Bisoprolol Tab n / a film about 5mg 50 pcs Izvarino Pharma

Description

Composition
Active substance:
1 tablet contains: bisoprolol fumarate 5 mg, 10 mg.
Excipients:
Croscarmellose sodium (primelloza), povidone (polyvinylpyrrolidone of middle), pregelatinized starch (starch 1500), colloidal silicon dioxide (Aerosil), talc, microcrystalline cellulose, lactose (milk sugar), magnesium stearate. composition of the film coating: Opadry II (polyvinyl alcohol, partially hydrolyzed, titanium dioxide, talc, Macrogol (polyethylene glycol 3350), iron oxide colorant (II)).
Description:
Tablets, film-coated from beige yellow to beige, round, biconvex; at the turn white or nearly white.
Product form:
Tablets, film-coated. 10 pieces. – packings Valium planimetric (3) – packs cardboard. 10 pieces. – packings Valium planimetric (5) – packs cardboard. 10 pieces. – packings Valium planimetric (10) – packs cardboard. 10 pieces. – packings Valium planimetric (200) – cardboard boxes. 10 pieces. – packings Valium planimetric (1000) – cardboard boxes. 30 pcs. – dark glass jars (1) – packs cardboard. 30 pcs. – banks polymer (1) – packs cardboard. 50 pcs. – banks polymer (1) – packs cardboard. 50 pcs. – dark glass jars (1) – packs cardboard. 100 pieces. – banks polymer (1) – packs cardboard. 100 pieces. – dark glass jars (1) – packs cardboard.
Contraindications
Shock (including cardiogenic); collapse; pulmonary edema; congestive heart failure; chronic heart failure decompensation; AV-block II and III degree; sinoatrial block; SSS; bradycardia; Prinzmetal angina; cardiomegaly (without heart failure); hypotension (systolic blood pressure less than 100 mm Hg, particularly in myocardial infarction..); severe bronchial asthma and chronic obstructive pulmonary disease in history; simultaneous MAO inhibitors (except MAO-B); later stages peripheral circulatory disorders, Raynaud’s disease; pheochromocytoma (without the simultaneous use of alpha blockers); metabolic acidosis; age 18 years (effectiveness and safety have been established); hypersensitivity to the drug and other beta-blockers.
Precautions should be prescribed with hepatic insufficiency, chronic renal failure, myasthenia gravis, thyrotoxicosis, diabetes, AV-I blockade degree of depression (including history), psoriasis, and elderly patients.
Dosage
5 mg
Indications
Arterial hypertension;
Coronary heart disease: prevention of angina attacks.
Interaction with other drugs
The allergens used for immunotherapy, or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol.
Iodine radiopaque drugs for i / v administration increases the risk of anaphylactic reactions.
Phenytoin at / in the introduction, the medicaments for inhalation general anesthesia (hydrocarbon derivatives) increase the severity cardiodepressive action and likely to reduce blood pressure.
Changes effectiveness of insulin and of oral hypoglycemic drugs, masking the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).
Reduces the clearance of lidocaine and xanthine (except dyphylline) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking.
The hypotensive effect of weakening the NSAID (delay Na + and blockage of prostaglandin synthesis by the kidneys), SCS and estrogens (delay ions Na +).
Cardiac glycosides, methyldopa, reserpine and guanfacine, blockers of slow calcium channels (verapamil, diltiazem), amiodoron and other antiarrhythmic drugs increase the risk of developing or worsening of bradycardia, AV-blockade, cardiac arrest and heart failure.
Nifedipine can lead to a significant reduction in blood pressure.
Diuretics, clonidine, sympatholytic, hydralazine, and other antihypertensive drugs may cause an excessive decrease of blood pressure.
Prolongs the action of non-depolarizing muscle relaxants and anticoagulant effect of coumarin.
Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics drugs increase CNS depression.
Not recommended simultaneous application with MAO inhibitors due to a significant increase in hypotensive action, a break in treatment between the reception of MAO inhibitors and bisoprolol should be at least 14 days.
Non-hydrogenated ergot alkaloids increase the risk of peripheral circulatory disorders.
Ergotamine increases the risk of peripheral circulatory disorders; sulfasalazine increases the concentration of bisoprolol in the plasma; rifampin shortens the half-life.
Overdose
Symptoms: arrhythmia, ventricular arrythmia, bradycardia, AV-block, marked decrease in blood pressure, chronic heart failure, cyanosis nails of fingers or hands, shortness of breath, bronchoconstriction, dizziness, fainting, convulsions.
