利奈唑胺
利奈唑胺(Linezolid)是第一个应用于临床的新型唑烷酮类抗菌药物。上市前的研究提示利奈唑胺对各类革兰阳性球菌具有高度抗菌活性,不良反应小且不易产...
利奈唑烷
53 6、利奈唑烷(Linezolid): 抗菌作用与万古霉素相似,对各类革兰氏阳 性菌包括耐药金葡菌和肠球菌,具有强大的抗 菌活性,对MRSA也有效。
雷奈佐利
述 : 中文名:雷奈佐利 英文名:Linezolid 别名:N-[[(5S)-3-[3-Fluoro-4-(4-Morpholinyl)Phenyl]-2-Oxo-5-Oxazolidinyl]Methyl]-
吗啉恶酮
...代)苯基]-2-氧代-5-恶唑烷基]甲基]乙酰胺的合成工艺 改进了R-(-)-丁酸缩水甘油酯的合成工艺 改进并转让了吗啉恶酮(Linezolid)的合成工艺 改进并转让了2′-脱氧胞苷的合成工艺 熟悉了仿制药物的立项,研发,材料的准备等程序。
Linezolid (INN, /lɪˈnɛzəlɪd/ li-NEZ-ə-lid or, less frequently, /lɪˈneɪzəlɪd/) is a synthetic antibiotic developed by a team at Pharmacia and Upjohn Company. It is used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to several other antibiotics.A member of the oxazolidinone class of drugs, linezolid is active against most Gram-positive bacteria that cause disease, including streptococci, vancomycin-resistant enterococci (VRE), and methicillin-resistant Staphylococcus aureus (MRSA). The main indications of linezolid are infections of the skin and soft tissues and pneumonia (particularly hospital-acquired pneumonia), although off-label use for a variety of other infections is becoming popular. Linezolid is marketed by Pfizer under the trade names Zyvox (in the United States, United Kingdom, Australia, and several other countries), Zyvoxid (in Europe), and Zyvoxam (in Canada and Mexico). Generics are also available, such as Linospan (in India, by Cipla) and Linzolid (in Bangladesh, by Incepta).Discovered in the 1990s and first approved for use in 2000, linezolid was the first commercially available 1,3-oxazolidinone antibiotic. As of 2014[update], it along with tedizolid are the only marketed oxazolidinones, although others are in development. As a protein synthesis inhibitor, it stops the growth of bacteria by disrupting their production of proteins, that is, it is a bacteriostatic agent, not bacteriocidal. Although many antibiotics work this way, the exact mechanism of action of linezolid appears to be unique in that it blocks the initiation of protein production, and not one of the later steps. Bacterial resistance to linezolid has remained very low since it was first detected in 1999, although it may be increasing.When administered for short periods, linezolid is a relatively safe drug; it can be used in patients of all ages and in people with liver disease or poor kidney function. Common adverse effects of short-term use include headache, diarrhea, and nausea. Long-term use, however, has been associated with serious adverse effects; linezolid can cause bone marrow suppression and low platelet counts, particularly when used for more than two weeks. If used for longer periods still, it may cause sometimes irreversible chemotherapy-induced peripheral neuropathy and optic nerve damage, and lactic acidosis (a buildup of lactic acid in the body), all most likely due to mitochondrial toxicity.Linezolid costs approximately US$100 per tablet in the United States. Nonetheless, it appears to be more cost-effective than generic alternatives such as vancomycin, mostly because of the possibility of switching from intravenous to oral administration as soon as patients are stable enough, without the need for dose adjustments.