Bisoprolol tablets is covered.pl.ob. 5 mg 30 pcs. pack (bisoprolol)

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Tablets, film-coated from beige yellow to beige, round, biconvex at a fracture of white or almost white. Buy Bisoprolol tablets is covered.pl.ob. 5 mg 30 pcs. pack (bisoprolol) in newyork free shipping. Fast international shipping USA, AU, EU, UK and others.
Release form

Tablets, film-coated from beige yellow to beige, round, biconvex at a fracture of white or almost white.

Pharmacological action

Selective beta1-blocker, without its own sympathomimetic activity, does not have a membrane-stabilizing effect. Reduces blood plasma renin activity, reduces myocardial oxygen demand, reduces heart rate (at rest and during exercise).

It has hypotensive, antiarrhythmic and antianginal effects. Blocking beta1-adrenoreceptors of the heart in low doses, it reduces the formation of cAMP stimulated by catecholamines from ATP, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect, inhibits myocardial conductivity and excitability, and reduces AV conductivity.

With an increase in the dose above the therapeutic, it has a beta2-blocking effect.

OPSS at the beginning of the drug, in the first 24 hours, increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of beta2-adrenergic receptor stimulation), which after 1-3 days returns to the original, and decreases with prolonged administration.

The antihypertensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (of great importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure and effects on the central nervous system. With arterial hypertension, the effect occurs after 2-5 days, a stable effect - after 1-2 months.

Antianginal effect is due to a decrease in oxygen demand of the myocardium as a result of a decrease in heart rate and reduction of contractility, lengthening of the diastole, and improvement of myocardial perfusion. By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, it can increase the need for oxygen, especially in patients with chronic heart failure.

Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, 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 medium therapeutic doses, unlike non-selective beta-blockers, has a less pronounced effect on organs, containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of the peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause a delay in sodium ions (Na +) in the body, the severity of the atherogenic effect does not differ from the action of propranolol.

Pharmacokinetics

Absorption and distribution

Absorption - 80-90%, food intake does not affect absorption. Cmax in blood plasma is observed after 1-3 hours.

Communication with plasma proteins - about 30%. It passes through the BBB and the placental barrier to an insignificant degree, in insignificant amounts it is excreted in breast milk.

Metabolism and excretion

50% of the dose is metabolized in the liver to form inactive metabolites.

T1 / 2 - 10-12 hours. About 98% is excreted in the urine - 50% unchanged, less than 2% - with bile.

Indications

- arterial hypertension

- CHD: prevention of angina attacks.

Contraindications

- shock (including cardiogenic)

- collapse

- pulmonary edema

- acute heart failure

- chronic heart failure at the stage of decompensation

- AV block II and III degree

- sinoatrial blockade

- SSSU srdlkardia stenocardia - stenocardia without signs of heart failure)

- arterial hypotension (systolic blood pressure less than 100 mm Hg, especially with myocardial infarction)

- severe forms of bronchial asthma and chronic obstructive pulmonary disease with a history of sr dlkp - concomitant use of MAO inhibitors (with the exception of MAO-B)

- late stages of peripheral circulation disturbance, Raynaud’s disease

- pheochromocytoma (without the simultaneous use of alpha-blockers)

- metabolic acidosis

- under the age of 18 years (efficacy and safety have not been established)

- hypersensitivity to the components of the drug and other beta-blockers.

With caution, the drug should be prescribed for liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, diabetes mellitus, AV blockade of the first degree, depression (including a history), psoriasis, as well as elderly patients.

Use during pregnancy and lactation

Use during pregnancy and lactation is possible if the benefit to the mother outweighs the risk of side effects in the fetus and the baby.

Special instructions

Monitoring of patients taking Bisoprolol should include measurement of heart rate and blood pressure (daily at the beginning of treatment, then 1 time every 3-4 months), an ECG, determination of blood glucose in patients with diabetes mellitus (1 every 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 calculating heart rate and instructed on the need for medical advice for heart rate less than 50 beats / min.

Before starting treatment, it is recommended to study the function of external respiration in patients with a history of bronchopulmonary burden.

In approximately 20% of patients with angina pectoris, beta-blockers are ineffective. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 beats / min) and an increased final diastolic volume of the left ventricle, which violates subendocardial blood flow.

In smokers, beta-blockers are less effective.

Patients using contact lenses should consider that tear fluid production may be reduced during treatment.

When used in patients with pheochromocytoma, there is a risk of developing paradoxical hypertension (unless effective alpha-adrenoblockade is previously achieved).

With thyrotoxicosis, bisoprolol may mask certain clinical signs of thyrotoxicosis, such as tachycardia. Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can enhance symptoms.

With diabetes, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal levels.

With the simultaneous administration of clonidine, its administration can be stopped only a few days after the cancellation of bisoprolol.

It is possible to increase the severity of the hypersensitivity reaction and the lack of effect of the usual doses of zpinephrine against the background of an aggravated allergic history. If it is necessary to carry out planned surgical treatment, drug withdrawal is carried out 48 hours before the start of general anesthesia. If the patient took the drug before surgery, he should choose a drug for general anesthesia with a minimally negative inotropic effect.

Reciprocal vagus nerve activation can be eliminated iv by administration of atropine (1-2 mg).

