Department of Clinical Pharmacy, Oita University Hospital, Japan.
Biol Pharm Bull. 2011;34(10):1640-3. doi: 10.1248/bpb.34.1640.
Pantethine and fursultiamine have been evaluated for their clinical usefulness in the treatment and prevention of uncomplicated postoperative adhesive intestinal obstruction. In recent years, the actions of drugs used to treat gastrointestinal diseases have been elucidated pharmacologically from the viewpoints of gastrointestinal peptide levels. We examined the effects of pantethine and fursultiamine on plasma levels of calcitonin gene-related peptide (CGRP)-, vasoactive intestinal polypeptide (VIP)-, motilin- and substance P (SP)-like immunoreactive substances (IS) in healthy subjects. An open-labeled study was conducted on five healthy volunteers. Each subject was administered a single oral dose of pantethine, fursultiamine and placebo at intervals of one month. Venous blood samples were collected before and at 20, 40, 60, 90, 120, 180 and 240 min after each administration. Plasma peptide levels were measured using a highly sensitive enzyme immunoassay. A single oral dose of pantethine resulted in significant increases of plasma CGRP- and VIP-IS levels compared to placebo. Furthermore, areas under the plasma concentration-time curves (AUC(0-240)) of CGRP- and VIP-IS were significantly higher after pantethine administration compared with placebo. On the other hand, fursultiamine had no effect on plasma levels and AUC(0-240) of CGRP-, VIP-, motilin- and SP-IS. This study demonstrated the different effects of pantethine and fursultiamine from the viewpoint of plasma gastrointestinal peptide changes. The pharmacological effects of pantethine may be closely related to the changes in plasma CGRP- and VIP-IS levels.
泛硫乙胺和呋喃硫胺已被评估用于治疗和预防非复杂性术后粘连性肠梗阻的临床用途。近年来，从胃肠肽水平的观点出发，阐明了用于治疗胃肠道疾病的药物的作用。我们研究了泛硫乙胺和呋喃硫胺对健康受试者血浆降钙素基因相关肽（CGRP）、血管活性肠肽（VIP）、胃动素和 P 物质（SP）样免疫反应物质（IS）水平的影响。在 5 名健康志愿者中进行了一项开放标签研究。每个志愿者在一个月的间隔内分别给予单次口服泛硫乙胺、呋喃硫胺和安慰剂。在给药前和给药后 20、40、60、90、120、180 和 240 分钟采集静脉血样。使用高度敏感的酶免疫测定法测量血浆肽水平。与安慰剂相比，单次口服泛硫乙胺可显著增加血浆 CGRP 和 VIP-IS 水平。此外，与安慰剂相比，CGRP 和 VIP-IS 的血浆浓度-时间曲线下面积（AUC（0-240））在泛硫乙胺给药后明显更高。另一方面，呋喃硫胺对 CGRP、VIP、胃动素和 SP-IS 的血浆水平和 AUC（0-240）没有影响。这项研究从血浆胃肠肽变化的角度展示了泛硫乙胺和呋喃硫胺的不同作用。泛硫乙胺的药理作用可能与血浆 CGRP 和 VIP-IS 水平的变化密切相关。
