英文药名: Avelox(Moxifloxacin) 中文药名: 莫西沙星片 生产厂家: Bayer Corporation 药品名称 别　名: 拜复乐 Avelox 英 文 名: moxifloxacin 药理作用 拜复乐(莫西沙星片)作用机制: 莫西沙星是广谱和具有抗菌活性的8-甲氧基氟喹诺酮类抗菌药。莫西沙星在体外显示出对革兰阳性细菌，革兰阴性菌，厌氧菌、抗酸菌和非典型微生物如支原体、衣原体和军团菌有广谱抗菌活性。抗菌作用机制为干扰II、IV拓扑异构酶。拓扑异构酶是控制DNA拓扑和在DNA复制、修复和转录中关键的酶。其杀菌曲线表明，莫西沙星具有浓度依赖性的杀菌活性。最低杀菌浓度和最低抑菌浓度基本一致。莫西沙星对β-内酰胺类和大环内酯类抗生素耐药的细菌亦有效。通过感染的实验动物模型证实，莫西沙星体内活性高。 对人类肠道菌群的作用: 拜复乐(莫西沙星片)通过对两名志愿者服用莫西沙星后的研究观察到下列的变化 ：大肠杆菌、芽孢杆菌、普通拟杆菌、肠球菌、克雷白杆菌和厌氧菌如 ：双歧杆菌、真杆菌和消化链球菌等的减少。这些变化在2周内可以恢复正常，未发现艰难梭菌毒素。 适应症 拜复乐(莫西沙星片)治疗患有上呼吸道和下呼吸道感染的成人（≥18岁），如急性窦炎、慢性支气管炎急性发作、社区获得性肺炎，以及皮肤和软组织感染。 用法用量 剂量范围：一次400 mg（1片），1日1次。 成年人服用方法: 片剂用一杯水送下，服用时间不受饮食影响。 -治疗时间：治疗时间应根据症状的严重程度或临床反应决定。 -治疗上呼吸道和下呼吸道的感染时可按照下列方法： --慢性气管炎急性发作：5天， --社区获得性肺炎：10天， --急性鼻窦炎：7天， --治疗皮肤和软组织感染的推荐治疗时间为7天， -莫西沙星400 mg片剂在临床试验中最多用过14天疗程。 老年人: 老年人不必调整用药剂量。 儿童:儿童和发育阶段的青少年不建议使用拜复乐(莫西沙星片)。 肝损伤：轻度肝功能异常（Child-Pugh A, B）的患者不必调整莫西沙星的剂量。目前尚缺乏严重肝功能受损者（Child-Pugh C）的药代动力学数据。 肾功能异常：任何程度的肾功能受损的病人均不必调整莫西沙星的剂量（包括肌酐清除率≤ 30 mL/分/1.73 m2。目前缺乏透析病人的药代动力学数据。 种族差别：不同种族间不必调整药物剂量。 用药过量: 关于过量的研究资料非常有限，单次最大剂量800 mg和每日600 mg多次口服，连用10天在健康志愿者身上未发现有任何明确不良反应。一但服用过量莫西沙星时，应根据患者状况采取适当支持措施。 任何疑问，请遵医嘱！ 不良反应 在莫西沙星的临床试验中，绝大多数的不良反应为轻中度（大于90%），由于不良反应导致不能使用莫西沙星治疗的病人为3.6%。根据莫西沙星的临床试验总结出的常见不良反应（其相关程度分为很可能、可能和无法评估）列表如下: 发生率≥1%且<10%： -全身症状：腹痛、头痛。 -消化系统：恶心、腹泻、呕吐、消化不良、肝功能化验异常。 -心血管系统: 合并低钾血症的患者QT间期延长。 发生率≥0.1%且<1%： -全身症状：乏力、念珠菌病、疼痛、不适、胸痛。 -心血管系统：心动过速、高血压、心悸、QT间期延长。 -消化系统: 口干、恶心和呕吐、腹胀、便秘、口腔念珠菌、食欲下降、口腔炎、胃肠失调、舌炎、γ谷氨酰胺转肽酶增高。 -血液和淋巴系统 ：白细胞减少、凝血酶原减少、嗜酸细胞增多。代谢和营养：淀粉酶增加，骨骼肌肉系统：关节痛、肌肉痛。 -神经系统: 失眠、眩晕、神经质、嗜睡、焦虑、颤抖、感觉异常。呼吸系统 ：呼吸困难。皮肤和附件：皮疹、瘙痒、多汗。 -泌尿生殖系统:阴道念珠菌病、阴道炎。 发生率≥0.01%且<0.1%： -全身症状：骨盆痛、面部浮肿、背痛、实验室检查异常、过敏反应、下肢痛。 -心血管系统：低血压、血管舒张、外周水肿。 -消化系统: 胃炎、舌苔异常、吞咽困难、黄疸、腹泻（难辨梭状芽胞杆菌）。 -血液和淋巴系统：凝血活酶减少、凝血酶原增加、血小板减少、贫血。 -代谢和营养：高血糖、高血脂、高尿酸血症、LDH升高（伴异常肝功能）。 -骨骼肌肉: 关节炎、肌腱异常。 -神经系统：幻觉、人格解体、紧张、运动失调、兴奋、健忘症、失语症、情绪不稳定、睡眠失调、语言障碍、思维异常、感觉减退、多梦、惊厥、精神错乱、抑郁。 -呼吸系统：哮喘。 -皮肤和附件：皮疹（斑丘疹、紫癜、脓泡）。 -特殊感官: 耳鸣、视觉异常、失味、嗅觉异常（包括嗅觉倒错、嗅觉减弱及嗅觉缺失）、弱视。 -泌尿生殖系统：肾功能异常。 未在上述不良反应中列出的与药物无关的最常见的试验室参数异常为：红细胞压积增加或减少、白细胞增加、红细胞增加或减少、血糖下降、血红蛋白减少、碱性磷酸酶升高、SGOT/AST升高、SGPT/ALT升高、胆红素升高、尿素升高、肌酐升高、尿素氮升高，上述异常是否由该药或治疗时患者状况导致尚属未知。 孕妇及哺乳期妇女用药 拜复乐(莫西沙星片)禁用于孕妇。 喹诺酮类已知能大量分泌到乳汁中。临床前试验证实小量的莫西沙星可以分泌到人类的乳汁中，尚缺乏哺乳期妇女的数据。因此，莫西沙星禁用于哺乳期的妇女。 注意事项 已知对该片剂的任何成份或其他喹诺酮类高度过敏者禁用。　　 喹诺酮类使用可诱发癫痫的发作，对于已知或怀疑有能导致癫痫发作或降低癫痫发作域值的中枢神经系统疾病的病人，莫西沙星在使用中要注意。　　 由于缺乏患有肝功能严重损伤病人使用莫西沙星时的药代动力学和药效动力学的数据，不推荐该药在这类病人中使用。　　 莫西沙星象其他喹诺酮类和大环内酯类抗生素一样在有些患者可能延长QT间期。因为缺乏相关的临床资料，该药应避免用于QT间期延长的病人。患有低钾血症或接受1a类（如奎宁丁、普鲁卡因）或III类（如胺碘酮、索托落尔）抗心律失常药物治疗的病人，在使用莫西沙星时应慎用。　　 莫西沙星与下列药物合用不排除有延长QT间期的效应西沙必利、红霉素、抗精神病药物、和三环类抗抑郁药，所以，应慎重与这些药物合用。因为临床资料有限，莫西沙星在有致心律失常的因素（如严重的心动过缓或急性心肌缺血）存在时应慎用。　　 QT间期延长的程度随着药物浓度的增加而增加，所以不应超过推荐剂量。QT间期延长可以导致室性心律失常包括尖端扭转型室速的发生危险。