Biprolol

Biprolol is a hypotensive drug, the active ingredient of which is the substance bisoprolol (a selective blocker of β1-adrenoreceptor activity). The introduction of its therapeutic doses does not lead to the appearance of sympathomimetic and membrane-stabilizing effects.

Bisoprolol also has some antianginal activity – it reduces the oxygen demand of the myocardium, reducing heart rate and blood pressure, as well as cardiac output. By lengthening diastole and reducing diastolic pressure, the drug helps improve the oxygen supply to the myocardium. [ 1 ]

Indications Biprolol

It is used as a treatment for elevated blood pressure.

In addition, it can be used in the combined treatment of people with CHF and coronary heart disease.

Release form

The release of the therapeutic substance is realized in tablets - 10 pieces inside a blister pack. The box contains 3 such packs.

Pharmacodynamics

The antihypertensive effect of the drug develops with a decrease in renal renin secretion, as well as a decrease in cardiac output and the effect on the baroreceptors of the aortic arch together with the carotid sinus. Long-term treatment with Biprolol causes a significant decrease in the resistance exerted by peripheral vessels.

In people with heart failure, the use of bisoprolol causes suppression of the RAAS activity, as well as the sympathoadrenal system. [ 2 ]

The drug has almost no effect on β2-adrenergic receptors or glucose metabolism processes.

With a single use, the therapeutic effect of the drug lasts for 24 hours. [ 3 ]

Pharmacokinetics

The active ingredient is well absorbed (without reference to food intake); the bioavailability index is 90%. The values of intraplasmic Cmax of bisoprolol are recorded after 1-3 hours from the moment of drug intake.

The drug is weakly subject to the first intrahepatic passage. About 50% of the administered portion is involved in metabolic processes with the formation of metabolic components that do not have a therapeutic effect.

Excretion is mainly via the kidneys; a small portion is excreted via the intestines. The half-life of bisoprolol is 10-12 hours.

Dosing and administration

Biprolol is taken orally. The daily dose is usually taken in one go – this should be done in the morning. There is no need to chew the tablet, but it can be divided in half if necessary. When stopping treatment, the drug is discontinued gradually – by reducing the dosage. The dose size and duration of the course are selected by the doctor.

It is often necessary to use 5 mg of the drug per day. The initial dose is usually 2.5-5 mg (taking into account the severity of the disease). Considering the effect of the drug, the daily dosage can be gradually increased to 10 mg.

The maximum dose of bisoprolol allowed per day is 20 mg.

In the presence of severe renal/hepatic dysfunction, it is allowed to consume no more than 10 mg of the drug per day.

• Application for children

Biprolol is contraindicated in pediatrics.

Use Biprolol during pregnancy

Biprolol should not be used during pregnancy. When the attending physician decides whether the drug can be taken by a pregnant woman, the portion size is selected for the patient individually. During such use of bisoprolol, it is necessary to monitor the blood flow processes inside the placenta and the condition of the newborn immediately after birth.

The medication is not used during breastfeeding; it can only be used if breastfeeding is stopped.

Contraindications

The drug is contraindicated for use in individuals with existing intolerance to bisoprolol. In addition, it is not used in the presence of galactosemia, glucose-galactose malabsorption, and lactase deficiency.

The drug is not used in people with heart failure in the decompensated phase, SSSU, stage 2-3 AV block (in the absence of a pacemaker), bradycardia and pronounced sinoatrial block; it is not prescribed to people with low blood pressure and cardiogenic shock.

The drug should not be used in cases of severe peripheral blood flow disorders, Raynaud's syndrome, asthma and severe chronic obstructive pulmonary diseases; at the same time, it is not prescribed to people with metabolic acidosis, psoriasis (also if psoriasis is present in the anamnesis) or pheochromocytoma that has not been cured.

The drug is not used in people taking sultopride, floctafenine or MAOIs (the only exception is MAOI-B).

Caution is required when prescribing Biprolol to individuals with stage 1 AV block or variant angina, as well as to diabetics and people on a strict diet.

The drug is prescribed with extreme caution in cases of myasthenia, a tendency to develop bronchial spasms, hyperthyroidism and depression.

