Bisoprofar

Bisoprofar is a member of the group of selective ß1-adrenoblockers. Use in therapeutic doses does not lead to the appearance of VSA and clinically noticeable membrane-stabilizing effect.

It has antianginal properties: it reduces the oxygen demand of the myocardium, reducing the heart rate, blood pressure and cardiac output; in addition, the drug increases the volume of oxygen supplied to the myocardium - prolonging diastole and lowering the values of end-diastolic pressure. [ 1 ]

Indications Bisoprofar

It is used for elevated blood pressure, as well as for the treatment of coronary heart disease (angina) and CHF accompanied by systolic left ventricular dysfunction (in combination with diuretics and ACE inhibitors, and, if necessary, with SG).

Release form

The medicinal substance is released in tablets - 10 pieces in a cell plate; there are 3 such plates in a pack.

Pharmacodynamics

The drug has an antihypertensive effect, reducing cardiac output and slowing renal renin secretion, and also influencing the baroreceptors of the aortic arch with the carotid sinus. Long-term use of bisoprolol primarily leads to a decrease in increased resistance of peripheral vessels. In the case of CHF, Bisoprofar inhibits activated RAAS and the sympathoadrenal system. [ 2 ]

Bisoprolol has an extremely low affinity for the ß2-endings of the smooth muscles of blood vessels and bronchi, and in addition to this, for the ß2-endings of the endocrine system. The drug can only occasionally affect the smooth muscles of peripheral arteries with bronchi and glucose metabolism. [ 3 ]

Pharmacokinetics

Bisoprolol is almost completely and rapidly absorbed in the gastrointestinal tract. In combination with the extremely weak effect of the first intrahepatic passage, this forms a high bioavailability index (approximately 90%). Approximately 30% of the substance is synthesized with blood protein. The level of distribution volume is 3.5 l/kg. Systemic clearance is approximately 15 l/hour.

The plasma half-life is 10-12 hours, so that with a single daily dose the therapeutic effect is observed for 24 hours.

Excretion of bisoprolol is realized in 2 ways. 50% of the dosage is involved in intrahepatic metabolic processes with the formation of inactive metabolites, which are then excreted through the kidneys. The remaining 50% of the dosage is excreted through the kidneys in an unchanged state.

When the drug is administered to people with CHF (stage 3), the plasma drug level and half-life duration increase. Plasma Cmax values at dynamic equilibrium are 64±21 ng/ml after administration of a daily dose of 10 mg; the half-life duration is 17±5 hours.

Dosing and administration

Bisoprofar is taken orally - the tablet should be swallowed whole, without chewing, with plain water. It is taken in the morning (can be taken with food). If necessary, the tablet can be divided into two equal portions.

The standard dosage for high blood pressure and angina is 5 mg once a day (no more than 20 mg once a day). The dosage regimen is changed by the doctor, individually for each patient.

• Application for children

There is no information regarding the therapeutic effect and safety of drug use in pediatrics.

Use Bisoprofar during pregnancy

Prescribing Bisoprofar during pregnancy is allowed only in cases where the probable benefit to the woman is more expected than the risks of complications in the fetus. Often, ß-blockers weaken blood circulation inside the placenta and can affect fetal development. If it is necessary to use ß-blockers, it is recommended to use selective ß1-blockers. It is necessary to monitor blood circulation inside the uterus and placenta.

After birth, the infant's condition must be carefully monitored. The development of signs of bradycardia and hypoglycemia occurs in the first 3 days.

There is no information on whether bisoprolol is excreted in breast milk, which is why it cannot be used during breastfeeding.

Contraindications

Main contraindications:

• severe intolerance to bisoprolol or other components of the drug;
• active form of heart failure or decompensated heart failure, which requires inotropic treatment;
• 2-3 degree block (without using a pacemaker);
• cardiogenic shock;
• severe form of sinoatrial block;
• SSSU;
• symptomatic bradycardia (heart rate below 60 beats per minute);
• decreased blood pressure (systolic blood pressure values are less than 100 mmHg);
• severe bronchial asthma or severe obstructive pulmonary lesions that are chronic;
• Raynaud's syndrome and peripheral circulatory disorders in the late stages of development;
• untreated pheochromocytoma;
• metabolic acidosis.

