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Studies on the Effect of the Opioid Receptor Agonist 'Trimebutine' on Inflammation, Pain and Gastric Ulceration in Rats

机译:阿片受体激动剂“曲美布汀”对大鼠炎症,疼痛和胃溃疡的作用研究

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The effects of trimebutine, a peripheral opiate agonist, were investigated on the development of paw oedema by carrageenan, on visceral nociception caused by i.p. injection of acetic acid, on gastric mucosal injury induced by indomethacin and on gastric acid secretion in rats. I.p administration of trimebutine at 30, 60 or 120 mg/kg, at 30-min pretreatment, decreased paw oedema caused by carrageenan injection by 18.2-21.6%, 27.3%- 22.8% and 33.6%- 29.3%, respectively, with maximal inhibition being observed at 1-2 hr post-carrageenan. In addition, trimebutine in doses of 30, 60 or 120 mg/kg (i.p.) 30 min after carrageenan challenge inhibited the paw oedema response by -21.2, -17%, 22.3, -21.2% and -33.1, -30% at 3 and 4 hr post-carrageenan, respectively. Trimebutine (60 mg/kg) co-administered with meloxicam (3.8 mg/kg), indomethacin (18 mg/kg) or dexamethasone (0.2 mg/kg) resulted in an additive effect. Abdominal writhes induced by i.p. injection of acetic acid were effectively inhibited by trimebutine. The drug enhanced the development of lesions by indomethacin in a dose-dependent manner. In anaesthetised rats, trimebutine caused dose-dependent inhibition of gastric acid secretion. Results indicate that trimebutine possesses anti-inflammatory properties in addition to its visceral analgesic effects. The drug likely exacerbates gastric mucosal lesions by non-steroidal anti-inflammatory drugs and consequently their concurrent administration is not advisable.
机译:研究了曲美布汀(一种外围的鸦片激动剂)对角叉菜胶对爪水肿的发展以及对腹腔注射引起的内脏伤害感受的影响。乙酸注射液对消炎痛诱导的胃黏膜损伤及大鼠胃酸分泌的影响在预处理30分钟时,以30、60或120 mg / kg的IP方式施用曲美布汀,分别减少了18.2-21.6%,27.3%-22.8%和33.6%-29.3%的角叉菜胶注射液所致的爪水肿,并具有最大的抑制作用在角叉菜胶后1-2小时观察到。此外,角叉菜胶攻击后30分钟,曲美布汀剂量为30、60或120 mg / kg(ip),在3时抑制爪水肿反应为-21.2,-17%,22.3,-21.2%和-33.1,-30%和角叉菜胶后4小时。曲美布汀(60 mg / kg)与美洛昔康(3.8 mg / kg),消炎痛(18 mg / kg)或地塞米松(0.2 mg / kg)共同给药可产生累加作用。 i.p.引起的腹部扭曲曲美布汀可有效抑制乙酸的注射。吲哚美辛以剂量依赖性方式增强了病灶的发展。在麻醉的大鼠中,曲美布汀引起胃酸分泌的剂量依赖性抑制。结果表明,曲美布汀除具有内脏止痛作用外,还具有抗炎特性。该药物可能通过非甾体类抗炎药加重胃粘膜损害,因此不建议同时使用。

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