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口服与胃肠外给予曲美布汀对犬胃肠及结肠动力的影响。

Effects of orally vs. parenterally administrated trimebutine on gastrointestinal and colonic motility in dogs.

作者信息

Buéno L, Hondé C, Pascaud X, Junien J L

出版信息

Gastroenterol Clin Biol. 1987;11(3 Pt 2):90B-93B.

PMID:3609630
Abstract

The influence of oral administration and intravenous infusion of trimebutine maleate (TMB) and N-desmethyl TMB (NDTMB), its main metabolite, was investigated in conscious dogs equipped with chronically implanted strain-gauges. In fasted dogs, TMB (10 to 20 mg/kg per os) delayed the occurrence of the next activity front on both stomach and duodenum by reinforcing the duration of the intestinal phase II. It also induced the occurrence of an additional migrating phase III. These effects were associated with a colonic stimulation generally followed by an inhibition. Comparatively NDTMB at similar dosages disrupted the antral cyclic phases which were replaced by continuous low amplitude contractions during 5-7 h. The MMC pattern persisted with a significant increase in the duration of phase II, and the colonic motility was inhibited during 4.3 to 6.7 h. Infused intravenously at a dose of 3 mg X kg-1 X h-1, TMB immediately inhibited the gastric cyclic contractions in fasted dogs. As for the oral route, the small bowel exhibited an increase in the duration of phase II frequently associated with the occurrence of an additional phase III. Furthermore an inhibition of the colonic motility was observed only at the end of the infusion and lasted at least 4 h. At similar dosage NDTMB had less pronounced inhibitory effects on gastric activity fronts and in contrast with TMB, the inhibitory effect on the colonic motility was observed as soon as the infusion of NDTMB started. These data demonstrate that orally administered TMB stimulates intestinal motility as previously described for i.v. route but in contrast to parenteral administration also stimulates antral and colonic motility.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在植入了慢性应变片的清醒犬中,研究了口服和静脉输注马来酸曲美布汀(TMB)及其主要代谢物N-去甲基TMB(NDTMB)的影响。在禁食犬中,TMB(10至20mg/kg口服)通过延长肠相II的持续时间,延迟了胃和十二指肠下一个活动波锋的出现。它还诱导了额外的移行相III的出现。这些作用与结肠刺激相关,随后通常是抑制。相比之下,相似剂量的NDTMB破坏了胃窦的周期性活动,在5至7小时内被持续的低幅收缩所取代。MMC模式持续存在,相II的持续时间显著增加,结肠动力在4.3至6.7小时内受到抑制。以3mg·kg-1·h-1的剂量静脉输注时,TMB立即抑制禁食犬的胃周期性收缩。对于口服途径,小肠相II的持续时间增加,常伴有额外相III的出现。此外,仅在输注结束时观察到结肠动力受到抑制,且持续至少4小时。在相似剂量下,NDTMB对胃活动波锋的抑制作用不明显,与TMB相反,在输注NDTMB一开始就观察到对结肠动力的抑制作用。这些数据表明,口服TMB可刺激肠道动力,如先前静脉途径所描述的那样,但与胃肠外给药不同,它也刺激胃窦和结肠动力。(摘要截短至250字)

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