安莫西林配伍中医药联合治疗慢性炎症的药理作用及使用禁忌探析

安莫西林(Amoxicillin),又名安默西林,羟氨苄青霉素,是一种青霉素类广谱β-内酰胺类抗生素,杀菌作用强,穿透细胞壁的能力也强,是目前应用较为广泛的口服青霉素之一,其制剂有胶囊、片剂、颗粒剂、分散片等。临床上,安莫西林常与其他一些药物配合治疗,通过共同作用提高疗效,如应用六味安消胶囊与安莫西林配伍联合治疗幽门螺杆菌(Hp)感染,或运用安莫西林胶囊配伍宁胃和中汤加减治疗慢性浅表性胃炎均取得了较好的疗效。分析安莫西林的理化特性及药理作用,阐述安莫西林的临床应用表现及使用禁忌。

替莫西林的临床应用进展

替莫西林是第一个上市的对多种β-内酰胺酶稳定的青霉素类抗生素。它对大多数超广谱β-内酰胺酶和AmpC酶非常稳定,对大多数革兰阴性菌有较强的抗菌活性,但对革兰阳性菌活性低。近几年的研究证明替莫西林有望成为"碳青霉烯类抗生素"的替代者。

青霉素类抗生素替莫西林二钠的合成

目的:合成青霉素类抗生素替莫西林二钠。方法:以青霉素类抗生素替卡西林二钠为原料,经3步反应得到产物。结果:经过MS和1H-NMR分析,证明产物是替莫西林二钠,总收率达到56.46%。结论:本方法便于操作,收率较高,适合工业化生产。

四逆散合半夏泻心汤联合西药治疗反流性胃炎随机平行对照研究

[目的]观察四逆散合半夏泻心汤联合西药治疗反流性胃炎疗效。[方法]使用随机平行对照方法,将142例门诊患者按掷骰子法简单随机分为两组。对照组71例多潘立酮,10mg/次,3次/d;硫糖铝,1g/次,3次/d;阿莫西林,0.5g/次,3次/d。治疗组71例四逆散合半夏泻心汤(柴胡、枳实、半夏、黄岑、竹茹、香附、川楝子、延胡索各10g,白芍20g,党参、蒲公英各15g,石斛12g,干姜、黄连各5g,甘草10g;胃黏膜充血、水肿明显去党参,加连翘、三七粉冲服;黏膜糜烂、溃疡加代赭石、旋覆花;反酸、嘈杂加瓦楞子煅;便秘加大黄;腹胀加木香、厚朴),1剂/d,水煎200m L,早晚口服;西药治疗同对照组。连续治疗20d为1疗程。观测临床症状、胃镜、不良反应。治疗1疗程,判定疗效。[结果]治疗组痊愈40例,显效18例,有效11例,无效2例,总有效率95.83%。对照组痊愈28例,显效12例,有效21例,无效10例,总有效率85.92%。治疗组疗效优于对照组(P<0.05)。[结论]四逆散合半夏泻心汤联合西药治疗反流性胃炎疗效满意,无严重不良反应,值得推广。

Furazolidone,amoxicillin,bismuth and rabeprazole quadruple rescue therapy for the eradication of Helicobacter pylori

AIM： To compare the efficacy and side effect profiles of three furazolidone and amoxicillin-based quadruple rescue therapies for the eradication of Helicobacter pylori （H pylonS. METHODS： Patients who failed in the Hpylori eradication therapy for at least one course were randomly allocated into three groups. Group A received rebaprazole 10 mg＋ amoxicillin 1 g ＋ furazolidone 100 mg, and bismuth subcitrate 220 mg, twice daily for 1 wk; group B received the same regimen of group A but for 2 wk; and group C received the same regimen of group B, but furazolidone was replaced by furazolidone 100 mg three times daily. To record the side effect profiles at the end of the treatment, Hpylori eradication was assessed with 13C-urea breath test 4 wk after therapy. RESULTS： Sixty patients were enrolled including 28 males, and 20 patients in each group. The average age of the patients was 49.2 years, ranging from 18 to 84 years. H pylori eradication rates with per-protocol analysis were 82%, 89% and 90% in the three groups, respectively. Side effects were found in 11 patients, including mild dizziness, nausea, diarrhea and increased bowel movement. None of the 11 patients needed treatment for their side effects. CONCLUSION： One- or two-week furazolidone and amoxicillin-based quadruple rescue therapy with a low dose furazolidone （100 mg bid） for the eradication of Hpylori is effective. Extending the antibiotic course to 14 d could improve the eradication rates.

