Biprolol

Biprolol is an antihypertensive medication, the active element of which is bisoprolol (a selective blocker of β1-adrenergic receptors). The introduction of its therapeutic portions 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 lowering diastolic pressure values, the medication helps to improve oxygen supply to the myocardium. [1]

Indications Biprolol

It is used as a treatment for increased blood pressure .

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

Release form

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

Pharmacodynamics

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

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

The drug has almost no effect on β2-adrenergic receptors, as well as glucose metabolism.

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

Pharmacokinetics

The active element lends itself well to absorption (without reference to the use of food); the bioavailability index is 90%. The values of intraplasma Cmax of bisoprolol are recorded after 1-3 hours from the moment of using the drug.

The drug is weakly exposed to the 1st intrahepatic passage. About 50% of the introduced portion is involved in metabolic processes with the formation of metabolic components that do not have a therapeutic effect.

Excretion is mainly carried out through the kidneys; a small part is excreted through the intestines. The half-life of bisoprolol is 10-12 hours.

Dosing and administration

Biprolol is taken orally. A daily serving is usually taken for 1 use - it should be done in the morning. There is no need to chew the tablet, but it can be halved if necessary. During the termination of treatment, the withdrawal of the medication is carried out gradually - by lowering the dosage. The size of the portion and the duration of the course are selected by the doctor.

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

A maximum of 20 mg of bisoprolol is allowed per day.

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

• Application for children

It is forbidden to prescribe Biprolol in pediatrics.

Use Biprolol during pregnancy

Biprolol should not be used during pregnancy. When the attending doctor decides on the possibility of taking drugs for a pregnant woman, the portion size is selected for the patient personally. During this use of bisoprolol, it is necessary to monitor the processes of blood flow inside the placenta and the condition of the newborn immediately after childbirth.

When breastfeeding, the medication is not used; it can be used only on condition of refusal to breastfeed.

Contraindications

It is contraindicated to use the medicine in persons with an existing intolerance to bisoprolol. In addition, it is not used in the presence of galactosemia, glucose-galactose malabsorption, and lactase deficiency.

The medication is not used in people with HF in the decompensated phase, SSS, AV blockade of the 2-3rd stage (in the absence of a pacemaker), bradycardia and pronounced sinoatrial blockade; not assigned to persons with low blood pressure values and cardiogenic shock.

The medicine should not be used in case of severe peripheral blood flow disorders, Raynaud's syndrome, BA and severe chronic obstructive pulmonary diseases; at the same time, it is not prescribed to persons with metabolic acidosis, psoriasis (also if there is a history of psoriasis) or pheochromocytoma that has not been cured.

The medication is not used in people using sultopride, floctaphenin or MAOIs (the only exceptions are MAOI-B).

Caution is necessary when prescribing Biprolol to persons with AV block in the 1st stage or variant angina pectoris, as well as to diabetics and people on a strict diet.

With extreme caution, the drug is prescribed for myasthenia gravis, a tendency to the appearance of bronchial spasms, hyperthyroidism and depression.

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

Side effects Biprolol

The use of a medication can provoke the development of some side signs associated with the action of bisoprolol:

• lesions affecting the CVS and the circulatory system: heart failure, cardialgia, heart rhythm disorder, numbness affecting the limbs, decreased blood pressure values (also orthostatic collapse), thrombocyto- or leukopenia, dyspnea, agranulocytosis and purpura. There may be a worsening of the condition in persons with intermittent claudication and other disorders associated with peripheral blood flow;
• problems with the function of the NS: headaches, paresthesias, severe fatigue, day / night disorders, dizziness, anxiety without a cause, and asthenia. The appearance of syncope, hallucinations or nightmares and a decrease in the speed of the psychomotor response is possible;
• disorders associated with the hepatobiliary system and the gastrointestinal tract: an increase in the activity of liver enzymes or hepatitis, and in addition gastralgia, stool disorders, symptoms of dyspepsia and vomiting;
• disorders affecting the sensory organs: ear noise, pain affecting the eyes, weakening of visual acuity, conjunctivitis, dryness of the ocular mucosa and hearing disorders;
• allergy symptoms: runny nose of allergic genesis, anaphylaxis, urticaria, active phase of psoriasis, bronchial spasm, Quincke's edema and cough;
• others: myasthenia gravis, dysuria, arthropathy, hyperhidrosis, convulsions, colic in the kidneys, weight changes, pain affecting the muscles and joints, decreased glucose tolerance, changes in libido and impotence. Along with this, it is possible to increase the indicators of creatinine, glucose, uric acid with urea, triglycerides and elements K with P inside the plasma.

An abrupt stop in the use of the drug can provoke a withdrawal syndrome.

The use of bisoprolol leads to a positive response during doping control.

Overdose

The introduction of excessively large portions of Biprolol can provoke a strong decrease in blood pressure values, bradycardia, HF, bronchial spasms, and in addition, hypoglycemia, seizures, loss of consciousness and heart rhythm disturbances (this includes AV blockade of the 2-3rd stage).

The medicine has no antidote.

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

With a strong decrease in blood pressure values, the introduction of vasoconstrictors and intravenous injection of glucagon are performed.

When HF appears, intravenous administration of diuretics is performed.

Drug-related AV block can be controlled with orciprenaline (intravenously); if necessary, pacing can be performed.

In the case of bronchial spasms, bronchodilators, aminophylline or β2-adrenomimetics are administered.

When hypoglycemia occurs, an intravenous injection of glucose is performed.

Poisoning with bisoprolol is treated in a hospital, under the constant supervision of doctors.

It will not be possible to eliminate an overdose with bisoprolol using hemodialysis.

Interactions with other drugs

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

The use together with antiarrhythmic drugs can cause the appearance of a negative inotropic effect.

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

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

The manifestations of hypoglycemia can be masked by the action of β-blockers.

The combination of drugs with anesthetics increases the likelihood of developing arrhythmias or myocardial ischemia.

Non-narcotic analgesics weaken the therapeutic effect of bisoprolol.

The introduction in combination with sympathomimetics leads to a weakening of the drug effect of these drugs, and in addition, it can potentiate the signs of intermittent claudication.

The use together with antihypertensive substances and agents that block the activity of Ca channels can potentiate the intensity of the negative manifestations of bisoprolol.

Storage conditions

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

Shelf life

Biprolol can be used for a 5-year term from the date of sale of the therapeutic product.

Analogs

Analogues of drugs are the substances Concor, Bidop with Bisoprolol, Aritel and Coronal, and besides this, Niperten with Bicard and Bisogamma.