Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
АТХ:C.01.E.B.17 Iwabradine
Pharmacodynamics:Selectively and specifically inhibits the f-channels of the sinus node of the heart, controlling spontaneous diastolic repolarization of the sinus node. Reduces the heart rate by 10-15 beats per minute, thereby reducing the need for myocardium in oxygen, as the work of the heart is reduced. Does not change the QT indicator, does not affect the process of repolarization of the ventricles of the heart, intracardiac conduction and contractility of the myocardium (does not cause negative inotropic effect).
At the same time, it interacts with h-channels of the retina, which are similar in structure to the f-channels of the sinus node of the heart, which can lead to transient disturbances of vision-the appearance of photopsias with a sharp change in illumination.
Pharmacokinetics:After oral administration, an empty stomach is absorbed in the gastrointestinal tract up to 100%. The maximum concentration in the blood plasma is reached after 1 hour. The connection with plasma proteins is 70%.
Therapeutic effect develops 2-3 weeks after the start of the procedure. Metabolism in the liver.
The elimination half-life is 2 hours. Elimination by the kidneys and with feces.
Indications:It is used for the treatment of stable angina pectoris, chronic heart failure in patients with sinus rhythm not less than 70 beats per minute.
IX.I20-I25.I20 Angina pectoris [angina pectoris]
Contraindications:Cardiogenic shock, sinoatrial block, weakness syndrome of the sinus node, the presence of the patient's artificial pacemaker, AV-blockade III degree, hypotension (arterial pressure below 95/50 mm Hg), unstable angina, myocardial infarction, severe hepatic insufficiency, individual intolerance, children under 18 years of age.
Carefully:Moderate hepatic insufficiency, renal failure, congenital lengthening of the interval QT, chronic heart failure IV functional class according to the NYHA classification.
Pregnancy and lactation:Recommendations for FDA - Category X. Contraindicated in pregnancy and lactation.
Dosing and Administration:Inside to 5 mg 2 times a day. If necessary, the dose in 3-4 weeks increases to 7.5 mg 2 times a day.
The highest daily dose: 15 mg.
The highest single dose: 7.5 mg.
Side effects:Central and peripheral nervous system: dizziness, headache - in the first days of taking the drug. Effects are dose-related, associated with bradycardia. Rarely, convulsions.
Respiratory system: rarely - shortness of breath.
The system of hematopoiesis: eosinophilia.
The cardiovascular system: bradycardia in the first 2-3 months of treatment. Rarely AV-blockade I degree, ventricular extrasystole.
Digestive system: nausea, constipation, diarrhea.
Sense organs: transient photopsy during the first 2 months of treatment, blurred vision.
Allergic reactions.
Overdose:Development of bradycardia.
Treatment is symptomatic. When the hemodynamic parameters are violated, intravenous administration of β-stimulating agents (isoprenaline) is indicated. In severe cases, temporary use of the pacemaker.
Interaction:It is not recommended simultaneous use with drugs that extend the interval QT: ziprasidone, pimozide, sertindole, halofantrine, pentamine, cisapride, erythromycin (intravenous injection).
The intake of grapefruit juice when treated with ivabradine leads to an increase in the concentration of the drug in the blood plasma,which increases the risk of bradycardia.
Simultaneous use with stimulants CYP3A4, such as barbiturates, rifampicin, phenytoin, St. John's wort (Hypericum perforatum) leads to a decrease in the concentration of ivabradine, therefore, requires a dose adjustment of ivabradine.
Simultaneous use with non-potassium-sparing diuretics (thiazide and "loop" diuretics) leads to hypokalemia that increases the risk of arrhythmia. Because the ivabradine can cause bradycardia, a combination of hypokalemia and bradycardia is a predisposing factor for the development of severe arrhythmia.
Special instructions:Monitoring of liver and kidney function. Regular monitoring of the electrocardiogram to detect atrial fibrillation.
During drug treatment, patients are not recommended to drive vehicles and work with moving mechanisms.