Bisopropel

Bisopropel belongs to the group of selective β-adrenergic receptor blockers. It is a selective β1-adrenergic blocker that does not have a membrane stabilizing effect and an internal sympathomimetic effect. The drug has antianginal and antihypertensive properties.

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

Indications Bisopropel

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

Release form

The release of the therapeutic substance is made in the form of tablets - 10 pieces inside the 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 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 weakened. [2]

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

Pharmacokinetics

When taken orally, bisoprolol is well absorbed inside the gastrointestinal tract. Bioavailability is approximately 90% and is not food-related. The Cmax values are noted after 1-3 hours. Protein synthesis is approximately 30%.

The activity of the 1st intrahepatic passage is rather weak (below 10%). Inside the liver, approximately 50% of the dosage is biotransformed with the formation of inactive metabolites.

About 98% of drugs are excreted through the kidneys (50% has an unchanged form, and the remainder is in the form of metabolic components). Approximately 2% of a serving is excreted by the intestines. The half-life is 10-12 hours.

Dosing and administration

You need to use the medicine orally, 5-10 mg, 1 time per day; the maximum daily serving size is 20 mg. It is necessary to select dosages personally, taking into account the heart rate values and therapeutic efficacy. The tablets are swallowed without chewing, washed down with plain water, on an empty stomach in the morning or with breakfast.

In the case of ischemic heart disease or elevated blood pressure, it is required to take 5-10 mg of Bisopropel 1 time per day.

With CHF, therapy should be started with a minimum dosage, gradually increasing it over several weeks. The size of the initial portion is 1.25 mg, once a day (within 7 days). On the 2nd week, a portion of 2.5 mg per day is used, and on the 3rd - 3.75 mg per day.

In the period of 4-8 weeks of therapy, 5 mg of drugs are taken. During weeks 8-12, the serving should be 7.5 mg. After the 12th week, the maximum dosage per day is applied - 10 mg.

The increase in the portion is adjusted taking into account the level of heart rate and blood pressure, as well as the general condition of the patient. If necessary, the dosage can be gradually reduced. It is forbidden to abruptly cancel therapy, the treatment cycle should be completed slowly, with a gradual decrease in the portion of the medicine.

Persons with severe renal (CC values - below 20 ml per minute) and hepatic dysfunctions should take no more than 10 mg of the substance per day.

• Application for children

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

Use Bisopropel during pregnancy

It is forbidden to use the medicine for hepatitis B or pregnancy, since there is no reliable clinical information confirming its safety. If it is absolutely necessary to take Bisopropel in pregnant women, therapy should be canceled 72 hours before the expected due date (since the newborn may develop hypoglycemia, bradycardia and respiratory depression). If it is impossible to cancel drugs after childbirth, you need to carefully monitor the condition of the baby. Signs of hypoglycemia develop during the first 3 days.

Contraindications

Among the contraindications:

• cardiogenic shock;
• SSSU;
• blockade (also sinoatrial) of the 2-3rd degree;
• bradycardia (heart rate indicators below 50 beats per minute);
• decreased blood pressure (systolic blood pressure - less than 90 mm Hg);
• BA and other obstructive respiratory tract lesions;
• disorders of peripheral blood flow in a severe degree;
• use in combination with IMAO (excluding IMAO-B);
• psoriasis (also a family history of it);
• increased intolerance to the drug and its elements.

Side effects Bisopropel

The main side symptoms:

• lesions in the NS area: the appearance (especially at the beginning of therapy) of dizziness, depression, fatigue, cephalalgia and sleep disorders is possible. Occasionally hallucinations occur (mostly weak and disappear after 1-2 weeks), sometimes paresthesias may develop;
• eye problems: conjunctivitis, visual disturbances and weakening of lacrimation (take into account people wearing contact lenses);
• disorders associated with the work of the CVS: the development of bradycardia, orthostatic collapse, AV conduction disorders, HF decompensation with the appearance of peripheral edema is possible. At the initial stage of therapy, the patient's condition may worsen - Raynaud's disease or intermittent claudication develops;
• problems with the respiratory system: dyspnoea is occasionally noted (in persons with a tendency to bronchial spasms);
• disorders of the digestive function: there may be nausea, constipation, abdominal pain, diarrhea and hepatitis, or an increase in the plasma index of liver enzymes (ALT with AST);
• damage to the musculoskeletal system: seizures, muscle weakness, arthropathy may occur (one or more joints are affected (poly- or monoarthritis));
• disorders of the endocrine system: a decrease in glucose tolerance (with latent diabetes mellitus) and the development of masked symptoms of hypoglycemia. Potency disorder and an increase in triglyceride levels are possible;
• epidermal signs: dermatological manifestations - sometimes there are rashes, itching, hyperhidrosis and redness of the epidermis.
• In the case of the use of β-adrenoreceptor blockers, ear noise or hearing impairment, alopecia, mood lability and a runny nose of an allergic nature may appear, and in addition, weight increase. Short-term memory loss and Peyronie's disease are also possible.

Overdose

Overdose manifestations: HF, decreased blood pressure, bradycardia and bronchial spasm.

Gastric lavage is performed, activated charcoal is prescribed.

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

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

Interactions with other drugs

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

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

The use in combination with guanfacine, clonidine and digitalis substances can lead to cardiac conduction disorders.

When combining Bisoprolol with sympathomimetics (contained in eye drops, 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 drugs with diltiazem or verapamil and other antiarrhythmic drugs can lead to a decrease in heart rate and blood pressure, and in addition to the development of heart failure or arrhythmia (it is forbidden to prescribe the drug together with antiarrhythmic drugs and Ca channel blockers).

When combining a drug with clonidine, the cancellation of the latter can be performed only after a few days have passed after the cessation of the administration of bisoprolol - since this can significantly increase the blood pressure.

The introduction together with derivatives of ergotamine (among them ergotamine-containing anti-migraine drugs) can potentiate the signs of a disorder of peripheral blood flow.

Concomitant use with rifampicin may not significantly decrease the half-life of bisoprolol.

The combination with oral hypoglycemic drugs or insulin causes a softening or masking of the manifestations of hypoglycemia (you need to constantly monitor the blood glucose values).

Storage conditions

Bisopropel must be kept in a dark and dry place, closed from small children. The temperature level is not more than 25 ° C.

Shelf life

Bisopropel can be used for a 36-month term from the date of sale of the pharmaceutical product.

Analogs

The analogs of the drug are the substances Biprolol, Concor, Bikard with Bisoprolol, and in addition to this Coronal, Bisoprol, and Eurobisoprolol with Dorez.