苯乙肼的体内过程和一些药理作用

应用二甲基胺苯甲醛作为显色剂,尚适用于測定血及組織內的苯乙肼?o小鼠以苯乙肼灌胃或腹腔注射,用药半小时后血浆浓度即到达最高峯,灌胃时t1/2(消除半量的时間)为3.39小时,腹腔注射时t1/2只有1.2小时。口服給药,苯乙肼主要由小腸吸收,吸收后能分布至主要脏器內,其中肝脏和脑內的浓度最高?揭译陆o小鼠一次腹腔注射的LD₅₀为151.4毫克/公斤,連續用药9天LD₅₀为45—50毫克/公斤,兔的致死量为75—100毫克/公斤。苯乙肼小剂量具有呼吸兴奋作用及升压作用;大剂量能延长环己巴比妥鈉麻醉作用时間,損伤肝脏排泄磺溴酞鈉的功能,使肝組織产生脂肪变性,并使心率明显減慢,但无退热作用。

STUDIES ON THE FATE AND CERTAIN PHARMACOLOGICAL ACTIONS OF PHENELZINE

1. A methed for estimation of phenelzine, based on the use of trichloroacetic acid to precipitate the protein of plasma and tissues, and the use of dimethylaminobenzaldehyde as a colour developing agent, was found to be adequate for our purpose. 2. When phenelzine was given to a mouse orally or intraperitoneally, the peak plasma level was obtained in 0.5—1 hour, which then declined gradually. The compound was distributed in the liver, brain, heart, kidney, and lung. The highest concentrations were attained for the first two organs, while the concentration of phenelzine for the lung was very low. The rate of disappearance of phenelzine from tissues was generally found to be slower than from the plasma. 3.In mice, the LD₅₀ of phenelzine for single dose of intraperitoneal injection was 151.4 mg/kg, and that for a series of 9 daily doses was 45—50 mg/kg.In rabbits, the lethal dose of phenelzine was 75—100mg/kg. 4. In rabbit, intravenous administration of 2, 5, 10 mg/kg of phenelzine stimulated the respiration, promptly abolished respiratory depression caused by morphine and slightly elevated the blood pressure. A dose of 25 mg/kg slowed the heart rate. Atropine partially blocked this action. After given 10 mg/kg daily for a week, the plasma retention of bromosulphthalein may be elevated, and the fatty degeneration of liver tissues developed. In mice, intraperitoneal administration of 0.4 mg/kg, of phenelzine increased the anaesthetic time of the evipan. Phenelzine was not an antipyretic.