Side effects Bisoprofar

Side effects include:

• disorders in the nervous system: syncope, headache*, dizziness*;
• problems with visual function: conjunctivitis and decreased lacrimation (must be taken into account by people using contact lenses);
• mental disorders: depression, paresthesia, sleep disorders, hallucinations and nightmares;
• symptoms associated with the work of the cardiovascular system: bradycardia (in people with CHF, coronary heart disease or high blood pressure), orthostatic collapse, numbness and coldness of the extremities, AV conduction disorder, decreased blood pressure, signs of worsening CHF;
• gastrointestinal tract lesions: abdominal pain, vomiting, constipation, nausea and diarrhea;
• digestive disorders: hepatitis or increased activity of liver enzymes (ALT and AST);
• problems associated with the mediastinal organs and the respiratory system: allergic rhinitis or bronchial spasm in individuals with asthma or a history of chronic obstructive respiratory diseases;
• connective tissue and musculoskeletal disorders: cramps, muscle weakness and arthropathy;
• auditory disorders: hearing loss;
• problems with the epidermis and subcutaneous layer: signs of intolerance (redness, hyperhidrosis, itching and rashes). Also, ß-blockers can cause the development of psoriasis, potentiate its symptoms or lead to the appearance of psoriasis-like rashes and alopecia;
• disturbances in nutritional and metabolic processes: hypoglycemia and increased triglyceride levels;
• manifestations associated with the reproductive system: erectile dysfunction;
• immune disorders: allergic rhinitis and the development of antinuclear antibodies, which are occasionally accompanied by clinical signs of SLE (they disappear after discontinuation of treatment);
• changes in test results: increase in plasma activity of liver enzymes (ALT with AST) and blood triglyceride levels;
• systemic disorders: fatigue* or asthenia.

*applies only to individuals with coronary heart disease or high blood pressure.

These symptoms often develop at the beginning of treatment, are mild and disappear after 1-2 weeks.

Overdose

Signs of poisoning: third-degree AV block, active heart failure, bradycardia, decreased blood pressure, dizziness, hypoglycemia and bronchial spasm.

In case of intoxication, therapy should be stopped immediately and the doctor should be informed. Taking into account the severity of the poisoning, symptomatic and supportive procedures are carried out:

• bradycardia – administration of isoprenaline and atropine, installation of pacemaker;
• low blood pressure – use of vasoconstrictors and fluid administration;
• AV block – administration of isoprenaline infusion and transvenous pacemaker implantation;
• bronchial spasm – use of ß-sympathomimetics and isoprenaline;
• potentiation of heart failure – use of diuretics, vasodilators and inotropic substances;
• hypoglycemia – the use of glucose.

Interactions with other drugs

The medication may potentiate the activity of other antihypertensive drugs.

Administration of the drug together with reserpine, clonidine or guanfacine can significantly reduce the heart rate and lead to cardiac conduction disorders.

Nifedipine and other substances that block Ca channels can potentiate the antihypertensive effect of Bisoprofar; when combined with the drug, diltiazem and verapamil, the heart rate may also decrease.

Combined use with ergotamine derivatives (including ergotamine-containing anti-migraine agents) potentiates signs of peripheral blood flow disorder.

Combination with oral hypoglycemic drugs or insulin leads to some weakening or masking of the manifestations of hypoglycemia (it is necessary to constantly monitor blood sugar levels).

Administration of medication with antiarrhythmic substances may disrupt the heart rhythm.

Allergens used in immunotherapy in combination with β-blockers can cause severe general allergic symptoms.

When using the drug with substances for inhalation anesthesia, myocardial function is suppressed, and the likelihood of developing antihypertensive symptoms increases.

Combined use with iodine-containing radiocontrast agents increases the likelihood of anaphylactic symptoms.

The introduction of rifampicin somewhat shortens the half-life of bisoprolol, but in this case an increase in the dosage of the latter is usually not required.

Storage conditions

Bisoprofar should be stored in a place inaccessible to small children. Temperature values should not exceed 25°C.

Shelf life

Bisoprofar can be used for a period of 24 months from the date of manufacture of the medicine.

Analogues

Analogues of the drug are Bidop, Bisoprol, Biprolol with Bisoprovel, and also Alotendin, Bisocard with Bicard, Dorez and Bisostad.