[Use of synthetic steroids, inhibitors of microsomal enzymes, for retention of hexenal in the body and for prolongation of hexenal anesthesia under experimental conditions].
17alpha-hydroxydeoxycorticosterone and its acetate derivative inhibited the activity of rat liver microsomal enzymes. The inhibitory effect of steroids was not accompanied by induction of the enzyme synthesis, which was characteristic for the other known inhibitors of mixed function oxydases (SKF 525-A, DPEA, MPDK). These properties of the steroids suggested their use for prolongation of the effect of drugs, which are inactivated by microsomal enzymes. The suggestion was tested using hexobarbital as an example. The transformation of hexobarbital in vitro by the rat liver microsomal enzymes was completely inhibited by the equimolar amount of the steroid acetate. Treatment of rats with the steroid acetate almost doubled the life-time of the hexobarbital in rat blood and resulted in the 1.5-fold increase of the sleeping time. The most effective dose of the steroid acetate was 5 mg per 100 g of body weight, the drug being injected 15 min before hexobarbital administration.
D000768:Anesthesia, General; D000818:Animals; D001189:Aryl Hydrocarbon Hydroxylases / Q000037:antagonists & inhibitors; D001711:Biotransformation; D004305:Dose-Response Relationship, Drug; D005938:Glucocorticoids / Q000008:administration & dosage / Q000494:pharmacology*; D006207:Half-Life; D006591:Hexobarbital / Q000378:metabolism*; D066298:In Vitro Techniques; D008297:Male; D008862:Microsomes, Liver / Q000201:enzymology*; D051381:Rats; D013997:Time Factors
D005938:Glucocorticoids; D006591:Hexobarbital; D001189:Aryl Hydrocarbon Hydroxylases
Ispol'zovanie ingibitorov mikrosomal'nykh fermentov - sinteticheskikh steroidov - dlia zaderzhki geksenala v organizme i prolongirovaniia geksenalovogo narkoza v eksperimente