86．阿奇霉素
出处：按学科分类—医药、卫生 军事医学科学出版社《临床常用进口药物手册》第485页（9106字）
【中文释文】：
胶囊，片剂
〔成分〕
每粒胶囊含250mg二水阿奇霉素
每片含500mg二水阿奇霉素
〔包装〕
每盒装250mg阿奇霉素胶囊6粒
每盒装500mg阿奇霉素3片
〔药理作用〕
阿奇霉素是一种氮环内酯类抗生素，结构与大环内酯类抗生素近似。它的作用机理的特点是通过与50S核糖体亚单位结合，因而抑制细菌蛋白质的合成。
阿奇霉素口服吸收很好，并迅速地从血清进入各种组织和器官，该药口服后37%被吸收，血清峰值浓度相对较低，为0．4μg／ml。它迅速地分布到各种组织中，达到很高的组织浓度，范围在1～9μg／mg，依组织类型而异，停药后，该药在组织中的治疗浓度可维持5～7d。由于该药的半衰期很长，因此可以每天给药一次，而且疗程短。
阿奇霉素主要以原型经胆汁排除，从肾脏排除的量较少。
阿奇霉素的最显着特性之一是被吞噬细胞吞噬，然后随吞噬细胞移向感染部位。这种特性作用为该药向感染部位的转运机制，使阿奇霉素在感染部位达到比非感染部位更高的组织浓度。
阿奇霉素在吞噬细胞内的浓度很高，因而表现出很好的细胞内抗菌作用。
阿奇霉素的抗菌谱很广，下列微生物的绝大多数菌株对之敏感：
革兰阳性菌：肺炎链球菌、酿脓链球菌、无乳链球菌、链球菌属C、F、G，绿色链球菌及金葡菌。耐红霉素的革兰阳性菌对此药不敏感。
革兰阴性菌：流感嗜血杆菌、副流感嗜血杆菌、粘膜炎莫拉菌、百日咳杆菌、副百日咳杆菌、嗜肺军团菌、杜克莱嗜血杆菌、空肠弯曲菌、淋病奈瑟球菌和阴道加德诺菌(旧称阴道嗜血杆菌)。
厌氧菌：双道拟杆菌，产气荚膜杆菌和消化链球菌属。
其它微生物：砂眼衣原体、肺炎支原体、尿素分解尿支原体，苍白密螺旋体和布氏疏螺旋体。
〔适应证〕
上呼吸道感染：链球菌咽炎／扁桃体炎，急性中耳炎及急性窦炎。
下呼吸道感染：慢性支气管炎急性发作，急性支气管炎，非典型性肺炎，轻、中度急性细菌性肺炎。
皮肤及软组织感染：丹毒，脓疱病，继发性脓皮病。
性传播疾病：淋球菌和非淋菌性尿道炎／子宫颈炎。
〔禁忌〕
对大环内酯类抗生素过敏者禁用。
与其它药物的相互作用。与氢氧化铝、硫酸镁等含抗酸成分的药物同时服用会降低阿奇霉素的血药浓度峰值，但不影响该药的吸收率。服用抗酸药2h后服用阿奇霉素不影响阿奇霉素的吸收。
目前还没有资料表明阿奇霉素与茶碱、口服抗血凝药、卡马西平、苯妥英、地高辛、麦角胺、二氢麦角胺和环胞素等有相互作用。阿奇霉素与这些药物同时应用时，建议对病人进行观察。
〔注意〕
由于阿奇霉素主要经胆汁排泄，肝功能不良者慎用。由于没有肾功能损害者应用阿奇霉素的有关资料，肾功能不良者慎用。
〔孕妇及哺乳期妇女〕
动物实验表明阿奇霉素没有致畸作用，但因缺少临床试验，目前还没有向孕妇推荐使用。由于没有阿奇霉素从乳汁中排泄的有关资料，不推荐哺乳期妇女使用。
〔用法和用量〕
由于食物可减少阿奇霉素的吸收，因此饭前至少1h或饭后至少2h服用。
阿奇霉素每天口服一次。
上呼吸道、下呼吸道感染，皮肤和软组织感染：总剂量为1．5g，分5次服用。
第1天500mg一次口服，第2～5天每天1次，每次250mg。
性传播疾病：1g一次口服(250mg胶囊4粒或500mg片剂2片)。
老年人剂量无需调整。
〔过量服用及治疗〕
没有过量服用阿奇霉素的有关资料。
〔副作用〕
阿奇霉素几乎不引起副作用，偶尔引起胃肠道不良反应。常见胃肠道反应有：恶心、腹泻、胃痛，偶尔呕吐和胃肠胀气。偶尔引起皮疹。有时可致转氨酶轻微高于正常值和嗜酸性细胞增多，停药2～3周后恢复正常。
〔有效期〕
见包装。
阿奇霉素超过有效期后请勿服用。
请放在儿童拿不到的地方。
〔药品分发〕
只根据处方给药
〔生产厂家〕
克罗地亚萨格勒布普利瓦药厂
(附本品别名：阿红霉素，阿泽红霉素，氮红霉素，舒羲特，希舒美，泰力特Sumaed，Zithyomax，Tailide)
【外文释文】：
azithromycin
capsules，tablets
Composition
Each capsule contains 250mg azithromycin as dihydrate．
Each tablet contains 500mg azithromycin as dihydrate．
Packages
Box with 6 capsules a 250mg azithromycin．
Box with 3 tabolts a 500mg azithromycin．
Pharmacotherapeutic group and action
Azithromycin is azalide antibiotic，structurally related to the macrolide antibiotics．Its mechanism of action is characterized by binding to the 50 S ribosome subunit，thus inhibiting bacterial protein synthesis．
Azithromycin is well absorbed following oral administration and rapidly passes from serum to tissues and various organs．After ingestion 37%of the drug is absorbed，reaching relatively low peak serum concentrations of 0．4μg／mg．It is rapidly distributed to a wide range of tissues and achieves high tissue concentrations ranging between 1 and 9μg／ml，depending on tissues type．Therapeutic concentrations of azithromycin are maintained in tissues for five to seven days after the ingestion of last oral dose．Its prolonged elimination half-life from tissues enables single daily dosage regimen and reduces treatment period．
A major route of elimination is biliary excretion，predominantly as unchanged drug．Urinary excretion is minor route of elimination．
One of the most interesting features of azithromycin is its uptake by phagocytic cells which migrate to infected sites．This property serves as a transport mechanism for the drug to infected tissue，where azithromycin achieves concentrations higher than those achieved in uninfected tissue．
Azithromycin achieves very high inrtacellular concentrations in phagocytic cells and exhibits very good intracellular activity．
Azithromycin has a broad spectrum of activity．
Azithromycin has been shown to be active against most strains of the following organisms：
Gram-positive bacteria：Streptococcus pneumoniae，S．pyogenes，S．agalactiae，streptococci of the group C，F and G，S．viridans and Staphylococcus aureus．It is not active against gram-positive bacteria resistant to erythromycin．