A new look at anti-Helicobacter pylori therapy

With the rising prevalence of antimicrobial resistance,the treatment success of standard triple therapy has recently declined to unacceptable levels (i.e.,80% or less) in most countries.Therefore,several treatment regimens have emerged to cure Helicobacter pylori (H.pylori) infection.Novel first-line anti-H.pylori therapies in 2011 include sequential therapy,concomitant quadruple therapy,hybrid (dual-concomitant) therapy and bismuth-containing quadruple therapy.After the failure of standard triple therapy,a bismuth-containing quadruple therapy comprising a proton pump inhibitor (PPI),bismuth,tetracycline and metronidazole can be employed as rescue treatment.Recently,triple therapy combining a PPI,levofloxacin and amoxicillin has been proposed as an alternative to the standard rescue therapy.This salvage regimen can achieve a higher eradication rate than bismuth-containing quadruple therapy in some regions and has less adverse effects.The best second-line therapy for patients who fail to eradicate H.pylori with first-line therapies containing clarithromycin,amoxicillin and metronidazole is unclear.However,a levofloxacin-based triple therapy is an accepted rescue treatment.Most guidelines suggest that patients requiring third-line therapy should be referred to a medical center and treated according to the antibiotic susceptibility test.Nonetheless,an empirical therapy (such as levofloxacin-based or furazolidone-based therapies) can be employed to terminate H.pylori infection if antimicrobial sensitivity data are unavailable.

Levofloxacin/amoxicillin-based schemes vs quadruple therapy for Helicobacter pylori eradication in second-line

Worldwide prevalence of Helicobacter pylori(H.pylori) infection is approximately 50%,with the highest being in developing countries.We compared cure rates and tolerability(SE) of second-line anti-H.pylori levofloxacin/amoxicillin(LA)-based triple regimens vs standard quadruple therapy(QT).An English language literature search was performed up to October 2010.A meta-analysis was performed including randomized clinical trials comparing 7-or 10-d LA with 7-d QT.In total,10 articles and four abstracts were identified.Overall eradication rate in LA was 76.5%(95% CI:64.4%-97.6%).When only 7-d regimens were included,cure rate was 70.6%(95% CI:40.2%-99.1%),whereas for 10-d combinations,cure rate was significantly higher(88.7%;95% CI:56.1%-109.9%;P < 0.05).Main eradication rate for QT was 67.4%(95% CI:49.7%-67.9%).The 7-d LA and QT showed comparable efficacy [odds ratio(OR):1.09;95% CI:0.63-1.87],whereas the 10-d LA regimen was significantly more effective than QT(OR:5.05;95% CI:2.74-9.31;P < 0.001;I 2 = 75%).No differences were reported in QT eradication rates among Asian and European studies,whereas LA regimens were more effective in European populations(78.3% vs 67.7%;P = 0.05).Incidence of SE was lower in LA therapy than QT(OR:0.39;95% CI:0.18-0.85;P = 0.02).A higher rate of side effects was reported in Asian patients who received QT.Our findings support the use of 10-d LA as a simple second-line treatment for H.pylori eradication with an excellent eradication rate and tolerability.The optimal second-line alternative scheme might differ among countries depending on quinolone resistance.

Sofalcone, a mucoprotective agent, increases the cure rate of Helicobacter pylori infection when combined with rabeprazole, amoxicillin and clarithromycin

AIM: The mucoprotective agents, sofalcone and polaprezinc have anti-Helicobacter pylori ( H pylori)activities. We determined the therapeutic effects of sofalcone and polaprezinc when combined with rabeprazole,amoxicillin and clarithromycin for Helicobacter pylori infection.METHODS: One hundred and sixty-five consecutive outpatients with peptic ulcer and H pylori infection were randomly assigned to one of the following three groups and medicated for 7 d. Group A: triple therapy with rabeprazole (10 mg twice daily), clarithromycin (200 mg twice daily) and amoxicillin (750 mg twice daily). Group B: sofalcone (100 mg thrice daily) plus the triple therapy.Group C: polaprezinc (150 mg twice daily) plus the triple therapy. Eradication was considered successful if 13C-urea breath test was negative at least 4 wk after cessation of eradication regimens or successive famotidine in the cases of active peptic ulcer.RESULTS: On intention-to-treat basis, H pyloricure wasachieved in 43 of 55 (78.2%) patients, 47 of 54 (87.0%)and 45 of 56 (80.4%) for the groups A, B and Crespectively. Using per protocol analysis, the eradication rates were 81.1% (43/53), 94.0% (47/50) and 84.9% (45/53) respectively. There was a significant difference in the cure rates between group A and B. Adverse events occurred in 10, 12 and 11 patients, from groups A, B and C respectively, but the events were generally mild.CONCLUSION: The addition of sofalcone, but not polaprezinc, significantly increased the cure rate of H pylori infection when combined with the rabeprazole-amoxicillinclarithromycin regimen.

