Ivabradin

Ивабрадин Constitutional formula

The description is actual on 19.09.2015

  • Latin name: Ivabradinum
  • ATH code: C01EB17
  • Chemical formula: C27H36N2O5
  • CAS code: 155974-00-8

Chemical name

(S)-3-(3-(((3,4-Dimetoksibitsiklo (4.2.0) octa-1,3,5-triene-7-silt) marked) methylamine) spent on drink) - 1,3,4,5-tetragidro-7,8-dimetoksi - 2H-3 - benzazepine - 2 - it

Chemical properties

Ivabradin – the first substance – inhibitor of if-channels, possessing specific and selective effect. Its development became possible after opening in 1980 of ionic if-channels which are responsible for heart rate. By 2005 substance was approved to use for treatment of stable stenocardia at a normal sinoatrial rate, at patients with intolerance of other means. Further connection was decided to use in a combination with beta adrenoblockers.

In drugs this component usually is present at a type of an ivabradin of a hydrochloride.

Pharmacological action

Anti-anginal, antiischemic.

Pharmacodynamics and pharmacokinetics

Substance possesses ability specifically and selectively to block operation of if-channels in a sinus node which are responsible for control of diastolic depolarization and regulation of ChSS. Medicine does not influence atrioventricular, intra atrial and intra ventricular conduction paths, does not change sokratitelny ability of a cardiac muscle, does not change process of repolarization of ventricles.

The effect of drug is dozozavisimy, the probability of development of bradycardia is considerably reduced. Medicine lowers ChSS at rest approximately by 10 beats per minute, cardiac performance becomes less intensive, the amount of oxygen consumed by a cardiac muscle decreases.

Substance interacts with ih-channels in an eye retina which on the structure are similar to if-channels in heart owing to what sensitivity of a retina of an eye to bright light impulses changes. There is a photopsia.

During treatment by drug tolerance or a withdrawal to this substance does not develop. Means does not influence the arterial pressure and the general peripheric resistance of vessels, lipidic and carbohydrate metabolism does not change.

After oral administration active ingredient is quickly and completely acquired. Its biological availability reaches 40%, it happens because of effect of" the first passing" through a liver. At parallel meal increase in time of system absorption for 60 minutes is observed. The maximum concentration is observed in 1,5 hours after taking the medicine. About 70% of substance contact proteins of plasma.

Means undergoes reactions of a metabolism in intestines and a liver owing to oxidation under the influence of CYP3A4 isoenzyme. The main active metabolite of connection is formed owing to N-dezmetilirovaniya.

The elimination half-life of means makes about 2 hours, an effective elimination half-life – 11. A conclusion of not changed substance, its inactive and active metabolites happens to the help of kidneys and intestines.

At diseases of kidneys pharmacokinetic parameters change slightly. Ivabradin's AUC and his metabolite increases for 20%.

Indications to use

Ivabradin appoint:

  • for treatment of stable stenocardia at patients with a normal sinoatrial rate if there is an allergy to beta adrenoblockers or contraindications to their reception;
  • in combination with beta adrenoblockers for control of stable stenocardia;
  • at chronic heart failure to reduce the frequency of development of complications if ChSS makes less than 70 beats per minute.

Contraindications

Medicine has certain restrictions to use.

It cannot be used:

  • at a myocardial infarction;
  • to the persons suffering from AV blockade 3 degrees;
  • the patient with strongly reduced arterial pressure;
  • at bradycardia;
  • to patients with cardiogenic shock;
  • at serious violations in work of a liver;
  • to persons with a sick sinus syndrome;
  • at sinuatrial blockade;
  • to patients with chronic heart failure 3 and 4 classes (classification of NYHA);
  • during breastfeeding;
  • the patient with an artificial pacemaker who is in the mode of continuous stimulation;
  • at unstable stenocardia;
  • to pregnant women;
  • at an allergy to Ivabradin;
  • to children and teenagers till 18 flyings.

Side effects

During therapy depending on the frequency of emergence can be observed:

  • photopsia (disturbance in perception of degree of illumination);
  • bradycardia, decrease in visual acuity, vertigo, AV blockade of the first degree;
  • extrasystoles, headaches, dizziness;
  • sometimes – nausea, a heart consciousness, a diarrhea, a lock, an asthma;
  • diplopia, fibrillation of auricles, syncope;
  • spasms in muscles, an eosinophilia, a hyperuricemia, a giperkreatininemiya.

Also connection between emergence of the following side reactions and Ivabradin's reception is not established: unstable stenocardia, ciliary arrhythmia, myocardial infarction, ventricular tachycardia, sinus arrhythmia, exacerbation of stenocardia, myocardium ischemia.

