The Effect of Azithromycin in Treating Mycoplasma Pneumonia in Children

Objective:To discuss and analyze the effect of azithromycin in the treatment of mycoplasma pneumonia in children.Methods:A total of 120 children with mycoplasma pneumonia who were admitted to the Department of Pediatrics of our hospital from January 2022 to December 2022 were selected as the research subjects.They were divided into an azithromycin group and a reference group according to the random number drawing method,with 60 cases in each group.The azithromycin group was treated with azithromycin,and the reference group was treated with conventional treatment.The efficacy of treatment,laboratory indicators,platelet count and D-dimer,and adverse reactions of both groups were compared.Results:The efficacy of the azithromycin group was significantly higher than that of the reference group(P<0.05).Before treatment,there were no significant differences in the laboratory indicators like ferritin,procalcitonin(PCT),and erythrocyte sedimentation rate(ESR)between the two groups(P>0.05);after treatment,the laboratory indicators of the azithromycin group were significantly better than those of the reference group(P<0.05).Before treatment,there was no statistically significant difference in platelet count and D-dimer between the groups(P>0.05);after medication,the platelet count,and D-dimer in the azithromycin group were significantly better than those in the reference group(P<0.05).The total incidence of adverse reactions in the azithromycin group was significantly lower than that in the reference group(P<0.05).Conclusion:Azithromycin is more effective in treating mycoplasma pneumonia in children,and has certain clinical value.

Improvement in synthesis of 3'-N-demethylazithromycin and its derivatives

3＇-N-demethylazithromycin is an impurity in azithromycin drug. It is derived by demethyl- ation of azithromycin, i. e. , azithromycin loses a methyl group on the 3＇-N position. In this study, bulk product was purified with chromatographic separation. It was observed that 3＇-N-demethylaz- ithromycin was also a precursor of other impurities. Simultaneously, another derivative was synthe- sized, i. e. , 3＇-N-demethyl-3＇-N-formylazithromycin. Reaction conditions were optimized with the HPLC method and good-quality and high-yield derivative product was achieved. The structures of de- rivatives were identified by 1H-NMR and MS.

Azithromycin的体外抗菌作用

测定ａｚｉｔｈｒｏｍｙｉｎ（ＡＺＭ）体外抗菌作用，以红霉素（ｅｒｙｔｈｒｏｍｙｃｉｎ，ＥＭ）为对照，并与其它几种大环内酯类抗生素进行了比较，结果表明国产ＡＺＭ对ＥＭ敏感的革兰氏阳性菌的抗菌作用与ＥＭ相似，ＭＩＣ９０在０．５～４．０ｍｇ／Ｌ范围内；对淋病奈瑟氏菌及流感嗜血杆菌的ＭＩＣ９０均为２ｍｇ／Ｌ，为ＥＭ的１／４；对大肠菌和肺炎克雷伯氏菌抗茵作用则明显优于ＥＭ。本品对金葡球菌无杀菌作用，浓度为０．５及０．２５ｍｇ／Ｌ时，对化脓性链球菌及肺炎球菌表现出较强的杀菌作用，并明显优于ＥＭ。

国产与进口azithromycin随机对照试验的临床评价

为评价国产ａｚｉｔｈｒｏｍｙｃｉｎ（ＡＺＭ）在临床治疗急性细菌性感染病人的有效性与安全性，我们以进口ＡＺＭ为对照药，进行随机对照试验治疗细菌性感染２００例。国产与进口ＡＺＭ组各１００例，治疗呼吸系统和皮肤软组织感染均为每日１次，首次５００ｍｇ，以后每次２５０ｍｇ，疗程７ｄ，治疗淋病均为单次口服１ｇ即可。两组痊愈率分别为８０．０％及８４．０％，有效率分别为９３．０％及９１．０％，细菌清除率分别为９３．３％及９２．１％，不良反应发生率分别为７％及６％，以上结果经统计学处理无显著性差异。国产ＡＺＭ临床疗效肯定，使用安全、方便。

