[Sulfonylurea receptors and their interaction with glimepiride]. / Retseptory k sul'fonilmochevine i ikh vzaimodeistvie s glimepiridom.

In the review, data are presented on glymepiride (amaril), a 3-d generation sulphanylamide. The drug interacts with receptors to sulphonylurea--SUR X, that are found only in B-cells of the pancreas, which fact has been shown to be associated with a higher secretion of insulin, an increased sensitivity of peripheral tissues to this hormone and with insulin-like extrapancreatic effects as well. Amaril does not affect SUR of the myocardium, myocytes of cerebral vessels and nervous cells. The use of the above drug combined with metformin, insulin, repaglynide, and nateglynide has been shown to be an optimum treatment option, however in the latter case, hypoglycemic states may come to be seen more frequently along with a rapid exhaustion of B-cells. In view of the fact that in many instances, type 2 diabetes mellitus runs its course concurrently with other illness, it is necessary that interaction of amaril with other drugs be taken into account.

[Antiandrogenic effects of hydroxyniftolide in male rats]. / Antiandrogennye éffekty gidroksiniftolida u samtsov krys.

Experiments on intact mature male Wistar rats showed the ability of hydroxyniftolide (4'-nitro-3'-trifluoromethyl-2-hydroxy-2-methylpropionylanilide), a hydroxylated antiandrogen derivative of niftolide, to inhibit the effects of male sex hormones in androgen target organs. At doses of 10 mg/kg and upwards administered intravenously or intramuscularly for 10 days, it stimulated the hypothalamohypophy-seogonadal system expressed in an increase in the activity of delta 5-steroid-3 beta-ol-dehydrogenase in the testicles and blood plasma testosterone concentration. Comparative studies on antiandrogenic properties of niftolide and hydroxyniftolide made it possible to show that the effect of the first agent was more noticeable with relation to the hypothalamic centers of gonadotropin secretion regulation whereas the effect of the second one was more noticeable in the accessory sex glands.