Tantcheva L, Stoytchev T
Institute of Physiology, Bulgarian Academy of Sciences.
Acta Physiol Pharmacol Bulg. 1989;15(2):33-9.
Single administration of desoxycorticosterone acetate (DOCA) in a dose of 50 mg/kg body mass intramuscularly in male Wistar rats revealed dose-dependent potentiation of hexobarbital sleeping time and inhibition of the activity of the oxidases with mixed functions in substrates of types I (hexobarbital, ethylmorphine) and II (aniline), although this is not accompanied by changes in the components of the electron-transport chain. It is assumed that DOCA may possibly inhibit the metabolism of the above mentioned substrates, being an alternative substrate of oxidases with mixed functions. In an acute experiment DOCA does not influence the activity of esterases (liver esterase A and intestinal esterase B), but the compound has an inhibitory effect on some synthetase reactions--cytosol glutathione-S-transferase. Repeated administration of DOCA for 3-27 days in doses of 10 and 20 mg/kg i.m. does not have an enzyme-inducing effect. There are no significant changes in the oxidases with mixed functions and in the content of cytochrome P-450. The effects of DOCA on drug metabolism after a single and after repeated application are compared with the effects of hydrocortisone.
对雄性Wistar大鼠肌肉注射50mg/kg体重的醋酸脱氧皮质酮（DOCA）进行单次给药后发现，己巴比妥睡眠时间呈剂量依赖性增强，且对I型（己巴比妥、乙基吗啡）和II型（苯胺）底物中具有混合功能的氧化酶活性有抑制作用，不过这并未伴随电子传递链组分的变化。据推测，DOCA可能作为具有混合功能的氧化酶的替代底物，从而抑制上述底物的代谢。在急性实验中，DOCA不影响酯酶（肝脏酯酶A和肠道酯酶B）的活性，但该化合物对某些合成酶反应——胞质谷胱甘肽-S-转移酶有抑制作用。以10和20mg/kg的剂量肌肉注射DOCA，连续给药3 - 27天，没有酶诱导作用。具有混合功能的氧化酶及细胞色素P - 450的含量没有显著变化。将DOCA单次给药和重复给药后对药物代谢的影响与氢化可的松的影响进行了比较。
