[Ivabradine--the first selective and specific I(f) inhibitor, novel preparation for treatment of stable angina].
Results of large epidemiological studies allowed to establish that heart rate (HR) is an independent risk factor, elevating rates of total, cardiovascular and sudden mortality. Ivabradine bounds specifically with f channels of sinus node cells providing HR lowering. In experiments with the use of the method of registration of transmembrane currents in cells of sinoatrial node it was revealed that Ivabradine blocks f-channels in a dose-dependent manner. Due to specific action on sinus node and selective suppression of I(f)-currents ivabradine causes dose dependent decrease of HR both at rest and maximal physical exercise without changes of mean blood pressure. It was shown in 3 large clinical studies that Ivabradine together with favorable tolerability profile possesses pronounced antianginal and anti-ischemic efficacy which is at least the same as efficacy of currently available drugs for the treatment of angina beta-adrenoblockers and calcium antagonists. Firstly this confirms clinical significance of concept of specific and selective inhibition of I(f) ionic current in the treatment of patients with ischemic heart disease and stable angina. Secondly this allows to consider the preparation as alternative to available antianginal drugs in case of the presence of contraindications to them or development of side effects at the background of standard therapy.
Belousov
Iu B
IuB
Erofeeva
S B
SB
Maneshina
O A
OA
D000787:Angina Pectoris / Q000188:drug therapy* / Q000503:physiopathology; D001552:Benzazepines / Q000627:therapeutic use*; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D000077550:Ivabradine; D012849:Sinoatrial Node / Q000187:drug effects / Q000503:physiopathology; D013237:Stereoisomerism; D016896:Treatment Outcome
D001552:Benzazepines; D000077550:Ivabradine