Azithromycin的体内抗菌作用研究

口服ａｚｉｔｈｒｏｍｙｃｉｎ对金葡球菌、肺炎球菌、化脓性链球菌各２株感染小鼠的ＥＤ５０值分别为５１．４０和５８．７４ｍｇ／ｋｇ、２０．４０和２８．７４ｍｇ／ｋｇ、２０．９０和２１．７４ｍｇ／ｋｇ，比对照药红霉素的ＥＤ５０（１０１；４２和１０６．８４ｍｇ／ｋｇ，１０４．１２和１６５．７９ｍｇ／ｋｇ，４３．７１和４３．４８ｍｇ／ｋｇ）低，两药ＥＤ５０值经统计学处理有显著性差异（Ｐ＜０．０１）。

azithromycin的临床评价

口服国产ａｚｉｔｈｒｏｍｙｃｉｎ治疗细菌性感染１１０例，评价其疗效和安全性。治疗结果有效率为９３．６％（１０３／１１０），细菌清除率为９１．４％（９６／１０５）。不良反应发生率为５．４％（６／１１０），症状轻微，以胃肠道反应为主，个别患者出现一过性实验室异常。同时对国产ａｚｉｔｈｒｏｍｙｃｉｎ与进口品治疗呼吸道感染的疗效和安全性进行了随机对照观察，分别治疗５２例和５０例。

Azithromycin临床药物动力学研究

对１０名健康志愿者口服ａｚｉｔｈｒｏｍｙｃｉｎ的药物动力学研究以及其干糖粉的相对生物利用度测定结果显示：空腹口服ａｚｉｔｈｒｏｍｙｃｉｎ单剂５００ｍｇ后，其体内过程符合二室模型，其消除半衰期为５０．３９±８．８７ｈ；高峰血浓度为０．４０３±０．２９９ｍｇ／Ｌ；达峰时间为２．６４±１．２６ｈ，ＡＵＣ为６．３９±１．８１ｈｍｇ／Ｌ。１４４ｈ累积尿排出率为１１．５２％±２．７０％。干糖粉与胶囊比较的相对生物利用度为１１０．６％。根据其药物动力学参数和抗微生物活性。

Azithromycin对临床常见致病菌的体外抗菌作用研究

研究了国产ａｚｉｔｈｒｏｍｙｃｉｎ及红霉素等５种大环内酯类抗生素对５２１株临床分离致病菌的体外抗菌作用。结果表明：ａｚｉｔｈｒｏｍｙｃｉｎ对敏感的金葡球菌、肺炎链球菌、化脓性链球菌、淋球菌、嗜血流感杆菌、粪链球菌及脆弱拟杆菌等均具有较好的抗菌作用（ＭＩＣ５０＜０．０１６～０．５ｍｇ／Ｌ）。对敏感的金葡球菌ＭＩＣ５０与ＭＩＣ９０分别为０．０１６与０．０３１ｍｇ／Ｌ，对脆弱拟杆菌ＭＩＣ５０与ＭＩＣ９０分别为０．０１６与０．１２５ｍｇ／Ｌ。ａｚｉｔｈｒｏｍｙｃｉｎ对所测试的多数致病菌的抗菌作用与红霉素相似或稍强，本品与红霉素有交叉耐药性。

Azithromycin胶囊剂与罗红霉素片剂随机对照治疗急性感染比较

用国产ａｚｉｔｈｒｏｍｙｃｉｎ（ＡＺＭ）和进口罗红霉素作随机对照，ＡＺＭ５００ｍｇ每日１次，疗程３ｄ。非淋球菌性尿道炎１ｇ单剂量；进口罗红霉素１５０ｍｇ每日２次，疗程７ｄ。两组各６１例（呼吸道感染各４１例，非淋球菌性尿道炎各２０例）。试验组和对照组的痊愈率和有效率分别为７７．０５％、９３．４４％；６８．８５％、９０．１６％（Ｐ＞０．０５）。开放试验４２例，呼吸系统感染２５例，皮肤软组织感染１７例，痊愈率和有效率分别为７３．８１％、９２．８６％。细菌的阴转率和消除率分别为９１．２３％、９０．４８％；８６．４４％、８６．１５％（Ｐ＞０．０５）。试验组和对照组细菌有效率分别为９２．９８％、９１．５２％（Ｐ＞０．０５）。试验组和对照组不良反应发生率都为３．２８％，不良反应相同，开放组为２．３８％。提示ＡＺＭ和进口罗红霉素疗效满意，不良反应少，但ＡＺＭ总用药量少、疗程短为其一大优点。

第一个15元大环内酯类抗生素Azithromycin

尽管大环内酯类抗生素的重要代表红霉素(EM)在临床上的应用已有30多年了,但是由于EM对军团菌病、弯曲杆菌腹泻,枝原体及衣原体感染与性病等的有效治疗作用,近年来又再次引起了人们的极大重视。然而EM本身具有的不良之处如抗菌谱较窄、口服吸收不规则、胃肠道与肝功能方面的不良反应等又限制了EM的应用。鉴此,欧、美。

