组胺受体在枳实调节小鼠小肠运动中的作用

目的：探讨枳实调节胃肠功能的作用机制,方法：采用活性碳末指示法,以小鼠在灌服不同药物一定时间后小肠碳末推进率为指标分析小肠的运动功能。结果：灌服枳实煎液可明显提高小鼠小肠碳末推进率,此效应可被H1受体拮抗剂苯海拉明阻断而不能被H2受体拮抗剂西米替丁阻断。结论：枳实增强小肠运动功能的作用与H1受体有关。     

新生儿应激性溃疡出血38例临床分析

目的 :探讨新生儿应激性溃疡出血病儿的防治措施。方法 :综合治疗原发病 ,纠正缺氧、酸中毒、抗感染等 ,静滴止血敏、甲氰咪胍止血 ,效果欠佳者加用云南白药鼻饲。结果 :治疗 3 8例 ,治愈率 86.84% ,病死率 10 .5 4% ,死因为多脏器功能衰竭和DIC。结论 :止血敏、甲氰咪胍合用止血效果好 ,加用云南白药可用于防治应激性溃疡出血。     

H1 and H2 receptor antagonists and hepatic oxygen supply-demand relationship in pigs

The hypothesis that histamine receptor (H1 and H2) blockade beneficially affects the hepatic oxygen supply-demand relationship was tested during experiments performed on 13 miniature pigs. Hepatic arterial and portal blood flows were measured with electromagnetic flowmeters. Cardiac output was determined by thermodilution. H1 and H2 receptor blockade was achieved with promethazine, 5 mg.kg-1 and cimetidine 30 mg.kg-1 IV, respectively. The study demonstrated no significant effect of H1 and H2 receptor blockade on hepatic oxygen uptake and no noticeable effects of cimetidine on hepatic circulation. However, promethazine decreased total hepatic blood flow, primarily by decreasing portal blood flow; this resulted in an increase in oxygen extraction as reflected in a decreased oxygen content in hepatic venous blood. The results reject the posed hypothesis: H1 receptor antagonist promethazine decreased, while H2 receptor antagonist cimetidine did not affect hepatic blood flow and oxygen supply; hepatic oxygen demand remained unaffected during H1 and H2 receptor blockade.     

奥美拉唑和西咪替丁治疗危重病儿应激性溃疡出血的随机对照试验

目的 :探讨奥美拉唑治疗危重病儿应激性溃疡出血的临床疗效。方法 :将 82例应激性溃疡出血的危重病儿随机分为奥美拉唑治疗组 4 7例 [男性2 5例 ,女性 2 2例 ,年龄 (6±s 3)a]和对照组 35例[男性 19例 ,女性 16例 ,年龄 (5 .9± 2 .8)a]。 2组均给予病因、对症及支持治疗 ,同时治疗组给予奥美拉唑 0 .6～ 0 .8mg·kg- 1,每日 1次口服或经胃管注入 ,连用 3～ 5d。对照组给予西咪替丁每日 10～ 2 0mg·kg- 1,静脉输注 ,连用 3～ 5d。观察应激性溃疡出血临床好转情况 ,同时观察不良反应的发生情况。结果 :奥美拉唑治疗组 ,显效 4 2 % ,有效 4 7% ,无效11% ,总有效 89% ;对照组 ,显效 14% ,有效4 6% ,无效 4 0 % ,总有效 60 % ,2组相比差异有非常显著的意义 (P <0 .0 1)。结论 :奥美拉唑治疗危重病儿应激性溃疡出血疗效显著 ,且不良反应少     

Effect of Cimetidine on Histamine- and Pentagastrin-stimulated Gastric Secretion in Healthy Subjects

Cimetidine-induced inhibition of gastric acid and pepsin secretion in response to histamine and pentagastrin stimulation was studied in four healthy young subjects. Different doses of histamine and pentagastrin were administered alone and in combination with cimetidine on separate days; the order of administration was randomized. As the dose of histamine increased, the inhibitory effect of 0.6 mg · kg^?1 h^?1 of cimetidine on acid output decreased. With supramaximal histamine stimulation the inhibition was completely overcome. These results are consistent with competitive inhibition of histamine-stimulated acid output by cimetidine in man. After pentagastrin stimulation the inhibition of acid output by cimetidine could not be overcome by increasing the dose of the stimulant, suggesting a noncompetitive inhibition of pentagastrin-evoked acid output. It is concluded that the kinetics of cimetidine-induced inhibition of histamine- and pentastrin-stimulated gastric acid output are different. At approximately half maximal stimulation of acid secretion, cimetidine was a more potent inhibitor of histamine than of pentagastrin. Pepsin output in response to both histamine and pentagastrin stimulation was also inhibited by cimetidine.     

Elevated gastric acid secretion in patients with Barrett's metaplastic epithelium

Gastric acid secretion in response to a protein meal and to exogenously administered synthetic human gastrin 17-I was measured in patients with Barrett's esophagus, patients with uncomplicated gastroesophageal reflux, and normal age- and sex-matched controls. Acid secretion, both basally and in response to gastrin 17-I, was significantly greater in patients with Barrett's esophagus compared to normal individuals without reflux. Basal gastrin levels and meal-stimulated levels of the hormone were similar among all three groups. Sensitivity to gastrin, expressed as the concentration causing half-maximal acid secretion, was also similar among the study groups. It is speculated that elevated basal acid production in Barrett's esophagus may contribute to the pathogenesis of the disorder.Study supported by Smith, Kline, and French, Inc.     

