Coronal pills 10 mg 30 pcs
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Active ingredients
Bisoprolol
Release form
Pills
Composition
Bisoprolol fumarate 10 mg; excipients: microcrystalline cellulose - 128 mg, corn starch - 7.5 mg, sodium lauryl sulfate - 1 mg, colloidal silicon dioxide - 2 mg, magnesium stearate - 1.5 mg. the composition of the film shell: hypromellose - 6.4 mg, macrogol 400 - 1.28 mg, titanium dioxide - 2.3 mg, iron dye red oxide (e172) - 0.02 mg.
Pharmacological effect
Selective beta1-blocker. Reduces plasma renin activity, reduces myocardial oxygen demand, reduces heart rate (at rest and under load). It has antihypertensive, antiarrhythmic and antianginal effects. By blocking β1-adrenoreceptors of the heart in low doses, it reduces catecholamine-stimulated cAMP formation from ATP, reduces the intracellular current of calcium ions, has a negative chrono-dromo, batmoy and inotropic effect (reduces heart rate, inhibits conductivity and excitability, reduces myocardial contractility). With increasing dose has a beta2-adrenoblokiruyuschee effect .; OPSS at the beginning of the drug, in the first 24 hours after ingestion, increases (as a result of the reciprocal increase in β-adrenoreceptor activity and the elimination of stimulation of β2-adrenoreceptors), which after 1-3 days returns to baseline, and with prolonged administration decreases .; The antihypertensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in RAAS activity (is more important for patients with initial renin hypersecretion) and the central nervous system, the restoration of aortic baroreceptor sensitivity (their activity does not increase in response to a decrease in blood pressure) and result in a decrease in peripheral sympathetic influences. In hypertension, the hypotensive effect develops in 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, a prolongation of diastole, an improvement in myocardial perfusion, and a decrease in myocardial sensitivity to the effects of sympathetic innervation. Reduces the number and severity of angina attacks and increases exercise tolerance.By increasing the end-diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, oxygen demand may increase, 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 content, arterial hypertension), a decrease in the rate of spontaneous stimulation of sinus and ectopic pacemakers, and a slower AV conduction through the AV node) and conduction along additional paths .; When used in moderate therapeutic doses, unlike non-selective beta-blockers, it has a less pronounced effect on organs containing β2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of the peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause a delay sodium ions in the body. When used in high doses (200 mg or more), it has a blocking effect on both subtypes of β-adrenoreceptors, mainly in the bronchi and vascular smooth muscles.
Pharmacokinetics
Absorption; Absorption is 80-90%, food intake does not affect absorption. Cmax in plasma is observed after 1-3 hours; Distribution; Plasma protein binding is about 30%. The permeability through the BBB and the placental barrier is low, the secretion from breast milk is low .; Metabolism; Metabolized in the liver to form inactive metabolites .; Withdrawal; T1 / 2 - 10-12 h. About 98% is excreted by the kidneys (50% - unchanged), less than 2% is excreted in the bile.
Indications
- arterial hypertension; - CHD: prevention of strokes.
Contraindications
- shock (including cardiogenic); - acute heart failure; - chronic heart failure in the stage of decompensation; - AV blockade of II and III degree (without artificial pacemaker); - sinoatrial block; - SSSU; - severe bradycardia; - Cardiomegaly (without signs of heart failure); - arterial hypotension (systolic blood pressure below 100 mm Hg, especially in myocardial infarction); - bronchial asthma and chronic obstructive pulmonary disease in history; - simultaneous administration of inhibitorsMAO (with the exception of inhibitors of MAO type B); - concomitant use of floctafenin and sultopride; - late stages of impaired peripheral circulation; - Raynaud's disease; - lactation period; - age up to 18 years (efficacy and safety have not been established); - hypersensitivity to the components of the drug and other beta-blockers .; Precautions should be prescribed for liver failure, renal failure (CC less than 20 ml / min), metabolic acidosis, pheochromocytoma (with the concomitant use of alpha blockers), diabetes mellitus in the stage of decompensation, AV blockade of I degree, Prinzmetal angina, restrictive cardiomyopathy , congenital heart defects or valvular heart disease with severe hemodynamic disorders, chronic heart failure with myocardial infarction during the last 3 months, psoriasis, depression ai (including in history), severe allergic reactions in history, during pregnancy, with a strict diet, carrying out desensitizing immunotherapy with allergens and allergen extracts, as well as elderly patients.