Azithromycin及其相关化合物的分析

azithromycin(CP-62993,XZ-450,AM)是具有15元的氮杂内酯(azalactone)环的半合成大环内酯类抗生素。化学结构上系在红霉素A内酯环的9a位内插一个含有取代甲基的氮原子,成为氮杂类(azalids)化合物。修饰后的产物即azithromycin,较母体化合物红霉素扩大了抗菌谱,提高了抗菌活力和对酸性环境的稳定性。口服后生物利用度高,半衰期较长,具有更高的组织浓度。1993年已收入美国药典Ⅹ Ⅹ Ⅱ版第8补编内。本文介绍AM的有关化学、酸稳定性研究。

Development of a New Azithromycin Glutamate for Parenteral Preparation, the Toxicity in Sprague-Dawley Rats and Pharmacokinetics in Human Healthy Volunteers

Aim In order to improve the solubility of azithromycin, the objectives of the present study were to screen an appropriate salt for azithromycin by comparing acute hepatic and renal toxicities in animals, and study the pharmacokinetics of final chosen azithromycin salt. Methods Various salts of azithromycin, such as glutamate, citrate, hydrochloride, sulphate, dihydrogen phosphate, lactobionate, tartrate, and aspartate were given intravenously to Sprague Dawley rats at a dose of 10 mg once daily for 14 consecutive days via tail vein. The acute hepatic and renal indicators were measured before and after administration. A pharmacokinetic study was performed on 12 healthy human volunteers. The subjects were equally divided into two groups by a randomized crossover design. Azithromycin glutamate injection was administered by intravenous infusion or intramuscular injection at a single dose of 500 mg, respectively. Azithromycin concentrations in plasma were determined by microbial inhibition zone assay, and the pharmacokinetic parameters were calculated using a practical pharmacokinetic software 3P87 program. Results Azithromycin glutamate was least toxic to the liver and kidney of the rats, thus being selected as a final salt for parenteral preparation of azithromycin. Pharmacokinetic results showed that the area under the plasma concentration-time curves （AUC0-120h） were 21.47 ± 1.57 h·μg·mL^-1 for intravenous infusion, and 19.36 ± 2.44 h·μg·mL^-1 for intramuscular injection. The absolute bioavailability of intramuscular injection was 92.59%. Conclusion Azithromycin glutamate is suitable for the future clinical application, and its pharmacokinetics is characterized in human volunteers in the present study.

Azithromycin-containing versus standard triple therapy for Helicobacter pylori eradication:A meta-analysis

AIM： To evaluate whether adding azithromycin to firstline Helicobacter pylori （H pylorl） eradication improved eradication and reduced side effects. METHODS： Eligible articles were identified by searches of electronic databases. We included all randomized trials that compared azithromycin-containing with standard triple-therapy regimens for first-line treatment of H pylori infection. Statistical analysis was performed with Review Manager 5.0.10. Sub-analyses were also performed. RESULTS： We identified 14 randomized trials （1431 patients）. Pooled Hpylori eradication rates were 72.01% （95% CI： 58.09%-85.93%） and 69.78% （95% CI： 66.47%-73.09%） for patients with or without azithromycin by intention-to-treat analysis, and the odds ratio （OR） was 1.17 （95% CI： 0.64-2.14）. The occurrence of side effects differed significantly and was 15.81% （95% CI： 12.50%-19.12%） and 25.20% （95% CI： 21.44%-28.96%） for treatment with or without azithromycin, respectively, and the summary OR was 0.58 （95% CI： 0.41-0.82）. Furthermore, the azithromycin-containing group had a lower occurrence of diarrhea, nausea and taste disturbance. CONCLUSION： Our review suggests that azithromycincontaining triple-therapy regimens could be equally effective in eradication of Hpylori compared with standard first-line triple-therapy regimens.

Azithromycin in one week quadruple therapy for H pylori eradication in Iran

AIM： To investigate eradication rates, patient compliance and tolerability of a 1-wk Azithromycin-based quadruple therapy versus the 2-wk conventional therapy. METHODS： A total of 129 Hpylori-positive patients were randomized to either omeprazole 20 mg, bismuth subcitrate 240 mg, azithromycin 250 mg, and metronidazole 500 mg, all twice daily for 1-wk （B-OAzM） or omeprazole 20 mg, bismuth subcitrate 240 mg, amoxicillin lg, and metronidazole 500 mg all twice daily for 2-wk （B-OAM）. Hpylori infection was defined at entry by histology and rapid urease test and cure of infection was determined by negative urea breath test. RESULTS： Hpylori eradication rates produced by B-OAzM and B-OAM were 74.1% and 70.4% respectively based on an intention to treat analysis, and 78.1% versus 75.7% respectively based on a per-protocol analysis. The incidence of poor compliance was lower, although not significantly so, in patients randomized to B-OAzM than for B-OAM （3.5% versus 4.3%） but intolerability was similar in the two groups （ 35% versus 33.3%）. CONCLUSION： 1-wk azithromycin based quadruple regimen achieves an Hpylori eradication rate comparable to that of standard 2-wk quadruple therapy, and is associated with comparable patient compliance and complications.

Classification and Quantitative Analysis of Azithromycin Tablets by Raman Spectroscopy and Chemometrics

Raman spectroscopy has been proven a noninvasive technique with high potential in pharmaceutical industry. In this study, micro Raman technique and chemometric tools were used for identification of azithromycin (AZM) tablets by different manufacturers and quantitative analysis of the active pharmaceutical ingredient (API) in the samples. Support vector machine (SVM), Bayes classifier and K-nearest neighbour (KNN) were employed for identification, partial least squares (PLS) regression was used for quantitative determination, and interval partial least squares (iPLS) and Monte Carlo based uninformative variable elimination (MC-UVE) methods were used to select informative variables for improving the models. The results show that all the samples can be classified into groups by manufacturers with high accuracy, and the correlation coefficient between the predicted API concentrations and reference values is as high as 0.96. Therefore, micro Raman spectroscopy coupled with chemometrics may be a fast and powerful tool for identification and quantitative determination of pharmaceutical tablets.

Azithromycin in a triple therapy for H.pylori eradication in active duodenal ulcer

AIM:To assess and compare the efficacy and safety of two triple regimes:A)metronidazole,amoxicillin and omeprazole, which is still widely used in Russia,and B)azithromycin, amoxicillin and omeprazole in healing active duodenal ulcer and H.pylori eradication. METHODS:100 patients with active duodenal ulcer were included in the open,multicentre,randomized study with comparative groups.Patients were randomly assigned to one of the following one-week triple regimes:A) metronidazole 500 mg bid,amoxicillin I g bid and omeprazole 20 mg bid(OAM,n=50)and B)azithromycin 1 god for the first 3 days(total dose 3 g),amoxicillin 1 g bid and omeprazole 20 mg bid(OAA,n=50).Omeprazole 20 mg od was given after the eradication course as a monotherapy for three weeks.The control endoscopy was performed 8 weeks after the entry.H.pyloriinfection was determined in the entry of the study and four weeks after the cessation of treatment by means of histology and CLO-test. RESULTS:97 patients completed the study according to the protocol(1 patient of the OAM group did not come to the control endoscopy,2 patients of the OAA group stopped the treatment because of mild allergic urticaria).Duodenal ulcers were healed in 48 patients of the OAM group(96 %, C190.5-100 %)and in 46 patients of the OAA group(92 %, CI 89.5-94.5 %)(p=ns).H.pyloHinfection was eradicated in 15 out of 50 patients with OAM(30 %,CI 17-43 %)and in 36 out of 50 patients treated with OAA(72 %;CI 59-85 %) (P<0.001)-ITT analysis.CONCLUSION: The triple therapy with omeprazole, amoxicillin and metronidazole failed to eradicate H.pylori'vc\ the majority of patients, which is an essential argument to withdraw this regimen out of the national recommendations. Macrolide with amoxicillin are preferable to achieve higher eradication rates. Azithromycin (1 g od for the first 3 days) can be considered as a successful component of the triple PPI-based regimen.

用Azithromycin治疗下尿路和男性生殖器官感染-炎症性疾病

下尿路和男性生殖器官感染-炎症性疾病的治疗是目前泌尿科最复杂的问题。这是由于病原体对广泛用于泌尿科的抗菌药物出现了耐药性;病原体常常是混合存在;病情顽固,经常复发并有转变为慢性疾病的倾向。 门诊治疗泌尿科疾病,由于慢性疾病应用抗菌疗法时间长,因此除抗菌药物的疗效外,给药次数和方式也具有重要意义。在这种情况下,最好用口服制剂。

Comparison of therapeutic effects of topical azithromycin solution and systemic doxycycline on posterior blepharitis