Ivabradin, application instruction (Way and dosage)

Ivabradin's tablets are appointed to accept 2 times a day, since morning and before going to bed, it is preferable during meal.

It is recommended to begin with a dosage 10 mg a day, dividing it into 2 receptions on 5 mg. In need of and depending on efficiency of carrying out therapy, it is possible to increase in 3-4 weeks a dosage to 15 mg a day.

If during treatment it is observed developments of undesirable side reactions, fatigue, bradycardia, decrease in the ABP, dizziness, then frequency rate of reception the same is recommended to lower a daily dosage to 5 mg a day.

If frequency cordial reductions becomes less than 50 beats per minute, then treatment needs to be stopped.

It is recommended to make correction of a dosage for elderly patients. Reception of 2,5 mg of drug, 2 times a day is recommended. At beneficial effect of substance the daily dosage in a month can be increased by an organism.

Overdose

At overdose severe bradycardia most often develops. As therapeutic measures carry out a symptomatic treatment, intravenous administration beta adrenostimulyatorov (for example, an izoprenalina), installation of the artificial driver of a cordial rhythm is shown.

Interaction

With care substance is combined with thiazide and loopback diuretics, it can lead to a hypopotassemia and cardiac arrhythmia.

The inductors CYP3A4 (barbiturates, Phenytoinum, drugs of the St. John's Wort which is made a hole rifampicin) reduce plasma concentration and efficiency of medicine, can lower its AUC.

With care it is necessary to combine drug with the drugs increasing QT interval (Disopyramidum, sotaloly, Amiodaronum, ziprasidony, meflokhiny, pentamidine, erythromycin, quinidine, bepridily, ibutilidy, Pimozidum, sertindoly, galofantriny, tsizapridy). It can lead to a strong urezheniye of heart rate and lengthening of an interval of QT. At an urgent need of such combination it is recommended to watch cardiac performance by means of the electrocardiogram.

As the metabolism of this substance happens to participation of system of CYP3A4 cytochrome, means igibirut this isoenzyme. However means significantly does not influence processes of a metabolism of other weak, moderate and strong inhibitors of cytochrome. During clinical and laboratory trials it was established that the inductors CYP3A4 reduce plasma concentration of Ivabradin, and inhibitors of this isoenzyme increase it that can lead to bradycardia.

Also drug is not recommended to be accepted at the same time with strong inhibitors of an isoenzyme, ketokonazoly, itrakonazoly, klaritromitsiny, dzhozamitsiny, erythromycin, telitromitsiny, ritonaviry, nelfinaviry, nefazodony.

It is better not to combine medicine with moderate inhibitors of an isoenzyme Verapamil and diltiazem. It leads to increase in AUC substance by 3 times and to decrease in ChSS by 5 beats per minute.

Means can be combined with flukonazoly provided that heart rate more than 60 beats per minute. It is in that case recommended to accept no more than 5 mg of Ivabradin a day and to control ChSS.

At a medicine combination to grapefruit juice or grapefruit increase of plasma concentration of drug is observed twice.

Terms of sale

The recipe can be required.

Storage conditions

The tablets containing Ivabradin usually do not demand special storage conditions.

Period of validity

Substance can be stored in the tableted form during 3 flyings.

Special instructions

For purpose of drug it is the best of all if the course of heart failure is stable. It is necessary to be careful at disturbances of intra ventricular conductivity or at a ventricular dissinkhroniya.

Medicine is not appointed for treatment of arrhythmias, it possesses insufficient efficiency.

During treatment this substance recommends to do periodically an ECG timely to reveal fibrillation of auricles. At deterioration in a course of stenocardia, a heart consciousness, to the shift of a cordial rhythm drug intake is recommended to stop and appoint adequate therapy.

Ivabradin's reception needs to be stopped per day before carrying out electric cardioinversion.

During treatment it is not recommended to steer the car, it is necessary to remember that drug distorts perception an illumination eye, especially at night.

Elderly

Patients of old age need to make correction of a dosage, with the subsequent its slow increase.

Ivabradin's drugs synonyms: Bravadin, Hydrochloride Ivabradina, Ivabradin, Koraksan.

About Ivabradin

About drugs on the basis of this substance generally good. Sometimes patients complain of decrease in sight and the ABP owing to long reception, the high cost of medicine does not arrange also some. Many note that after the reception termination high ChSS and pressure return.

Ivabradin's price where to buy

The cost of tablets film coated Koraksan makes about 1000-1100 rubles for packaging of 56 pieces, a dosage of 5 mg.

Section: Active ingredients
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