Bisoprovel

Bisoprovel is a member of the group of selective β-adrenoreceptor blockers. It is a selective β1-adrenoreceptor blocker that does not have a membrane-stabilizing effect or internal sympathomimetic effect. The drug has antianginal and antihypertensive properties.

With prolonged use of the drug, the primary effect is a decrease in increased general peripheral vascular resistance. In addition, in people with CHF, the drug inhibits the activity of the sympathoadrenal system, as well as the RAAS. [ 1 ]

Indications Bisoprovel

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

Release form

The therapeutic substance is released in the form of tablets - 10 pieces inside a cell plate; inside a pack - 2 or 3 such plates.

Pharmacodynamics

The antihypertensive effect is associated with a decrease in minute blood volume, suppression of renal renin release processes and a decrease in sympathetic stimulation in relation to peripheral vessels.

The antianginal effect develops with the blockade of β1-adrenergic receptors, which causes a weakening of cardiac function by reducing cardiac output and heart rate. As a result, the oxygen demand of the myocardium is reduced. [ 2 ]

The drug has an extremely weak affinity for the β2-terminals of the smooth muscles of blood vessels and bronchi, and in addition to this, with the β2-terminals of the endocrine system. After a single dose of Bisoprovel, its effect lasts for 24 hours. [ 3 ]

Pharmacokinetics

When taken orally, bisoprolol is well absorbed in the gastrointestinal tract. Bioavailability rates are approximately 90% and are not tied to food intake. Cmax values are noted after 1-3 hours. Protein synthesis is approximately 30%.

The first intrahepatic pass activity is quite weak (less than 10%). In the liver, approximately 50% of the dose is biotransformed to form inactive metabolites.

About 98% of the drug is excreted through the kidneys (50% is unchanged, and the remainder is in the form of metabolic components). Approximately 2% of the portion is excreted by the intestine. The half-life is 10-12 hours.

Dosing and administration

The medicine should be taken orally, 5-10 mg, once a day; the maximum daily dose is 20 mg. Dosages should be selected individually, taking into account the heart rate values and therapeutic effectiveness. The tablets are swallowed without chewing, washed down with plain water, on an empty stomach in the morning or with breakfast.

In case of coronary heart disease or high blood pressure, it is necessary to take 5-10 mg of Bisoprovel once a day.

In case of CHF, therapy should be started with a minimum dosage, gradually increasing it over several weeks. The initial dose is 1.25 mg, 1 time per day (over a period of 7 days). On the 2nd week, a dose of 2.5 mg per day is used, and on the 3rd week, 3.75 mg per day.

During the 4th-8th week of therapy, 5 mg of the drug is taken. During the 8th-12th week, the dose should be 7.5 mg. After the 12th week, the maximum daily dosage is used - 10 mg.

The increase in the dose is adjusted taking into account the heart rate and blood pressure, as well as the general condition of the patient. If necessary, the dosage can be gradually reduced. It is prohibited to abruptly stop the therapy, the treatment cycle should be completed slowly, with a gradual reduction in the dose of the drug.

People with severe renal (creatinine clearance values below 20 ml per minute) and liver dysfunction should take no more than 10 mg of the substance per day.

• Application for children

There is no clinical data regarding the therapeutic effect and safety of the drug when prescribed in pediatrics, which is why it is not used in children.

Use Bisoprovel during pregnancy

It is prohibited to use the drug during breastfeeding or pregnancy, since there is no reliable clinical information confirming its safety. If it is absolutely necessary to take Bisoprovel in pregnant women, the therapy should be discontinued 72 hours before the expected date of delivery (since the newborn may develop hypoglycemia, bradycardia and respiratory depression). If it is impossible to discontinue the drug after delivery, the baby's condition should be closely monitored. Signs of hypoglycemia develop during the first 3 days.

Contraindications

Among the contraindications:

• cardiogenic shock;
• SSSU;
• block (also sinoatrial) 2-3 degree;
• bradycardia (heart rate below 50 beats per minute);
• reduced blood pressure (systolic blood pressure level is less than 90 mm Hg);
• BA and other obstructive respiratory tract disorders;
• severe peripheral blood flow disorders;
• use in combination with MAOIs (excluding MAOI-B);
• psoriasis (also its presence in the family history);
• increased intolerance to the drug and its components.