Use during pregnancy and lactation
In pregnancy, Coronal is prescribed only under strict indications if the intended benefit to the mother outweighs the potential risk to the fetus. 72 hours before delivery, taking the drug Coronal must be discontinued due to the possible development of fetal / newborn bradycardia, hypotension, hypoglycemia and respiratory depression .; If taking Coronal is necessary during lactation, breastfeeding should be stopped .; When taking bisoprolol during pregnancy, the fetus may have intrauterine growth retardation, hypoglycemia, bradycardia.
Dosage and administration
In hypertension and coronary heart disease (prevention of attacks of stable angina), the initial dose is 2.5-5 mg 1 time / day. If necessary, increase the dose to 10 mg 1 time / day. The maximum daily dose is 20 mg. In patients with impaired renal function with CC <20 ml / min or with severe impaired liver function, the maximum daily dose is 10 mg. Dose adjustment in elderly patients is not required .; Tablets should be taken orally, in the morning on an empty stomach, without chewing, with a small amount of liquid.
Side effects
The frequency of occurrence of side effects is determined as follows: very often (≥1 / 10), often (≥1 / 100 and <1/10), infrequently (≥1 / 1000 and <1/100), rarely (≥1 / 10 000 and <1/1000), very rarely (<1/10 000, including individual communications) .; From the side of the central nervous system: infrequently - increased fatigue, asthenia, dizziness, headache, drowsiness or insomnia, depression; rarely - hallucinations, nightmares, convulsions .; On the part of the senses: rarely - impaired vision, reduced secretion of the tear fluid, dry and sore eyes, impaired hearing; conjunctivitis is very rare; Since the cardiovascular system: very often - sinus bradycardia; often - reduction of blood pressure, manifestation of angiospasm (increased disturbance of peripheral circulation, cooling of the lower extremities, paresthesia); rarely - a violation of AV-conduction, orthostatic hypotension, decompensation of chronic heart failure, peripheral edema .; On the part of the digestive system: often - dryness of the oral mucosa, nausea, vomiting, diarrhea, constipation; rarely - hepatitis, increased activity of hepatic transaminases .; On the part of the respiratory system: infrequently - difficulty in breathing when administered in high doses (loss of selectivity) and / or in predisposed patients - laryngitis and bronchospasm; rarely nasal congestion, allergic rhinitis .; On the part of the endocrine system: rarely - hyperglycemia (in patients with type 2 diabetes), hypoglycemia (in patients receiving insulin) .; Allergic reactions: rarely - pruritus, rash, urticaria .; For the skin: rarely - increased sweating, skin flushing; very rarely - psoriasis-like skin reactions, exacerbation of the symptoms of psoriasis, alopecia .; On the part of the musculoskeletal system: infrequently - muscular weakness, cramps in the calf muscles, arthralgia .; From the side of blood-forming organs: in some cases - thrombocytopenia, agranulocytosis .; Other: very rarely - a violation of potency; rarely - hypertriglyceridemia, "withdrawal" syndrome (increased angina pectoris attacks, increased blood pressure).
Overdose
Symptoms: arrhythmia, ventricular premature beats, severe bradycardia, AV blockade, decreased blood pressure, acute heart failure, acrocyanosis, difficulty breathing, bronchospasm, dizziness, fainting, convulsions .; Treatment: it is necessary to wash the stomach and prescribe adsorbing drugs.Symptomatic therapy is carried out: with advanced AV-blockade - in / in the introduction of 1-2 mg of atropine, epinephrine or staging of a temporary pacemaker; with ventricular extrasystole - in / in lidocaine (I class A drugs do not apply); with a decrease in blood pressure, the patient should be in the Trendelenburg position; in the absence of symptoms of pulmonary edema - in / in plasma-substituting solutions, with the ineffectiveness - the introduction of epinephrine, dopamine, dobutamine (to maintain chrono-and inotropic action and eliminate pronounced decrease in blood pressure); in heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam; with bronchospasm - beta2-adrenostimulators inhalation.
