Biprol coated pills 10mg N30
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Active ingredients
Bisoprolol
Release form
Pills
Composition
Bisoprolol fumarate 10 mg adjuvants: microcrystalline cellulose - 62.4 mg, ludipress lce (lactose monohydrate - 94.7-98.3%, povidone - 3-4%) - 38.5 mg, corn starch - 11 mg, colloidal silicon dioxide (aerosil) - 0.6 mg, Crospovidone (collidon cl) - 1.25 mg, magnesium stearate - 1.25 mg. film coating composition: titanium dioxide - 0.43 mg, macrogol (polyethylene glycol 4000) - 0.43 mg, hypromellose (hydroxypropylmethylcellulose) - 1.968 mg, talc - 0.172 mg.
Pharmacological effect
Selective beta1-adrenergic blocker without internal sympathomimetic activity, does not possess membrane stabilizing properties. It reduces plasma renin activity, reduces the need for myocardium in oxygen, reduces heart rate at rest and under load. It has hypotensive, antiarrhythmic and antianginal effects. When used in low doses, it blocks the β1-adrenoreceptors of the heart, reduces catecholamine-stimulated cAMP formation from ATP, reduces the intracellular current of calcium ions, has a negative chrono, dromo, batmo and inotropic effect, inhibits conductivity and excitability, reduces myocardial contractility. in high doses has a beta2-adrenoblokiruyuschee effect. OPSS at the beginning of the drug (in the first 24 hours) increases (as a result of the reciprocal increase in the activity of α-adrenergic receptors and elimination of st β2-adrenoreceptors), then after 1-3 days returns to the original, and with prolonged use of the drug - decreases. The hypotensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin-aldosterone system ( for patients with initial renin hypersecretion), recovery of sensitivity in response to a decrease in blood pressure and effect on the central nervous system. In case of arterial hypertension, the initial effect occurs after 2-5 days, stable - 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 oxygen demand of the myocardium, 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, an increased content of cAMP, arterial hypertension), 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 through the AV node) and along additional paths . When used in moderate therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing β2-adrenoreceptors (pancreas gel for, skeletal muscle, smooth muscle of peripheral arteries, bronchial and uterine) and carbohydrate metabolism, does not cause delays sodium ions in the body; the severity of atherogenic action does not differ from that of propranolol. 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 and distributionWhen ingestion is well absorbed from the gastrointestinal tract (absorption - 80-90%); food intake does not affect absorption. Cmax in plasma is achieved after 1-3 hours. Binding to plasma proteins is about 30%. In small quantities it penetrates the blood-brain barrier, placental barrier, excreted in breast milk. Metabolism and elimination Metabolized in the liver, T1 / 2 - 10-12 hours. Excreted by the kidneys (50% - unchanged); less than 2% is excreted in the 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 II and III degree blockade; - sinus syndrome; sinus node weakness syndrome; - severe bradycardia; - Prinzmetal's angina; - cardiomegaly (without signs of heart failure); - arterial hypotension (systolic blood pressure less than 100 mmHg, especially in myocardial infarction); - bronchial asthma and chronic obstructive pulmonary disease in history; - simultaneous taking inhibitors AO (with the exception of MAO type B inhibitors); - 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. With caution, the drug is prescribed to patients with hepatic insufficiency,chronic renal failure, myasthenia, thyrotoxicosis, diabetes mellitus, AV block I degree, depression (including history), psoriasis, as well as the elderly.
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
The use of the drug during pregnancy and lactation is possible if the benefit to the mother exceeds the risk of side effects in the fetus and child.
Dosage and administration
Is inside, in the morning, on an empty stomach, the pills are not chewed. The drug is prescribed in a dose of 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 a CC of less than 20 ml / min or with severe impaired liver function, the maximum daily dose is 10 mg.
Side effects
CNS and peripheral nervous system: fatigue, weakness, dizziness, headache, sleep disorders, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenia, myasthenia gravis, paresthesia in the extremities (in patients with intermittent claudication and syndrome) Rayno), tremor. On the part of the organ of vision: impaired vision, decreased secretion of the tear fluid, dryness and soreness of the eyes, conjunctivitis. On the part of the cardiovascular system: sinus bradycardia, heartbeat infusion, myocardial conduction disturbance, AV-blockade (up to the development of complete transverse blockade and cardiac arrest), arrhythmia, weakening of myocardial contractility,development (aggravation) of chronic heart failure (swelling of the ankles, feet; shortness of breath), lowering blood pressure, orthostatic hypotension, manifestation of angiospasm (increased disturbance of the peripheral circulation, cooling of the lower extremities, Raynaud's syndrome), chest pain, withdrawal syndrome (increased angina attacks, increased AD). From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, changes in the activity of liver enzymes (increased ALT and ACT), bilirubin level, disturbance liver function (dark urine, sclera or skin yellowness, cholestasis), changes in taste. On the respiratory system: nasal congestion, difficulty breathing when administered in high doses (loss of selectivity) and / or in susceptible patients - laryngo and bronchospasm. side of the endocrine system: hyperglycemia (in patients with type 2 diabetes), hypoglycemia (in patients receiving insulin), hypothyroid state. Allergic reactions: pruritus, rash, urticaria. Dermatological reactions: increased sweating, hyperemia to azhi, exanthema, psoriasis-like skin reactions, exacerbation of psoriasis symptoms. From the hematopoietic system: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia. From the reproductive system: weakening of libido, decrease in potency triglycerides, withdrawal syndrome (increased angina attacks, increased blood pressure). Effect on the fetus: during the use of the drug may be intrauterine growth retardation, hypoglycemia, fetal bradycardia.
