Scarpellini E, Pauwels A, Vos R, Rommel N, Tack J
Division of Gastroenterology, Department of Internal Medicine, University Hospital Gasthuisberg, Catholic University of Leuven, Leuven, Belgium.
Neurogastroenterol Motil. 2017 Mar;29(3). doi: 10.1111/nmo.12938. Epub 2017 Jan 22.
Endogenous opioids (EO) acting on μ-opiod receptors in central and enteric nervous system (ENS) control gastrointestinal motility but it is still unclear whether EO in ENS may control esophageal function in man, thus we will study the effects of methylnaltrexone (MNTX), a peripherally selective, and naloxone (NA), a non-selective μ-opiod receptor antagonist, on esophageal motility in healthy subjects.
Fifteen HV (6 M; 34.1 ± 0.6 years; BMI: 22.1 ± 0.1 kg/m ) underwent three esophageal high-resolution manometry impedance (HRiM) studies with 10 saline swallows administered every 30 minutes: drug was administered after 30 minutes (MNTX subcutaneously/NA or saline intravenously), a solid meal after 90 minutes; measurements continued for 120 minutes postprandially.
Methylnaltrexone did not significantly decrease the upper esophageal sphincter (UES) percentage of relaxation preprandially (72.5 ± 5 vs 66.9 ± 4.6 and 73 ± 3.8%, ANOVA between placebo, MNTX and NA, P=NS) and postprandially (60 minutes: 68.2 ± 5.6 vs 61 ± 5.5 and 67.1 ± 5.6%; 120 minutes: 68 ± 5.9 vs 59.3 ± 5.2 and 67.7 ± 4.7%; ANOVA between placebo, MNTX and NA, P=NS). MNTX and NA did not significantly alter preprandial and postprandial LES resting pressures and integrated relaxation pressure (ANOVA between placebo, MNTX and NA, all P=NS). Peak front velocity and distal contractile integral were not altered pre- and postprandially by MNTX and NA (ANOVA between placebo, MNTX and NA, P=NS). Transient lower esophageal sphincter relaxations (TLESRs') number was not altered by MNTX and NA (ANOVA between placebo, MNTX and NA, all P=NS).
The peripheral selective and non-selective μ-opioid receptor antagonists MNTX and NA, respectively, do not alter TLESRs occurrence and esophageal peristalsis.
内源性阿片类物质（EO）作用于中枢和肠神经系统（ENS）中的μ-阿片受体，控制胃肠动力，但ENS中的EO是否可控制人类食管功能仍不清楚。因此，我们将研究外周选择性μ-阿片受体拮抗剂甲基纳曲酮（MNTX）和非选择性μ-阿片受体拮抗剂纳洛酮（NA）对健康受试者食管动力的影响。
15名健康志愿者（6名男性；年龄34.1±0.6岁；体重指数：22.1±0.1kg/m²）接受了三项食管高分辨率测压阻抗（HRiM）研究，每30分钟吞咽10次生理盐水：30分钟后给药（MNTX皮下注射/NA或生理盐水静脉注射），90分钟后进食固体餐；餐后持续测量120分钟。
甲基纳曲酮在餐前（72.5±5% vs 66.9±4.6%和73±3.8%，安慰剂、MNTX和NA之间的方差分析，P=无显著性差异）和餐后（60分钟：68.2±5.6% vs 61±5.5%和67.1±5.6%；120分钟：68±5.9% vs 59.3±5.2%和67.7±4.7%；安慰剂、MNTX和NA之间的方差分析，P=无显著性差异）均未显著降低食管上括约肌（UES）的松弛百分比。MNTX和NA对餐前和餐后LES静息压力及综合松弛压力均无显著影响（安慰剂、MNTX和NA之间的方差分析，P均=无显著性差异）。MNTX和NA在餐前和餐后均未改变峰值前向速度和远端收缩积分（安慰剂、MNTX和NA之间的方差分析，P=无显著性差异）。MNTX和NA未改变短暂下食管括约肌松弛（TLESRs）的次数（安慰剂