Interaction with other drugs
Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol .; With simultaneous use with Coronal iodine-containing radiopaque drugs for intravenous administration increase the risk of anaphylactic reactions .; With simultaneous use with Coronal phenytoin for IV administration, drugs for general inhalation anesthesia (hydrocarbon derivatives) increase the severity of the cardiodepressant effect and the likelihood of a decrease in blood pressure .; With the simultaneous use of Coronal changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure) .; With the simultaneous use of Coronal reduces the clearance of lidocaine and xanthines (except for difillina) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking .; NSAIDs (due to the delay of sodium ions and the blockade of prostaglandin synthesis by the kidneys), GCS and estrogens (due to the delay of sodium ions) weaken the anti-hypertensive effect of Coronal .; When used simultaneously with the coronal 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 .; With simultaneous use with Coronal nifedipine can lead to a significant decrease in blood pressure .; When used simultaneously with Coronal diuretics, clonidine, sympatholytic, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure .; Coronal lengthens the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins .; When used simultaneously with the coronal, tricyclic and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics increase the inhibition of the central nervous system, can trigger heart rhythm disorders, bradycardia and orthostatic hypotension .; The simultaneous use of Coronal with MAO inhibitors due to a significant increase in the hypotensive effect is not recommended; the treatment gap between taking MAO and Coronal inhibitors should be at least 14 days .; When used simultaneously with the Coronal, nonhydrated ergot alkaloids, ergotamine increase the risk of developing peripheral circulatory disorders .; With simultaneous use with Coronal sulfasalazine increases the concentration of bisoprolol in the plasma .; When applied simultaneously with the coronal rifampicin shortens T1 / 2 bisoprolol .; There is a potential danger of an additive effect with the development of hypotension and / or significant bradycardia, when used together with beta-blockers for topical use (eye drops) .; There is a decrease in the antihypertensive effect of the drug against the use of adrenaline and noradrenaline .; The likelihood of violations of automatism, conduction and contractility of the heart increases (mutually) during therapy with quinidine drugs (mefloquine, chloroquine) .; In the case of shock or arterial hypotension caused by floctafenin, when used together, it is possible to reduce compensatory cardiovascular reactions .; With simultaneous use with baclofen or amifostine, there is also an increased antihypertensive effect.
special instructions
When prescribing Coronal, one should regularly monitor heart rate and blood pressure (at the beginning of treatment - daily, then - once every 3-4 months), conduct an ECG, determine the level of glucose in the blood of 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 counting heart rate and instructed on the need for medical consultation with a heart rate less than 50 bpm; Before starting treatment, it is recommended to conduct a study of the function of external respiration in patients with a burdened bronchopulmonary history. It should be borne in mind that in approximately 20% of patients with stenocardia, beta-adrenergic blockers are ineffective due to 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 the subendocardial blood flow .; In smoking patients, the effectiveness of beta-blockers decreases .; Patients using contact lenses should take into account that a decrease in the production of tear fluid is possible during treatment .; When using Coronal, patients with pheochromocytoma are at risk of developing paradoxical hypertension (unless effective alpha-adrenoblockade is previously achieved) .; Bisoprolol may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt cancellation of Coronal in patients with thyrotoxicosis is contraindicated, as it can enhance the symptoms of the disease .; In case of diabetes mellitus, bisoprolol may mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the recovery of glucose concentration in the blood to normal levels .; With simultaneous use with clonidine, the latter can be discontinued only a few days after discontinuation of the drug Coronal .; Perhaps the increased severity of hypersensitivity reactions and the lack of effect from the usual doses of epinephrine on the background of burdened allergological anamnesis .; 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 the operation, he should choose a drug for general anesthesia with minimal negative inotropic effects .; Reciprocal activation of the vagus nerve can be eliminated by / in the introduction of atropine (1-2 mg) .; Drugs that reduce the supply of catecholamines (includingreserpine), can enhance the action of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect pronounced decrease in blood pressure or bradycardia .; Patients with concomitant bronchospastic diseases can be prescribed cardioselective blockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs. Overdose is dangerous for the development of bronchospasm .; In the case of elderly patients with increasing bradycardia (less than 50 beats / min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV blockade, reduce the dose or discontinue treatment .; It is recommended to discontinue therapy in the development of depression .; The drug should be discontinued before conducting a study of the content in the blood and urine of catecholamines, normetanephrine, vanillimindal acid, and titers of antinuclear antibodies .; You can not abruptly interrupt treatment because of the danger of severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose for 2 weeks or more (the dose is reduced by 25% in 3-4 days) .; Use in pediatrics; The use of the drug Coron in children and adolescents under the age of 18 years is contraindicated, because efficacy and safety not established .; Influence on the ability to drive vehicles and control mechanisms; During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.