Coronal pills 10 mg 60 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, film composition: 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-induced 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). Increasing the 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 a reciprocal increase in β-adrenoreceptor activity and the removal of β2-adrenoreceptor stimulation), which after 1-3 days returns to its original , and with prolonged administration decreases.; The antihypertensive effect is associated with a decrease in the minute volume of blood, sympathetic stimulation of peripheral vessels, a decrease in the activity of the RAAS (is more important for patients with and Khodnev renin hypersecretion) and central nervous system, reduction of the aortic arch baroreceptor sensitivity (not enhance their activity occurs in response to a decrease in blood pressure) and as a result the decrease of peripheral sympathetic effects. In hypertension, the hypotensive effect develops after 2-5 days, a stable effect after 1-2 months; the anti-anginal 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 of diastole, improvement in myocardial perfusion, and also 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 be increased, especially in patients with chronic heart failure. hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown in AV bridges (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the AV node) and conductivity in additional ways. 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 peripheral arteries, bronchi and uterus) and for carbohydrate metabolism, does not cause a delay of 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; Binding to plasma proteins is about 30%. Permeability through the BBB and placental barrier is low, secretion from breast milk is low.; Metabolism; Metabolized in the liver to form inactive metabolites; Excretion; T1 / 2 - 10-12 h. form), 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 MAO inhibitors(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. With caution, you should prescribe the drug for liver failure, renal failure (CC less than 20 ml / min), metabolic acidosis, pheochromocytoma (with the concomitant use of alpha-blockers), diabetes in stage decompensation, AV blockade I degree, Prinzmetal angina pectoris, restrictive cardiomyopathy, congenital heart defects or valvular heart disease with severe hemodynamic disorders, chronic cardio failure with myocardial infarction during the last 3 months, psoriasis, depression (including 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 age
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 Coronal should be stopped due to 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 severe liver function, the maximum daily dose is 10 mg. Dose adjustment in elderly patients is not required.; Tablets should be taken by mouth 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 reports) .; On the CNS side: infrequently - increased fatigue, asthenia, dizziness, headache, drowsiness or insomnia, depression; rarely - hallucinations, nightmares, convulsions. From the sense organs: rarely - impaired vision, reduced secretion of the tear fluid, dryness and soreness of the eyes, hearing loss; very rarely - conjunctivitis. From the side of 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 susceptible patients - laryngo and bronchospasm; rarely - nasal congestion, allergic rhinitis. From the endocrine system: rarely - hyperglycemia (in patients with type 2 diabetes), hypoglycemia (in patients receiving insulin) .; Allergic reactions: rarely - pruritus, rash, urticaria; side of the skin: rarely - increased sweating, skin flushing; very rarely - psoriasis-like skin reactions, exacerbation of psoriasis symptoms, alopecia.; From the musculoskeletal system: infrequently - muscular weakness, cramps in the gastrocnemius muscles, arthralgia; 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, lowering blood pressure, acute heart failure, acrocyanosis, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.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. When used with Coronal, iodine radiopaque drugs for IV injection increase the risk of anaphylactic reactions. simultaneous use with Coronal phenytoin for intravenous administration, drugs for general inhalation anesthesia (derivatives of hydrocarbons) increase the expression The cardiodepressive effect and the likelihood of a decrease in blood pressure. With simultaneous use, Coronal alters the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure); With simultaneous use, Coronal reduces the clearance of lidocaine and xanthines (except diphillin) and increases them plasma concentration, especially in patients with initially increased clearance of theophylline under the influence of smoking.; NSAIDs (due to the delay of sodium ions and blockade of prostagl synthesis Andina kidneys), corticosteroids and estrogens (due to the delay of sodium ions) weaken the antihypertensive effect of Coronal. With simultaneous use with the Coronal, cardiac glycosides, methyldopa, reserpine and guanfacine, blockers of slow calcium channels (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.; With simultaneous use with Coronal diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure. muscle relaxants and the anticoagulant effect of coumarins.; With simultaneous use with Coronal tricyclic and tetracyclic antidepressants, antipsychotic drugs These drugs (neuroleptics), ethanol, sedatives and hypnotic drugs increase CNS depression, can provoke cardiac rhythm disturbances, bradycardia and orthostatic hypotension. Simultaneous use of Coronal with MAO inhibitors is not recommended due to a significant increase in hypotensive action, a break in treatment between taking MAO inhibitors and Coronal should be at least 14 days.; When used simultaneously with Coronal, nonhydrated ergot alkaloids, ergotamine increase the risk of developing ; When used with Coronal, sulfasalazine increases plasma concentration of bisoprolol.; When used simultaneously with Coronal, rifampicin shortens T1 / 2 of bisoprolol.; There is a potential danger of an additive effect with the development of hypotension and / or significant bradycardia when used together with beta. -adrenergic blockers for topical use (eye drops) .; There is a decrease in the antihypertensive effect of the drug against the use of adrenaline and noradrenaline.; Be An increase in automatism, conductivity and contractility of the heart increases (mutually) during therapy with quinidine drugs (mefloquine, chloroquine) .; In case of shock or arterial hypotension caused by floctafenin, when combined, it is possible to reduce compensatory cardiovascular reactions; baclofen or amifostine also 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).Elderly patients should be monitored for kidney function (1 every 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, it is recommended to conduct a study of respiratory function in patients with a history of bronchopulmonary history; It should be noted that in approximately 20% of patients with angina pectoris, beta-adrenergic blockers are ineffective due to severe coronary atherosclerosis with a low ischemia threshold (HR less than 100 beats / min) and of the inferior diastolic volume of the left ventricle, which violates the subendocardial blood flow.; In smoking patients, the effectiveness of beta-adrenergic blockers decreases.; Patients using contact lenses should take into account that with the treatment, a reduction in the production of tear fluid is possible. risk of development of paradoxical arterial hypertension (unless effective alpha adrenergic blockade is previously achieved); Bisoprolol may mask certain clinical s symptoms of hyperthyroidism (e.g., tachycardia). Abrupt cancellation of Coronal in patients with thyrotoxicosis is contraindicated because it can enhance the symptoms of the disease. In diabetes mellitus, bisoprolol can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-adrenergic blockers, the insulin-induced hypoglycemia practically does not increase and does not delay the restoration of glucose concentration in the blood to a normal level. With simultaneous use with clonidine, the latter can be stopped only a few days after discontinuation of the Coronal drug. hypersensitivity and lack of effect from the usual doses of epinephrine on the background of the burdened allergic history. If necessary, conduct a plan In a new 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 effect.; The reciprocal activation of the vagus nerve can be eliminated by intravenous administration of atropine (1-2 mg). Drugs that reduce catecholamine stores (in . h.reserpine), 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. the ineffectiveness of other antihypertensive drugs. Overdose is dangerous for the development of bronchospasm.; In the case of elderly patients, increasing bradycardia (less than 50 beats / min), pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV blockade, reduce the dose or stop treatment .; It is recommended to stop therapy in case of depression.; The drug should be discontinued before conducting a study of catecholamines, normetanephrine, vanillimindal acid, and antinuclear antibody titers in blood and urine; 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; Use of the drug Coronal in children and adolescents under the age of 18 years is contraindicated, because efficacy and safety have not been established.; Impact on ability to drive motor vehicles and control mechanisms; During the period of treatment, care must be taken when driving motor vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor reactions.