Omeprazole-based triple therapy with low-versus high-dose of clarithromycin plus amoxicillin for H pylori eradication in Iranian population

AIM： To investigate the efficacy and tolerability of H pylori eradication in an omeprazole-based triple therapy with high and low dose of clarithromycin and amoxicillin. METHODS： One hundred and sixty H pylori positive patients were randomly assigned to two groups based on the following 2 wk investigation; （1） group A or low-dose regimen received omeprazole 20 mg b.i.d, clarithromycin 250 mg b.i.d and amoxicillin 500 mg b.i.d; and （2） group B or high-dose regimen received omeprazole 20 mg b.i.d, clarithromycin 500 mg b.i.d and amoxicillin 1000 mg b.i.d. During the study Hpylori status was assessed by histology and rapid urease test prior and by 13C-urea breath test 6 wk after the therapy. Standard questionnaires were administered to determine the compliance to treatment and possible adverse events of therapy. Data were subject to x^2 to compare the eradication rates in the two groups. The significant level of 95% （P ≤ 0.05） was considered statistically different. RESULTS： We found that the per-protocol eradication rate was 88% （68/77） in group A, and 89% （67/75） in group B. The intension-to-treat eradication rate was 85% （68/80） in group A and 83.75% （67180） in group B. Overall adverse events were 26% in group A and 31% in group B. The adverse events were generally mild in nature and tolerated well in both groups with a compliance of 98% in group A vs 96% in group B. CONCLUSION： The omeprazole-based low dose regimen of darithromycin and amoxicillin for two weeks in Hpylori eradication is as effective as high dose regimen in Iranian population.

Efficacy of omeprazole and amoxicillin with either clarithromycin or metronidazole on eradication of Helicobacter pylori in Chinese peptic ulcer patients

AIM: One-week triple therapy with proton pump inhibitors, clarithromycin and amoxicillin has recently been proposed as the first-line treatment for Helicobacter pylori (H pylori) infection; however, data regarding the effects of this regimen in China are scarce. The aim of this prospective and randomized study was to compare the efficacy of clarithromycin and metronidazole when they were combined with omeprazole and amoxicillin on eradication of H pylori and ulcer healing in Chinese peptic ulcer patients. METHODS: A total of 103 subjects with Hpylori-positive peptic ulcer were randomly divided into two groups, and accepted triple therapy with omeprazole 20 mg, amoxicillin 1 000 mg and either clarithromycin 500 mg (OAC group, n = 58) or metronidazole 400 mg (0AM group, n - 45). All drugs were given twice daily for 7 d. Patients with active peptic ulcer were treated with omeprazole 20 mg daily for 2-4 wk after anti-H pylori therapy. Six to eight weeks after omeprazole therapy, all patients underwent endoscopies and four biopsies (two from the antrum and two others from the corpus of stomach) were taken for rapid urease test and histological analysis (with modified Giemsa staining) to examine H pylori. Successful eradication was defined as negative results from both examination methods. RESULTS: One hundred patients completed the entire course of therapy and returned for follow-up. The eradication rate of H pylori for the per-protocol analysis was 89.3% (50/56) in OAC group and 84.1% (37/44) in 0AM group. Based on the intention-to-treat analysis, the eradication rate of H pylori was 86.2% (50/58) in OAC group and 82.2% (37/45) in 0AM group. There were no significant differences in eradication rates between the two groups on either analysis. The active ulcer-healing rate was 96.7% (29/30) in OAC group and 100% (21/21) in 0AM group (per-protocol analysis, P>0.05). Six patients in OAC group (10.3%) and five in OAM group (11.1%) reported adverse events (P>0.05). CONCLUSION: One-week triple therapy with omeprazole and amoxicillin in combination with either clarithromycin or metronidazole is effective for the eradication of H pylori. The therapeutic regimen comprising metronidazole with low cost, good compliance and mild adverse events may offer a good choice for the treatment of peptic ulcers associated with H pylori infection in China.