Treatment: gastric lavage and the appointment of adsorbents; Symptomatic therapy: the AV blockade which developed – in / in a 1-2 mg atropine, epinephrine or staging temporary pacemaker; with ventricular arrhythmia – lidocaine (IA class of drugs does not apply); while lowering blood pressure – the patient must be in the Trendelenburg position; if no signs of pulmonary edema – in / plasma-substituting solutions in ineffectiveness – administration of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and removal of significant decrease in blood pressure); in heart failure – cardiac glycosides, diuretics, glucagon; at cramps – in / diazepam; with bronchospasm beta adrenostimulyatorov inhalation.
pharmachologic effect
Pharmacological group:
Beta1-selective blocker.
Pharmacodynamics:
Selective beta1-adrenergic blocker, without own sympathomimetic activity, has no membrane stabilizing effect. Reduces plasma renin activity, reduces myocardial oxygen demand, reduce heart rate (resting and under a load).
It has a hypotensive, antiarrhythmic and antianginal effects. Blocking in low doses beta1-adrenergic receptors of the heart, stimulated by catecholamines reduces the formation of cAMP from ATP, reduces intracellular calcium ion current has a negative chronotropic, dromo-, BATM inotropic effect and inhibits the conduction and excitability infarction reduces AV-conduction.
With increasing doses of the above therapeutic exerts beta2-adrenoceptor blocking effect.
OPSS at the beginning of the drug in the first 24 hours, is increased (as a result of reciprocal increase in the activity of alpha-adrenoceptor stimulation and removal of beta2-adrenoceptor), which is 1-3 days returns to the original, and prolonged decreases appointment.
The hypotensive effect was associated with reduced cardiac output, peripheral vascular sympathetic stimulation, decreased activity of the renin-angiotensin system (important for patients with initial hypersecretion renin), restoration of the sensitivity in response to the blood pressure reduction and influence on the CNS. When hypertension effect occurs within 2-5 days, stable operation – in 1-2 months.
Antianginal effect due to a decrease in myocardial oxygen demand by reducing heart rate and decrease contractility, lengthening of diastole, improving myocardial perfusion. By increasing the end-diastolic pressure in the left ventricle and increased tensile ventricular muscle fibers may increase the oxygen demand, especially in patients with chronic heart failure.
Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased sympathetic nervous system activity, increased cAMP levels, hypertension), decrease the rate of spontaneous excitation of the sinus and ectopic pacemakers and slowing AV-conducting (preferably antegrade and to a lesser extent, in the retrograde direction through the AV-node) and additional routes.
When applied in high therapeutic doses, unlike nonselective beta-blockers, has a less pronounced effect on organs containing beta 2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchial and uterine) and carbohydrate metabolism, does not cause delays sodium ions (Na +) in the body; atherogenic action expression is not different from that of propranolol.
Pharmacokinetics:
Absorption and distribution
Absorption – 80-90%, food intake does not affect absorption. Cmax in plasma observed after 1-3 hours.
Communication with plasma proteins – about 30%. It passes through the BBB and the placental barrier to a small extent, in small amounts excreted in breast milk.
Metabolism and excretion of 50% of the dose is metabolized in the liver to inactive metabolites.
T1 / 2 -. 10-12 h About 98% is excreted in the urine – 50% intact, less than 2% – with bile.
Pregnancy and breast-feeding
Application of pregnancy and lactation is possible if the benefit to the mother outweighs the risk of side effects in the fetus and child.
Conditions of supply of pharmacies
Prescription.
side effects
CNS: 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 Peyno), tremor.
From the senses: visual disturbances, reduced secretion of tear fluid, dryness and soreness of the eyes, conjunctivitis.
With the cardiovascular system: sinus bradycardia, heart rate, conduction disturbances infarction, the AV -blokada (until the development of a complete transverse blockade and heart failure), arrhythmia, weakening of the myocardial contractility, the development of (worsening) of chronic heart failure (swelling of ankles, feet, dyspnea), reduced blood pressure, orthostatic hypotension, a manifestation of vasospasm (strengthening of peripheral blood circulation, cooling of the lower extremities, Raynaud’s syndrome), pain in the chest.
From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, liver dysfunction (dark urine, yellow skin or sclera, cholestasis) changes the taste.
