Magnussen I, Jensen T S, Rand J H, Van Woert M H
Acta Pharmacol Toxicol (Copenh). 1981 Sep;49(3):184-9. doi: 10.1111/j.1600-0773.1981.tb00890.x.
Single oral doses of L-5-hydroxytryptophan (5-HTP) were administered in combination with L-aromatic amino acid decarboxylase inhibitors. The time courses of plasma concentrations of 5-HTP, 5-hydroxytryptamine (5-HT) and 5-hydroxyindoleacetic acid (5-HIAA) and the concentrations of 5-HT in blood platelets were measured. Carbidopa enhanced the rise in plasma concentrations of 5-HTP 5-15 fold and counteracted the increase in plasma 5-HIAA levels induced by 5-HTP alone. A single dose of the decarboxylase inhibitor was equipotent to 14 days' pretreatment. Plasma or platelet concentrations of 5-HT failed to reflect the metabolism of 5-HTP. The ratio of 5-HTP to carbidopa influenced the systemic bioavailability of single dose administered 5-HTP indicating dose dependent absorption kinetics. Co-administration of L-dopa with 5-HTP and decarboxylase inhibitors had no effect on gastrointestinal absorption of 5-HTP in six parkinsonian patients.
单次口服L - 5 - 羟色氨酸(5 - HTP)并联合使用L - 芳香族氨基酸脱羧酶抑制剂。测定了5 - HTP、5 - 羟色胺(5 - HT)和5 - 羟吲哚乙酸(5 - HIAA)的血浆浓度时间进程以及血小板中5 - HT的浓度。卡比多巴使5 - HTP的血浆浓度升高5至15倍,并抵消了单独使用5 - HTP引起的血浆5 - HIAA水平升高。单次剂量的脱羧酶抑制剂与14天的预处理等效。5 - HT的血浆或血小板浓度未能反映5 - HTP的代谢情况。5 - HTP与卡比多巴的比例影响单次给药5 - HTP的全身生物利用度,表明存在剂量依赖性吸收动力学。在6例帕金森病患者中,左旋多巴与5 - HTP和脱羧酶抑制剂联合使用对5 - HTP的胃肠道吸收没有影响。