Bisoprolol - instructions for use, dose, side effects, contraindications

Antiarrhythmic - a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers, retardation of atrial-ventricular conduction (beta blockade₁adrenoreceptors).

Antihypertensive:

- Decrease in the minute volume of the heart;

- reduction of sympathetic stimulation of peripheral vessels;

- suppression of renin release by the kidneys (beta blockade₁adrenoreceptors).

Antiremoral (mainly peripheral beta₂adrenoceptors).

Anxiolytic - attenuation somaticallyx symptoms of anxiety.

Prevention of vascular headache due to obstruction of the expansion of arteries, increasing the concentration of coagulation factors (beta blockade₂adrenoreceptors), decreased aggregation and adhesion of platelets, suppression of the release of renin.

Enhancement of uterine contractions (spontaneous and caused by means stimulating myometrium), caused by blockade of beta₂adrenoreceptors.

Pharmacokinetics:

Lipophilicity moderate.Poorly penetrates the blood-brain barrier, penetrates the placenta. The connection with plasma proteins is 26-33%. Biotransformation in the liver (CYP2D6). The half-elimination (half-life) period is 9-12 hours. The total clearance is 3.71 ml per minute, renal - 2.29 ml per minute. It is excreted by the kidneys (50% unchanged) and with feces (less than 2%).

Indications:

Arterial hypertension.

Stenocardia of tension.

Myocardial infarction (secondary prevention) - reduces the likelihood of a fatal outcome in high-risk patients within 2 years after successful revascularization.

arrhythmias: sinus tachycardia, supraventricular and ventricular premature beats, arrhythmias on the background of mitral valve prolapse, hyperthyroidism - 10 mg per day.

ICD-10

IX.I10-I15.I10 Essential [primary] hypertension

IX.I20-I25.I20 Angina pectoris [angina pectoris]

Contraindications:

Hypersensitivity.

Acute congestive heart failure or decompensated chronic heart failure.

Cardiogenic shock.

AV-blockade II-III degree, sinoatrial block, weak sinus node syndrome.

Bradycardia (heart rate - less than 60 per minute in treatment chronic heart failure, less than 50 per minute - for other indications).

Cardiomegaly (no signs of heart failure).

Hypotension (systolic blood pressure less than 100 mm Hg -.. In the treatment of chronic heart failure and 90 mm Hg. Art. - for other indications).

Chronic obstructive pulmonary disease (including bronchial asthma).

Violation of peripheral circulation (late stages).

Pregnancy and lactation.

Simultaneous administration of monoamine oxidase inhibitors (except for monoamine oxidase B inhibitors).

Carefully:

Low fraction of the left ventricle of Echocardiography, pheochromocytoma, psoriasis, diabetes mellitus (may mask symptoms of hypoglycemia), metabolic acidosis, severe allergic reactions (history), Prinzmetal angina holding desensitizing therapy, AV-block I degree, adherence to a strict diet, severe kidney (liver) failure, children's age (efficacy and safety have not been studied).

Pregnancy and lactation:

Use of the drug is possible in the event that the potential benefit to the mother exceeds the potential harm for the child - strictly according to the prescribing physician.

Therapy with bisoprolol should be discontinued 2-3 days before delivery.

The isolation of bisoprolol with breast milk has not been studied, and therefore infants of mothers undergoing therapy should be under the supervision of a doctor.

Action category for the fetus by Food and Drug Administration (US Food and Drug Administration) - C.

Dosing and Administration:

Inside (on an empty stomach in the morning), without chewing, in a dose of 2.5-5 mg once (up to 10 mg once a day). The maximum dose for adults is 20 mg per day. With the clearance of creatinine > 60 ml per minute interdose interval - 24 hours, 20-60 ml per minute - 48 hours, less than 20 ml per minute - 72 hours. The daily dose is 10 mg.

Side effects:

Cardiovascular system: bradycardia, congestive heart failure, impaired peripheral blood supply, orthostatic hypotension.

Respiratory system: bronchospasm, nasal congestion.

Nervous system: unusual tiredness or weakness, sleep disorders, depression, anxiety, nervousness, nightmares or vivid dreams, dizziness.

Blood system: hypoglycemia (suppression of glycogenolysis stimulated by catecholamines), hyperglycemia (a violation of the metabolism of carbohydrates, an increase in peripheral resistance to insulin), an increase in the content of triglycerides, low density lipoprotein, decrease in concentration high-density lipoproteins, leukopenia, thrombocytopenia.

Digestive system: nausea, vomiting, unpleasant sensations in the stomach, constipation, diarrhea, reversible hepatotoxic effect.

Allergies: skin rashes, pain in the joints or back.

Others: impairment of sexual function, withdrawal syndrome (increased frequency of angina attacks, increased blood pressure).

Overdose:No data.

Interaction:

Allergens (with immunotherapy), allergen extracts for skin tests, iodine-containing radiopaque substances - increase the possibility of developing severe allergic reactions or anaphylaxis.

Amiodarone, verapamil, diltiazem, phenytoin, flecainide - an increase in cardiodepressive action, a bradycardia with severe hemodynamic effects.

Calcium channel blockers - decreased hepatic metabolism of propranolol, metoprolol and other beta-blockers with significant metabolism in the liver.

Inhibitors of monoamine oxidase, procarbazine, selegiline, furazolidone - within 14 days after discontinuation of treatment against the background of the use of beta-blockers, significant hypertension is possible.

Insulin, hypoglycemic drugs taken orally, - a violation of the regulation of glucose concentration. Beta-adrenoblockers mask the symptoms of hypoglycemia (for example, increased heart rate and blood pressure).

Ketoconazole, cimetidine, erythromycin - Decreased presystemic metabolism, increased bioavailability of propranolol and other beta-blockers with significant metabolism in the liver.

Clonidine - beta-blockers can enhance withdrawal syndrome (hypertensive reaction).

Clonidine, reserpine - excessive hypotension, bradycardia.

Xanthines, especially theophylline (aminophylline), - mutual weakening of therapeutic effects.

Smoking, barbiturates, rifampicin - Increased metabolism of beta-adrenoblockers with significant metabolism in the liver and a decrease in their effectiveness.

Lidocaine, theophylline - suppression of their metabolism and elimination.

Non-depolarizing muscle relaxants - an increase in the duration of muscle relaxation.

Propafenone - an increase in the plasma concentration of beta-blockers.

Sympathomimetic drugs, estrogens (dobutamine, dopamine, isoproterenol, norepinephrine, phenylephrine, epinephrine, ephedrine) - mutual suppression of effects; possibly excessive increase of arterial pressure on the background of pronounced bradycardia.

Means for inhalation anesthesia (halothane, methoxyflurane, trichlorethylene, cyclopropane) - increased risk of oppression of myocardial function and hypotension.

Phenotiazines - mutual increase in concentrations.

Cimetidine - reduced clearance of beta-blockers.

Special instructions:

The sudden withdrawal of the drug is unacceptable, the course of bisoprolol therapy ends slowly, with a gradual decrease in the dose. Before the operation, an anesthesiologist must be informed of the remedy used.

Do not exceed the dose of bisoprolol more than 10 mg per day for renal failure (creatinine clearance less than 20 ml per minute) and severe violations of liver function.

During the period of treatment, alcohol is not allowed.

Bisoprolol should be used with caution to people who have a kind of activity the need to concentrate attention and have a high rate of psychomotor reactions.

Instructions

Bisoprolol (Bisoprololum)