In 1860 by the method of the syntheses of salicylic acids was opened a group of nonsteroid anti-inflammatory preparations (NAIP). At present NAIP is refereed to the number of the most efficient and widely used in rheumatologic practice of medicinal facilities. The most wide-spread preparation of this group is acetylsalicylic acid, synthesized in 1898. Its has already used on an extent more than 100 years. The groups of ten new preparation appeared for this time, which had firmly occupied their own "positions" in clinical practice...
In 1971 British researchers under the direction of J. Vane have opened the main mechanism of the NAIP action, the ferment cyclooxigenase caused by blocking the ferment of cyclooxigenase (COG). It is established that COG exists in two, deferring one from another isoforms: COG-1 (constitutive) and COG-2 (induced by inflammation). In 1994 J. Vane supposed that anti-inflammatory and anaesthetizing action of NAIP is conditioned by inhibition of COG-2, but development of the side effects are conditioned by inhibition of COG-1.
Side effects that appear more frequently (ulcerogenic action, toxic influence on kidneys, disturbance of aggregation thrombocytes) are connected with suppression of activities COG-1. According to the analysis, held on FDA in 1991, annually defeat of the mucous membrane of the digestive tract, conditioned by acceptance NAIP, is a reason of 100 - 200 thousand hospitalization and 10 - 20 thousands death. As a whole the patients which have rheumatic diseases, which take NAIP, risk of the development gastroenterology complications increases in 7 times, necessity in stationary treatment in 6 times, and death-rate in 2 times above, than in the general population. In the USA only at patients with rheumatoid arthritis development of serious complications on the part of digestive tract, connected with reception of NAIP, annually brings to about 20 thousand hospitalization and 2 thousand death.
It has created the theoretical premises for creation of the new more safe class of NAIP, possessing ability selectively inhibit COG-2. One of them is preparation NIMULID (nimesulid), which produces the Indian pharmaceutical company "Panacea Biotec" and is promoted on Ukrainian market by wholesale company "Rainbow".
In present time nimesulid is widely used in many countries of the world. It is one of the first NAIP, in the course of studies which is confirmed its high selectivity in respect of COG-2, than in attitude to COG-1: approximately in 1,3 - 2,51 times. This characteristic of the preparation allows considerably to reduce frequency of the development of such side effects, as dyspepsia, sickness, stomachache, gastrointestinal bleeding and others.
Unlike rest of NAIP, pH of NIMULID forms 6,5. Thus, preparation is an anti-inflammatory remedy with pH close to neutral that reduces frequency of the development of the complications on the part of digestive tract, as damage of the mucous membrane of the ventricle, appearing on background of the acceptance other NAIP, it is conditioned not only by suppression them COG-1, but also its own high pH.
NIMULID quickly and effectively avoids inflammation and pain at, inflammatory diseases of ear, throat and nose, at postoperative period, under primary dysmenorrhea and others.
Alongside with others, broadly wide-spread preparations of nimesulid in the form of the tablets, it is registered single formula of this preparation in the form of transdermal gel. NIMULID in the form of gel is made with using the microcarriers, providing deep penetration of acting material in tissues. Uniform micromembrance is formed on the surfaces of the skin under its using, which prevents dehydration, enlarging time of the action of the preparation.