenoreceptor OPSS increases. After 1-3 days OPSS returns to baseline, and decreases with long-term use. 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 (important for patients with initial renin hypersecretion), and recovery 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 action 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, lengthening diastole, and an 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. The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased sympathetic nervous system activity,increased cAMP, arterial hypertension), as well as a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown of AV conduction (mainly in antegrade and, to a lesser extent, in retrograde directions through the AV node) and along additional paths. non-selective beta-adrenergic blockers, when administered in moderate therapeutic doses, bisoprolol has a less pronounced effect on organs containing β2-adrenoreceptors (pancreas, skeletal muscle, smooth muscle tour of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause sodium retention in the body. The severity of the atherogenic action does not differ from the action of propranolol. When used in large doses, it has a blocking effect on both subtypes of β-adrenoreceptors.
Pharmacokinetics
AbsorptionAfter taking the drug inside of the gastrointestinal tract, 80-90% of bisoprolol is absorbed. Reception simultaneously with food does not affect absorption. Cmax in plasma is reached after 1-3 hours. The distribution of plasma plasma binding is about 35%. The permeability through the BBB and the placental barrier, as well as the degree of penetration into breast milk, is low. Metabolism and excretion of 50% of the dose taken is metabolized in the liver to form inactive metabolites. 50% is excreted unchanged. T1 / 2 is 9-12 hours. About 98% of the substance is excreted by the kidneys, less than 2% is with bile.
Indications
- arterial hypertension; - ischemic heart disease (prevention of strokes).
Contraindications
- shock (including cardiogenic); - collapse; - pulmonary edema; - acute heart failure; - chronic heart failure in the decompensation stage; - AV block II and III degree (without pacemaker); - sinoatrial blockade; - SSS - severe bradycardia (heart rate <50 beats / min); - Prinzmetal angina; - cardiomegaly (without signs of heart failure); - arterial hypotension (systolic blood pressure <100 mmHg, especially myocardial infarction); - bronchial asthma and history of COPD - simultaneous administration of MAO inhibitors (with the exception of type B MAO); - n zdnie stage peripheral circulatory disorders; - Raynaud's disease; - pheochromocytoma (without simultaneous application of alpha-blockers) - metabolic acidosis; - childhood and adolescence to 18(efficacy and safety have not been established); - hypersensitivity to other beta-blockers; - hypersensitivity to components of the drug. The drug should be prescribed with caution in liver failure, chronic renal failure, myasthenia, thyrotoxicosis, diabetes mellitus, AV-blockade of I degree , depression (including history), psoriasis, elderly patients.
Precautionary measures
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
Use during pregnancy and lactation is possible if the potential benefits for the mother outweigh the risk of side effects in the fetus and child.
Dosage and administration
The drug is taken orally, in the morning, on an empty stomach. Tablets should be swallowed whole, without chewing. A single dose is 2.5-5 mg. Usually 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 hepatic or renal function of mild or moderate degree usually does not require dose adjustment. In patients with severe impaired renal function (CC <20 ml / min) or liver, the maximum daily dose is 10 mg. In elderly patients, dose adjustment is not required.
Side effects
On the part of 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,paresthesias in the extremities (in patients with intermittent claudication and Raynaud's syndrome), tremor. For the sense organs: impaired vision, reduced secretion of the tear fluid, dryness and soreness of the eyes, conjunctivitis. For the cardiovascular system: sinus bradycardia, palpitations, disturbance myocardial conduction, impaired AV conduction (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakening of myocardial contractility, development (aggravation) of chronic heart failure (edema ankles, feet; shortness of breath), decrease in blood pressure, orthostatic hypotension, manifestation of angiospasm (increased disturbance of peripheral circulation, cooling of the lower extremities, Raynaud’s syndrome), chest pain. From the alimentary system: dry mouth, nausea, vomiting, abdominal pain, constipation or diarrhea, abnormal liver function (dark urine, jaundice of the sclera or skin, cholestasis), changes in the activity of liver enzymes (increased ALT, ACT), bilirubin, triglycerides, changes in taste. On the part of the respiratory system: nasal congestion, ore respiration when prescribed in high doses (due to loss of selectivity) and / or in susceptible patients - laryngo- and bronchospasm. From the endocrine system: hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid state. Allergic reactions: pruritus, rash, urticaria. Dermatological reactions: increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions, exacerbation of symptoms of psoriasis, alopecia. rhenium: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia. On the side of the musculoskeletal system: muscle weakness, cramps in the gastrocnemius muscles, back pain, arthralgia. On the part of the reproductive system: weakening of the libido and reduction of potency. (increased angina attacks, increased blood pressure). Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.
