Efficacy of the H2-receptor antagonist famotidine on chronic spontaneous urticaria in children

Urticaria is a common pediatric skin disorder. Histamine H1-receptor antagonists are effective in chronic as well as acute urticaria. When H1-anti-histamines are ineffective, add-on use of H2-receptor antagonists is thought to give better symptom relief. However, there are few reports on the therapeutic efficacy in pediatric patients. We retrospectively reviewed the medical records of pediatric patients with chronic spontaneous urticaria (csU) who met the following criteria. They were consulted our outpatient clinic between April 2010 and March 2012;were unsuccessfully treated with H1 antihistamines;and were treated with add-on H2-receptor antagonist (famotidine). In six patients who met the inclusion criteria (mean age 6.1 ± 5.1 years), urticaria activity score was significantly decreased from 4.3 ± 0.8 just before administration of famotidine to 1.3 ± 1.0 on the first outpatient visit within 4 weeks after the first administration of famotidine

Head-to-head comparison of H_2-receptor antagonists and proton pump inhibitors in the treatment of erosive esophagitis: A meta-analysis

AIM: To systematically evaluate the efficacy of H2-receptor antagonists (H2RAs) and proton pump inhibitors in healing erosive esophagitis (EE).METHODS: A meta-analysis was performed. A literature search was conducted in PubMed, Medline, Embase, and Cochrane databases to include randomized controlled head-to-head comparative trials evaluating the efficacy of H2RAs or proton pump inhibitors in healing EE. Relative risk (RR) and 95% confidence interval (CI) were calculated under a random-effects model.RESULTS: RRs of cumulative healing rates for each comparison at 8 wk were: high dose vs standard dose H2RAs,1.17 (95%CI, 1.02-1.33); standard dose proton pump inhibitors vsstandard dose H2RAs, 1.59 (95%CI, 1.44-1.75);standard dose other proton pump inhibitors vs standard dose omeprazole, 1.06 (95%CI, 0.98-1.06). Proton pump inhibitors produced consistently greater healing rates than H2RAs of all doses across all grades of esophagitis, including patients refractory to H2RAs. Healing rates achieved with standard dose omeprazole were similar to those with other proton pump inhibitors in all grades of esophagitis.CONCLUSION: H2RAS are less effective for treating patients with erosive esophagitis, especially in those with severe forms of esophagitis. Standard dose proton pump inhibitors are significantly more effective than H2RAs in healing esophagitis of all grades. Proton pump inhibitors given at the recommended dose are equally effective for healing esophagitis.

Comparison of PPIs and H_2-receptor antagonists plus prokinetics for dysmotility-like dyspepsia

AIM： To compare efficacy of proton pump inhibitors （PPIs） with H2-receptor antagonists （H2RA$） plus pro- kinetics （Proks） for dysmotility-like symptoms in func- tional dyspepsia （FD）. METHODS： Subjects were randomized to receive openlabel treatment with either rabeprazole 10 mg od （n = 57） or famotidine 10 mg bid plus mosapride 5 mg tid （n = 57） for 4 wk. The primary efficacy endpoint was change （%） from baseline in total dysmotility-like dyspepsia symptom score. The secondary efficacy endpoint was patient satisfaction with treatment. RESULTS： The improvement in dysmotility-like dyspep- sia symptom score on day 28 was significantly greater in the rabeprazole group （22.5% ± 29.2% of baseline） than the famotidine ＋ mosapride group （53.2%±58.6% of baseline, P 〈 0.0001）. The superior benefit of rabeprazole treatment after 28 d was consistent regardless of Helicobacter pylori status. Significantly more subjects in the rabeprazole group were satisfied or very satisfied with treatment on day 28 than in the famotidine ＋ mosapride group （87.7% vs 59.6%, P = 0.0012）. Rabeprazole therapy was the only significant predictor of treatment response （P 〈 0.0001）, defined as a total symptom score improvement ≥ 50%. CONCLUSION： PPI monotherapy improves dysmotil- ity-like symptoms significantly better than H2RAs plus Proks, and should be the treatment of first choice for Japanese FD.

