药品信息: 部份中文Zyvox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。
专家点评
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。
English name drugs
Linezolid
Drug Aliases
Chennai azole profits, Zyvox
Pharmaceutical dosage forms
1 tablet: 200mg;
(2) Injection: 200mg (100ml), 400mg (200ml);
3 suspension:. 100mg (5ml).
Pharmacological effects
This product features for the enterococci and staphylococci from the inhibitory effect of most strains of Streptococcus bactericidal effect. Can also be used for methicillin-resistant Staphylococcus aureus (MR-SA) by the use of vancomycin (norvancomycin) valid cases. Application of this product requires strict indications, avoid undue widely used to promote the development of bacterial resistance to antibiotics (vancomycin-resistant enterococci are resistant to other antibiotics, this product is currently the only effective treatment).
Pharmacokinetics
This product is completely absorbed orally, oral 400mg, about 1.5h peak plasma concentration, Cmax of 8 ~ 10mg / L, high-fat diet may reduce the plasma concentration of this product, but AUC similar. Intravenous infusion 600mg, drip finished plasma concentration of 12.9mg / L, considered between oral and intravenous do not have to adjust the dose, plasma protein binding rate of about 31%, the apparent volume of distribution of 40 ~ 50L. In vivo metabolism to inactive metabolites. Metabolites in the urine of 30%, 10% is excreted in the feces. Half-life of 4.4 ~ 5.2h.
Indications
System is mainly used to control vancomycin-resistant enterococci caused by infections, including sepsis and pneumonia.
Contraindications
1 who are allergic to the chemicals.
2 pregnant and lactating women.
Precautions
1. Pregnant and lactating women with caution.
2 FDA indications should be strictly controlled to avoid abuse, prevent drug resistant strains (vancomycin-resistant enterococci are resistant to other antibiotics, this product is currently the only effective drug).
3 The FDA has a history of hypertension should be observed.
Adverse reactions
Adverse reactions are gastrointestinal symptoms, insomnia, dizziness, drug fever, skin rash. Laboratory examination showed thrombocytopenia, there are white blood cells, neutropenia, AST, ALT, LDH, ALP, amylase, total bilirubin, BUN and creatinine and other changes.
Dosage
Oral and intravenous infusion of the same dose. Every 600mg, every 12 hours, depending on the condition once every 10 to 28 days.
Drug corresponding action
This product has MAO inhibition, Taboo and adrenergic drugs (pseudoephedrine, dopamine, epinephrine, etc.) and 5-HT reuptake inhibitors (such as antidepressants) combination, disabled tyramine-containing foods (cheese, meat, etc.) and certain beverages containing alcohol (beer, wine, etc.), so as not to cause abnormally elevated blood pressure.
Expert Comments
This product azole ketones antibacterials. The main clinical system for controlling vancomycin-resistant enterococci caused by infections, including pneumonia, septicemia. |