阿托莫汀，一种胃动素受体激动剂，对食管、食管下括约肌和胃压的影响。
Effect of atilmotin, a motilin receptor agonist, on esophageal, lower esophageal sphincter, and gastric pressures.
机构信息
Division of Gastroenterology, Department of Medicine, Temple University School of Medicine, Philadelphia, PA, USA.
出版信息
Dig Dis Sci. 2010 Feb;55(2):300-6. doi: 10.1007/s10620-009-1056-1.
BACKGROUND
Motilin, an endogenous gastrointestinal (GI) hormone, increases upper gastrointestinal tract motility and is associated with phase III of the gastric migrating motor complex. The motilin receptor agonist, atilmotin, at doses of 6, 30 or 60 microg intravenously (IV), increases the early phase of gastric emptying. Prior studies at higher doses of 100-450 microg IV demonstrated that some subjects developed noncardiac chest pain.
AIMS
The aim of this study is to determine the effects of atilmotin on esophageal, lower esophageal sphincter (LES), and gastric contractility and the development of esophageal-related symptoms.
METHODS
Ten healthy volunteers underwent esophageal manometry to study the effects of atilmotin on upper GI motility. Five subjects were studied on three separate days following administration of saline placebo and subsequent IV bolus dose of atilmotin (6, 30 or 150 microg). Another five subjects were studied at the highest dose (150 microg).
RESULTS
Atilmotin at 150 microg increased proximal gastric pressure by 6.5 mmHg (P = 0.001 compared with placebo). Atilmotin increased LES pressure at all studied doses; LES pressure increased from 24 +/- 2 mmHg following placebo injection to 34 +/- 4 mmHg following a 30 microg dose of atilmotin (P = 0.007). In the esophagus, atilmotin increased the percentage of failed swallows at the highest dose studied. Failed swallows increased from 17 +/- 7% following placebo injection to 36 +/- 7% following a 150 microg dose of atilmotin (P = 0.016). Atilmotin decreased distal esophageal contractile amplitude only at the highest dose studied, from 69 +/- 8 mmHg (placebo) to 50 +/- 5 mmHg following 150 microg atilmotin (P = 0.018). There were no serious adverse effects or episodes of chest pain with atilmotin.
CONCLUSIONS
Atilmotin affects esophageal, LES, and gastric motility. LES and gastric pressures were increased, whereas there was disruption of esophageal peristalsis characterized by lower amplitude and failed contractions.
背景
胃动素是一种内源性胃肠道（GI）激素，可增加上消化道的运动，并与胃移行性运动复合波的第三期相关。胃动素受体激动剂，阿托莫丁，以 6、30 或 60 微克静脉内（IV）的剂量给药，可增加胃排空的早期阶段。先前在更高剂量（100-450 微克 IV）的研究表明，一些受试者出现了非心源性胸痛。
目的
本研究旨在确定阿托莫丁对食管、食管下括约肌（LES）和胃收缩性以及食管相关症状的发展的影响。
方法
10 名健康志愿者接受食管测压术，以研究阿托莫丁对上 GI 运动的影响。5 名受试者在接受盐水安慰剂和随后的 IV 推注剂量的阿托莫丁（6、30 或 150 微克）的 3 个不同日子进行研究。另外 5 名受试者在最高剂量（150 微克）下进行研究。
结果
阿托莫丁在 150 微克时使近端胃压增加 6.5mmHg（与安慰剂相比，P = 0.001）。阿托莫丁增加了所有研究剂量的 LES 压力；LES 压力从注射安慰剂后的 24 +/- 2mmHg 增加到 30 微克阿托莫丁后的 34 +/- 4mmHg（P = 0.007）。在食管中，阿托莫丁在研究的最高剂量下增加了吞咽失败的百分比。吞咽失败从注射安慰剂后的 17 +/- 7%增加到 150 微克阿托莫丁后的 36 +/- 7%（P = 0.016）。阿托莫丁仅在研究的最高剂量下降低了远端食管收缩幅度，从 69 +/- 8mmHg（安慰剂）降至 150 微克阿托莫丁后的 50 +/- 5mmHg（P = 0.018）。阿托莫丁没有严重的不良反应或胸痛发作。
结论
阿托莫丁影响食管、LES 和胃的运动。LES 和胃压增加，而食管蠕动功能紊乱，表现为幅度降低和收缩失败。
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