Proton pump inhibitors therapy vs H_2 receptor antagonists therapy for upper gastrointestinal bleeding after endoscopy: A meta-analysis

AIM: To compare the therapeutic effects of proton pump inhibitors vs H2 receptor antagonists for upper gastrointestinal bleeding in patients after successful endoscopy.METHODS: We searched the Cochrane library, MEDLINE, EMBASE and Pub Med for randomized controlled trials until July 2014 for this study. The risk of bias was evaluated by the Cochrane Collaboration's tool and all of the studies had acceptable quality. The main outcomes included mortality, re-bleeding, received surgery rate, blood transfusion units and hospital stay time. These outcomes were estimated using odds ratios(OR) and mean difference with 95% confidence interval(CI). Rev Man 5.3.3 software and Stata 12.0 software were used for data analyses. RESULTS: Ten randomized controlled trials involving 1283 patients were included in this review; 678 subjects were in the proton pump inhibitors(PPI) group and the remaining 605 subjects were in the H2 receptor antagonists(H2RA) group. The meta-analysis results revealed that after successful endoscopic therapy, compared with H2 RA, PPI therapy had statistically significantly decreased the recurrent bleeding rate(OR = 0.36; 95%CI: 0.25-0.51) and receiving surgery rate(OR = 0.29; 95%CI: 0.09-0.96). There were no statistically significant differences in mortality(OR = 0.46; 95%CI: 0.17-1.23). However, significant heterogeneity was present in both the numbers of patients requiring blood transfusion after treatment [weighted mean difference(WMD),-0.70 unit; 95%CI:-1.64- 0.25] and the time that patients remained hospitalized [WMD,-0.77 d; 95%CI:-1.87- 0.34]. The Begg's test(P = 0.283) and Egger's test(P = 0.339) demonstrated that there was no publication bias in our meta-analysis.CONCLUSION: In patients with upper gastrointestinal bleeding after successful endoscopic therapy, compared with H2 RA, PPI may be a more effective therapy.

Stronger inhibition of gastric acid secretion by lafutidine, a novel H_2 receptor antagonist, than by the proton pump inhibitor lansoprazole

AIM: To compare the antisecretory activity and plasma drug concentrations of a single oral dose of 10 mg lafutidine, a novel H2 receptor antagonist, with those of the proton pump inhibitor lansoprazole (LPZ) 30 mg. METHODS: Ten volunteers without H pylori infection participated in this crossover study comparing lafutidine 10 mg with LPZ 30 mg. Intragastric pH was monitored for 6 h in all participants, and blood samples were collected from four randomly selected individuals after single-dose administration of each drug. RESULTS: The median intragastric pH was significantly higher in individuals who received lafutidine 10 mg than in those who received LPZ 30 mg 2, 3, 4, 5, and 6 h after administration. Maximal plasma drug concentration was reached more promptly with lafutidine 10 mg than with LPZ 30 mg. CONCLUSION: In H pylori-negative individuals, gastric acid secretion is more markedly inhibited by lafutidinethan by LPZ.

睡前加服H_2-受体拮抗剂抑制夜间酸突破的系统评价

目的继2004年系统评价之后,对睡前加服H2-受体拮抗剂抑制夜间酸突破的疗效和安全性进行再评价。方法计算机检索Cochrane图书馆临床对照试验资料库、MEDLINE、EMbase、中国生物医学文献数据库,手工检索8种相关中文期刊和所获文献的参考文献,全面收集全世界关于睡前加服H2-受体拮抗剂抑制夜间酸突破的临床随机对照试验,并按照Cochrane协作网的方法进行系统评价。结果仅有2篇随机对照交叉试验包括32例受试者符合纳入标准,由于这2个研究在设计及药物的剂量和疗程存在较大差别,无法进行Meta分析,仅进行定性的系统评价。这2个研究对睡前加服H2-受体拮抗剂抑制夜间酸突破的疗效没有一致性的结论。结论基于目前的证据尚不能确定睡前加服H2-受体拮抗剂能有效抑制夜间酸突破的发生,还需要大样本、高质量,且随访时间足够的随机对照试验来提供证据。

