Jauch R, Kopitar Z, Prox A, Zimmer A
Arzneimittelforschung. 1976;26(11):2084-9.
After intravenous, intramuscular and oral administration of 25 mg 14C-labelled 2-(3-[4-(m-chlorophenyl)-1-piperazinyl]-propyl)-s-triazolo[4,3-a]pyridin-3-(2H)-one-hydrochloride (trazodone), plasma levels, elimination and metabolite pattern in plasma and urine were investigated. The plasma levels after all routes of administration are almost identical. The absorption of the compound is fast and complete. The elimination of radioactivity occurs in a biphasic manner with a half-life of 1 h for the earlier and 13 h for the second phase, no matter what application route had been chosen. The comparison of the plasma levels of fasted and non-fasted subjects shows a shift of the plasma maximum from 1.5 to 2.5 h following administration and a decrease in the maximum level of 30%. The radioactivity is excreted predominantly by renal processes (70-75% within 72 h). The main product in plasma is unchanged trazodone, whereas in urine it is found only in minute amounts. The radioactivity in urine is represented by conjugates that had formed after hydroxylation on the chlorophenyl residue (20%), by a dihydrodiol-metabolite of trazodone (15%) and by a carboxylic acid originating from oxidative cleavage of the parent compound (35%).
静脉注射、肌肉注射及口服25毫克14C标记的2-(3-[4-(间氯苯基)-1-哌嗪基]-丙基)-s-三唑并[4,3-a]吡啶-3-(2H)-酮盐酸盐（曲唑酮）后，对血浆水平、消除情况以及血浆和尿液中的代谢物模式进行了研究。所有给药途径后的血浆水平几乎相同。该化合物吸收迅速且完全。无论选择何种给药途径，放射性的消除均呈双相方式，早期半衰期为1小时，第二阶段为13小时。禁食和非禁食受试者血浆水平的比较显示，给药后血浆峰值从1.5小时推迟至2.5小时，且峰值水平降低了30%。放射性主要通过肾脏排泄（72小时内排泄70 - 75%）。血浆中的主要产物是未变化的曲唑酮，而在尿液中仅发现微量。尿液中的放射性由氯苯基残基羟基化后形成的缀合物（20%）、曲唑酮的二氢二醇代谢物（15%）以及母体化合物氧化裂解产生的羧酸（35%）代表。
