Coraxan tablets 7.5 mg, 56 pcs. (Yvabradyn)

Release form

Film-coated tablets.



packaging 56 pcs

Indications

Stable angina pectoris

Therapy of stable angina pectoris in patients with normal sinus rhythm:

- with intolerance or contraindications to the use of beta-adrenoblockers

in combination with beta-adrenergic blocking dose-stable adrenergic blocking Chronic heart failure

To reduce the incidence of cardiovascular complications (mortality from cardiovascular disease and hospitalization due to with increasing symptoms of heart failure) in patients with chronic heart failure, with sinus rhythm and heart rate of at least 70 beats / min.

Contraindications

Hypersensitivity to ivabradine or any of Coraxan’s excipients

Bradycardia (resting heart rate less than 60 beats / min (before treatment))

cardiogenic shock

acute myocardial infarction systolic pulmonary arteriosis mild arterial pulmonary hypertension 90 mm Art. and diastolic blood pressure less than 50 mm Hg )

severe liver failure (more than 9 points on the Child-Pugh scale)

sinus weakness syndrome

sinoatrial blockade

presence of an artificial pacemaker

unstable angina pectoris

atrioventricular blockade of atherosclerosis 3 degree 4chromic isoforms 4chromytochromic s4l4 4-phase sroml4 such as antifungal agents of the azole group (ketoconazole, itraconazole), macrolide antibiotics (clarithromycin, erythromycin for oral administration, josamycin, telithromycin), inhibitors proof operation of the HIV protease (nelfinavir, ritonavir) and nefazodone

pregnancy and lactation

age of 18 years (effectiveness and safety of the drug in this age group has not been studied)

lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome.

Precautions: Moderately severe liver failure (less than 9 Child-Pugh score) severe renal failure (CC less than 15 ml / min) congenital lengthening of the QT interval (see section “Interaction with other medicinal products) while taking medications that lengthen QT interval simultaneous administration of moderate inhibitors of cytochrome CYP3A4 isoenzymes and grapefruit juice asymptomatic left ventricular dysfunction atrioventricular block II degree recent stroke pigmented degene radio retina (retinitis pigmentosa) hypotension simultaneous application blockers "slow" calcium channel (BCCI) slows heart rate, such as verapamil or diltiazem.

Use during pregnancy and lactation

Coraxan is contraindicated for use during pregnancy. At the moment, there is insufficient data on the use of the drug during pregnancy. In preclinical studies of ivabradine revealed embryotoxic and teratogenic effects.

The use of Coraxan during breastfeeding is contraindicated. There is no evidence of the penetration of ivabradine into breast milk.

Composition

1 tablet of 7.5 mg contains: active substance: ivabradine hydrochloride 8.085 mg, which corresponds to 7.5 mg of base.

excipients: lactose monohydrate 61.215 mg, magnesium stearate 0.5 mg, corn starch 20 mg, maltodextrin 10 mg, anhydrous colloidal silicon dioxide 0.20 mg.

Shell: glycerol 0.08740 mg, hypromellose 1.45276 mg, dye iron oxide yellow (E172) 0.01457 mg, dye iron oxide red (E172) 0.00485 mg, macrogol 6000 0.09276 mg, magnesium stearate 0, 08740 mg, titanium dioxide (E171) 0.26026 mg.

Dosage and administration of

Coraxan should be taken orally 2 times a day, in the morning and in the evening during meals.

Stable angina pectoris. The recommended initial dose of the drug is 10 mg per day (1 tablet 5 mg 2 times a day).

Depending on the therapeutic effect, after 3-4 weeks of use, the daily dose of the drug can be increased to 15 mg (1 tablet 7.5 mg 2 times a day). If, during therapy with Coraxan®, heart rate at rest is reduced to values ​​less than 50 beats / min, or the patient has symptoms associated with bradycardia (such as dizziness, increased fatigue, or a marked decrease in blood pressure), it is necessary to reduce the dose of Coraxan (for example, to 2 5 mg (1/2 tablet of 5 mg) 2 times a day). If, with a decrease in the dose of Coraxan, heart rate remains less than 50 beats / min, or symptoms of severe bradycardia persist, then the drug should be discontinued.

