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Active ingredients
Bisoprolol
Release form
Pills
Composition
Active ingredient: Bisoprolol fumarat Concentration of active ingredient (mg): 5
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). 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 α-adrenoreceptor activity and removal of β2-adrenoreceptor stimulation), which after 1-3 days returns to its original , and with long-term 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 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 of diastole, improvement in myocardial perfusion, and also a decrease in myocardial sensitivity to 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 activity of the sympathetic nervous system, increased cAMP, arterial hypertension ),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, in retrograde directions through the AV node) and conduction along additional paths. When used in moderate therapeutic doses, unlike non-selective beta -adrenoblockers, has a less pronounced effect on organs containing β2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate exchange, does not cause the 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 the blood 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 of T1 / 2 is 10–12 h. Excreted by the kidneys about 98% (50% - unchanged), less than 2% excreted 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; - sinoatrial blockade; - SSSU; - severe bradycardia - angiospastic stenocardia (Prinzmetal's stenocardia); - 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 reception inhibitor s of MAO (with the exception of inhibitors of MAO type B); - late stages of impaired peripheral circulation; - Raynaud's disease; - pheochromocytoma (without simultaneous use of alpha-blockers); - metabolic acidosis; - age up to 18 years (efficacy and safety not established); - hypersensitivity to the components of the drug and other beta-blockers.
Precautionary measures
Do not exceed the recommended dose. 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 mellitus in the stage of decompensation, AV-blockade of I degree, Prinzmetal angina pectoris, restrictive cardiomyopathy, congenital heart defects or valvular heart disease with severe hemodynamic disorders, chronic heart failure with myocardial infarction during Lednov 3 months, psoriasis, depression (including history), severe allergic reactions in history, pregnancy, subject to a strict diet, conducting desensitizing immunotherapy 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 Coronal should be discontinued due to possible development of fetal / newborn bradycardia, hypotension, hypoglycemia and respiratory depression. If Coronal is needed during lactation, breastfeeding should be stopped. When taking bisoprolol during pregnancy, the fetus possible intrauterine growth retardation, hypoglycemia, bradycardia.
Dosage and administration
The drug is administered orally at 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. Tablets should be taken in the morning on an empty stomach without chewing.
Side effects
The frequency of occurrence of side effects is determined as follows: very often (≥1 / 10), often (≥1/100 and On the part of the central nervous system and peripheral 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 tear fluid, dryness and soreness of the eyes,hearing impairment; very rarely - conjunctivitis. From 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); infrequently - a violation of AV-conductivity, orthostatic hypotension, decompensation of chronic heart failure, peripheral edema. From the digestive system: often - dryness of the oral mucosa, nausea, vomiting, diarrhea, constipation; rarely - hepatitis, increased activity of hepatic transaminases. For 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 mellitus), hypoglycemia (in patients receiving insulin). Allergic reactions: rarely - pruritus, rash, urticaria. Dermatological reactions: rarely - increased sweating, skin flushing; very rarely - psoriasis-like skin reactions, exacerbation of symptoms of psoriasis, alopecia. On the part of the musculoskeletal system: infrequently - muscular weakness, convulsions in the gastrocnemius muscles, arthralgia. ; very rarely - a violation of potency, rarely - withdrawal syndrome (increased angina 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. 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 the 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 simultaneously with Coronal, iodine radiopaque drugs for IV injection increase the risk of anaphylactic reactions. with Coronal phenytoin for IV administration, drugs for inhalation general anesthesia (derivatives of hydrocarbons) increase the expression cardiodepressive action 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 of Coronal reduces the clearance of lidocaine and xanthines (except diphillin) and increases their concentration plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking. NPVS (due to the delay of sodium ions and the blockade of prostaglan synthesis ina 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 Crown, 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. When used simultaneously with Coronal nifedipine can lead to a significant decrease in blood pressure. At the same time Coronal mennom application with diuretics, clonidine, sympatholytic, hydralazine, and other antihypertensive drugs may lead to excessive decrease AD.Koronal prolongs the action of nondepolarizing neuromuscular blocking drugs and anticoagulant effect kumarinov.Pri simultaneous application with Coronal tricyclic and tetracyclic antidepressants,antipsychotic 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 and Coronal should be not less than 14 days. When used simultaneously with Coronal, non-hydrated ergot alkaloids, ergot They increase the risk of developing peripheral circulatory disorders. When used simultaneously with Coronal, sulfasalazine increases plasma concentration of bisoprolol. When used simultaneously with Coronal, rifampicin shortens T1 / 2 of bisoprolol. beta-blockers for local use (eye drops). There is a decrease in the antihypertensive effect of the drug against the use of adrenal Alina and noradrenaline. The likelihood of disorders in automatism, conduction and contractility of the heart increases (mutually) during therapy with quinidine drugs (mefloquine, chloroquine). use with baclofen or amifostine also increases the 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). 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 burdened bronchopulmonary history. It should be noted that in approximately 20% of patients with angina, beta-blockers are ineffective due to severe coronary atherosclerosis with a low ischemia threshold (HR less than 100 beats / min) and nnogo end-diastolic volume of the left ventricle violating subendocardial krovotok.U smoking patients the effectiveness of beta-blockers snizhaetsya.Bolnye,contact lenses should take into account that the treatment may reduce the production of tears. When using Coronal, patients with pheochromocytoma risk paradoxical hypertension (unless effective alpha-adrenergic blockade is 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 diabetes mellitus, bisoprolol can mask tachycardia caused by hypoglycemia. In contrast to non-selective beta-adrenergic blockers, 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 of clonidine, the latter can be stopped only a few days after discontinuation of Coronal. and the lack of effect of the usual doses of epinephrine on the background of burdened allergological anamnesis. If necessary, a plan th surgery abolition of the drug is carried out for 48 hours before general anesthesia. If the patient took the drug before the operation, he should choose a drug for general anesthesia with minimal negative inotropic action. Reciprocal activation of the vagus nerve can be eliminated by intravenous administration of atropine (1-2 mg). Drugs that reduce catecholamine stores (including . Reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect pronounced decrease in blood pressure or dikardii.Bolnym with concomitant diseases bronhospasticheskimi cardioselective blockers may be administered in case of intolerance and / or ineffectiveness of other antihypertensive drugs. Overdose is dangerous for the development of bronchospasm. In case of an increase in bradycardia (less than 50 beats / min) in elderly patients, a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg),AV blockade is necessary to reduce the dose or discontinue treatment. It is recommended to stop therapy during the development of depression. It is necessary to discontinue the drug before conducting a study of blood and urine catecholamines, normetanephrine, vanillimndalnoy acid, titers of antinuclear antibodies. 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 pediatricsThe 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 the 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 dangerous activities that require an increased concentration of attention and psychomotor speed.