Bisoprofar

Bisoprofar belongs to the group of selective ß1-blockers. Use in therapeutic portions does not lead to the appearance of ICA and a clinically noticeable membrane stabilizing effect.

Possesses antianginal properties: weakens 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 end-diastolic pressure. [1]

Indications Bisoprofar

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

Release form

The release of the drug substance is made in tablets - 10 pieces inside the cell plate; inside the pack - 3 such plates.

Pharmacodynamics

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

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

Pharmacokinetics

Bisoprolol is absorbed almost completely and at a high rate inside the gastrointestinal tract. In combination with the extremely weak effect of the 1st intrahepatic passage, this forms a high bioavailability (approximately 90%). Approximately 30% of the substance is synthesized with blood protein. The level of the distribution volume is 3.5 l / kg. Systemic clearance is approximately 15 l / h.

The term plasma half-life is 10-12 hours, due to which, with a 1-time intake of a daily portion, the therapeutic effect is noted 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 non-active metabolites, then excreted through the kidneys. The remaining 50% of the dosage is excreted through the kidneys unchanged.

When drugs are administered to people with CHF (stage 3), the plasma index of the drug and the duration of the half-life increase. Indicators of plasma Cmax at dynamic equilibrium are equal to 64 ± 21 ng / ml after the introduction of a daily dosage of 10 mg; the term half-life is 17 ± 5 hours.

Dosing and administration

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

The size of the standard dosage with increased blood pressure and angina pectoris is 5 mg once a day (no more than 20 mg once a day). Changes in the dosage regimen are carried out by the doctor, personally for each patient.

• Application for children

There is no information on the therapeutic effect and safety of the use of drugs in pediatrics.

Use Bisoprofar during pregnancy

Prescribing Bisoprofar during pregnancy is allowed only in cases where the likely benefit for 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 ß-blockers are required, it is recommended to use selective ß1-blockers. It is required to monitor blood circulation inside the uterus and placenta.

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

There is no information as to whether bisoprolol is excreted in mother's milk, which is why it cannot be used for hepatitis B.

Contraindications

The main contraindications:

• severe intolerance to bisoprolol or other elements of the drug;
• active form of HF or decompensated HF, in which inotropic treatment is necessary;
• blockade of the 2-3rd degree (without the use of a pacemaker);
• cardiogenic shock;
• pronounced form of sinoatrial blockade;
• SSSU;
• symptomatic bradycardia (heart rate indicators are below 60 beats per minute);
• decreased blood pressure (systolic blood pressure values - less than 100 mm Hg);
• severe asthma or severe obstructive pulmonary lesions with a chronic form;
• Raynaud's syndrome and late-stage peripheral blood flow disorders;
• untreated pheochromocytoma;
• metabolic acidosis.

Side effects Bisoprofar

Among the side signs:

• violations in the area of the National Assembly: syncope, cephalalgia *, dizziness *;
• problems with visual function: conjunctivitis and decreased lacrimation (must be taken into account for people using contact lenses);
• mental disorders: depression, paresthesias, sleep disorders, hallucinations and nightmares;
• symptoms associated with the work of the CVS: bradycardia (in people with CHF, IHD or high blood pressure), orthostatic collapse, numbness and cooling of the extremities, AV conduction disorder, decreased blood pressure, manifestations of worsening CHF;
• lesions in the gastrointestinal tract: abdominal pain, vomiting, constipation, nausea and diarrhea;
• digestive disorders: hepatitis or an increase in the activity of liver enzymes (ALT and AST);
• problems associated with the mediastinal organs and the respiratory system: allergic-type runny nose or bronchial spasm in people with asthma or a history of chronic obstructive respiratory tract diseases;
• lesions of the connective tissues and the musculoskeletal system: cramps, muscle weakness and arthropathy;
• hearing disorders: hearing impairment;
• 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 a psoriasis-like rash and alopecia;
• disorders of nutrition and metabolism: hypoglycemia and an increase in triglyceride indicators;
• manifestations associated with the reproductive system: erectile dysfunction;
• immune disorders: a runny nose of an allergic nature and the emergence of antinuclear antibodies, which is individually accompanied by clinical signs of SLE (disappear after treatment is discontinued);
• change in test readings: an increase in the plasma activity of liver enzymes (ALT with AST) and blood triglycerides;
• systemic disorders: fatigue * or asthenia.

* applies only to persons with coronary artery disease or elevated blood pressure.

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

Overdose

Signs of poisoning: 3rd degree AV block, active heart failure, bradycardia, decreased blood pressure, dizziness, hypoglycemia and bronchial spasm.

In case of intoxication, you must immediately cancel the therapy and inform the doctor about it. Taking into account the severity of the poisoning, symptomatic and supportive procedures are carried out:

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

Interactions with other drugs

The medication can potentiate the activity of other antihypertensive drugs.

The introduction 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 are capable of potentiating the antihypertensive effect of Bisoprofar; when a drug is combined with diltiazem and verapamil, the heart rate may also decrease.

Combined use with ergotamine derivatives (including ergotamine-containing anti-migraine drugs) potentiates the signs of peripheral blood flow disorders.

The combination with oral hypoglycemic drugs or insulin leads to some weakening or masking of the manifestations of hypoglycemia (it is required to constantly monitor blood sugar parameters).

The introduction of a medication with antiarrhythmic substances can disrupt the rhythm of the heart.

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

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

Combined use with iodine-containing X-ray contrast 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 must be kept out of the reach of small children. Temperature values - no more than 25 ° С.

Shelf life

Bisoprofar can be used for a 24-month term from the date of manufacture of the drug.

Analogs

The analogues of the drug are Bidop, Bisoprol, Biprolol with Bisopropel, and besides this, Alotendin, Bisokard with Bikard, Dorez and Bisostad.