质子泵抑制剂联合H_2受体拮抗剂治疗门脉高压性胃病

目的探讨质子泵抑制剂(PPI)联合H2受体拮抗剂(H2RA)在治疗门脉高压性胃病(PHG)中的作用。方法将46例肝硬化门脉高压性胃病患者随机分为治疗组和对照组,每组均给予奥美拉唑40mg静脉滴注1次/日×7日,心得安10mg口服3次/日。治疗组每晚加服雷尼替丁150mg。观察治疗后1周临床症状缓解率、1月后胃镜下胃黏膜改变、3月后患者再入院率。结果治疗组和对照组1周临床症状缓解率分别为73.91%和39.13%(P<0.05)。与对照组比较,治疗组1月后胃镜下胃黏膜充血、水肿减轻(P<0.05)。3月后治疗组再入院2例,对照组5例。结论联合治疗对PHG胃黏膜的改善有较好的治疗作用。

腹腔镜胃十二肠溃疡穿孔修补辅助H_2受体拮抗剂治疗急性胃十二指肠溃疡穿孔

目的:总结腹腔镜下胃十二指肠溃疡穿孔修补术的临床经验。方法:回顾分析采用腹腔镜行胃十二指肠溃疡穿孔修补术的33例临床资料。结果:除1例十二指肠溃疡穿孔时间较长中转手术外,29例十二指肠球部穿孔和3例胃穿孔患者腹腔镜手术均获得成功,无并发症发生;术后辅助H2受体拮抗剂治疗,胃镜复查无复发。结论:腹腔镜修补并H2受体阻断剂口服治疗胃十二指肠溃疡急性穿孔的效果是肯定的,值得临床应用推广。

急性脑血管病院内感染危险因素及H2受体阻滞剂应用相关性分析

目的探讨急性脑血管病患者住院期间使用H2受体阻滞剂预防应激性溃疡与医院感染的关系。方法对612例脑血管病患者进行院内感染易感因素分析。单因素分析院内感染的危险因素,并根据患者48h Glassgow评分分层分析使用H2受体阻滞剂与医院感染的关系。结果612例脑血管病患者住院期间感染发生率为34.48%,其中患者卒中类型、吞咽困难、H2受体阻滞剂使用、昏迷程度及侵入性操作是发生院内感染的主要危险因素。患者入院后48h Glassgow评分9-15时,使用H2受体阻滞剂预防应激性溃疡能显著增加患者院内感染的发生率（P〈0.001）;入院后48h Glassgow评分≤8分时,使用H2受体阻滞剂对患者发生感染无明显影响。结论急性脑血管病患者使用H2受体阻滞剂预防应激性溃疡与院内感染有密切相关。