Overdose
Symptoms: arrhythmia, ventricular premature beats, severe bradycardia, AV blockade, decreased blood pressure, chronic heart failure, finger nail or palm nail cyanosis, difficulty breathing, bronchospasm,dizziness, fainting, convulsions. Treatment: gastric lavage and prescription of absorbent drugs; symptomatic therapy: in case of the developed AV blockade - in / in the introduction of 1-2 mg of atropine, epinephrine (adrenaline) or staging a temporary pacemaker; for ventricular extrasystole - the introduction of lidocaine (class IA drugs are not used); with a decrease in blood pressure - the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema, plasma-substituting solutions should be administered intravenously, with ineffectiveness - administration of epinephrine (adrenaline), dopamine, dobutamine (to maintain chronotropic and inotropic action and eliminate marked reduction in blood pressure); in heart failure - the introduction of cardiac glycosides, diuretics, glucagon; with convulsions - in / in the introduction of diazepam; with bronchospasm - inhalation beta2-adrenostimulyatory.
Interaction with other drugs
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 radiopaque drugs for i / v administration increase the risk of anaphylactic reactions. drugs for general inhalation anesthesia (derivatives of hydrocarbons) increase the severity of the cardiodepressive effect and the likelihood of a decrease in blood pressure. Changes in bisoprolol alters 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 difillin) and increases their concentration in plasma, especially in patients with initially increased clearance of teofilin and increases their plasma concentration, especially in patients with initially elevated clearance of teofilin the influence of smoking. The antihypertensive effect of the drug when used together weakens NSAIDs (due to the delay of sodium ions and the blockade of prostaglandin synthesis by the kidneys), GCS and trogens (due to sodium ion retention). 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, stopping heart and heart failure. With simultaneous use of nifedipine can lead to a significant decrease in blood pressure. Diuretics, clonidine, sympatholytics,hydralazine and other antihypertensive drugs with simultaneous use may lead to an excessive decrease in blood pressure. . It is not recommended simultaneous use with MAO inhibitors due to a significant increase in hypotensive o action, a break in treatment between taking MAO inhibitors and bisoprolol should be at least 14 days. When used together, dehydrated ergot alkaloids increase the risk of developing peripheral circulation disorders. Ergotamine when used together increases the risk of developing peripheral circulation disorders. Sulfasalazine increases plasma concentration of bisoprolol. Rifampicin with the simultaneous use shortens T1 / 2 bisoprolol.
special instructions
The patient should know that they should not abruptly interrupt the treatment or change the recommended dose without first consulting with the doctor. Control of patients taking Cordinorm should include monitoring of heart rate and blood pressure (at the beginning of treatment - daily, then every 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). Patients should be trained in how to calculate heart rate and instruct on the need for medical consultation with heart rate less than 50 beats / min. Before starting treatment in patients with a history of broncho-pulmonary history It is recommended to conduct a study of respiratory function. Approximately in 20% of patients with angina, beta-blockers are ineffective. The main reasons for this are severe coronary atherosclerosis with a low ischemia threshold (HR less than 100 beats / min) and an increased end diastolic volume of the left ventricle that violates subendocardial blood flow. In tobacco smoking, the effectiveness of beta-adrenergic blockers is lower. Patients using contact lenses should consider that against the background of treatment, there may be a decrease in the production of tears. When using Cordinorm, patients with pheochromocytoma have a riskdevelopment of paradoxical arterial hypertension (if effective alpha-adrenergic blockade is not previously achieved). In patients with thyrotoxicosis, Cordinorm may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated because it can enhance symptoms. In diabetes mellitus, the effect of bisoprolol may mask tachycardia caused by hypoglycemia. Unlike non-selective beta-adrenergic blockers, Cordinorm practically does not increase insulin-induced hypoglycemia and does not delay the restoration of glucose in the blood to a normal level. With simultaneous treatment with clonidine, its administration can be stopped only a few days after canceling Cordinorm. lack of effect from the usual doses of epinephrine (adrenaline) on the background of the burdened allergological history. If it is necessary to conduct a planned surgical treatment, the drug is discontinued 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 activation of the vagus nerve can be eliminated by introducing atropine (1-2 mg). Drugs that reduce catecholamine stores (eg, reserpine ), can enhance the action of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision for arterial ipotenzii or bradikardii.Bolnym with bronhospasticheskimi diseases cardioselective blockers may be administered in case of intolerance and / or ineffectiveness of other antihypertensive drugs, but it should strictly control the dose. Overdose is dangerous for the development of bronchospasm. In the case of elderly patients, increasing bradycardia (less than 50 beats / min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe hepatic and renal dysfunction should be reduced. or discontinue treatment. It is recommended to discontinue therapy in the development of depression caused by taking beta-blockers. You can not abruptly interrupt treatment because of the risk of 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 canceled before the study of the content in the blood and urine of catecholamines, normetanephrine, vanillin-alindic acid, titers of antinuclear antibodies. The effect on the ability to Driving and controlling machinery During the period of treatment, care must be taken when driving and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed reactions.