Chronic heart failure. The recommended initial dose of Coraxan is 10 mg per day (1 tablet 5 mg 2 times a day).

After two weeks of use, the daily dose of Coraxan can be increased to 15 mg (1 tablet 7.5 mg 2 times a day) if the heart rate at rest is stable for more than 60 beats / min. If the heart rate is stable no more than 50 beats / min or in case of symptoms of bradycardia, such as dizziness, increased fatigue or hypotension, the dose can be reduced to 2.5 mg (1/2 tablet 5 mg) 2 times a day .

If the heart rate is in the range from 50 to 60 beats / min, it is recommended to use the drug Coraxan in a dose of 5 mg 2 times a day.

If, during use of the drug, heart rate at rest is stably less than 50 beats / min or if the patient has symptoms of bradycardia, for patients receiving Coraxan in a dose of 5 mg 2 times a day or 7.5 mg 2 times a day, dose the drug should be reduced.

If patients receiving Coraxan at a dose of 2.5 mg (1/2 tablet 5 mg) 2 times a day or 5 mg 2 times a day, heart rate at rest is stable over 60 beats / min, the dose may to be increased.

If heart rate is not more than 50 beats / min or the patient has symptoms of bradycardia, the drug should be discontinued.

For patients 75 years of age and older, the recommended initial dose of Coraxan is 2.5 mg (1/2 tablet of 5 mg) 2 times a day. In the future, an increase in the dose of the drug is possible.

Impaired renal function. For patients with CC more than 15 ml / min, the recommended initial dose of Coraxan is 10 mg per day (1 tablet 5 mg 2 times a day). Depending on the therapeutic effect, after 3-4 weeks of use, the dose of the drug can be increased to 15 mg (1 tablet 7, 5 mg 2 times a day).

Due to a lack of clinical data on the use of Coraxan in patients with CC less than 15 ml / min, the drug should be used with caution.

Impaired liver function. For patients with a mild degree of liver failure (up to 7 points on the Child-Pugh scale), the usual dosage regimen is recommended. The recommended initial dose of Coraxan is 10 mg per day (1 tablet 5 mg 2 times a day). Depending on the therapeutic effect, after 3-4 weeks of use, the dose of the drug can be increased to 15 mg (1 tablet 7.5 mg 2 times a day).

Side effects

On the part of the organ of vision:

Very often: changes in light perception (photopsy): was observed in 14.5% of patients and was described as a transient change in brightness in a limited area of ​​the visual field. As a rule, such phenomena were provoked by a sharp change in the intensity of illumination in the area of ​​the visual field. Basically, photopsia appeared in the first two months of treatment, followed by a repeat. The severity of photopsia was usually mild or moderate. The appearance of photopsy ceased on the background of continued therapy (in 77.5% of cases) or after its completion. In less than 1% of patients, the appearance of photopsy was the reason for refusing treatment.

Often: blurred vision.

From the cardiovascular system: Often: bradycardia: in 3.3% of patients, especially in the first 2-3 months of therapy, in 0, 5% of patients developed severe bradycardia with a heart rate of not more than 40 beats / min AV block I degree ventricular extrasystole.

Infrequently: palpitations, supraventricular extrasystole.

Unspecified frequency: arterial hypotension, possibly associated with bradycardia

The following adverse events identified in clinical trials occurred with the same frequency both in the group of patients treated with ivabradine and in the comparison group, which suggests their association with the disease as such, and not with ivabradine: sinus arrhythmia, angina pectoris, including unstable atrial fibrillation, myocardial ischemia, myocardial infarction and ventricular tachycardia.

From the digestive system: infrequently: nausea, constipation, diarrhea.

From the central nervous system:

Often: headache, especially in the first month of therapy, dizziness, possibly associated with bradycardia.

Infrequently: shortness of breath, vertigo, muscle spasms.

Unspecified frequency: fainting, possibly associated with bradycardia.

Laboratory indicators: infrequently: hyperuricemia, eosinophilia, increased plasma creatinine concentration.

From the skin and subcutaneous fat: skin rash, itching, erythema, angioedema, urticaria.

General disorders and symptoms: asthenia, fatigue, malaise, possibly related to bradycardia.

