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英文药名: Ketek(Telithromycin Tablets)
中文药名: 泰利霉素片(肯立克)
生产厂家: Aventis
药品说明
泰利霉素为第一个获准应用于临床的酮内酯类药物，体外试验显示对呼吸道病原菌，包括耐青霉素和大环内酯类／氮环类肺炎链球菌具有良好活性。半衰期长，社区获得性感染每天只需口服给药1次。替利霉素为CYP3A4的底物，能够抑制CYP3A4代谢的药物。轻中度消化道不良反应发生率较高。对照试验证明，替利霉素治疗社区获得性肺炎、急性副鼻窦炎、慢性支气管炎急性加剧和咽喉炎等所取得的临床和病原有效率与现有抗菌药物近似甚至更好，尤其是对耐青霉素和红霉素肺炎链球菌引起的呼吸道感染也可能取得良好疗效。
泰利霉素的作用机制与大环内酯类相似，即与细菌核糖体50S亚单位结合，并终止其蛋白合成，为一用于治疗对大环内酯类耐药细菌感染的新型大环内酯类药物。泰利霉素含有1、12环氨基甲酸盐，与红霉素A和芳香烃或芳香丙烯链的2个羟基团连接，其在体外抗菌活性与新型大环内酯类相同甚至更强，对多种病原核糖体的结合力比大环内酯类强6~10倍。
泰利霉素（每日800mg口服剂量）已经获准用于治疗18岁以上的轻中度社区获得性肺炎（CAP）、慢性支气管炎急性发作（AECB）、急性鼻窦炎以及A组β链球菌引起的扁桃体炎／咽炎患者，12岁以上不能使用β-内酰胺类抗生素治疗的病人也可替代使用该药。泰利霉素不仅对耐药的肺炎链球菌有效，而且比目前使用的抗生素更容易耐受，安全性也更高。Ⅲ期临床研究显示，报道最多的泰利霉素相关药物不良反应包括腹泻、恶心、头晕和呕吐。
泰利霉素对上下呼吸道感染都非常有效，包括那些耐药致病菌引起的感染由每日一次的短程治疗也可见显著疗效。泰利霉素属大环内酯－林可霉素－链阳性菌素（MLSb）类抗生素。体外实验（与实际临床情况未必相关）资料显示，Ketek通过结合核糖体的两个不同位点、抑制核糖体的蛋白装配来减少细菌繁殖必需的蛋白合成而发挥其抗菌作用。
上市情况
欧洲委员会于2001年7月授权允许泰利霉素投入市场。该药获准用于治疗社区获得性上下呼吸道感染，包括那些对常用抗生素耐药的细菌感染。泰利霉素也在墨西哥投入使用。
分类名称
一级分类：抗生素 二级分类：大环内酯类 三级分类：
药品英文名
Telithromycin
药品别名
Ketek、HMR3647
药物剂型
片剂: 300mg，400mg。
药理作用
本品抗菌谱类似于红霉素，但本品对野生型细菌核糖体的结合力较红霉素和克拉霉素强，分别为10倍及6倍；抗菌作用比阿奇霉素强。对其他大环内酯类抗生素耐药的细菌，本品尚可能有效。
药动学
口服吸收良好，生物利用度约57%，吸收不受食物影响。在肝脏大部分被CYP3A4代谢成4种代谢产物。原形药物的肾清除率为每小时12.5L，半衰期约10h。在肝功能不全者其半衰期可延长1.4倍。
适应证
主要用于敏感菌所致的呼吸道感染，包括社会获得性肺炎、慢性支气管炎、急性上颌窦咽炎及扁桃体炎。
禁忌证
对本品过敏者禁用。
注意事项
对轻度肝、胆、肾损伤者不需调整剂量。本品对心电图Q-T间期无明显影响。本品可被嗜中性多形核细胞高度浓缩，较其他细胞浓度高约300倍，提示本品易被细胞内细菌吞噬。
不良反应
1.本品耐受性良好，不良反应少且轻，多为轻、中度，发生率为4.0%。常见恶心、呕吐、腹痛、腹泻、头晕、头痛、尿痛、皮疹、瘙痒等。
2.少见咳嗽、疲乏、呼吸困难、哮喘、鼻炎等。
用法用量
每天1次800mg，疗程5～10天。
药物相应作用
本品不影响华法林的药动学参数，也不影响避孕药的效果。氢氧化铝、西咪替丁、雷尼替丁等不影响本品的生物利用度。抗真菌药酮康唑、伊曲康唑可分别增加本品的药-时曲线下面积约2倍或1.5倍，其他大环内酯类抗生素、西沙比利、辛伐他汀、咪哒唑仑等也有类似作用。
专家点评
本品为酮内酯类抗生素，是红霉素的6-O-甲基-3-酮衍生物。是一种专门用于治疗呼吸道感染的抗生素。对耐青霉素类抗生素和耐大环内酯类抗生素菌株也敏感。国外报道，1373例呼吸系统感染患者经本品连续7～10天治疗，临床治愈率为93%～94%，与服用阿莫西林1次1000mg，每天3次、连续10天的疗效相似，有效率分别为95%和90%，细菌学清除率对金黄色葡萄球菌为95%、流感嗜血杆菌为90%。另一报道，本品每次800mg，每天1次，连续5天治疗慢性支气管炎急性发作与服用头孢呋辛酯每次500mg，每天2次，连续10天的疗效相似，治愈率分别为86%和83%，细菌学清除率为76%和79%。
Ketek (telithromycin)
Company: Sanofi-aventis
Approval Status: Approved April 2004
Treatment for: Respiratory Infections
Areas: Immunology/Infectious Diseases; Pulmonary/Respiratory Diseases
General Information
Ketek oral tablets contain telithromycin, a semisynthetic antibacterial in the ketolide class.
