[Evolution of oral drug forms of metoprolol: advantages of long acting modified release forms with modified release].

Review oral modified release drug forms of beta-adrenoblocker metoprolol which is used in arterial hypertension and ischemic heart disease is presented. Metoprolol has salts such as tartrate which is used for production of immediate release (IR) and sustained release (SR) forms and succinate used for production of controlled release form (CR/XL). Metoprolol SR has monolith matrix type, metoprolol CR/XL-system of multiple pellets. Effect of metoprolol tartrate (IR) on mortality was demonstrated in a number of studies in patients with arterial hypertension (AH) (MAPHY), myocardial infarction (SMT, GMT, MIAMI), dilated cardiomyopathy and heart failure (MDC). Studies of efficacy of metoprolol SR are scarce. Antihypertensive efficacy of metoprolol SR in patients with AH did not exceed that of a metoprolol IR or CR/XL. First retrospective analysis of efficacy of metoprolol tartrate and succinate (CR/XL) in patients after myocardial infarction allowed to obtain comparable results of 34% mortality lowering. In a prospective study in patients with chronic heart failure (COMET) metoprolol tartrate IR was not superior to carvedilol when mortality lowering was concerned. At the same time administration of controlled release metoprolol (CR/XL) in 2 large clinical trials (RESOLVD, MERITAHF) was advantageous in patients with chronic heart failure relative to lowering of mortality and rate of hospitalizations. A novel controlled release form of metoprolol has been created as a tartrate salt on the basis of pellet technology (CD/ERT) and its bioequivalence to metoprolol CR/XL has been proved.

[Interaction of omnic (tamsulozine) and its generic analogues with alpha-adrenoreceptors].

In current practice of pharmacotherapy of prostatic adenoma alpha1-adrenoblockers are first-line drugs the efficacy and safety of which have been proved in many randomized studies. Because of the appearance of a large amount of generic analogues of tamsulozine on the market we studied the ability of tamsulozine analogues to bind with alpha-adrenoreceptors on rat and human prostate affected by adenoma. Significant differences on the receptor level of interaction were found. Omnik, compared to other generic analogues of tamsulozine, has the highest affinity to alpha1-adrenoreceptors.

[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.