The respiratory system: nasal congestion, difficulty breathing when administered at high doses (loss of selectivity) and / or in predisposed patients – laryngo and bronchospasm.
From endocrine system: hyperglycemia (in patients insulinezavisimym diabetes), hypoglycemia (in patients receiving insulin), hypothyroid state.
Allergic reactions: itching, rash, urticaria.
Dermatologic reactions: sweating, skin redness, rash, psoriasiform skin reactions, exacerbation of psoriasis symptoms.
From the laboratory parameters: thrombocytopenia (unusual bleeding or hemorrhage), agranulocytosis, leukopenia, changes in liver enzymes (ALT increase, ACT), bilirubin, triglycerides.
Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.
Other: back pain, arthralgia, weakening of libido, reduced potency, withdrawal syndrome (increased angina attacks, increased blood pressure).
special instructions
Monitoring patients receiving bisoprolol should include measurement of heart rate and blood pressure (at the beginning of treatment – daily, then – 1 every 3-4 months) holding an electrocardiogram, determination of blood glucose levels in diabetic patients (1 every 4-5 months). In elderly patients it is recommended to monitor renal function (1 every 4-5 months).
It should teach the patient’s heart rate counting procedure and to instruct the need of medical advice in heart rate less than 50 bpm. / Min.
Before treatment is recommended to study the external breathing function in patients with a history of bronchopulmonary history.
Approximately 20% of patients with angina, beta-blockers are ineffective. The main reasons – severe coronary atherosclerosis low threshold ischemia (heart rate less than 100 beats / min.) And increased end-diastolic volume of the left ventricle, which violates the subendocardial bloodstream.
At smoking patients the effectiveness of beta-blockers lower.
Patients who use contact lenses should bear in mind that during treatment may decrease the production of tear fluid.
When used in patients with pheochromocytoma has a risk of paradoxical hypertension (if not previously reached effective alpha adrenoblockade).
Thyrotoxicosis bisoprolol may mask certain clinical signs of hyperthyroidism, such as tachycardia. Abrupt withdrawal in patients with hyperthyroidism contraindicated because the symptoms can increase.
In diabetes may mask tachycardia caused by hypoglycemia. In contrast, nonselective beta-blockers practically no increase insulin-induced hypoglycemia and delay recovery of blood glucose to normal levels.
At the same time taking clonidine his appointment may be terminated only a few days after discontinuation of Bisoprolol.
May increase the severity of hypersensitivity reactions and the lack of effect of conventional doses zpinefrina with aggravated allergologicheekogo history. In case of need for surgical planning preparation carried cancellation for 48 hours prior to general anesthesia. If the patient took the drug before surgery, he must pick a medicament for general anesthesia with minimal negative inotropic effect.
Reciprocal activation of the vagus nerve can be eliminated in / atropine (1.2 mg).
Drugs that reduce stocks catecholamines (including reserpine), may enhance the action of beta-blockers, so patients taking such drug combinations should be under constant medical supervision for identifying expressed lowering blood pressure or bradycardia.
Patients with diseases bronhospasticheskimi cardioselective blockers may be administered in case of intolerance and / or ineffectiveness of other antihypertensive drugs. Overdose risk of developing bronchoconstriction.
In case of elderly patients increasing bradycardia (less than 50 u. / Min.), Expressed lowering blood pressure (systolic blood pressure below 100 mm Hg. V.), AV -blokady necessary to reduce the dosage or discontinue treatment.
It is recommended to discontinue therapy in the development of depression.
Do not abruptly discontinue treatment because of the risk of severe arrhythmias and myocardial infarction. Cancellation are gradually reducing the dose for 2 weeks or more (dose reduced by 25% in 3-4 days). Should be lifted before testing of blood and urine catecholamines, normetanephrine and vanilinmindalnoy acid antinuclear antibody titers.
Effects on ability to drive vehicles and management mechanisms:
During the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions.
Storage conditions
The preparation should be stored in a dry place, protected from light, out of reach of children at a temperature not higher than 25 ° C.
Dosing and Administration
The drug is taken orally, in the morning, fasting, not liquid, in an initial dose of 5 mg 1 time / day. If necessary to increase the dose of 10 mg 1 time / day. The maximum daily dose – 20 mg / day.
Patients with impaired renal function with CC less than 20 ml / min or with severe liver function impairment maximum daily dose should be 10 mg.
No dose adjustment in elderly patients is not required.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist