英文药名：ZYVOX Tablets（linezolid）

中文药名：利奈唑胺片

生产厂家：辉瑞公司
药物分类名称
恶唑烷酮合成抗菌剂
批准日期：2001年6月
商標名
ZYVOX Injection 600mg
一般名
リネゾリド（linezolid）
略号
LZD
化学名
(-)-N-[[(S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl]methyl]acetamide
分子式
C16H20FN3O4
分子量
337.35
構造式

性状
这是一种白色到微黄色的白色粉末。
溶于苯甲醇，微溶于乙腈，微溶于二氯甲烷，几乎不溶于乙醇（99.5）或水，难溶于己烷。
药效药理
1. 抗菌作用
(1)抗菌活性
利奈唑胺具有抗万古霉素耐药肠球菌（VRE）和耐甲氧西林金黄色葡萄球菌（MRSA）的抗菌活性。 在日本，美国和欧洲进行的研究中，利奈唑胺对VRE（屎肠球菌，粪肠球菌）和MRSA的MIC 90值均≤4μg/ mL（临床和实验室标准研究所（CLSI） 这相当于）。 由于粪肠球菌几乎没有临床经验，所以没有指出。
(2) 灵敏度测试方法和标准
在VRE和MRSA中，制造这种药物敏感细菌的测试方法和标准符合CLSI标准方法。
（见表6）
2. 耐性
(1)利奈唑胺与现有抗生素对VRE和MRSA的交叉耐药性尚无报道。
(2)在体外试验中，金黄色葡萄球菌和表皮葡萄球菌自然发生突变的频率为10-8至10-11。 在20个使用屎肠球菌和粪肠球菌的传代培养物中，通过增加药物的继代培养，在体外耐受性测试中，MIC为4μg/mL-8μg/ml和2μg/ml 至64μg/mL。 在金黄色葡萄球菌中，19次传代中从4μg/ mL到>64μg/mL的敏感性降低。
3. 作用机序
利奈唑胺与细菌核糖体结合，干扰翻译过程中70S起始复合物的形成并抑制细菌蛋白质合成。 另一方面，它不抑制多核糖体延长或肽键合成，其作用机制与常规抗菌药物不同。
表6.利奈唑胺的敏感性标准

病原菌	感受性判定基準 希釈法による最小発育阻止濃度（μg/mL） S	感受性判定基準 希釈法による最小発育阻止濃度（μg/mL） I	感受性判定基準 希釈法による最小発育阻止濃度（μg/mL） R	感受性判定基準 ディスク拡散法による阻止円径（mm） S	感受性判定基準 ディスク拡散法による阻止円径（mm） I	感受性判定基準 ディスク拡散法による阻止円径（mm） R
Enterococcus spp.	≦2	4	≧8	≧23	21-22	≦20
Staphylococcus spp.	≦4	－	≧8	≧21	－	≦20

S：易感性，I：中度耐受性，R：耐受性
适应病症
1. <适应的真菌种类>
对这种药物敏感的耐甲氧西林金黄色葡萄球菌（MRSA）
<适应症>
二次感染，如败血症，深层皮肤感染，慢性脓皮病，创伤·烧伤和手术创伤，肺炎
2. <适应性真菌种类>
对耐万古霉素屎肠球菌的敏感性
<适应症>
各种传染病
用法与用量
通常，对于12岁以上的成年人和儿童，每天1200毫克利奈唑胺被分成两剂，600毫克每12小时一次口服。
通常，12岁以下儿童每8小时口服利奈唑胺10mg / kg。 另外，单次剂量不应超过600毫克。
包装规格
片
600毫克：10片（PTP）

制造商
辉瑞公司
注：以上中文资料不够完整，使用者以原资料为准。
完整说明书附件：http://www.info.pmda.go.jp/go/pack/6249002F1024_4_10/
ZYVOX Injection（linezolid）ザイボックス
On April 20, 2006, the addition of indication for "methicillin-resistant Staphylococcus aureus infection (MRSA) infection" was newly approved for synthetic antimicrobial linezolid (trade name: ZYBOX tablet 600 mg, same injection 600 mg) The package insert was also revised (right picture). Specifically, in addition to the conventional 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 (tablet) and injection (intravenous drip infusion) as an antimicrobial agent that acquired the first indication for vancomycin-resistant enterococci in Japan. 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 drug, 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. Currently available anti-MRSA drugs in Japan are vancomycin sulfate (trade name: Havekacin), Teicoplanin (trade name: Tagosid), in addition to the aforementioned vancomycin, linezolid is the fourth agent for anti-MRSA drug injection , 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 the dosage and dose in (1) renal hypofunctional cases, (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.
In this way, linezolid is easier to use than existing anti-MRSA drugs and is the first oral agent for the treatment of MRSA infection, so the frequency of use may increase in the future. However, on the other hand, the same drug will continue to be positioned as the final therapeutic agent for vancomycin-resistant enterococci, so it is pointed out that the proper use is necessary, such as strictly limiting its use to avoid the appearance of resistant bacteria Has been done.
In terms of side effects, although the onset of renal injury like existing anti-MRSA drugs is small, the incidence of bone marrow suppression such as thrombocytopenia tends to increase with administration of 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 them and perform blood tests once a week including cases where they are administered to other patients . Also, during the administration period, patients should be confirmed at all times to try to prevent the development of myelosuppression.
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.