Bidop, tablets 5 mg 56 pcs.

A selective beta₁-adrenoblocker without intrinsic sympathomimetic activity, has no membrane stabilizing effect. Reduces plasma renin activity, reduces myocardial oxygen demand, reduces HR (at rest and under load).

It has hypotensive, antiarrhythmic and antianginal action. In low doses it blocks β₁-adrenoceptors of heart, decreases catecholamine-stimulated cAMP formation from ATP, decreases intracellular calcium ion current, produces negative chrono-, dromo-, batmo- and inotropic effects, inhibits conduction and excitability.

If the therapeutic dose is exceeded, it has beta₂-adrenoblocking effect.

In the beginning of the drug administration, during the first 24 h, RPS increases (as a result of reciprocal increase of α-adrenoreceptor activity and elimination of β₂-adrenoreceptor stimulation), after 1-3 days RPS returns to baseline, and with long-term treatment it decreases.

Hypotensive effect is associated with decreased minute blood volume, sympathetic stimulation of peripheral vessels, decreased activity of renin-angiotensin system (of greater importance for patients with initial renin hypersecretion), restoration of sensitivity in response to BP reduction and influence on CNS. For arterial hypertension the effect develops in 2-5 days, stable effect – in 1-2 months.

The antianginal effect is caused by decrease of myocardial oxygen demand as a result of HR shortening and decrease of contractility, prolongation of diastole, improvement of myocardial perfusion. By increasing left ventricular end-diastolic pressure and increasing ventricular muscle fiber stretch may increase oxygen demand, especially in patients with chronic heart failure.

The antiarrhythmic effect is caused by the removal of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased content of CAMF, arterial hypertension), decrease of spontaneous excitation rate of sinus and ectopic pacemakers and slowing of AV conduction (mainly in antegrade and, to a lesser extent, in retrograde direction through the AV node) and through additional pathways.

When used in medium therapeutic doses, unlike non-selective beta-adrenoblockers, it has less pronounced effect on organs containing β₂-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and carbohydrate metabolism, does not cause retention of sodium ions in the body; intensity of atherogenic action does not differ from that of propranolol.

Indications

Arterial hypertension; CHD: prevention of stable angina attacks.

Active ingredient

Composition

1 tablet contains bisoprolol hemifumarate 5 mg.

Auxiliary substances:

Lactose monohydrate,

Microcrystalline cellulose,

Magnesium stearate, crosspovidone,

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

How to take, the dosage

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

In case of arterial hypertension and CHD (prevention of stable angina attacks), the initial dose is 5 mg once daily. If necessary, the dose is increased to 10 mg once daily. The maximum daily dose is 20 mg.

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

There is no need for dose adjustment in elderly patients.

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 IV administration increase the risk of anaphylactic reactions. Phenytoin when administered by IV, drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive effects and the likelihood of BP reduction.

Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, BP increase).

Limits clearance of lidocaine and xanthines (except theophylline) and increases their plasma concentrations, especially in patients with initially increased clearance of theophylline under the influence of smoking. Hypotensive effect is weakened by NSAIDs (retention of sodium ions and blockade of prostaglandin synthesis by kidneys), GCS and estrogens (retention of sodium ions).

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

Special Instructions

Control of patients taking Bidop should include measurement of HR and BP (at the beginning of treatment – daily, then once every 3-4 months), ECG, determination of blood glucose in diabetic patients (once every 4-5 months).

In elderly patients it is recommended to monitor kidney function (once every 4-5 months).

Contraindications

Side effects

The side effects observed with the use of Bidop are classified into categories according to their frequency of occurrence: very frequently (≥ 1/10); frequently (≥ 1/100, < 1/10); infrequently (≥ 1/1000, < 1/100); rarely (≥ 1/10 000, < 1/1000); very rarely (< 1/10 000), including individual reports.

CNS and peripheral nervous system disorders: infrequent – increased fatigue, weakness, asthenia, dizziness, headache, sleep disturbances, depression, anxiety, confusion or short-term memory loss; rare – hallucinations, myasthenia, nightmares, seizures (including cramps in the calves).calf muscles), paresthesias in extremities (in patients with intermittent claudication and Raynaud’s syndrome), tremor.

Sensory system disorders: rare – vision disorders, decreased tear fluid secretion, dry and painful eyes; very rare – conjunctivitis.

Cardiovascular system disorders: very often – sinus bradycardia, palpitations; often – marked decrease in BP, manifestation of angiospasm (increased impairment of peripheral circulation, coldness of the lower extremities, Raynaud’s syndrome); infrequent – orthostatic hypotension, myocardial conduction disorders, AV-blockade (up to complete transverse blockade and cardiac arrest), arrhythmias, decreased myocardial contractility, development of chronic heart failure (edema of ankles, feet, shortness of breath), chest pain.

Digestive system disorders: frequently – dry mouth, nausea, vomiting, abdominal pain, constipation or diarrhea; rarely – liver disorders (dark urine, jaundice of sclerae or skin, cholestasis), changes of taste, hepatitis, increased liver enzyme activity (ACT, ALT), hyperbilirubinemia, hypertriglyceridemia.

Respiratory system disorders: infrequent – difficulty in breathing when administered in high doses (loss of selectivity) and / or in susceptible patients – laryngo- and bronchospasm; rarely – nasal congestion.

Endocrine system: hyperglycemia (in patients with insulin-independent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroidism.

Allergic reactions: rare – skin itching, rash, urticaria.

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

Hematopoietic system: in single cases – thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia.

Others: infrequent – arthralgia; rarely – back pain, decreased libido, decreased potency, withdrawal syndrome (increased angina pectoris attacks, increased BP).

Overdose

Symptoms: arrhythmia, ventricular extrasystole, marked bradycardia, AV-blockade, marked BP decrease, chronic heart failure, cyanosis of finger or palm nails, difficulty breathing, bronchospasm, dizziness, fainting, seizures, hypoglycemia.

Treatment: gastric lavage and administration of adsorptive drugs; symptomatic therapy: if AV blockade has developed – IV 1-2 mg of atropine, epinephrine or placement of a temporary pacemaker; if ventricular extrasystole – lidocaine (Class I A drugs are not used); if BP decreases – the patient should be in Trendelenburg position; if there are no signs of pulmonary edema – IV plasma exchange solutions, if ineffective – injection of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and eliminate marked BP decrease); in heart failure – cardiac glycosides, diuretics, glucagon; in seizures – IV diazepam; in bronchospasm – beta2-adrenostimulants inhaled.

Pregnancy use

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

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

Similarities