在莫西沙星治疗的超过4000名患者中，没有心血管的发病率或死亡率归因于QT间期延长，但某些潜在条件可以增加室性心律失常的危险。　　 在使用喹诺酮类治疗中有可能出现肌腱炎和肌腱断裂，特别是在老年病人和使用激素治疗的病人中。一旦出现疼痛或炎症，患者需要停止服药并休息患肢。　　 有报导，在使用包括莫西沙星在内的广谱抗生素中出现伪膜性肠炎，因此，在使用莫西沙星治疗中如患者出现严重的腹泻，需要考虑这个诊断，这一点很重要。在这种情况下需立即采取足够的治疗措施。　　 光敏感性其他喹诺酮类有导致光过敏的报导。但是，在一项健康志愿者中进行的试验未发现有光过敏的出现。尽管如此，应建议病人避免在紫外线及日光下过度暴露。在有些病例，首次服用后就可发生过敏反应和变态反应。过敏性反应在极少的病例能够在首次服用后导致发生威胁生命的休克。在这些病例莫西沙星应停用并给予治疗（如针对休克的治疗）。 贮藏/有效期 干燥条件下储藏，盐酸莫西沙星片剂需储藏于生产者的原包装内。有效期2年。 包装规格： ·400mg *14 片 ·400mg *25 片 Side Effects of Avelox Contact your doctor immediately if any of these serious side effects occur when using Avelox: Severe allergic reactions (rash, hives, itching, difficulty breathing, tightness in the chest, swelling of the mouth, face, lips, or tongue), bloody or tarry stools, burning, numbness, tingling, pain or weakness in the arms, hands , legs and feet, chest pain, dark urine, decreased urination, fainting, coughing, fever, chills, or unusual, hallucinations, inability to move or bear weight on a common area or tendons, irregular heartbeat, joint pain, from moderate to severe sunburn; mood or mental changes (eg, new or worsening anxiety, agitation, confusion, depression, nervousness, restlessness, insomnia), pain or muscle weakness, weakness, pain, irritation, redness, swelling, or bruises of a tendon or common area, pale stools, persistent sore throat, blows to the chest, red, swollen, blistering or peeling skin, seizures, severe or persistent diarrhea, severe or persistent dizziness, shortness of breath or difficulty breathing, stomach pain / cramps, suicidal thoughts or actions, tremor, unusual bleeding or bruising, unusual tiredness or weakness, vaginal yeast infection, vision changes, yellowing of the skin or eyes. This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the body properly, please read the Guide to Reporting Problems to the FDA. Avelox tablets All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome when using tablets Avelox: Diarrhea, dizziness, headache, nausea, sleep disturbance, vomiting. Contact your doctor immediately if any of these serious side effects occur when using tablets Avelox: Severe allergic reactions (rash, hives, itching, difficulty breathing, tightness in the chest, swelling of the mouth, face, lips, or tongue), bloody or tarry stools, burning, numbness, tingling, pain or weakness in the arms, hands , legs and feet, chest pain, dark urine, decreased urination, fainting, coughing, fever, chills, or unusual, hallucinations, inability to move or bear weight on a common area or tendons, irregular heartbeat, joint pain, from moderate to severe sunburn; mood or mental changes (eg, new or worsening anxiety, agitation, confusion, depression, nervousness, restlessness, insomnia), pain or muscle weakness, weakness, pain, irritation, redness, swelling, or bruises of a tendon or common area, pale stools, persistent sore throat, blows to the chest, red, swollen, blistering or peeling skin, seizures, severe or persistent diarrhea, severe or persistent dizziness, shortness of breath or difficulty breathing, stomach pain / cramps, suicidal thoughts or actions, tremor, unusual bleeding or bruising, unusual tiredness or weakness, vaginal yeast infection, vision changes, yellowing of the skin or eyes. This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the body properly, please read the Guide to Reporting Problems to the FDA. Top Avelox side effects – for professional Avelox clinical efficacy trials enrolled over 9,200 moxifloxacin orally and intravenously treated patients, of whom more than 8,600 patients received a dose of 400 mg. Most adverse events reported in moxifloxacin trials were described as mild to moderate severity and required no treatment. Moxifloxacin was discontinued due to adverse reactions considered drug-related in 2.9% of patients treated orally and 6.3% of sequentially (intravenous followed by oral) treated patients. Studies have been conducted in recent community-acquired pneumonia and complicated skin and skin structure infections and complicated intra-abdominal, in general, a sicker patient population compared to the tablet studies. Adverse reactions, judged by investigators to be at least possibly drug-related, occurring in greater than or equal to 2% of moxifloxacin treated patients were diarrhea, nausea (6%) (5%), dizziness (2%) . Additional clinically relevant uncommon events, judged by investigators to be at least possibly drug-related, that occurred in greater than or equal to 0.1% and less than 2% of moxifloxacin treated patients were: BODY AS A WHOLE: abdominal pain, headache, fatigue, dehydration (secondary to diarrhea or reduced fluid intake), injection site reaction (including phlebitis), malaise, moniliasis reaction, pain, allergic Cardiovascular: cardiac arrhythmia (not otherwise specified), tachycardia, palpitations, vasodilation, QT prolonged DIGESTIVE: vomiting, abnormal liver function tests (increases in transaminases, bilirubin), dyspepsia, dry mouth, flatulence, oral candidiasis, constipation, GGTP increased, anorexia, stomatitis, glossitis Hemic and Lymphatic: leukopenia, eosinophilia, prothrombin decrease (prothrombin time / International Normalized Ratio (INR) increased), thrombocythemia Metabolism and nutrition