Biol, 10 mg 50 pcs.

Biol is a selective beta1-adrenoblocker without its own sympathomimetic activity. It has no membrane stabilizing effect. Reduces blood plasma renin activity, reduces myocardial oxygen demand, reduces HR at rest and under load. It has hypotensive, antiarrhythmic and antianginal effects. By blocking in low doses β1-adrenoreceptors of heart, it reduces catecholamine-stimulated formation of cAMP from ATP, decreases intracellular calcium ion current, has negative chrono-, dromo-, batmo- and inotropic effect. It suppresses conduction and excitability, slows down AV conductivity. PPS increases in the first 24 hours of usage (as a result of reciprocal increase of α-adrenoreceptor activity and elimination of β2-adrenoreceptor stimulation). It returns to initial level after 1-3 days and decreases with prolonged use.

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 of aortic arch baroreceptors (there is no increase of their activity in response to BP decrease and influence on CNS). In arterial hypertension the effect comes in 2-5 days, stable hypotensive effect in 1-2 months.

The antianginal effect is caused by decrease of myocardial oxygen demand as a result of shortening of HR and decrease of contractility, prolongation of diastole, improvement of myocardial perfusion. By increasing left ventricular end-diastolic pressure and increasing ventricular muscle fiber stretch can 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), the 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.

In contrast to non-selective beta-adrenoblockers, when administered in medium therapeutic doses, it has less pronounced effect on the organs containing β2-adrenoreceptors (pancreas, skeletal muscles, smooth muscle of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism. It does not cause retention of sodium ions in the body. When increasing the dose above the therapeutic it has a beta2-adrenoblocking effect.

Indications

Active ingredient

Composition

1 tablet contains bisoprolol hemifumarate 10 mg;

excipients:

microcrystalline cellulose,

calcium hydrophosphate,

corn starch,

croscarmellose sodium,

magnesium stearate,

colloidal anhydrous silicon dioxide.

How to take, the dosage

The tablets should be taken in the morning, regardless of meals, not chewed, with a small amount of liquid

In arterial hypertension and angina pectoris in all cases, the dosing regimen is set individually by the doctor, taking into account the heart rate and the patient’s condition. The initial daily dose is 5 mg (sometimes 2.5 mg) once a day, if necessary, the dose is increased to 10 mg once a day. The maximum daily dose is 20 mg.

In patients with severe renal insufficiency (CKR less than 20 ml/min) or with severe hepatic impairment, the maximum daily dose should not exceed 10 mg.

Dose adjustment for elderly patients is usually not necessary, but for some patients a dose of 5 mg daily may be optimal.

Interaction

Allergens used for immunotherapy (or allergen extracts for skin tests) increase the risk of severe systemic allergic reactions and anaphylaxis in patients receiving bisoprolol.

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

Diuretics, clonidine, sympatholytics, hydralazine, nifedipine, and other hypotensive agents can cause excessive BP lowering.

Iodine-containing radiopaque agents for IV administration increase the risk of anaphylactic reactions.

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

Bisoprolol masks the adrenergic symptoms of thyrotoxicosis and hypoglycemia (e.g., tachycardia).

Decreases clearance of lidocaine and xanthines (except diphylline) and increases their plasma concentrations, especially in patients with initially increased clearance of theophylline due to tobacco smoking.

The hypotensive effect of bisoprolol is impaired by NSAIDs (sodium ion retention and renal blockade of prostaglandin synthesis), GCS and estrogens (sodium ion retention).

Longens the effect of nondepolarizing myorelaxants and the anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives and hypnotics increase CNS depression.

The concomitant use with MAO inhibitors is not recommended due to the significant increase in hypotensive effect; a treatment break of at least 14 days between MAO inhibitors and bisoprolol should be taken.

Unhydrogenated ergot alkaloids increase the risk of peripheral circulatory disorders.

Sulfasalazine increases the plasma concentration of bisoprolol.

Rifampicin shortens the T 1/2 of bisoprolol.

Special Instructions

Biol should not be abruptly interrupted because of the risk of severe arrhythmias and myocardial infarction. Discontinuation is done gradually, reducing the dose by 25% every 3 to 4 days.

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

Contraindications

Side effects

CNS disorders:fatigue, weakness, asthenia, dizziness, headache, sleep disorders, nightmares, mental disorders (depression), paresthesias in the extremities (in patients with intermittent claudication and Raynaud’s syndrome), impaired concentration, myasthenia, tremor.

Overlooking organ: visual disturbances, decreased tear fluid secretion (should be considered when wearing contact lenses), dry and painful eyes, conjunctivitis.

Cardiovascular system side: orthostatic hypotension, pain behind the sternum, sinus bradycardia, myocardial conduction disorders, AV blockade, withdrawal syndrome (increased angina pectoris attacks, increased BP), manifestation of angiospasm (increased peripheral circulation disorders, coldness of the lower extremities, Raynaud’s syndrome), development (aggravation) of the course of chronic heart failure.

From the digestive system: dry oral mucosa, nausea, vomiting, dyspepsia, diarrhea, change in taste, disorders of liver function (symptoms of cholestasis), hepatitis, increased levels of ALT, AST, bilirubin.

In the respiratory system:nasal congestion, pharyngitis, rhinitis, sinusitis, cough, in predisposed patients – laryngo- and bronchospasm.

Skin disorders: increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions, exacerbation of psoriasis symptoms, alopecia.

With the hematopoietic system: thrombocytopenia, agranulocytosis, leukopenia.

Allergic reactions:cutaneous itching, rash, urticaria.

Other:sweating, back pain, arthralgia, muscle pain, impaired sexual function, dysuria, hyperglycemia (in patients with insulin-independent diabetes), hypoglycemia (in patients receiving insulin), hypothyroidism, increased triglyceride levels.

Overdose

Symptoms: arrhythmia, ventricular extrasystole, marked bradycardia, AV-blockade, marked BP decrease, acute heart failure, hypoglycemia, acrocyanosis, breathing difficulties, bronchospasm, dizziness, fainting, seizures.

Treatment: gastric lavage and administration of adsorptive drugs. Symptomatic therapy is carried out: if AV-blockade has developed – intravenous injection of atropine (1-2 mg), 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); in heart failure – cardiac glycosides, diuretics, glucagon ; in convulsions – IV diazepam ; in bronchospasm – inhaled beta 2-adrenomimetics.

Similarities