Overdose
Symptoms: arrhythmias, ventricular premature beats, severe bradycardia, AV blockade, marked reduction in blood pressure, chronic heart failure, cyanosis of finger and palm nails, difficulty breathing, bronchospasm, dizziness, syncope, cramps. Treatment: gastric lavage, prescription of adsorbents. If necessary, carry out symptomatic therapy: with developed AV-blockade in / in the introduction of atropine (1-2 mg), epinephrine or staging a temporary pacemaker; with ventricular extrasystole - lidocaine (I class A 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, inject intravenously plasma-substituting solutions; with ineffectiveness - the introduction of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and eliminate the pronounced decrease in blood pressure).In heart failure, cardiac glycosides, diuretics, glucagon are prescribed; with convulsions - in / in diazepam; with bronchospasm - beta2-adrenostimulators inhalation.
Interaction with other drugs
The use of allergens used for immunotherapy or extracts of allergens for skin tests during the treatment with Biprol increases the risk of severe systemic allergic reactions or anaphylaxis. At the same time as using iodine radiopaque drugs for bisoprolol for intravenous administration, the risk of anaphylactic reactions increases. with bisoprolol phenytoin for the on / in the introduction, drugs for inhalation general anesthesia (derivatives of hydrocarbons) severity of cardiodepressive action and the likelihood of a decrease in blood pressure. With simultaneous use, bisoprolol alters the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure). With simultaneous use of bisoprolol reduces the clearance of lidocaine and xanthines (except diphylin) and also promotes boosters (except diphilin) and also promotes boosters, except for diphlina, and also boosts xanthines (except diphilin) and also boosts promoters (diphline), and also boosts xanthines (except diphilin), and boosters also increase the clearance of lidocaine and xanthines (except diphilin) and also promotes boosters. in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking. The hypotensive effect of bisoprolol reduces H VS (delayed Na + and blockade of prostaglandin synthesis by the kidneys), GCS and estrogens (delayed Na + ions). With simultaneous use of cardiac glycosides, methyldopa, reserpine and guanfacine, calcium channel blockers (verapamil, diltiazem), amiodoron and other antiarrhythmic drugs increase the risk of development or worsening bradycardia, AV blockade, cardiac arrest, and heart failure. When used simultaneously with bisoprolol, nifedipine can lead to a significant decrease in BP. When used simultaneously with bisoprolol diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs may lead to an excessive decrease in blood pressure. Bisoprolol prolongs the effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins. Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroptics, non-psychotic drugs)sedative and hypnotic drugs increase the inhibitory effect of bisoprolol on the central nervous system. It is not recommended to use bisoprolol with MAO inhibitors simultaneously due to a significant increase in the hypotensive effect (the interval between taking MAO inhibitors and bisoprolol should be at least 14 days). ergotamine increases the risk of developing peripheral circulatory disorders. With simultaneous use of sulfasalazine increases the concentration Plasma Bisoprolol. When used concurrently, rifampicin reduces T1 / 2 bisoprolol.
special instructions
Monitoring the condition of patients taking Biprol should include measuring heart rate and blood pressure (at the beginning of treatment - daily, then once every 3-4 months), conducting an ECG, and measuring blood glucose in patients with diabetes mellitus (1 time every 4-5 months). In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months). Before starting treatment, it is recommended to conduct a study of the function of external respiration in patients with respiratory diseases in history. Patients should be trained in how to calculate heart rate and instruct on the need for medical consultation in heart rate less than 50 beats / min. Approximately in 20% of patients with angina, beta-blockers are ineffective. The main reasons are severe coronary atherosclerosis with a low ischemic threshold (HR less than 100 beats / min) and an increased end diastolic volume of the left ventricle that disrupts subendocardial blood flow. In smoking patients, the effectiveness of beta-adrenergic blockers is lower. Patients using contact lenses should take into account that against the background of treatment, there may be a decrease in the production of tears. When used in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (unless effective Single adrenoceptor blockade of α-) .If thyrotoxicosis Biprol can mask certain clinical signs of hyperthyroidism (e.g., tachycardia). Abrupt cancellation in patients with thyrotoxicosis is contraindicated, since in this case the symptoms may increase. In diabetes mellitus, the drug may 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. While taking clonidine at the same time, its reception can be stopped only a few days after Biprol’s withdrawal. effect of the usual doses of epinephrine in patients with a burdened allergic history. If necessary, a planned surgical treatment of drug withdrawal is carried out 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 a minimally negative inotropic effect. 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 action of beta-blockers, so patients taking such combinations of medicines should be under constant medical supervision to detect pronounced decrease in blood pressure or scars. ikardii.Patsientam bronhospasticheskimi with conditions or diseases may be administered cardioselective blockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs. Overdose is dangerous for the development of bronchospasm. In case of increasing bradycardia (less than 50 beats / min) in elderly patients, a pronounced decrease in blood pressure (systolic blood pressure below 100 mmHg), AV blockade, reduce the dose or stop treatment. It is recommended to stop therapy in the development of depression. You can not abruptly interrupt treatment because of the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose for 2 weeks or more (by 25% in 3-4 days). The drug should be canceled before the examination of the content in the blood and urine of catecholamines, normetanephrine and vanillin-almond acid; antinuclear antibody titers. Effect 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 an increased concentration of attention and speed of psychomotor reactions.