Bisoprolol pills 5mg 50pcs

Composition

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of bisoprolol fumarate 5 mg.

Auxiliary substances:

croscarmellose sodium (primellose),

povidone (polyvinylpyrrolidone medium molecular weight),

pregelatinized starch (starch 1500),

colloidal silicon dioxide (aerosil),

talc,

microcrystalline cellulose,

lactose (milk sugar),

magnesium stearate.

Composition of the film shell:

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

Pharmacological action

Selective beta-1-adrenoblocker, without its own sympathomimetic activity, does not have a membrane-stabilizing effect. Reduces the activity of blood plasma renin, reduces the need for myocardial oxygen, reduces heart rate (at rest and during exercise).

It has antihypertensive, antiarrhythmic and antianginal effects. Blocking the beta-1-adrenergic receptors of the heart in low doses, it reduces the catecholamine-stimulated formation of cAMP from ATP, reduces the intracellular flow of calcium ions, has a negative chrono -, dromo -, batmo-and inotropic effect, inhibits the conduction and excitability of the myocardium, and reduces AV conduction.

When the dose is increased above the therapeutic dose, it has a beta-2-adrenoblocking effect.

OPSS at the beginning of the drug use, in the first 24 hours, increases (as a result of a reciprocal increase in alpha-adrenergic activity and elimination of beta-2-adrenergic stimulation), which returns to its original value after 1-3 days, and decreases with prolonged use.

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 system (which is of great importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure, and an effect on the central nervous system. With arterial hypertension, the effect occurs in 2-5 days, stable effect – in 1-2 months.

The antianginal effect is due to a decrease in the myocardial oxygen demand as a result of a decrease in heart rate and reduced contractility, an elongation of the diastole, and an improvement in 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.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, 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 the retrograde directions through the AV node) and along additional pathways.

When used in medium therapeutic doses, unlike non-selective beta-blockers, it has a less pronounced effect on organs containing beta-2-adrenergic receptors (pancreas, skeletal muscles, smooth musculature of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause sodium (Na+) ion retention in the body; the severity of the atherogenic effect does not differ from that of propranolol.

Pharmacokinetics

Suction and distribution

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

The connection with plasma proteins is about 30%. Passes through the BBB and placental barrier to a small extent, in small amounts is excreted in breast milk.

Metabolism and elimination

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—

– IHD: prevention of angina attacks.

Contraindications

— shock (including cardiogenic);

collapse;

pulmonary edema;

acute heart failure;

— chronic heart failure in the stage of decompensation;

— AV-block II and III degree;

— sinoatrial block;

— SSSU;

— bradycardia;

— Prinzmetal’s angina;

— cardiomegaly (without signs of heart failure);

— arterial hypotension (systolic blood pressure less than 100 mm Hg. St., especially in myocardial infarction);

— severe forms of bronchial asthma and chronic obstructive pulmonary disease in the anamnesis;

— simultaneous reception of MAO inhibitors (except MAO-B);

— late stages of peripheral circulation, Raynaud’s disease;

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

metabolic acidosis;

— age under 18 years (effectiveness and safety not established);

— hypersensitivity to the medication and other beta-blockers.

With caution, the drug should be prescribed for hepatic insufficiency, chronic renal failure, myasthenia gravis, thyrotoxicosis, diabetes mellitus, grade I AV block, depression (including in the anamnesis), psoriasis, as well as elderly patients.

Side effects

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 Raynaud’s syndrome), tremor.

From the side of the senses:  visual impairment, decreased lacrimal fluid secretion, dry and painful eyes, conjunctivitis.

From the cardiovascular system:  sinus bradycardia, palpitations, impaired myocardial conduction, AV block (up to the development of complete transverse block and cardiac arrest), arrhythmias, weakening of myocardial contractility, development (aggravation) of chronic heart failure (swelling of the ankles, feet, shortness of breath), decreased blood pressure, orthostatic hypotension, angiospasm (increased peripheral circulatory disorders, cold of the lower extremities, Raynaud’s syndrome), chest pain.