Gram-negative bacteria：Haemophilus influenzae，H．parainfluenzae，Moraxella catarrhalis，Bordetella perturssis，B．parapertussis，Legionella pneumophila，Haemophilus ducreyi，Campyolbacter jejuni，Neisseria gonorrhoeae and Gardnerella vaginalis．
Anaerobic bacteria：Bacteroides bivius，Clostridium perfringens and Peptostreptococcus species．
Other microorganisms：Clamydia trachomatis，Mycoplasma pneumoniae，Ureaplasma urealyticum，Treponema pallidum and Borrelia burgdorferi．
Indications
Upper respiratory tract infections：streptococcal pharyngitis／tosillitis，acute otitis mediaand acute sinusitis．
Lower respiratory tract infections：acute exacerbations of chronic bronchitis，atypical andacute bacterial pneumonias from mild to moderate intensity．
Skin and soft tissue infections：erysipelas，impetigo and secondary pyodermatoses．Sexually transmitted diseases：gonorrhoeal and nongonorrhoeal urethritis／cervicitis．
Contraindications
Hypersensitivity to macrolide antibiotics．
Interactions
Aluminium-and magnesium-containing antacids reduce the peak serum levels but not the rate(AUC)of azithromycin absorption．Administration of antacides 2 hours prior to azithromycin had no effect on azithromycin absorption．
Interactions of azithromycin with theophylline，oral anticoagulants，carbamazepine，phenytoin，digoxin，ergotamine or dihydroergotamine and cyclosporine have not been reported in clinical trials．When azithromycin and these drugs are used concomitantly careful monitoring of patients is advised．
Special warnings
Because azithromycin is principally eliminated by bile，caution is recommended when azithromycin is administered in patients with impaired hepatic function，There are no data regarding azithromycin usage in patients with renal failure and caution should be exercised when prescribing azithromycin to these patients．
Pregnancy and lactation
Animal reproductive studies show no evidence of harmful fetal effects，but due to lack of clinical data in humans，azithromycin should be administered to pregnant women only if potential benefits outweigh the possible hazards．
Drug is not recommended to nursing mothers because there are no data on azithromycin excretion in human milk．
Dosage and administration
Food reduces the absorption of azithromycin and it should be given atleast one hour before or two hours after a meal．
Azithromycin is administered in single daily dose．
Upper and lower respiratory tract infections and skin and soft tissue infections(the total dose of 1．5g is administered over 5 days)：
500 mg(two 250 mg capsules)as single dose on the first day；and 250 mg(one 250 mg capsule)once daily on days 2-5．
Sexually transmitted diseases：1 g as single dose(four capsules a 250 mg or two tables a 500mg)．
It is not necessary to modify dosage for elderly patients．
Overdosage and treatment
There has been no data of overdosage with azithromycin．
Adverse effects
Azithromycin seldom causes side effects．Some gastro-intestinal disturbances may occur，such as：nausea，diarrhoea and stomach pain，and rarely vomiting and flatulence．Skin rash is an infrequent adverse effect．A moderate increase in hepatic enzymes above upper limit of normal as well as eozinophilia may occur，if changed，those values return back to normal two to three weeks after the drug therapy．
Shelf life
Denoted on the packing．
Drug should not be used after the expiry of its shelf life．
Keep out of the reach of children!
Dispensation
To be dispensed on medical prescription only．
Manufacturer
Pliva Pharmaceutical，Chemical，Food and Cosmetic Industry Zgreb-Croatai