阿苯达唑脂质体治疗肝、腹部细粒棘球蚴病的动物实验研究

应用阿苯达唑脂质体（ＬｉｐｏｓｏｍａｌＡｌｂｅｎｄａｚｏｌｅ，Ｌ－ＡＢＺ）联合西咪替丁（Ｃｉｍｅｔｉｄｉｎｅ，ＣＭＤ）治疗继发性感染细粒棘球蚴（Ｅｃｈｉｎｏｃｏｃｃｕｓｇｒａｎｕｌｏｓｕｓ，Ｅ．ｇ．），并比较单纯或联合用药的优劣。经囊减重率、药物浓度监测、病理及超微结构指标观察，结果表明：（１）阿苯达唑脂质体治疗包虫病的效果优于单纯阿苯达唑，尤其联合西米替丁效果更佳（囊减重率９５．７４％）；（２）脂质体包封阿苯达唑具有靶器官作用，可提高肝药浓度（１．５～２倍），使囊组织及囊液有较高浓度有效成分直接发挥抗包虫的作用；（３）西咪替丁可改变阿苯达唑代谢过程，提高药物浓度在小鼠体内分布，具有明显的抗包虫协同作用     

Increased apoptosis in osteoclasts and decreased RANKL immunoexpression in periodontium of cimetidine‐treated rats

It has been demonstrated that histamine interferes with the recruitment, formation and activity of osteoclasts via H₁‐ and H₂‐receptors. Cimetidine is a H₂‐receptor antagonist used for treatment of gastric ulcers that seems to prevent bone resorption. In this study, a possible cimetidine interference was investigated in the number of alveolar bone osteoclasts. The incidence of osteoclast apoptosis and immunoexpression of RANKL (receptor activator of nuclear factor κB ligand) was also evaluated. Adult male rats were treated with 100 mg kg^?1 of cimetidine for 50 days (CimG); the sham group (SG) received saline. Maxillary fragments containing the first molars and alveolar bone were fixed, decalcified and embedded in paraffin. The sections were stained by H&E or submitted to tartrate‐resistant acid phosphatase (TRAP) method. TUNEL (terminal deoxynucleotidyl transferase‐mediated dUTP nick‐end labeling) method and immunohistochemical reactions for detecting caspase‐3 and RANKL were performed. The number of TRAP‐positive osteoclasts, the frequency of apoptotic osteoclasts and the numerical density of RANKL‐positive cells were obtained. Osteoclast death by apoptosis was confirmed by transmission electron microscopy (TEM). In CimG, TRAP‐positive osteoclasts with TUNEL‐positive nuclei and caspase‐3‐immunolabeled osteoclasts were found. A significant reduction in the number of TRAP‐positive osteoclasts and a high frequency of apoptotic osteoclasts were observed in CimG. Under TEM, detached osteoclasts from the bone surface showed typical features of apoptosis. Moreover, a significant reduction in the numerical density of RANKL‐positive cells was observed in CimG. The significant reduction in the number of osteoclasts may be due to cimetidine‐induced osteoclast apoptosis. However, RANKL immunoexpression reduction also suggests a possible interference of cimetidine treatment in the osteoclastogenesis.     

Combination therapy of ecabet sodium and cimetidine compared with cimetidine alone for gastric ulcer: prospective randomized multicenter study

BACKGROUND AND AIM: Little is known about the clinical efficacy of co-therapy of ecabet sodium, a mucoprotective agent, and a histamine H2-receptor antagonist. The aim of the present study was to assess its additive benefit in combination with cimetidine for gastric ulcer. METHODS: In this prospective randomized study, after gastric ulcer was confirmed by endoscopy, 200 patients in 47 hospitals received either ecabet sodium 1 g b.i.d and cimetidine 400 mg b.i.d. (EC), or cimetidine 400 mg b.i.d. alone (C) for 8 weeks. Healing was examined by endoscopy at 4 and 8 weeks. RESULTS: Of the intention-to-treat (ITT) population (EC, 103; C, 97), 181 patients comprised the per protocol (PP) analysis (EC, 93; C, 88). At 4 weeks, healing rates were significantly higher in the EC group (60%) than in the C group (36%) ( p < 0.01). At 8 weeks, those by the ITT and PP analyses were 82% (EC) versus 58% (C), and 90% (EC) versus 64% (C), respectively ( p < 0.01 and p < 0.001). Symptom relief rates (EC vs C) at 2, 4 and 8 weeks were 73%versus 47% ( p < 0.01), 89%versus 66% ( p < 0.001), and 97%versus 73% ( p < 0.001), respectively. Significant additive effects of ecabet sodium were observed in patients aged 60 years or older, with solitary and medium to large ulcer, and without smoking or drinking habits. No adverse effects were critical. CONCLUSION: Ecabet sodium significantly augmented gastric ulcer healing and symptom relief by cimetidine, especially in the elderly.     

国产法莫替丁治疗上消化道出血效果观察

对156名上消化道出血病人,根据性别、年龄及出血量随机分成法莫替丁试验组(20mg,静注,每日两次)和西米替丁对照组(400mg,静注,每日两次)。用药后三天内的显效率法莫替丁为65.4％,西米替丁为26.9％;用药后五天内总有效率分别为97.4％及84.6％,无论三天内的显效率还是五天内的总有效率法莫替丁组均高于西米替丁组。