组胺H_2受体激动剂和拮抗剂及抗癌药对正常人造血祖细胞和HL－60白血病细胞生长的作用

采用体外微量克隆培养体系研究了组胺Ｈ＿２受体激动剂４－甲基组胺（４－ＭＨ）和拮抗剂雷尼替叮（ｒａｎｉｔｉｄｉｎｅ）及抗癌药阿糖胞苷分别对正常人外周血粒－巨噬系祖细胞（ＰＢＣＦＵ－ＧＭ）和ＨＬ－６０白血病细胞生长的作用。当４－ＭＨ的浓度为１０￣（－９）～１０￣（－６）ｍｏｌ·Ｌ￣（－１）时，可促进ＰＢＣＦＵ－ＧＭ的增殖，４－ＭＨ的浓度增加至１０￣（－１）ｍｏｌ·Ｌ￣（－１）时则表现为抑制ＰＢＣＦＵ－ＧＭ的增殖。Ｒａｎｉｔｉｄｉｎｅ的浓度为１０￣（－９）～１０￣（－５）ｍｏｌ·Ｌ￣（－１）时，表现出对ＰＢＣＦＵ－ＧＭ增殖的抑制作用，但在１０－６ｍｏｌ·Ｌ￣（－１）剂量时对ＰＢＣＦＵ～ＧＭ的抑制率低于５０％，而在该剂量时对ＨＬ－６０白血病细胞的抑制率已达１００％，具有一定的选择性。抗癌药阿糖胞苷（Ａｒａ－Ｃ）对ＨＬ－６０白血病细胞的抑制作用比对ＰＢＣＦＵ－ＧＭ的抑制作用较强，但两者的ＩＣ＿（５０）值处于同一个数量级。在强化化疗剂量１０￣（－５）ｍｏｌ·Ｌ￣（－１）时，Ａｒａ－Ｃ对ＨＬ－６０白血病细胞和ＰＢＣＦＵ－ＧＭ正常造血祖细胞的抑制率均达１００％。

泮托拉唑与H_2受体阻滞剂治疗消化道出血患者的对比分析

目的泮托拉唑与H2受体阻断药物用于临床,以评价其治疗消化道出血的疗效。方法分析比较泮托拉唑与H2受体阻滞剂给药后治疗情况。结果表明泮托拉唑治疗上消化道出血有效率达96%,止血迅速,且无不良反应,故96%的出血患者无须外科手术治疗,减少了患者的手术痛苦具有一定的临床意义。结论泮托拉唑(Pantoprazole)应用于治疗消化性溃疡以来取得显著效果,是有希望取代H2受体拮抗剂的药物。

药物透过血脑屏障的3D-QSPR:H_2受体拮抗剂的CoMFA和EVA分析

目的：药物透过血脑屏障是药代动力学的重要过程，Ｈ２受体拮抗剂是作用于神经外周的抗溃疡药物，为避免该类药物透过血脑屏障损伤中枢神经，产生毒副作用，指导该类药物的设计与合成。方法和结果：选择了不依赖于实验参数的比较分子力场分析（ＣｏＭＦＡ）方法和最近发展的本征值（ＥＶＡ）方法，建立了有关的三维药代动力学性质（３ＤＱＳＰＲ）模型。ＣｏＭＦＡ模型的统计参数为：交叉验证系数ｒ２ｃｖ＝０６２５，相关系数ｒ２＝０８９３，Ｆ３，１７＝４７２７０，标准偏差ＳＥ＝０２５４；ＥＶＡ模型的统计参数为：交叉验证系数ｒ２ｃｖ＝０６９７，相关系数ｒ２＝０９２２，Ｆ３，１７＝６７７６６，标准偏差ＳＥ＝０２０３。结论：两种方法都能建立三维定量构效模型，ＥＶＡ模型有更高的预测能力。

长效H_2受体拮抗剂—拉呋替丁的合成

以2-溴-4-(哌啶基甲基)吡啶为原料,与2-丁烯-1,4-二醇醚化,经氯化、G abrie l反应、肼解,然后再与2-呋喃甲硫基-S-氧代乙酸对硝基苯酚酯进行胺解反应,制得第二代长效H2受体拮抗剂拉呋替丁,总收率为29.89%[以2-溴-4-(哌啶基甲基)吡啶计]。

H_2受体及其拮抗剂与大肠癌关系研究

近年来,随着消化道肿瘤内分泌治疗相关理念的提出,H2受体及其拮抗剂与大肠癌的关系逐渐引起了学者们的重视。由于H2受体具有独特的生物学特性,H2受体拮抗剂在大肠癌治疗中可能存在潜在的应用价值。现就H2受体生物学特性与其拮抗剂,以及H2受体拮抗剂与大肠癌关系的研究进展予以综述。

