Bisocard

Bisocard is a cardioselective β1-adrenergic blocker.

The drug has a weak affinity for bronchial and vascular smooth muscle β2-adrenoreceptors, as well as for β2-endings, which regulate metabolic processes. Because of this, it has a weak effect on the resistance of the bronchial tree and metabolic processes that depend on β-endings. [ 1 ]

The drug's selectivity for β1-adrenergic receptors is maintained even when the required medicinal dosages are exceeded.

Indications Bisocard

It is used to treat coronary heart disease (angina pectoris), high blood pressure and CHF.

Release form

The drug is released in tablets with a volume of 5 or 10 mg, 30 pieces in a cell package; there are 1 or 2 such packages in a box.

Pharmacodynamics

There are no definitive data regarding the exact principle of the drug's action at elevated blood pressure levels. It is known that the drug significantly weakens intraplasmic renin activity. [ 2 ]

In people with angina, Bisocard reduces the oxygen demand of the myocardium, lowering the values of cardiac output and heart rate. The minute blood volume decreases slightly; the increase in the wedge pressure inside the pulmonary capillaries and the pressure inside the right atrium is also insignificant. [ 3 ]

Clinical trials have shown that in individuals with heart failure and stable symptomatic systolic failure (ejection fraction <35%), when using the drug:

• the mortality rate decreases;
• the number of incidents of sudden coronary death and cases of heart failure and subsequent hospitalization is reduced;
• Improves performance as assessed by the NYHA registry.

In people with coronary artery disease and without CHF, the drug reduces the heart rate and systolic volume, which reduces the oxygen demand of the myocardium and ejection volumes.

When using drugs, the values of OPSS initially increase, and then, with prolonged use, decrease.

Pharmacokinetics

After oral administration, it is almost completely absorbed. The bioavailability index is approximately 90%. Protein synthesis is 30%.

The half-life of bisoprolol is approximately 10-12 hours (which allows it to be taken once a day).

The drug is excreted through the kidneys (unchanged substance makes up 50%, and the remainder is inactive metabolites formed in the liver), only 2% is excreted with feces. Due to the fact that the kidneys and liver are equal participants in the elimination of bisoprolol, people with insufficiency of one of these organs do not require dosage adjustment.

The pharmacokinetic properties of the drug are linear. In individuals using 10 mg of the drug per day, the plasma Cmax values are 64±21 ng/ml, and the half-life term is 17±5 hours.

In people with CHF (class III according to the NYHA registry), bisoprolol levels and half-life were higher than those recorded in volunteers.

Dosing and administration

The recommended daily dosage is 5 mg. If necessary, this portion can be increased to 10 mg (but only in extreme cases). A maximum of 20 mg of the drug is allowed per day. The dosage is selected individually.

The tablets are swallowed whole with plain water. Bisocard should be taken before or with meals (it is recommended to take the medicine at the same time of day).

The therapeutic cycle is quite long. Its duration depends on the course and severity of the disease. It is forbidden to suddenly stop the therapy, the course ends with a gradual reduction in dosage.

Persons with renal/liver impairment.

People with severe liver/renal dysfunction (creatinine clearance less than 20 ml per minute) should not take more than 10 mg of the drug per day.

• Application for children

The medicine cannot be used in pediatrics (in persons under 18 years of age).

Use Bisocard during pregnancy

It is prohibited to prescribe Bisocard during pregnancy and breastfeeding.

Contraindications

Main contraindications:

• severe intolerance to the components of the drug;
• decompensated heart failure, SSSU, cardiogenic shock, severe sinoatrial block, as well as 2nd-3rd degree AV block;
• symptomatic bradycardia with a heart rate below 50 beats per minute, decreased blood pressure (systolic pressure less than 100 mm Hg);
• obstructive bronchitis and severe stage of bronchial asthma;
• Raynaud's syndrome, late-stage peripheral circulatory disorders;
• untreated pheochromocytoma;
• metabolic acidosis.

Side effects Bisocard

Side effects include:

