药品详细
Gemifloxacin (吉米沙星 )
化学结构式图
中文名
吉米沙星
英文名
Gemifloxacin
分子式
Not Available
化学名
7-[(4E)-3-(aminomethyl)-4-(methoxyimino)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
分子量
Average: 389.3809
Monoisotopic: 389.149932358
Monoisotopic: 389.149932358
CAS号
175463-14-6
ATC分类
J01M 未知
药物类型
small molecule
阶段
商品名
Factive;
同义名
Gemifloxacin mesilate;gemifloxacin mesylate;
基本介绍
Gemifloxacin is an oral broad-spectrum quinolone antibacterial agent used in the treatment of acute bacterial exacerbation of chronic bronchitis and mild-to-moderate pneumonia. Gemifloxacin acts by inhibiting DNA synthesis through the inhibition of both DNA gyrase and topoisomerase IV, which are essential for bacterial growth.
生产厂家
- Cornerstone therapeutics inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Tablet | Oral |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Factive 5 320 mg tablet Box | 148.08 USD | box |
| Factive 320 mg tablet | 28.48 USD | tablet |
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 infection caused by susceptible strains such as S. pneumoniae, H. influenzae, H. parainfluenzae, or M. catarrhalis, S. pneumoniae (including multi-drug resistant strains [MDRSP]), M. pneumoniae, C. pneumoniae, or K. pneumoniae. |
| Pharmacodynamics | Gemifloxacin is a quinolone/fluoroquinolone antibiotic. Gemifloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Gemifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. |
| Mechanism of action | The bactericidal action of gemifloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination. |
| Absorption | Rapidly absorbed from the gastrointestinal tract. The absolute bioavailability averages approximately 71%. |
| Volume of distribution |
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| Protein binding | 60-70% |
| Metabolism |
Gemifloxacin is metabolized to a limited extent by the liver. All metabolites formed are minor (<10% of the administered oral dose); the principal ones are N-acetyl gemifloxacin, the E-isomer of gemifloxacin and the carbamyl glucuronide of gemifloxacin. |
| Route of elimination | Gemifloxacin and its metabolites are excreted via dual routes of excretion.Following oral administration of gemifloxacin to healthy subjects, a mean (卤 SD) of 61 卤 9.5% of the dose was excreted in the feces and 36 卤 9.3% in the urine as unchanged drug and metabolites. The mean (卤 SD) renal clearance following repeat doses of 320 mg was approximately 11.6 卤 3.9 L/hr (range 4.6-6 L/hr), which indicates active secretion is involved in the renal excretion of gemifloxacin. |
| Half life | 7 (± 2) hours |
| Clearance |
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| Toxicity | Not Available |
| Affected organisms |
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| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | Not Available | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Aluminium | Formation of non-absorbable complexes |
| Iron | Formation of non-absorbable complexes |
| Iron Dextran | Formation of non-absorbable complexes |
| Magnesium | Formation of non-absorbable complexes |
| Magnesium oxide | Formation of non-absorbable complexes |
| Magnesium salicylate | Formation of non-absorbable complexes |
| Sucralfate | Formation of non-absorbable complexes |
| Zinc | Formation of non-absorbable complexes |
食物相互作用
- Take without regard to meals.
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