应用H_2-受体拮抗剂及胃动力药治疗胃性哮喘的护理

目的 :研究胃性哮喘的护理。方法 :观察胃性哮喘 2 5例应用H2 -受体拮抗剂及胃动力药后的反应并采取积极有效的护理措施。结果 :2 5例哮喘症状均得到了明显的缓解与改善。结论 :对哮喘患者应严密观察病情变化 ,在应用糖皮质激素及支气管扩张药无效时 。

A Prospective, Multicentric, Post Marketing Surveillance to Evaluate Efficacy & Safety of Ranitidine HCl (150 & 300 mg IR/CR) in Indian Patients with Gastroesophageal Reflux Disease (PROGRADE)

Purpose: Ranitidine hydrochloride (HCl) remains an important medication for treating acid-peptic ailments such as Gastroesophageal reflux disease (GERD). The main objective of this Post Marketing Surveillance (PMS) clinical study was to test the efficacy and safety of Ranitidine HCl in Indian patients suffering from GERD. Patients and Methods: Data of 2446 patients (1307 males;1121 females) from 21 centers across India were analyzed. Patients received either of the three treatments: Ranitidine HCl 150 mg twice a day (BID) (ARM-A), Ranitidine HCl 300 mg once daily (OD) or BID (ARM-B), and Ranitidine HCl 300 mg OD (ARM-C). Gastroesophageal Reflux Disease Symptom Assessment Scale (GSAS) score and Heartburn Severity score were used to assess the drug’s efficacy. The adverse events reported by patients or investigators were analyzed to assess the safety profile of Ranitidine. Results: Of the 2446 subjects screened, 2428 were enrolled. There was a significant reduction in GSAS scores from baseline to the end of the study visit in all three ARMs. The GSAS scores reduced from 2.02 to 0.23 in ARM-A, 2.01 to 0.24 in ARM-B, and 2.07 to 0.26 in ARM-C patients. In ARM A, 72.82% had 24 hours heartburn-free days, and 66.89% had 7 consecutive heartburn-free days, which was more significant than the other two ARMs. 128 (5.27%) patients reported ADRs due to Ranitidine HCl at different doses. The most frequently reported ADR was constipation (17.18%), followed by oliguria (14.06%), cold (13.28%), and dysuria (12.5%). Of 128 ADRs, 113 (88.28%) were mild, and only 11 (8.59%) ADRs were related to the study drug. No severe ADRs were reported during the study. Conclusion: Ranitidine HCl 150/300 mg tablet was found to be an effective and safe H2-receptor antagonist for treating GERD in Indian Patients.

H2-受体拮抗剂的流动注射-化学发光分析方法的研究

碱性介质中K3Fe（CN）6与H2-受体拮抗剂发生氧化-还原反应产生化学发光,罗丹明6G可显著增强其发光信号,且强度与药物浓度呈良好的线性关系。据此,建立了采用K3Fe（CN）6-罗丹明6G体系测定制剂中H2-受体拮抗剂的流动注射-化学发光分析方法。在优化的实验条件下,西咪替丁在1.0×10^-9-7.0×10^-5g/mL范围内呈良好的线性关系,检出限为8.6×10^-10g/mL;盐酸雷尼替丁在1.0×10^-9-5.0×10^-5g/mL范围内呈线性关系,检出限为8.7×10^-10g/mL;法莫替丁在5.0×10^-9-7.0×10^-5g/mL范围内呈线性关系,检出限为2.4×10^-9g/mL。通过对浓度为1.0×10^-6g/mL的3种H2-受体拮抗剂分别进行的11次平行测定,其RSD分别为4.0%,3.8%和2.9%。

