药品详细
Lomefloxacin (洛美沙星 )
化学结构式图
中文名
洛美沙星
英文名
Lomefloxacin
分子式
Not Available
化学名
1-ethyl-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
分子量
Average: 351.3479
Monoisotopic: 351.139447899
Monoisotopic: 351.139447899
CAS号
98079-51-7
ATC分类
J01M 未知;S01A 抗感染药
药物类型
small molecule
阶段
商品名
Bareon;Maxaquin;
同义名
LFLX;lomefloxacin hydrochloride;Lomefloxacine [French];Lomefloxacino [Spanish];Lomefloxacinum [Latin];
基本介绍
Lomefloxacin is a fluoroquinolone antibiotic, used to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery.
生产厂家
- Pharmacia corp
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Tablet | Oral |
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
antibacterials 抗细菌;
药理
| Indication | For the treatment of bacterial infections of the respiratory tract (chronic bronchitis) and urinary tract, and as a pre-operative prophylactic to prevent urinary tract infection caused by: S.pneumoniae, H.influenzae, S.aureus, P.aeruginosa, E. cloacae, P. mirabilis, C. civersus, S. asprphyticus, E.coli, and K.pneumoniae. |
| Pharmacodynamics | Lomefloxacin is a fluoroquinolone antibiotic used to treat chronic bronchitis, as well as complicated and uncomplicated urinary tract infections. It is also used as a prophylactic or preventative treatment to prevent urinary tract infections in patients undergoing transrectal or transurethral surgical procedures. Flouroquinolones such as lomefloxacin possess excellent activity against gram-negative aerobic bacteria such as E.coli and Neisseria gonorrhoea as well as gram-positive bacteria including S. pneumoniae and Staphylococcus aureus. They also posses effective activity against shigella, salmonella, campylobacter, gonococcal organisms, and multi drug resistant pseudomonas and enterobacter. |
| Mechanism of action | Lomefloxacin is a bactericidal fluoroquinolone agent with activity against a wide range of gram-negative and gram-positive organisms. The bactericidal action of lomefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited. |
| Absorption | Rapid and nearly complete with approximately 95% to 98% of a single oral dose being absorbed. |
| Volume of distribution | Not Available |
| Protein binding | 10% |
| Metabolism |
Minimally metabolized although 5 metabolites have been identified in human urine. 65% appears as the parent drug in urine and 9% as the glucuronide metabolite. |
| Route of elimination | The urinary excretion of lomefloxacin was virtually complete within 72 hours after cessation of dosing, with approximately 65% of the dose being recovered as parent drug and 9% as its glucuronide metabolite. |
| Half life | 8 hours |
| Clearance |
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| Toxicity | Adverse reactions include peripheral neuropathy, nervousness, agitation, anxiety, and phototoxic events (rash, itching, burning) due to sunlight exposure. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | 239-240.5 oC | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Calcium | Formation of non-absorbable complexes |
| Iron Dextran | Formation of non-absorbable complexes |
| Magnesium | Formation of non-absorbable complexes |
食物相互作用
Not Available
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