Drug Interaction

Pharmacodynamic Interaction

Not recommended combinations of

drugs that prolong the QT interval (eg, quinidine, disopyramide, bepridil, sotalol, ibutilide, amiodarone).

drugs that prolong the QT interval, not related to cardiovascular agents (eg pimozide, ziprasidone, sertindol, mefloquine, halofantrine, pentamidine, cisapride, erythromycin IV).

Co-administration with drugs that prolong the QT interval may increase the rate of heart rate, so careful cardiac monitoring should be performed when required jointly.

Pharmacokinetic interaction of

Cytochrome P4503A4 (CYP3A4). Ivabradine is metabolized in the liver by enzymes of the cytochrome P450 (CYP3A4) system and is a very weak inhibitor of this cytochrome. Ivabradine has no significant effect on the metabolism and plasma concentration of other cytochrome CYP3A4 substrates. At the same time, CYP3A4 inhibitors and inducers interact with ivabradine and affect its metabolism and pharmacokinetic properties. Cytochrome CYP3A4 inhibitors have been found to increase and cytochrome CYP3A4 inducers decrease ivabradine plasma concentrations. Increasing the concentration of ivabradine in blood plasma increases the risk of developing pronounced bradycardia.

Contraindications combinations

Concomitant use with potent cytochrome P450 inhibitors, such as antifungal agents of the azole group (ketoconazole, itraconazole), macrolide antibiotics (clarithromycin, erythromycin oral, jazzamycin, telithromycin), HIV protease inhibitors (nelfinavir, ritonavir) and nefazodone, ketoconazole (200 mg once daily) or jazzamycin 2 times a day , increase average concentrations of ivabradine in blood plasma by 7-8 times.

Not recommended combinations

Moderate CYP3A4 inhibitors. The combined use of ivabradine and heart rate-reducing agents - diltiazem or verapamil, was well tolerated by patients and was accompanied by an increase in ivabradine concentration of 2-3 times, with an additional reduction of heart rate of approximately 5 beats / min.

This combination is not recommended.

Cautions when using

Moderate-acting CYP3A4 inhibitors. Concomitant administration of ivabradine with other CYP3A4 inhibitors (eg fluconazole) should be initiated with an initial dose of 2.5 mg twice daily. At a heart rate of at least 60 beats / min, careful monitoring of the heart rate is required.

Grapefruit juice. Against the background of grapefruit juice, there was a 2-fold increase in the concentration of ivabradine in the blood. Grapefruit juice should be kept to a minimum during ivabradine therapy.

CYP3A4 inducers, such as rifampicin, barbiturates, phenytoin, and herbal preparations containing Hypericum perforatum, combined with Hypericum perforatum, may result in decreased blood concentrations and ivabradine activity and may require a higher dose selection. During the period of ivabradine therapy, the use of drugs and products containing perforated St. John's wort should be minimized.

Combined use with other drugs

The absence of a clinically pronounced effect on the pharmacodynamics and pharmacokinetics of ivabradine of the following drugs was demonstrated: proton pump inhibitors (omeprazole, lansoprazole), phosphodephosphor inhibitors - derivatives of the dihydropyridine series (amlodipine, lacidipine), digoxin and warfarin.

It has been shown that ivabradine has no clinically pronounced effect on the pharmacokinetics of simvastatin, amlodipine, lacidipine, the pharmacokinetics and pharmacodynamics of digoxin, warfarin, and the pharmacodynamics of acetylsalicylic acid.

In the Phase III pilot study, the use of the following drugs did not have special limitations, in connection with which they can be prescribed in combination with ivabradine without special precautions: ACE inhibitors, angiotensin II receptor antagonists, diuretics, short and prolonged action nitrates, HMG-CoA reductase inhibitors, fibrates, inhibitors, protozoa acid and other antithrombotic agents.

Overdose

Symptoms: severe and prolonged bradycardia.

Treatment of marked bradycardia should be symptomatic and carried out in specialized wards. In the case of bradycardia, in combination with disorders of hemodynamics, symptomatic treatment with intravenous administration of beta-adrenomimetics such as isoprenaline has been shown.

If necessary, it is possible to set an artificial rhythm driver.

Storage conditions

No special storage conditions are required. Out of the reach of children.

Expiration

3 years.

Deystvuyuschee substances

Yvabradyn

Formulation

Dosage form

tablets

Servye, France



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