质子泵抑制剂和H_2受体拮抗剂预防低剂量阿司匹林引起上消化道损伤的Meta分析

目的比较质子泵抑制剂和H_2受体拮抗剂对口服低剂量阿司匹林患者上消化道损伤的预防作用。方法系统检索Pub Med、The Cochrane Library、Embase、中国知网(CNKI)及万方数据库,检索时间至2016年10月31日。同时查阅相关文献的引文目录,纳入符合入选标准的临床研究。结果最终纳入随机对照试验15篇。总样本量为2 093例,其中质子泵抑制剂组1 116例,H_2受体拮抗剂组977例。总体结果显示,与H_2受体拮抗剂相比,质子泵抑制剂能够减少低剂量阿司匹林引起的上消化道出血事件(RR 0.33,95%CI 0.20~0.54,P<0.01)。质子泵抑制剂比H_2受体拮抗剂更能降低口服低剂量阿司匹林患者的上消化道糜烂或溃疡的风险(RR0.35,95%CI 0.24~0.52,P<0.01)。结论相比H_2受体拮抗剂,质子泵抑制剂能更有效地预防低剂量阿司匹林导致的上消化道损伤。

壁细胞对H_2受体拮抗剂和质子泵抑制剂耐受性研究

目的研究鼠胃黏膜壁细胞对H2受体拮抗剂和质子泵抑制剂的耐受性(脱敏)。方法用酶消化法分离壁细胞后,分为西咪替丁、法莫替丁、奥美拉唑和潘托拉唑4组,每组均包括三部分实验。其一是给予药物100mg/L干预细胞不同时间;其二是给予药物100mg/L干预细胞不同时间,然后洗涤细胞,再给予100mg/L作用1h;其三是给予不同浓度药物干预细胞2h后,洗涤细胞,再加入100mg/L作用2h。最后测定各组壁细胞H+K+ATP酶活力。结果H2受体拮抗剂和质子泵抑制剂均对H+K+ATP酶具有抑制作用;在不同干预时间下,西咪替丁1、2h组酶活性均显著高于对照组(4.96±0.247,4.63±0.054vs4.18±0.324),法莫替丁、2、4h组酶活性均显著高于对照组(3.71±0.017,5.11±0.053,4.01±0.029vs0.63±0.019);在不同干预浓度下,西咪替丁、法莫替丁0、100、1000mg/L组酶活性均显著高于对照组(分别为4.56±0.159,4.62±0.275,4.05±0.026vs3.69±0.145和3.42±0.391,4.32±0.315,4.48±0.120vs1.92±0.144);质子泵抑制剂各组无显著性差别。结论H2受体拮抗剂能够诱导壁细胞H2受体出现脱敏,质子泵抑制剂未出现耐受现象。

Antagonistic Potential against Pathogenic Microorganisms and Hydrogen Peroxide Production of Indigenous Lactobacilli Isolated from Vagina of Chinese Pregnant Women

Objective To investigate the indigenous lactobacilli from the vagina of pregnant women and to screen the isolates with antagonistic potential against pathogenic microorganisms. Methods The strains were isolated from pregnant women＇s vagina and identified using the API50CH system. The ability of the isolates to produce hydrogen peroxide was analyzed semi-quantitatively using the TMB-HRP-MRS agar. The antagonistic effects of the isolates on pathogenic microorganisms were determined with a double layer agar plate. Results One hundred and three lactobacilli strains were isolated from 60 samples of vaginal secretion from healthy pregnant women. Among them, 78 strains could produce hydrogen peroxide, in which 68%, 80%, 80%, and 88% had antagonistic effects against Candida albicans CMCC98001, Staphylococcus aureus CMCC26003, Escherichia coli CMCC44113, and Pseudomonas aeruginosa CMCC10110, respectively. Conclusion The recovery of hydrogen peroxide-producing lactobacilli decreases with the increasing pregnant age and time. The most commonly isolated species from vagina of Chinese pregnant women are Lactobacillus acidophilus and Lactobacillus crispatus. Most of L. acidophilus and L. crispatus produce a high H2O2 level.