简介：

部份中文斯沃处方资料（仅供参考）
药品英文名 Linezolid
药品别名 奈唑利得、Zyvox
药物剂型
1.片剂：200mg；
2.注射剂：200mg(100ml)，400mg(200ml)；
3.混悬液：100mg(5ml)。 药理作用
本品特点为对肠球菌和葡萄球菌起抑菌作用，对链球菌的多数菌株起杀菌作用。也可用于耐甲氧西林金黄色葡萄球菌(MR-SA)经用万古霉素(去甲万古霉素)无效的病例。本品的应用需严格掌握适应证，避免不适当的广泛应用，促使细菌耐药性的发展(耐万古霉素肠球菌对其他抗生素均耐药，本品是目前惟一有效的治疗药物)。
药动学
本品口服吸收完全，口服400mg，约1.5h血药浓度达峰值，Cmax为8～10mg/L，高脂饮食可降低本品血药浓度，但AUC相近。静脉滴注600mg，滴注完毕血药浓度为12.9mg/L，认为口服与静脉滴注间不必调整给药剂量，血浆蛋白结合率约31%，表观分布容积为40～50L。体内代谢成无效代谢产物。代谢物30%由尿液、10%由粪便排泄。半衰期为4.4～5.2h。
适应证
主要用于控制耐万古霉素肠球菌所致的系统感染，包括败血症、肺炎等。
禁忌证
1.对本品过敏者。
2.孕妇和哺乳期妇女。
 注意事项
1.孕妇和哺乳期妇女慎用。
2.使用本品要严格掌握适应证，避免滥用，严防耐药菌株的产生(耐万古霉素肠球菌对其他抗生素均耐药，本品是目前惟一有效药物)。
3.有高血压病史者使用本品应注意观察。
不良反应
不良反应有消化道症状，失眠、头晕、药物热、皮疹等。实验室检查可见血小板减少、尚有白细胞、中性粒细胞减少，AST、ALT、LDH、ALP、淀粉酶、总胆红素、BUN和肌酐等变化。
用法用量
口服与静脉滴注的剂量相同。每次600mg，每12小时1次，依病情连用10～28天。
药物相应作用
本品有MAO抑制作用，禁忌与拟肾上腺素药物(伪麻黄碱、多巴胺、肾上腺素等)和5-HT再摄取抑制药(如抗抑郁药)合用、禁用含酪胺食物(奶酪、肉干等)和某些含醇饮料(啤酒、红酒等)，以免引起血压异常升高。
临床研究
本品为唑酮类抗菌药。临床主要用于控制耐万古霉素肠球菌所致的系统感染，包括肺炎、败血症等。
完整资料附件：
http://www.info.pmda.go.jp/go/pack/6249002F1024_4_10/

Zy Box: Adapted to MRSA infection Expansion
On April 20, 2006, the addition of indication for "methicillin-resistant Staphylococcus aureus infection (MRSA) infection" was newly approved for synthetic antimicrobial linezolid (product name: ZYBOX tablet 600 mg, same injection 600 mg) The package insert was also revised (right picture). Specifically, in addition to the previous indications "various infections caused by vancomycin-resistant enterococci", "MRSA-induced pulmonary disease, deep skin infection, chronic pyoderma, trauma / burn injury, and surgical wound Secondary infection, such as pneumonia "has been added.
In May 2001, Linezolid was approved and released orally (tablets) and injections (intravenous drip infusion) as an antibacterial agent for the first time in Japan to obtain indication for vancomycin-resistant enterococci. Since the 1980s, MRSA, a type of multidrug-resistant bacteria, became a problem as a cause of nosocomial infection, but at the time vancomycin hydrochloride (trade name: vancomycin hydrochloride) appeared as the specific medicine. However, due to frequent use of the same drugs, vancomycin-resistant enterococci emerged from around 1990 in the United States and from 1996 in Japan. It was Linezolid that appeared as its "trump card".
This linezolid also expanded the indication for MRSA infection this time. In addition to the above-mentioned vancomycin, arbekacin sulfate (trade name: Havekacin), Teicoplanin (trade name: Tagosid) is currently available in Japan, and Linezolid is the fourth agent , It is the first drug for oral administration. Since linezolid is unique in its mechanism of action, it is characterized by showing no cross-resistance with other antimicrobials, including three anti-MRSA drugs already on sale.
In the United States where linezolid was developed, it has already been widely used clinically because it has strong antibacterial activity against gram-positive bacteria and has high utility for MRSA infection. In addition, (1) it is not necessary to adjust dosage and dose in (1) renal hypofunctional case, (2) since the bioavailability of the tablet is almost 100%, it is the same for intravenous administration or oral administration It can also be switched by dose - also features pharmacokinetic aspects.
Thus, linezolid is easier to use than existing anti-MRSA drugs and is the first oral agent for the treatment of MRSA infection, there is a possibility that frequency of use will increase in the future. On the other hand, however, since the same medicine will continue to be positioned as the final therapeutic agent for vancomycin-resistant enterococci, it is pointed out that the proper use is restricted, such as restricting the use strictly to avoid the appearance of resistant bacteria Has been done.
In terms of side effects, although the onset of renal injury like the existing anti-MRSA drugs is small, the incidence of bone marrow suppression such as thrombocytopenia tends to increase with administration for 14 days or more. Based on this, on the package insert of linezolid, patients who already had bone marrow suppression prior to administration, patients who need to be combined with drugs with myelosuppressive action, other antibiotics to treat infections already For patients who are being administered, patients requiring administration for more than 14 days, it is necessary to carefully administer it and perform blood tests once a week including cases where it is administered to other patients . Also, during the administration period, patients should be checked at all times to prevent bone marrow suppression.
Furthermore, when administered for 28 days or more, optic nerve injury develops and sometimes progresses to loss of visual acuity, so even for severe infections in principle, administration limit is 28 days. In the package insert in Japan, the recommended administration period is not stated, but in the US linezolid package insert, 10 to 14 days for various MRSA infections and 14 to 28 for VRE infection (including coinfection of bacteremia) Day is recommended.