• Disorders of the nervous system: dizziness, fatigue, strange weakness, headache and insomnia are often observed. Sometimes depression, difficulty concentrating, asthenia, paresthesia, drowsiness, tinnitus and anxiety, emotional instability, seizures, visual disturbances and decreased secretion of tear fluid are observed. Hallucinations occur rarely;
• problems with visual function: decreased lacrimation is occasionally observed (this should be taken into account when wearing contact lenses). Conjunctivitis occurs occasionally;
• disorders of the cardiovascular system and blood system: bradycardia often appears. Sometimes heart failure, arrhythmia, decreased blood pressure (also orthostatic collapse), blockade, intermittent claudication, thrombocytopenia, agranulocytosis, Raynaud's disease and thrombocytopenic purpura are observed;
• Gastrointestinal tract lesions: vomiting, constipation, xerostomia, nausea, dyspeptic symptoms, diarrhea and ischemic colitis often occur. Metabolic disorders (increased blood triglyceride levels) and hepatitis occasionally develop, and the intraplasmic activity of liver enzymes (ALT with AST) also increases;
• respiratory disorders: sometimes dyspnea, pharyngitis, cough, sinusitis, laryngeal and bronchial spasm, respiratory tract infection and allergic rhinitis occur;
• signs associated with the urogenital system: occasionally there is a decrease in libido, cystitis, peripheral edema, impotence, colic in the kidney area and Peyronie's disease;
• epidermal lesions: sometimes there is itching, hyperhidrosis, allergy symptoms, rashes, redness of the epidermis, acne, psoriatic rash (psoriasis worsens) and dermatitis. Alopecia is observed sporadically;
• musculoskeletal dysfunction: sometimes cramps and myasthenia appear;
• Metabolic problems: hyperuricemia occasionally develops, insulin resistance increases, and weight increases.
• others: myalgia, asthenia, arthralgia, hearing loss.

Overdose

Signs of poisoning: bronchial spasm, hypoglycemia, bradycardia, blockade, decreased blood pressure and active heart failure.

Rarely, when the maximum dose of 2 g was administered, a decrease in heart rate or a decrease in blood pressure was observed. People with heart failure are more sensitive to increased doses of bisoprolol, so their dose of the drug should be increased gradually.

Hemodialysis procedures are ineffective. In case of intoxication, it is necessary to stop using the drug, perform gastric lavage, take activated carbon and carry out symptomatic procedures:

• bradycardia – intravenous administration of atropine (isoprenaline or other drugs with a chronotropic effect); if necessary, a temporary pacemaker is used;
• decreased blood pressure values – use of vasoconstrictors, intravenous injections of plasma-substituting fluids, glucagon;
• AV block of 2-3 degree – intravenous injection of isoprenaline, monitoring of the patient’s condition; if necessary, use a pacemaker;
• active stage of CHF – intravenous administration of inotropic drugs, diuretics and vasodilators;
• bronchial spasm – inhalation of β2-adrenergic agonists, use of aminophylline or bronchodilators (isoprenaline);
• hypoglycemia – intravenous injection of glucose.

Interactions with other drugs

It is prohibited to use the medicine together with the following substances:

• Ca channel blockers (diltiazem, verapamil and nifedipine) – this has a negative effect on AV conduction, myocardial contractility and blood pressure levels;
• clonidine - there is a possibility of a decrease in heart rate and disruption of impulse conduction within the myocardium; discontinuation of clonidine may cause a sharp increase in blood pressure;
• MAOIs (excluding MAOI-B) – hypertensive crisis may develop after discontinuation of MAOI use.

Caution is required when combining with such drugs:

• barbiturates, tricyclics, phenothiazine derivatives and other antihypertensive drugs - there is a possibility of a strong decrease in blood pressure values;
• agents that inhibit COX activity – reduce the antihypertensive effect of bisoprolol;
• anticholinergics (tacrine) – there is a possibility of prolongation of AV conduction;
• digitalis glycosides – risk of developing arrhythmia and bradycardia;
• ergotamine derivatives - this combination potentiates peripheral blood flow disorders;
• other β-blockers (also in the form of eye drops) – mutual enhancement of therapeutic effects;
• antiarrhythmic drugs of class I (quinidine with disopyramide) – prolongation of the atrial conduction period and negative inotropic effect;
• sympathomimetics – mutual reduction of drug activity (when using Bisocard with adrenaline, the dosage of the latter must be increased);
• substances for general anesthesia and inhalation anesthesia - the probability of suppression of myocardial function and reflex tachycardia, a decrease in blood pressure values; at the same time, the combination of bisoprolol and anesthetics reduces the probability of arrhythmia during intubation and the initial stage of anesthesia. It is necessary to notify the anesthesiologist about the use of the drug before surgery;
• Orally taken antidiabetic drugs and insulin - increased likelihood of hypoglycemia;
• rifampicin - slight decrease in the half-life of bisoprolol;
• NSAIDs – decrease in the antihypertensive activity of the drug.

Storage conditions

Bisocard should be stored in a place out of reach of children. Temperature indicators – no more than 30°С.

Shelf life

Bisocard can be used for a period of 3 years from the date of production of the therapeutic agent.

Analogues

The analogs of the drug are Tirez, Concor, Biprol with Bisoprolol, Aritel and Coronal, as well as Bidop and Biol with Niperten, Cordinorm and Bisogamma with Bisomor.