Medicines that reduce the reserves of catecholamines (including reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs, should be under constant medical supervision to detect a pronounced decrease in blood pressure or bradycardia.

Patients with bronchospastic diseases can be prescribed cardioselective adrenergic blockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs. An 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, it is necessary to reduce the dose or stop treatment.

It is recommended that therapy be discontinued if depression develops.

Do not abruptly interrupt treatment because of the danger of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose for 2 weeks or more (reduce the dose by 25% in 3-4 days). It should be canceled before the study of the content in the blood and urine of catecholamines, normetanephrine and vanillinindic acid, antinuclear antibody titers.

Effect on the ability to drive vehicles and control mechanisms

During treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Composition

bisoprolol fumarate 5 mg.

Excipients:

croscarmellose sodium (primellose),

povidone (polyvinylpyrrolidone medium molecular weight),

starch pregelatinized (starch 1500),

silicon dioxide colloidal (aerosyllcrystal srlcrystal srlcrystall

magnesium stearate.

Composition of the film coat:

opadray II (polyvinyl alcohol, partially hydrolyzed, titanium dioxide, talc, macrogol (polyethylene glycol 3350),

iron dye oxide (II)).

Dosage and administration

The drug is taken orally, in the morning, on an empty stomach, without chewing, in an initial 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 / day.

In patients with impaired renal function with CC less than 20 ml / min or severely impaired liver function, the maximum daily dose should be 10 mg.

Dose adjustment in elderly patients is not required.

Side effects of the

From the central nervous system: increased 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 Raino), tremoR.

From the sensory organs: impaired vision, decreased secretion of lacrimal fluid, dry and sore eyes, conjunctivitis.

From the cardiovascular system: sinus bradycardia, palpitations, impaired myocardial conduction, AV block (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakened myocardial contractility, development (worsening) of chronic heart failure (swelling of the ankles, feet , shortness of breath), decreased blood pressure, orthostatic hypotension, the manifestation of angiospasm (increased impairment of peripheral circulation, cooling of the lower extremities, Raynaud's syndrome), chest pain.

From the digestive system: dry oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, impaired liver function (dark urine, yellowness of the sclera or skin, cholestasis), taste changes.

From the respiratory system: nasal congestion, difficulty breathing when prescribed in high doses (loss of selectivity) and / or in predisposed patients - laryngo- and bronchospasm.

From the endocrine system: hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid state.

Allergic reactions: pruritus, rash, urticaria.

Dermatological reactions: increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions, exacerbation of psoriasis symptoms.

On the part of laboratory indicators: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, changes in the activity of liver enzymes (increased ALT, ACT), bilirubin levels, triglycerides.

Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

Other: back pain, arthralgia, decreased libido, decreased potency, withdrawal syndrome (increased angina attacks, increased blood pressure).

Drug Interactions

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-containing radiopaque drugs for iv administration increase the risk of anaphylactic reactions.

Phenytoin with iv administration, drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.

Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

Reduces clearance of lidocaine and xanthines (except diphillin) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking.

The antihypertensive effect is weakened by NSAIDs (Na + retention and blockade of prostaglandin synthesis by the kidneys), GCS and estrogens (Na + ion retention).

Cardiac glycosides, methyldopa, reserpine and guanfacine, slow calcium channel blockers (verapamil, diltiazem), amiodoron, and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV blockade, heart failure, and heart failure.

Nifedipine can lead to a significant decrease in blood pressure.

Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.

Extends the effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotic drugs (antipsychotics), ethanol, sedative and hypnotic drugs increase CNS depression.

The simultaneous use with MAO inhibitors is not recommended due to a significant increase in the antihypertensive effect, the break in treatment between taking MAO inhibitors and bisoprolol should be at least 14 days.

Non-hydrogenated ergot alkaloids increase the risk of peripheral circulation disorders.

Ergotamine increases the risk of developing peripheral circulatory disorders sulfasalazine increases the plasma concentration of bisoprolol rifampicin shortens the elimination half-life.

Overdose

Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV block, marked decrease in blood pressure, chronic heart failure, cyanosis of fingernails or palms of the fingers, difficulty breathing, bronchospasm, dizziness, fainting, court.

Treatment: gastric lavage and the use of adsorbents symptomatic therapy: with developed AV blockade - iv administration of 1-2 mg of atropine, epinephrine or staging of a temporary pacemaker with ventricular extrasystole - lidocaine (IA class 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 - iv plasma-replacing solutions, with inefficiency - the introduction of epinephrine, dopamine, dobutamine (to maintain a chronotropic and inotropic effect and eliminate a pronounced decrease in blood pressure) with heart failure - cardiac glycosides, diuretics, glucagon in convulsions - iv diazepam with bronchospasm beta-adrenostimulator inhalation.

Storage Conditions

List B. The product should be stored in a dry, dark place out of the reach of children at a temperature not exceeding 25 ° C.

Expiration

3 years.

active substance

bisoprolol

Terms leave through pharmacies

In retseptu

Medicines twin tablet

form

Prescribing

For adults as prescribed by a doctor

Indications



Indications Hypertension, Arrhythmia, Heart failure

Izvarino Pharma, Russia



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