The antibacterial kills many of the types of bacteria that can infect the lungs and
sinuses, and has been found to treat these infections safely.
The drug was designed to deliver targeted coverage in community-acquired upper and lower respiratory tract infections.
Ketek tablets are indicated for the treatment of infections caused by the following:
Acute bacterial exacerbation of chronic bronchitis due to Streptococcus pneumoniae, Haemophilus influenzae, or Moraxella catarrhalis.
Acute bacterial sinusitis due to Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, or Staphylococcus aureus Community-acquired pneumonia due to Streptococcus pneumoniae.
Clinical Results
FDA approval of Ketek for the treatment of community-acquired pneumonia (CAP) was based on eight clinical trials enrolling a total of 2,016 subjects.
These included four randomized, double-blind, controlled studies and four open-label studies.
Results showed that of the 333 evaluable subjects with CAP due to Streptococcus pneumoniae, 312 or 93.7% achieved clinical success.
FDA approval of Ketek for the treatment of acute sinusitis was based on two randomized, double-blind, comparative studies.
Results showed that subjects who received Ketek showed a clinical cure rate at post-therapy follow-up of 75.3% compared with 74.5% for subjects who received the comparator drug(amoxicillin/clavulanic acid). Data showed that subjects who received Ketek showed a clinical cure rate at post-therapy follow-up of 85.2% compared with 82.0% for subjects who
received the comparator drug (cefuroxime axetil). A third study compared 5 days with 10 days of KETEK for the treatment of acute bacterial sinusitis, clinical cure rates for the two treatments were similar (91.1% vs. 91.0% respectively).
FDA approval of Ketek for the treatment exacerbation of chronic bronchitis was based on three randomized, double-blind, controlled studies.
Results showed that subjects who received Ketek showed a clinical cure rate at post-therapy follow- up of 86.4% compared with 83.1% for subjects who received the comparator drug (cefuroxime axetil). Data showed that subjects who received Ketek showed a clinical cure rate at post-therapy follow- up of 86.1% compared with 82.1% for subjects who received the comparator drug (amoxicillin/clavulanic).
Side Effects
Adverse events associated with the use of Ketek may include (but are not limited to) the following:
Diarrhea
Nausea
Headache
Dizziness
Vomiting
Loose Stools
Dysgeusia
Mechanism of Action
Telithromycin blocks protein synthesis by binding to domains II and V of 23S rRNA of the 50S ribosomal subunit. By binding at domain II, telithromycin retains activity against
gram-positive cocci (e.g., Streptococcus pneumoniae) in the presence of resistance mediated by methylases (erm genes) that alter the domain V binding site of telithromycin.
Telithromycin may also inhibit the assembly of nascent ribosomal units.
附件：
201151120311440.pdf
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注：以下产品不同规格和不同价格，购买时请以电话咨询为准！
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产地国家: 美国
原产地英文商品名:
KETEK 400mg/tab 60tabs/bottle
原产地英文药品名:
TELITHROMYCIN
中文参考商品译名:
肯立克 400毫克/片 60片/瓶
中文参考药品译名:
泰利霉素
生产厂家中文参考译名:
赛诺菲安万特
生产厂家英文名:
SANOFI AVENTIS US
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产地国家: 美国
原产地英文商品名:
KETEK 300mg/tab 60tabs/bottle
原产地英文药品名:
TELITHROMYCIN
中文参考商品译名:
肯立克 300毫克/片 60片/瓶
中文参考药品译名:
泰利霉素
生产厂家中文参考译名:
赛诺菲安万特
生产厂家英文名:
SANOFI AVENTIS US | 
