Bidop, pills 10mg, 56pcs

Composition

1 tablet contains bisoprolol hemifumarate 10 mg.

Auxiliary substances:

lactose monohydrate,

microcrystalline cellulose,

magnesium stearate,

crospovidone,

PB 27215 beige pigment (lactose monohydrate 87%, iron oxide red and yellow 13%).

Pharmacological action

Selective beta_-1-adrenoblocker without internal sympathomimetic activity, does not have a membrane-stabilizing effect. Reduces the activity of 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, and inhibits conduction and excitability.

If the therapeutic dose is exceeded, it has a beta_-2-adrenoblocking effect.

At the beginning of the drug use, in the first 24 hours, OPSS increases (as a result of a reciprocal increase in the activity of α-adrenergic receptors and elimination of stimulation of β2-adrenergic receptors), after 1-3 days, OPSS returns to its original value, and with prolonged treatment – 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 system (which is more important 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 develops 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 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 the medium therapeutic doses, unlike nonselective beta-blockers, has a less pronounced effect on the organs containing the β₂-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause the delay of sodium ions in the body; the manifestation of atherogenic action is different from the action of propranolol.

Indications

Arterial hypertension; prevention of angina attacks.

Use during pregnancy and lactation

The use of the drug during pregnancy and lactation is possible only if the intended benefit to the mother outweighs the potential risk to the fetus and child.

There is no data on whether bisoprolol penetrates into breast milk. If it is necessary to use the drug during lactation, it is recommended to stop breastfeeding.

Contraindications

• hypersensitivity to bisoprolol and other beta-blockers;
• shock (including cardiogenic), collapse;
• cardiac pulmonary edema;
• chronic heart failure in the stage of decompensation (including cardiogenic shock);
• AV blockade II–III century, sinoatrial block, the syndrome of weakness of the sinus node;
• bradycardia;
• Prinzmetal’s angina;
• cardiomegaly (without signs of heart failure);
• hypotension (SBP
• bronchial asthma and COPD in history;
• simultaneous reception of MAO inhibitors (except MAO-B);
• the later stages of peripheral circulation;
• Raynaud’s disease;
• pheochromocytoma (without the simultaneous use of alpha-blockers);
• metabolic acidosis;
• the age of 18 years (effectiveness and safety not established).

Side effects

Side effects observed with the use of Bidop are classified into categories depending on the frequency of their occurrence: very common (≥ 1/10); common (≥ 1/100, < 1/10); infrequent (≥ 1/1000, < 1/100); rare (≥ 1/10 000, < 1/1000); very rare (

From the central nervous system and peripheral nervous system: infrequently-increased fatigue, weakness, asthenia, dizziness, headache, sleep disorders, depression, anxiety, confusion or short-term memory loss; rarely-hallucinations, myasthenia gravis, nightmares, convulsions (including in the calf muscles), paresthesia in the extremities (in patients with intermittent claudication and Raynaud’s syndrome), tremor.

From the sensory organs: rarely-visual impairment, decreased secretion of tear fluid, dry and painful eyes; very rarely-conjunctivitis.

From the cardiovascular system: very often-sinus bradycardia, palpitations; often – a pronounced decrease in blood pressure, angiospasm (increased peripheral circulatory disorders, cold of the lower extremities, Raynaud’s syndrome); infrequently – orthostatic hypotension, impaired myocardial conduction, AV block (up to the development of complete transverse block and cardiac arrest), arrhythmias, weakening of myocardial contractility, development of chronic heart failure (ankle swelling, stop; shortness of breath), chest pain.

From the digestive system: often-dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea; rarely-liver function disorders (dark urine, jaundice of the sclera or skin, cholestasis), taste changes, hepatitis, increased activity of liver enzymes (ACT, ALT), hyperbilirubinemia, hypertriglyceridemia.

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

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

Allergic reactions: rarely-skin pruritus, rash, urticaria.

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

From the hematopoietic system: in some cases – thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia.

Other: infrequently-arthralgia; rarely-back pain, 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 theophylline) 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 (sodium ion retention and blockade of prostaglandin synthesis by the kidneys), corticosteroids and estrogens (sodium ion retention).

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

How to take it, course of use and dosage

Tablets are taken orally, in the morning, on an empty stomach, without chewing, once. The dose should be selected individually.

In patients with arterial hypertension and CHD (prevention of stable angina attacks), the initial dose is 5 mg 1 time/day. If necessary, the dose is increased to 10 mg 1 time/day. The maximum daily dose is 20 mg.

In patients with impaired renal function with creatinine clearance less than 20 ml/min. or with severe hepatic impairment, the maximum daily dose is 10 mg. Increasing the dose in such patients should be carried out with extreme caution.

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, hypoglycemia.

Treatment: gastric lavage and the appointment of adsorbing of medications; symptomatic treatment: with advanced AV-blockade – in/1-2 mg of atropine, epinephrine or staging temporary pacemaker; ventricular premature beats – lidocaine (drugs I A class not applicable); the decrease in blood pressure, the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema, in/plasma-substituting solutions, the ineffectiveness of the epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic actions and elimination of severely impaired BP); heart failure – cardiac glycosides, diuretics, glucagon; in convulsions – in/diazepam; with bronchospasm – beta₂-agonists with inhaled the.

Special instructions

Monitoring of patients taking Bidop should include measurement of heart rate and blood pressure (at the beginning of treatment — daily, then once every 3-4 months), ECG, blood glucose determination in patients with diabetes mellitus (once every 4-5 months).

In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months).

Form of production

Pills.

Storage conditions

The drug should be stored out of the reach of children, dry, protected from light at a temperature not exceeding 25°C.

Shelf

life is 3 years.

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Heart Failure, Hypertension, Arrhythmia