Bisokard

Bisokard is a β1-adrenergic blocker of the cardioselective type.

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

The selectivity of the drug to β1-adrenergic receptors is maintained even when the required drug dosages are exceeded.

Indications Bisokard

It is used for the treatment of coronary artery disease (angina pectoris), high blood pressure and heart failure .

Release form

The release of the medication is made in tablets with a volume of 5 or 10 mg, 30 pieces each inside a cell package; inside the box - 1 or 2 such packages.

Pharmacodynamics

There is no final data on the exact principle of drug exposure with increased blood pressure. It is known that the drug significantly weakens the intraplasmic activity of renin. [2]

In people with angina pectoris, Bisokard reduces the oxygen demand of the myocardium, lowering the values of cardiac output and heart rate. At the same time, the minute blood volume decreases slightly; the increase in the wedging pressure inside the capillaries of the lungs and the pressure inside the right atrium is also insignificant. [3]

Clinical tests have shown that in people with heart failure and stable symptomatic insufficiency of the systolic type (ejection fraction is <35%) when using the medication:

• the mortality rate decreases;
• the number of incidents with sudden coronary death and cases with heart failure and further hospitalization is decreasing;
• improved when evaluated by NYHA.

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

The values of OPSS with the use of drugs first 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 you to take it once a day).

The excretion of the drug is realized through the kidneys (the unchanged substance is 50%, and the remainder is metabolites with no activity, formed inside the liver), only 2% is excreted in feces. Due to the fact that the kidneys with the liver are equivalent participants in the elimination of bisoprolol, people with insufficient function of one of these organs do not need to adjust the dosage.

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

In people with CHF (NYHA class III), the bisoprolol level and half-life term exceeded the values 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 size is selected individually.

The tablets are swallowed whole with plain water. You need to use Bisokard before meals or with it (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 abruptly cancel therapy, the course ends with a gradual decrease in dosage.

Persons with impaired renal / liver function.

People with severe hepatic / renal dysfunctions (CC values less than 20 ml per minute) should not use more than 10 mg of the drug per day.

• Application for children

You can not use the medicine in pediatrics (in persons under the age of 18).

Use Bisokard during pregnancy

It is forbidden to prescribe Bisokard during pregnancy and GV.

Contraindications

The main contraindications:

• severe intolerance to the elements of the drug;
• decompensated HF, SSS, cardiogenic shock, pronounced form of sinoatrial blockade, as well as degree 2-3 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 asthma;
• Raynaud's syndrome, late stage peripheral blood flow disorders;
• untreated pheochromocytoma;
• metabolic acidosis.

Side effects Bisokard

Among the side effects:

• disturbances in the work of the NA: dizziness, fatigue, strange weakness, cephalgia and insomnia are often noted. Depression, attention disorder, asthenia, paresthesia, drowsiness, tinnitus and anxiety, emotional instability, seizures, visual disturbances, and decreased tear production are sometimes observed. Hallucinations occur occasionally;
• problems with visual function: rarely, there is a decrease in lacrimation (must be taken into account when wearing contact lenses). Conjunctivitis occurs singly;
• disorders of the cardiovascular system and the circulatory system: bradycardia often appears. Sometimes HF, arrhythmia, decreased blood pressure values (also orthostatic collapse), blockade, intermittent claudication, thrombocytopenia, agranulocytosis, Raynaud's disease and thrombocytopenic purpura are noted;
• lesions in the gastrointestinal tract: often there is vomiting, constipation, xerostomia, nausea, dyspeptic symptoms, diarrhea and ischemic colitis. Occasionally, metabolic disorders (an increase in the blood values of triglycerides) and hepatitis develop, and the intraplasmic activity of liver enzymes (ALT with AST) also increases;
• respiratory disorders: sometimes there is dyspnea, pharyngitis, cough, sinusitis, laryngo- and bronchial spasm, respiratory tract infection and a runny nose of an allergic nature;
• signs associated with the urogenital system: rarely, there is a weakening of libido, cystitis, peripheral edema, impotence, colic in the kidney and Peyronie's disease;
• epidermal lesions: itching, hyperhidrosis, allergy symptoms, rashes, reddening of the epidermis, acne, psoriatic rash (psoriasis worsens) and dermatitis are sometimes observed. Alopecia is singularly noted;
• dysfunction of the musculoskeletal system: sometimes convulsions and myasthenia gravis appear;
• metabolic problems: occasionally hyperuricemia develops, insulin resistance increases and weight increases.
• others: myalgia, asthenia, arthralgia, hearing impairment.

Overdose

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

Occasionally, with the introduction of a maximum portion of 2 g, there was a decrease in the heart rate or a decrease in blood pressure. Persons with heart failure are more sensitive to increased dosages of bisoprolol, therefore, it is necessary to increase the dose of drugs gradually.

Hemodialysis procedures are ineffective. In case of intoxication, you need to cancel the use of the medication, perform gastric lavage, take activated charcoal 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;
• reduced blood pressure values - the use of vasoconstrictors, intravenous injection of plasma-replacing fluids, glucagon;
• AV blockade of the 2-3rd degree - intravenous injection of isoprenaline, monitoring the patient's condition; use a pacemaker if necessary;
• active stage of CHF - intravenous use of inotropic drugs, diuretics and vasodilators;
• bronchial spasm - inhalation of β2-adrenostimulants, the use of aminophylline or bronchodilators (isoprenaline);
• hypoglycemia - intravenous injection of glucose.

Interactions with other drugs

It is forbidden to use the medicine together with such substances:

• agents blocking Ca channels (diltiazem, verapamil and nifedipine) - this negatively affects AV conduction, myocardial contractility and blood pressure;
• clonidine - there is a possibility of a decrease in heart rate and impaired conduction of impulses inside the myocardium; cancellation of clonidine can cause a sharp increase in blood pressure;
• MAOIs (excluding MAOI-B) - after the cancellation of the use of MAOIs, a hypertensive crisis may develop.

Caution is needed 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;
• drugs that slow down the activity of COX - reduce the antihypertensive effect of bisoprolol;
• anticholinergics (tacrine) - there is a possibility of prolongation of AV conduction;
• digitalis glycosides - the risk of 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 the therapeutic effect;
• class I antiarrhythmic substances (quinidine with disopyramide) - prolongation of the atrial conduction period and negative inotropic effect;
• sympathomimetics - a mutual decrease in drug activity (when using Bisokard with adrenaline, you need to increase the dosage of the latter);
• substances for general anesthesia and inhalation anesthesia - the likelihood of suppression of myocardial function and reflex tachycardia, a decrease in blood pressure values; while the combination of bisoprolol and anesthetics reduces the likelihood of arrhythmia during intubation and the initial stage of anesthesia. It is required to notify the anesthesiologist about the use of the medication before the operation;
• taken orally antidiabetic drugs and insulin - an increase in the likelihood of hypoglycemia;
• rifampicin - a slight decrease in the half-life of bisoprolol;
• NSAIDs - a decrease in the antihypertensive activity of the drug.

Storage conditions

The bisokard must be kept out of the reach of children. Temperature indicators - no more than 30 ° С.

Shelf life

Bisokard can be used for a 3-year term from the date of manufacture of the therapeutic agent.

Analogs

The analogues of the medication are the drugs Tirez, Concor, Biprol with Bisoprolol, Aritel and Coronal, and besides this Bidop and Biol with Niperten, Cordinorm and Bisogamma with Bisomor.