Efficacy of a therapeutic strategy for eradication of Helicobacter pylori infection

AIM: To determine the efficacy of our therapeutic strategy for Helicobacter pylori (H. pylori) eradication and to identify predictive factors for successful eradication. METHODS: From April 2006 to June 2010, we retrospectively assessed 2428 consecutive patients (1025 men, 1403 women; mean age 55 years, age range 18-92 years) with gastric histology positive for H. pylori infection referred to our unit for 13-C urea breath test(UBT), after first-line therapy with proton pump inhibitor (PPI) b.i.d. + amoxicillin 1 g b.i.d. + clarithromycin 500 mg b.i.d. for 7 d. Patients who were still positive to UBT were recommended a second-line therapy (PPI b.i.d. + amoxicillin 1 g b.i.d. + tinidazole 500 mg b.i.d. for 14 d). Third choice treatment was empirical with PPI b.i.d. + amoxicillin 1 g b.i.d. + levofloxacin 250 mg b.i.d. for 14 d. RESULTS: Out of 614 patients, still H. pylori-positive after first-line therapy, only 326 and 19 patients respectively rechecked their H. pylori status by UBT after the suggested second and third-line regimens. "Per protocol" eradication rates for first, second and thirdline therapy were 74.7% (95% CI: 72.7%-76.4%), 85.3% (95% CI: 81.1%-89.1%) and 89.5% (95% CI: 74.9%-103%) respectively. The overall percentage of patients with H. pylori eradicated after two treatments was 97.8% (95% CI: 97.1%-98.4%), vs 99.9% (95% CI: 99.8%-100%) after three treatments. The study found that eradication therapy was most effective in patients with ulcer disease (P < 0.05, P = 0.028), especially in those with duodenal ulcer. Smoking habits did not significantly affect the eradication rate. CONCLUSION: First-line therapy with amoxicillin and clarithromycin produces an H. pylori eradication rate comparable or superior to other studies and secondline treatment can still be triple therapy with amoxicillin and tinidazole.

Examination of the Stability of Amoxicillin in Compounded Suppositories and Ointments

We examined the stability of amoxicillin trihydrate from the preparation Augmentin in compounded forms of drugs such as vaginal suppositories and ointments. The quantity of the antibiotic in the preparations studied was determined directly after they had been made and after a lapse of 7 and 14 days. We also carried out comparative examinations of the stability of sodium amoxicillin （Tarommentin） and sodium ampicillin （Ampicillin） in ointments with an addition of a boric acid solution. The examinations confirmed the stability of amoxicillin trihydrate in suppositories and in anhydrous and hydrated ointments. The content of this antibiotic in ointmems with an addition of a boric acid solution decreases slightly. Comparative studies of the stability of sodium amoxicillin and sodium amoxicillin revealed a markedly lower stability of the two antibiotics in comparison to the stability of amoxicillin trihydrate.

Issuing the Antibiotics for Children with and without Prescription in Pharmacies in Republic of Macedonia

The use of medicines for infants and children is presenting one unique set of challenges, because children are the most vulnerable population in any society. In this study, we set out to present the characteristics and classification of antibiotics recommended for children according to WHO, EMA and EBM. Also, the aim of this study was to analyze the most prescribed pediatric antibiotics in 2013 in Republic of Macedonia compared with standard treatments. Presented data was collected according to the number of prescribed recipes of pediatric dosage forms covered by the Fund of Republic of Macedonia. The obtained results showed that the most prescribed pediatric antibiotic is amoxicillin with clavulanic acid （875mg ＋ 125mg） in form of tablet, with 280 863 prescribed recipes which corresponds to the recommendations of EBM.

Corrosion inhibition and mechanism of mild steel in hydrochloric acid by ceftriaxone and amoxicillin

Corrosion inhibition of mild steel in 1 mol/L HC1 by amoxicillin and ceftriaxone in the concentration range of 1.00×10^-5-1.00×10^-2 mol/L has been studied using weight loss, electrochemical potentiodynamic polarization, electrochemical impedance spectroscopy （EIS）, scanning electron microscopy （SEM） and quantum chemistry tests at 298 K. The weight loss experiment showed that the inhibition efficiency increased with amoxicillin and ceftriaxone concentrations to attain the maximums of 80.3% and 94.1%, respectively at 1.00×10^-2 mol/L. Potentiodynamic polarization indicated that amoxicillin and ceftriaxone acted as mixed-type inhibitors but mainly inhibited cathode hydrogen evolution reaction for mild steel in 1 mol/L HC1. The electrochemical impedance spectroscopy （EIS） demonstrated the inhibitors covered the active points of metal surface to inhibit corrosion. The absorption of both inhibitors on the mild steel surface was found to follow Langmuir adsorption isothermal and dominantly involve chemical adsorption at 298 K. Scanning electron microscopy （SEM） confirmed both of the inhibitors played a significant protective effect in mild steel corrosion in 1 mol/L HC1. The relationship between the inhibition properties and molecular structure had been discussed by quantum chemistry calculation. All the experimental results concluded that both amoxicillin and ceftriaxone acted as good corrosion inhibitors and their inhibition efficiency was in the order of ceftriaxone 〉 amoxicillin.