Side effects Bisoprovel

Main side effects:

• lesions in the nervous system: dizziness, depression, fatigue, headaches and sleep disorders may occur (especially at the beginning of therapy). Hallucinations may occasionally occur (mostly weak and disappearing after 1-2 weeks), and paresthesia may sometimes develop;
• eye problems: conjunctivitis, visual disturbances and decreased lacrimation (to be taken into account by people wearing contact lenses);
• disorders associated with the functioning of the cardiovascular system: bradycardia, orthostatic collapse, AV conduction disorders, heart failure decompensation with the appearance of peripheral edema may develop. At the initial stage of therapy, the patient's condition may worsen - Raynaud's disease or intermittent claudication may develop;
• problems with the respiratory system: dyspnea is occasionally observed (in people with a tendency to bronchial spasms);
• digestive disorders: nausea, constipation, abdominal pain, diarrhea and hepatitis may occur, or plasma liver enzymes (ALT and AST) may increase;
• lesions of the musculoskeletal system: possible occurrence of cramps, muscle weakness, arthropathy (one or more joints are affected (poly- or monoarthritis));
• endocrine system dysfunction: decreased glucose tolerance (in latent diabetes mellitus) and development of masked hypoglycemia symptoms. Potency disorder and increased triglyceride levels are possible;
• Epidermal signs: dermatological manifestations – sometimes rashes, itching, hyperhidrosis and redness of the epidermis occur.
• In the case of beta-adrenergic receptor blockers, tinnitus or hearing loss, alopecia, mood swings, allergic rhinitis, and weight gain may occur. Short-term memory loss and Peyronie's disease are also possible.

Overdose

Manifestations of overdose: heart failure, decreased blood pressure, bradycardia and bronchial spasm.

Gastric lavage is performed and activated charcoal is prescribed.

In case of a decrease in blood pressure or bradycardia, glucagon is administered in a dose of 1-5 mg (no more than 10 mg) or atropine in a dosage of 1.5 mg (no more than 2 mg).

For bronchial spasm, β2-adrenergic agonists (for example, fenoterol or salbutamol) are used.

Interactions with other drugs

Administration with other antihypertensive drugs may lead to potentiation of their effect.

The use of the drug together with clonidine, reserpine, α-methyldopa or guanfacine can cause a sharp decrease in heart rate.

Use in combination with guanfacine, clonidine and digitalis substances may lead to cardiac conduction disorders.

When combining Bisoprolol with sympathomimetics (contained in eye, nasal drops, antitussive drugs), the activity of bisoprolol may decrease.

Ca antagonists (dihydropyridine derivatives) are able to potentiate the antihypertensive effect of the drug.

The combination of the drug with diltiazem or verapamil and other antiarrhythmic drugs can lead to a decrease in heart rate and blood pressure, and also to the development of heart failure or arrhythmia (it is prohibited to prescribe the drug together with antiarrhythmic drugs and Ca channel blockers).

When combining the drug with clonidine, the latter can be discontinued only after several days have passed since the administration of bisoprolol has been stopped, since this can significantly increase blood pressure.

Administration together with ergotamine derivatives (including ergotamine-containing anti-migraine drugs) may potentiate signs of peripheral blood flow disorder.

Concomitant use with rifampicin may slightly decrease the half-life of bisoprolol.

Combination with orally administered hypoglycemic drugs or insulin causes a softening or masking of the manifestations of hypoglycemia (it is necessary to constantly monitor blood glucose levels).

Storage conditions

Bisoprovel must be stored in a dark and dry place, out of the reach of small children. The temperature level should not exceed 25°C.

Shelf life

Bisoprovel can be used for a period of 36 months from the date of sale of the pharmaceutical product.

Analogues

The analogs of the drug are Biprolol, Concor, Bicard with Bisoprolol, and in addition Coronal, Bisoprol, and Eurobisoprolol with Dorez.