Rainsford K D, James C, Johnson D M, Stetsko P I, Hill R E, Salena B J, Hunt R H
Department of Biomedical Sciences, McMaster University Faculty of Health Sciences, Hamilton, Ontario, Canada.
Agents Actions. 1993;39 Spec No:C21-3. doi: 10.1007/BF01972708.
The relationship between endoscopically observed gastric mucosal damage, elicited following repeated oral intake for 7 d of four NSAIDs, to their effects on antral and fundic production of PGE2, 6-keto-PGF1 alpha and TxB2 (assayed by GC-MS), mucosal histology and plasma concentration profiles was studied in 40 normal males. Subjects received azapropazone (APZ) 600 mg b.i.d., indomethacin (IND) 50 mg t.i.d., naproxen (NAP) 500 mg b.i.d., piroxicam (PIR) 20 mg qq.d., or one placebo capsule t.i.d. (N = 8/group). Plasma NSAIDs (HPLC) levelled at 7 d. Mucosal damage occurred in the antrum region with IND and NAP. APZ and PIR exhibited no differences compared to placebo. NAP and IND reduced all three prostanoids in the antrum while APZ and PIR were ineffective. Fundic PGE2 was reduced by IND, NAP and PIR; APZ had no effects. Thus, mucosal damage relates to effects on prostanoid production in the antrum but not in the fundus.
在40名正常男性中研究了连续7天口服四种非甾体抗炎药（NSAIDs）后内镜观察到的胃黏膜损伤与它们对胃窦和胃底前列腺素E2（PGE2）、6-酮-前列腺素F1α（6-keto-PGF1α）和血栓素B2（TxB2）（通过气相色谱-质谱法测定）生成的影响、黏膜组织学以及血浆浓度曲线之间的关系。受试者分别接受阿扎丙宗（APZ）600毫克，每日两次；吲哚美辛（IND）50毫克，每日三次；萘普生（NAP）500毫克，每日两次；吡罗昔康（PIR）20毫克，每日一次；或每日三次服用一粒安慰剂胶囊（每组n = 8）。血浆NSAIDs（通过高效液相色谱法测定）在第7天达到稳定水平。IND和NAP导致胃窦区域出现黏膜损伤。与安慰剂相比，APZ和PIR没有差异。NAP和IND降低了胃窦中所有三种前列腺素的水平，而APZ和PIR无效。IND、NAP和PIR降低了胃底的PGE2水平；APZ没有影响。因此，黏膜损伤与对胃窦而非胃底前列腺素生成的影响有关。