It is necessary to stop taking the drug at least 2 days before performing general anesthesia, and at the same time carefully monitor the condition of people who undergo specific desensitizing immunotherapy procedures during the use of bisoprolol.

Side effects Biprolol

The use of the medication may provoke the development of some side effects associated with the action of bisoprolol:

• lesions affecting the cardiovascular system and blood system: heart failure, cardialgia, heart rhythm disorder, numbness affecting the extremities, decreased blood pressure (also orthostatic collapse), thrombocytopenia or leukopenia, dyspnea, agranulocytosis and purpura. Worsening of the condition may be observed in individuals with intermittent claudication and other disorders associated with peripheral blood flow;
• problems with the nervous system function: headaches, paresthesia, severe fatigue, day/night disorders, dizziness, unexplained anxiety and asthenia. Syncope, hallucinations or nightmares and a decrease in the speed of psychomotor response may occur;
• disorders associated with the hepatobiliary system and gastrointestinal tract: increased activity of liver enzymes or hepatitis, as well as gastralgia, bowel disorders, symptoms of dyspepsia and vomiting;
• disorders affecting the sense organs: tinnitus, pain affecting the eyes, decreased visual acuity, conjunctivitis, dry eye and hearing disorders;
• allergy symptoms: allergic rhinitis, anaphylaxis, urticaria, active phase of psoriasis, bronchial spasm, Quincke's edema and cough;
• Others: myasthenia, dysuria, arthropathy, hyperhidrosis, cramps, renal colic, weight change, pain affecting muscles and joints, decreased glucose tolerance, changes in libido and impotence. Along with this, it is possible to increase the levels of creatinine, glucose, uric acid with urea, triglycerides and elements of K with P in plasma.

Abruptly stopping the use of the drug may cause withdrawal symptoms.

The use of bisoprolol results in a positive result in doping control.

Overdose

Administration of excessively large doses of Biprolol can cause a strong decrease in blood pressure, bradycardia, heart failure, bronchial spasms, and in addition hypoglycemia, convulsions, loss of consciousness and heart rhythm disorders (this includes AV block of 2-3 stages).

The medicine has no antidote.

In case of overdose, gastric lavage and enterosorbents are administered. If the patient develops bradycardia, an intravenous injection of atropine is administered.

If blood pressure values drop significantly, vasoconstrictors and intravenous glucagon are administered.

When heart failure occurs, diuretics are administered intravenously.

Drug-induced AV block can be treated with orciprenaline (via IV drip); cardiac pacing may be performed if required.

In case of bronchial spasms, bronchodilators, euphyllin or β2-adrenergic agonists are administered.

If hypoglycemia occurs, an intravenous injection of glucose is administered.

Bisoprolol poisoning is treated in a hospital, under constant medical supervision.

It is not possible to eliminate an overdose of bisoprolol using hemodialysis.

Interactions with other drugs

When combining the drug with tricyclics, agents that block Ca channels, phenothiazine, substances that block the activity of β-adrenergic receptors, MAOIs and barbiturates, the antihypertensive activity of bisoprolol is enhanced.

Use together with antiarrhythmic drugs may cause the appearance of a negative inotropic effect.

The combination of the drug with CG and parsympathomimetics increases the likelihood of AV conduction disorders or the development of bradycardia.

Administration together with orally administered hypoglycemic agents and insulin increases the risk of hypoglycemia.

Manifestations of hypoglycemia may be masked by the action of β-blockers.

The combination of the drug with anesthetic substances increases the likelihood of developing arrhythmia or myocardial ischemia.

Non-narcotic analgesics weaken the therapeutic effect of bisoprolol.

Administration in combination with sympathomimetics leads to a weakening of the medicinal effect of these drugs, and in addition, may potentiate the signs of intermittent claudication.

Use together with antihypertensive substances and agents that block the activity of Ca channels may potentiate the intensity of the negative effects of bisoprolol.

Storage conditions

Biprolol should be stored at temperatures in the range of 15-25°C.

Shelf life

Biprolol can be used for a period of 5 years from the date of sale of the therapeutic product.

Analogues

The analogs of the drug are the substances Concor, Bidop with Bisoprolol, Aritel and Coronal, and also Niperten with Bicard and Bisogamma.