Jenner P J, Ellard G A, Gruer P J, Aber V R
J Antimicrob Chemother. 1984 Mar;13(3):267-77. doi: 10.1093/jac/13.3.267.
The blood levels and urinary excretion of the anti-mycobacterial drugs ethionamide and prothionamide have been compared after oral dosage in man. High pressure liquid chromatographic methods were used to determine the two closely related thioamides and their microbiologically active sulphoxide metabolites after the ingestion of both single and combined doses of the two drugs. Both drugs were rapidly eliminated from the body, the half-life for the urinary excretion and removal from the plasma of prothionamide being slightly less than that of ethionamide. Less than 0.1% of the orally administered doses were excreted unchanged in the faeces. Plasma concentrations of ethionamide and its sulphoxide metabolite were substantially higher than those of prothionamide and prothionamide sulphoxide. The implications of these findings for the use of ethionamide or prothionamide in the treatment of lepromatous leprosy are discussed.
对人体口服抗分枝杆菌药物乙硫异烟胺和丙硫异烟胺后的血药浓度及尿排泄情况进行了比较。采用高压液相色谱法测定单次和联合服用这两种药物后两种密切相关的硫代酰胺及其具有微生物活性的亚砜代谢产物。两种药物均迅速从体内消除，丙硫异烟胺从尿中排泄及从血浆中清除的半衰期略短于乙硫异烟胺。口服剂量中不到0.1%以原形经粪便排泄。乙硫异烟胺及其亚砜代谢产物的血浆浓度显著高于丙硫异烟胺及其亚砜代谢产物。讨论了这些发现对乙硫异烟胺或丙硫异烟胺用于治疗瘤型麻风的意义。
