Tubaro E, Belogi L, Mezzadri C M, Ruco L, Stopacciaro A
Medosan Ricerca S.r.l., Albano Laziale, Rome, Italy.
Arzneimittelforschung. 1995 Dec;45(12):1298-302.
Unexpectedly high levels of gastric tolerance to the new non-steroidal anti-inflammatory drug (NSAID) amtolmetin guacyl (CAS 87344-06-7, MED15) were observed in clinical practice. Further investigation of the drug was, therefore, undertaken in order to evaluate its gastrointestinal side-effects in animals. This new agent, which possesses high anti-inflammatory, analgesic and antipyretic activity, was recently introduced into medical therapy. In rats, repeated administration of MED15, even at high dosages, failed to produce any adverse effects on the gastric mucosa, unlike the reference NSAIDs used; the effect on the gastric mucosa was evaluated macro- and microscopically with a staining technique. In immature rat isolated stomachs MED15 strongly down-regulated the HCl output evoked by histamine, acetylcholine and gastrin. An effective NSAID which presents the added advantage of antisecretory properties has not previously been described amongst the many currently available, and reverses the dogma of the inevitable correlation between NSAID assumption and gastrointestinal reactions.
在临床实践中观察到,新型非甾体抗炎药安多美汀胍酯(CAS 87344-06-7,MED15)的胃耐受性水平出乎意料地高。因此,对该药物进行了进一步研究,以评估其在动物体内的胃肠道副作用。这种具有高抗炎、镇痛和解热活性的新型药物最近被引入医学治疗。在大鼠中,与所用的参比非甾体抗炎药不同,即使高剂量重复给予MED15,也未对胃黏膜产生任何不良影响;采用染色技术从宏观和微观层面评估其对胃黏膜的影响。在未成熟大鼠离体胃中,MED15强烈下调组胺、乙酰胆碱和胃泌素诱发的盐酸分泌。在目前众多可用的非甾体抗炎药中,尚未有兼具抗分泌特性这一额外优势的有效药物被报道,这颠覆了非甾体抗炎药使用与胃肠道反应之间必然存在关联的定论。