AIM：To compare the effect of azithromycin drop and doxycyciine capsule on treatment of posterior blepharitis.METHODS：Fifty patients（100 eyes） with moderate posterior blepharitis,randomly divided into two therapeutic groups;all the patients got warm eyelid compress and massage three times a day for 3wk.In addition the first group got azithromycin 1% drop,twice daily for 1wk and then one drop daily for 2wk.The second group got oral doxycyciine 100 mg daily for 3wk.At the end of the research,patients＇ signs and symptoms were compared together.ANOVA,Chi-square and MannWhitney tests were used for statistical analysis.RESULTS：Topical therapy with azithromycin and oral therapy with doxycyciine relieved signs and symptoms after 3wk.There were no significant differences between symptoms healing rate and foreign body sensation healing in these two groups（P〉0.05）.However,azithromycin drop was more effective in reduction of eye redness and doxycyciine was more effective in meibomian glands plugging healing and reducing the corneal staining.CONCLUSION：Topical azithromycin could have similar effects as oral doxycyciine on posterior blepharitis in improving subjective symptoms.However,doxycyciine can reduce objective signs such as ocular surface staining and meibomian gland plugging more than azithromycin.

Efficacy and Safety of Intravenous Moxifloxacin Versus Cefoperazone with Azithromycin in the Treatment of Community Acquired Pneumonia

Summary： To compare the efficacy, safety, and tolerability of intravenous moxifloxacin with those of a commonly used empirical antibiotic regimen, cefoperazone and azithromycin in the treatment of community acquired pneumonia （CAP） in adult patients requiring initial parenteral therapy, 40 patients with CAP were divided into two groups, a moxifloxacin group （n=20） and a control group （n=20）, which were treated for 7 to 14 days. The patients in the moxifloxacin group were intravenously given 400 mg of moxifloxacin （AveloxR） once a day. Patients in the control group were administered 2.0 g of cefoperazone twice a day and azithromycin 0.5 g once a day. Clinical, bacteriological, and laboratory examinations were performed before the treatment, and at the end of the treatment. Our results showed that there was no significant difference in the clinical efficacy rate between two treatment groups at end of therapy （90 % for moxifloxacin, 95 % for cefoperazone plus azithromycin） （P〉0.05）. The bacteriologic eradication rate at the end of treatment was 90 % in the moxifloxacin group and 80 % in the cefoperazone-plus-azithromycin group, whereas there was no significant difference between the two groups （P〉0.05）. In addition, both drugs were well-tolerated in this trial, with the number of drug-related adverse events being comparable. It is concluded that moxifloxacin is an effective and well-tolerated treatment for CAP and was equivalent to the com- monly used empirical treatment of cefoperazone plus azithromycin. Moxifloxacin is likely to offer clinicians an alternative for reliable empirical CAP treatment in the face of increasing antibiotic resistance.

Impact of Azithromycin on Forsythiaside Pharmacokinetics in Rats:A Population Modeling Method

Objective:Lianhuaqingwen and Shuanghuanglian are drug treatment options for Corona Virus Disease 2019(COVID-19).In China,use of traditional Chinese medicine with Shuanghuanglian or Lianhuaqingwen(for them,forsythiaside is the active antiviral and antibacterial component)in combination with azithromycin is common for the treatment of pediatric pneumonia.It is important to understand the reason why the combination of these compounds is better than a single drug treatment.This study aimed to explore the pharmacokinetic interaction between forsythiaside and azithromycin.Methods:Twelve male Sprague-Dawley rats were randomly divided into an experimental group(Forsythia suspensa extract and azithromycin)and a control group(a single dose of Forsythia suspensa extract in 5%glucose solution).Plasma samples were collected at scheduled time points,and the high-performance liquid chromatography combined with ultraviolet method was used to determine the plasma forsythiaside concentration.Non-compartmental analysis and population pharmacokinetic methods were used to investigate the forsythiaside pharmacokinetic difference between the experimental and control group.Results:Compared with a single administration,the area under the curve and half-life of forsythiaside increased,and forsythiaside clearance decreased significantly after co-administration with azithromycin.The in vivo behavior of forsythiaside could be described by the one compartment model.The forsythiaside clearance decreased when combined with azithromycin.Visual evaluation and bootstrap results suggested that the final model was precise and stable.Conclusion:Co-administration of azithromycin can significantly decrease the forsythiaside clearance and increase drug exposure.A lower dose of azithromycin can obtain sufficient forsythiaside concentration to provide antiviral and antibacterial activity.