部份中文利奈唑胺信息（仅供参考）
通用名：利奈唑胺
英文名：Linezolid
剂型：
利萘唑胺注射液：200mg／100ml；400mg／200ml 600mg／300ml.
利萘唑胺片：400mg／片；600mg／片。
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。
包装规格：
片剂：600mg*20
注射剂：200mg/100ml
Linezolid(Film Coated Tablets)
Composition:
Each film coated tablet contains 600mg Linezolid.
Mechanism of Action:
Linezolid is an oxazolidinone antibacterial, is active against Gram-positive bacteria including methicillin-resistant staphylococcus aureus (MRSA), and vancomycin-resistant enterococci. It’s effective mainly against aerobic gram-positive bacteria, but in vitro it has certain activity against gram-negative bacteria and anaerobic bacteria.
Linezolid is not sufficiently active against common gram-negative organisms. Linezolid inhibits bacterial protein synthesis through a mechanism of action different from that of other antibacterial agents. Therefore, cross-resistance between Linezolid and other classes of antibiotics is unlikely. Linezolid binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, which is an essential component of the bacterial translation process. Linezolid should be reserved for infections resistant to other antibacterial, or when other antibacterial are not tolerated.
Indications:
Vancomycin- resistant enterococcus faecium infection, and including cases with concurrent bacteremia. Nosocomial pneumonia caused by staphylococcus aureus (methicillin-susceptible and resistant strains), or streptococcus pneumoniae (penicillin-susceptible strains only). Combination therapy may be clinically indicated if the documented or presumptive pathogens include gram-negative organisms. Complicated skin and skin structure infections caused by staphylococcus aureus (methicillin-susceptible and resistant strains), streptococcus pyogenes, or streptococcus agalactiae. Linezolid can be used in the treatment of diabetic foot and decubitus ulcers.
Dosage and administration:
Linezolid is indicated for adults or children over 12 years (Linezolid may be taken with or without food).
| Infection |
Dosage |
Recommended period |
|
600mg |
14 – 28 days |
|
600mg |
10 – 14 days |
|
400mg |
10 – 14 days |
In case of over dosage, hemodialysis facilitates rapidly the elimination of Linezolid.
Side Effects:
Diarrhea (antibiotic-associated colitis), nausea, vomiting, taste disturbances, headache, rash, insomnia.
Contraindications:
Hypersensitivity to Linezolid.
Drug Interactions:
Linezolid is a reversible, nonselective inhibitor of monoamine oxidase, it should not be given with another MAOI or within 2 weeks of stopping another MAOI. Unless close observation and blood pressure monitoring is possible, avoid in those receiving SSRIS, 5HT1 agonists (triptans), tricyclic antidepressants, sympathomimetic, dopaminergics, buspirone, pethidine and possibly other opioid analgesics.
Precautions:
Myelosuppression has been reported in patients receiving Linezolid, blood counts should be monitored weekly in patients who are at increased risk for bleeding, who have pre-existing thrombocytopenia, who receive concomitant medications that may decrease platelet count or blood count or who may require longer than 2 weeks of Linezolid therapy, or who have pre-existing myelosuppression, or who have severe renal impairment.
Use in Pregnancy or Lactation:
Category C (There are no adequate and well controlled studies in pregnant women). It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
The drug is excreted in human milk, caution should be exercised when Linezolid is administered to nursing women.
Pharmacokinetic:
Linezolid is rapidly and extensively absorbed after oral dosing. Maximum plasma concentrations are reached approximately 1 to 2 hours after dosing, and the absolute bioavailability is approximately 100%.
Information for patients:
1.They should inform their physician if they have a history of hypertension.
2.Linezolid is a reversible, non-selective monoamine oxidase inhibitor; patients should avoid consuming large amounts of foods or beverages with high tyramine while taking Linezolid. Tyramine-rich food such as mature cheese, yeast extracts, alcoholic beverages and fermented soya bean products meal.
3.They should inform their physician if they are taking medications containing pseudoephedrine HCL, or serotonin re-uptake inhibitors or other antidepressants.
Presentation:
Carton pack contains 2 blisters of 10 tablets in each, with leaflet.