disorders: increased lactic dehydrogenase, amylase increased Musculoskeletal: arthralgia, myalgia NERVOUS SYSTEM: insomnia, nervousness, dizziness, drowsiness, anxiety, tremor Skin / Appendages: rash (maculopapular, purpuric, pustular), pruritus, sweating, urticaria Special Senses: taste perversion vaginal moniliasis, vaginitis: UROGENITAL Additional clinically relevant rare events, judged by investigators to be at least possibly drug-related, that occurred in less than 0.1% of moxifloxacin treated patients were: abnormal dreams, impaired vision (visual disturbances temporally associated with CNS symptoms), agitation, amblyopia, amnesia, anemia, aphasia, arthritis, asthma, atrial fibrillation, back pain, chest pain, confusion, seizures of various clinical manifestations (including most mal seizures), depersonalization, depression (potentially culminating in a self-injurious behavior), dysphagia, dyspnea, ECG abnormal, emotional lability, face edema, gastritis, gastrointestinal disorder, hallucinations, hyperglycemia, hyperlipidemia, hypertension, hypertonia, hyperuricemia, hypoesthesia, hypotension , incoordination, jaundice (predominantly cholestatic), kidney function abnormal, lab test abnormal (not specified), leg pain, numbness, parosmia, pelvic pain, peripheral edema, photosensitivity / phototoxicity reactions, pseudomembranous colitis, prothrombin increase (time prothrombin decreased / International Normalized Ratio (INR) decreased), sleep disturbances, speech disorders, supraventricular tachycardia, syncope, taste loss, tendon disorder, thinking abnormal, thrombocytopenia, thromboplastin decrease, tinnitus, tongue discoloration , ventricular tachycardia Reports of post-marketing adverse events: Additional adverse events were reported by the worldwide post-marketing experience with moxifloxacin. Because these events are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. These events, some of them life threatening, include anaphylactic reaction, anaphylactic shock, angioedema (including laryngeal edema), liver failure, including fatal cases, hepatitis (predominantly cholestatic), photosensitivity / phototoxicity reaction, psychotic reaction (very rarely ends with self-risk behavior), renal dysfunction or renal failure, Stevens-Johnson Syndrome, tendon rupture, toxic epidermal necrolysis, and ventricular tachyarrhythmias (including in very rare cases cardiac arrest and torsades de pointes, and usually in patients with concomitant severe underlying disease proarrhythmic). Cases of coordination and impaired gait, as well as exacerbation of myasthenia gravis have also been reported.