(体内的选择性非甾体类抗炎药COX-1-COX-2和胃肠道溃疡、老鼠)。

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Laudanno OM、Cesolari JA Esnarriaga J, Flaherty P, Vada J, Guastalli G, San Miguel P Bedini OA

(体内的选择性非甾体类抗炎药COX-1-COX-2和胃肠道溃疡、老鼠)。

学报杂志Latinoam。1998; 28 (3): 249 - 55。

PubMed ID

9773153 (在PubMed

]

文摘

这项工作的目的是研究COX-1和cox - 2选择性在16个非甾体抗炎药(非甾体抗炎药),在产生溃疡的剂量2实验模型:1)提供皮下注射(sc)、固体食物(SF)、后(腔溃疡和肠道侵蚀);和2)口头(O)(胃底和肠道侵蚀)。方法:17组女性Wistar鼠每组(n = 7),重200克,36小时禁食水随意,提交以下实验:1。科幻小说(嘉吉chow)在1 h,然后sc: 1.1毫升生理盐水;2。双氯芬酸(Di);3所示。indomethacine(印度);4所示。Ketorolac(客); 5. meloxicam (Mel); 6. Pyroxicam (P); 7. tenoxicam (T). The dose for the aforementioned drugs was 60 mg/kg; 8. aceclofenac (Ace); 9. 200 mg/kg nimesulide (Ni); 10. mefenamic acid (Mac); 11. aspirin (A); 12. etodolac (E); 13. ibuprophen (Ibu); 14. nabumetone (Na); 15. naproxene (Nap); 16. ketoprophen (Ket); 17. paracetamol (Pa), 500 mg/kg. II. The drugs where administered by orogastric tubing to the same groups of fasting animals. After 24 h the animals were killed by ether overdose. Laparotomy was performed and the stomach and the small intestine was removed. The percentage of antum ulcer, and fundic and intestinal erosion (mm2) was tabulated by planimetry. Blood and histological samples were obtained. RESULTS: The NSAIDs Indo, Ibu, Ke, Ket, P and Te yielded an antrum ulcer area: 5-29% and intestinal erosion, 101-395 mm2, similar to Indo (p > 0.50). In contrast there were neither ulcers nor intestinal erosions with Mac, A, Di, E and Nap (p > 0.50). While there were absence of ulcers with Ace, Me, Na, Ni and Pa and slight intestinal erosion (0-23 mm2; p < 0.01). II. There were differences in the following oral (NAIDs: Ace, Me, NA, Ni and Pa, yielding 0-5% fundic erosion and 0-22 mm2 intestinal erosion (p < 0.001). The other NSADs yielded 33-90% fundic erosion and 116-550 mm2 intestinal erosion, similarly to Indo (p > 0.50). HISTOLOGY: Leukocyte infiltrate in the gastrointestinal mucosa with all the NSADs, except Ibu and Pa. There was also neutrophilia (5000-20,000), but not with Ibu and Pa (700-1200). CONCLUSIONS: COX-2-COX-1 selectivity was demonstrated "in vivo" in aceclofenac, meloxicam, nabumetone, nimesulide and paracetamol.

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药物靶点

药物	目标	类	生物	药理作用	行动
甲灭酸	前列腺素合成酶1 G / H	蛋白质	人类	未知的	抑制剂	细节