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Ivabradin (English: Ivabradine, ATC code C01EB17) is a medicament also excluding heart-frequency-lowering effect. It is the prototype of a new substance class (If-channel-Hemmer or If-inhibitors) and leads at the heart to a slowing down of the pulse impact, without affecting the excitation line system or the muscle power of the heart (Inotropie).

Ivabradin is used for the treatment of the chronic stable angina pectoris with patients with sine rhythm, with whom beta blockers are contraindicated or an incompatibility for beta blockers is present. It has the marketing permission of the European medicament agency (EMEA) on 31 July 2005 and on 25 October 2005 the European permission receive. Brought on 2 January 2006 the preparation of the manufacturer serve under the label name in Germany on the market.

Impact and indication

Ivabradin restrains selectively and specifically the If-Ionenstrom, which adjusts so the heart frequency as intrinsischer pacesetters the diastolic depolarization in the sine knot, spontaneous in the heart, controlled and. The kardialen effects are specific for the sine knot and have neither influence on intraatriale, (PQ-time) or still on the myokardiale (heart muscle power) or repolarization (QTc time). Also the and thus the blood pressure remain constant.

Darreichungsformen and dosage

Ivabradin is available in film tablet form to the oral income in the effect strengths 5 mg and 7.5 mg. The usual initial dose amounts to twice daily 5 mg, depending upon effect can the dose after three to four weeks on twice daily 7.5 mg be increased.

Side effects

Serious side effects did not arise on in the context of the permission studies over 4000 patients. When most frequent unwanted medicament effect arose with 2-14,5 per cent of the patients dose-dependently and recoveryable so-called Phosphene (light perceptions in the sense of isolated clarifications in the visual field), which disappeared during (with 77,5 per cent of the patients) or after the treatment again. This is because of the kompetitiven inhibition of a variation of the If-channel, which is in the Retina. To everyday life changes or therapy abort Phosphene led with less than a per cent. Effects of a Langzeitbehandlung over one year on the function of the retina are not well-known. With patients with Retinitis pigmentosa caution is appropriate.

Contraindications

Ivabradin is not to be used

  • Hypersensitivity to Ivabradin,
  • a quiescent heart frequency under 60/min before the treatment,
  • cardiogenic shock,
  • acute myocardial infarction,
  • Hypotonie < 90/50 mmHg,
  • heavy liver insufficiency,
  • Crimping sine syndrome,
  • SA block,
  • Patient with heart insufficiency NYHA class III-IV for lack of available data,
  • Patient with a cardiac pacemaker,
  • unstable angina pectoris,
  • AV-block 3. Degree,
  • Use of strong Cytochrom P450 3A4-Hemmern such as Antimykotika of the Azoltyp (Ketoconazol, Itraconazol), macro eyelid antibiotics (Clarithromycin, Erythromycin p." o., Josamycin, Telithromycin), HIV Protease inhibitor EN (Nelfinavir, Ritonavir) and Nefazodon,
  • Pregnancy and quiet time.

Pharmakokinetik

Ivabradin is absorbed after oral income fast and nearly completely. Maximum plasma mirrors are reached soberly after about one hour. The bio-availability is with about 40 per cent (roofridge passport effect). The absorption was retarded by food around approximately one hour. Ivabradin is bound to approximately 70 per cent at plasma protein.

Ivabradin is diminished to a large extent in the liver and in the intestine over the Cytochrom P450 3A4 (CYP3A4) metabolisiert (amplifier-off-changed) and with an effective radioactive half-life from eleven hours.

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