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

Respiratory system disorders:  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 non-insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroidism.

Allergic reactions:  skin pruritus, rash, urticaria.

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

From the side of laboratory parameters:  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 services:  back pain, arthralgia, decreased libido, decreased potency, withdrawal syndrome (increased angina attacks, increased blood pressure).

Interaction

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 intravenous use increase the risk of anaphylactic reactions.

Phenytoin with intravenous use, drugs for inhaled general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive effects 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 the clearance of lidocaine and xanthines (except diphylline) 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), corticosteroids and estrogens (Na+ion retention).

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

Nifedipine can lead to a significant decrease in blood pressure.

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

It prolongs the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.

Tri-and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives, and sleeping pills increase CNS depression.

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

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

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

How to take, course of use and dosage

The drug is taken orally, in the morning, on an empty stomach, without chewing, at an initial dose of 5 mg 1 time/day. If necessary, the dose is increased to 10 mg 1 time/day. The maximum daily dose is 20 mg/day.

In patients with impaired renal function with creatinine clearance less than 20 ml/min or severe hepatic impairment, the maximum daily dose should be 10 mg.

No dose adjustment is required in elderly patients.

Overdose

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

Treatment: gastric lavage and use of adsorbents; symptomatic therapy: if AV block develops – intravenous use of 1-2 mg of atropine, epinephrine or a temporary pacemaker; with ventricular extrasystole – lidocaine (class IA 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 – intravenous plasma – substituting solutions, if ineffective – use of epinephrine, dopamine, dobutamine (to maintain normal blood pressure). chronotropic and inotropic effects and elimination of a pronounced decrease in blood pressure); in heart failure – cardiac glycosides, diuretics, glucagon; in convulsions-IV diazepam; in bronchospasm, beta-adrenostimulants by inhalation.

Special instructions

Monitoring of patients taking Bisoprolol should include measurement of heart rate and blood pressure (at the beginning of treatment – daily, then – 1 time in 3-4 months), ECG, determination of blood glucose in 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).

The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.

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

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

In smoking patients, the effectiveness of beta-blockers is lower.

Patients who use contact lenses should take into account that during treatment, there may be a decrease in the production of tear fluid.

When used in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (if an effective alpha-adrenoblockade is not previously achieved).

In thyrotoxicosis, Bisoprolol may mask certain clinical signs of thyrotoxicosis, such as tachycardia. Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can increase symptoms.

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

When taking clonidine at the same time, it can be stopped only a few days after the withdrawal of Bisoprolol.

It is possible to increase the severity of the hypersensitivity reaction and the lack of effect from conventional doses of zpinephrine against the background of a burdened allergic history. If elective surgical treatment is necessary, the drug is withdrawn 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 minimal negative inotropic effect.

Reciprocal activation of the vagus nerve can be eliminated by intravenous use of atropine (1-2 mg).

Drugs that reduce the supply of catecholamines (including reserpine) can increase the effect of beta-blockers, so patients taking such combinations of drugs should be constantly monitored by a doctor for a pronounced decrease in blood pressure or bradycardia.

Patients with bronchospastic diseases can be prescribed cardioselective adrenoblockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs. Overdose is dangerous for the development of bronchospasm.

If elderly patients are found to have increasing bradycardia (less than 50 beats/min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV-blockade, the dose should be reduced or treatment should be discontinued.

It is recommended to stop therapy if depression develops.

Do not abruptly interrupt treatment due to the risk of developing severe arrhythmias and myocardial infarction. Withdrawal 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 testing the content of catecholamines, normetanephrine and vanillinmindalic acid in the blood and urine, and titers of antinuclear antibodies.

Influence on the ability to drive motor vehicles and manage mechanisms

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

Form of production

Film-coated tablets, beige-yellow to beige in color, round, biconvex; white or almost white at the break.

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Arrhythmia, Heart Failure, Hypertension