Taylor W B, Bateman D N
Br J Clin Pharmacol. 1987 Feb;23(2):137-42. doi: 10.1111/j.1365-2125.1987.tb03021.x.
The pharmacokinetics and pharmacodynamics of prochlorperazine were studied in healthy volunteers using a recently developed h.p.l.c. assay. Eight subjects received 12.5 mg and 6.25 mg i.v. doses of prochlorperazine, a 25 mg oral dose and placebo in random order. Plasma half-life (t1/2) of prochlorperazine was 6.8 +/- 0.7 h and 6.9 +/- 0.8 h for the 12.5 mg and 6.25 mg i.v. doses respectively. Apparent volume of distribution and plasma clearance were high and the kinetics did not appear to be dose-related. Absorption of oral prochlorperazine appeared to be slow and bioavailability was very low. A metabolite, possibly prochlorperazine sulphoxide, was noted after oral dosing. Mild sedation was common after i.v. prochlorperazine, but cardiovascular effects were minimal. The main adverse effect was akathisia which was reported by five out of eight subjects after the higher i.v. dose. These results provide preliminary information on the pharmacokinetics of i.v. prochlorperazine which were previously unknown.
采用最近开发的高效液相色谱法，在健康志愿者中研究了丙氯拉嗪的药代动力学和药效学。8名受试者随机接受12.5毫克和6.25毫克静脉注射剂量的丙氯拉嗪、25毫克口服剂量及安慰剂。12.5毫克和6.25毫克静脉注射剂量的丙氯拉嗪血浆半衰期（t1/2）分别为6.8±0.7小时和6.9±0.8小时。表观分布容积和血浆清除率较高，且动力学似乎与剂量无关。口服丙氯拉嗪的吸收似乎较慢，生物利用度非常低。口服给药后发现一种代谢物，可能是丙氯拉嗪亚砜。静脉注射丙氯拉嗪后常见轻度镇静，但心血管效应极小。主要不良反应是静坐不能，8名受试者中有5名在较高静脉注射剂量后报告出现此症状。这些结果提供了关于静脉注射丙氯拉嗪药代动力学的初步信息，而此前这些信息尚不清楚。
