药品详细
Levofloxacin (左氧氟沙星 )
化学结构式图
中文名
左氧氟沙星
英文名
Levofloxacin
分子式
Not Available
化学名
(2S)-7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.0^{5,13}]trideca-5,7,9(13),11-tetraene-11-carboxylic acid
分子量
Average: 361.3675
Monoisotopic: 361.143784348
Monoisotopic: 361.143784348
CAS号
100986-85-4
ATC分类
J01M 未知;S01A 抗感染药
药物类型
small molecule
阶段
商品名
Cravit;Cravit Ophthalmic;Elequine;Floxel;Iquix;Leroxacin;Lesacin;Levaquin;Levokacin;Levox;Levoxacin;Mosardal;Nofaxin;Quixin;Reskuin;Tavanic;Volequin;
同义名
L-Ofloxacin;levofloxacin;
基本介绍
A synthetic fluoroquinolone (fluoroquinolones) antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. [PubChem]
生产厂家
- Ortho mcneil janssen pharmaceuticals inc
- Ortho mcneil pharmaceutical inc
- Santen inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Solution | Intravenous | 125 mg/5 ml |
| Tablet, film coated | Oral | 250 mg |
| Tablet, film coated | Oral | 500 mg |
| Tablet, film coated | Oral | 750 mg |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Iquix 1.5% Solution 5ml Bottle | 81.68 USD | bottle |
| Levofloxacin hemihydr 100% powder | 42.69 USD | g |
| Levaquin 750 mg tablet | 28.06 USD | each |
| Levaquin 750 mg leva-pak tablet | 27.51 USD | tablet |
| Levaquin 500 mg tablet | 16.57 USD | tablet |
| Iquix 1.5% eye drops | 15.71 USD | ml |
| Levaquin 250 mg tablet | 13.71 USD | tablet |
| Quixin 0.5% eye drops | 12.21 USD | ml |
| Quixin 0.5% Solution | 11.4 USD | ml |
| Levaquin i.v. 25 mg/ml vial | 1.94 USD | ml |
| Levaquin 500 mg/100 ml d5w | 0.44 USD | ml |
化合物类型
| Type | small molecule |
| Classes |
|
| Substructures |
|
适应症
antibacterials 抗细菌;
药理
| Indication | For the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms: Corynebacterium species, Staphylococus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus (Groups C/F/G), Viridans group streptococci, Acinetobacter lwoffii, Haemophilus influenzae, Serratia marcescens. |
| Pharmacodynamics | Levofloxacin, a fluoroquinolone antiinfective, is the optically active L-isomer of ofloxacin. Levofloxacin is used to treat bacterial conjunctivitis, sinusitis, chronic bronchitis, community-acquired pneumonia and pneumonia caused by penicillin-resistant strains of Streptococcus pneumoniae, skin and skin structure infections, complicated urinary tract infections and acute pyelonephritis. |
| Mechanism of action | Levofloxacin inhibits bacterial type II topoisomerases, topoisomerase IV and DNA gyrase. Levofloxacin, like other fluoroquinolones, inhibits the A subunits of DNA gyrase, two subunits encoded by the gyrA gene. This results in strand breakage on a bacterial chromosome, supercoiling, and resealing; DNA replication and transcription is inhibited. |
| Absorption | Absorption of ofloxacin after single or multiple doses of 200 to 400 mg is predictable, and the amount of drug absorbed increases proportionately with the dose. |
| Volume of distribution | Not Available |
| Protein binding | 24-38% (to plasma proteins) |
| Metabolism |
Mainly excreted as unchanged drug (87%); undergoes limited metabolism in humans. |
| Route of elimination | Mainly excreted as unchanged drug in the urine. |
| Half life | 6-8 hours |
| Clearance | Not Available |
| Toxicity | Side effects include disorientation, dizziness, drowsiness, hot and cold flashes, nausea, slurring of speech, swelling and numbness in the face |
| Affected organisms |
|
| 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 |
|---|---|
| Acenocoumarol | The quinolone antibiotic, levofloxacin, may increase the anticoagulant effect of acenocoumarol. |
| Aluminium | Formation of non-absorbable complexes |
| Amiodarone | Increased risk of cardiotoxicity and arrhythmias |
| Anisindione | The quinolone antibiotic, levofloxacin, may increase the anticoagulant effect of anisindione. |
| Artemether | Additive QTc-prolongation may occur. Concomitant therapy should be avoided. |
| Bepridil | Increased risk of cardiotoxicity and arrhythmias |
| Bretylium | Increased risk of cardiotoxicity and arrhythmias |
| Calcium | Formation of non-absorbable complexes |
| Chlorpromazine | Increased risk of cardiotoxicity and arrhythmias |
| Dicumarol | The quinolone antibiotic, levofloxacin, may increase the anticoagulant effect of dicumarol. |
| Dihydroquinidine barbiturate | Increased risk of cardiotoxicity and arrhythmias |
| Disopyramide | Increased risk of cardiotoxicity and arrhythmias |
| Erythromycin | Increased risk of cardiotoxicity and arrhythmias |
| Fluphenazine | Increased risk of cardiotoxicity and arrhythmias |
| Iron | Formation of non-absorbable complexes |
| Iron Dextran | Formation of non-absorbable complexes |
| Josamycin | Increased risk of cardiotoxicity and arrhythmias |
| Lumefantrine | Additive QTc-prolongation may occur. Concomitant therapy should be avoided. |
| Magnesium | Formation of non-absorbable complexes |
| Magnesium oxide | Formation of non-absorbable complexes |
| Mesoridazine | Increased risk of cardiotoxicity and arrhythmias |
| Methotrimeprazine | Increased risk of cardiotoxicity and arrhythmias |
| Perphenazine | Increased risk of cardiotoxicity and arrhythmias |
| Procainamide | Levofloxacin may increase the effect of procainamide. |
| Prochlorperazine | Increased risk of cardiotoxicity and arrhythmias |
| Promazine | Increased risk of cardiotoxicity and arrhythmias |
| Promethazine | Increased risk of cardiotoxicity and arrhythmias |
| Propiomazine | Increased risk of cardiotoxicity and arrhythmias |
| Quinidine | Increased risk of cardiotoxicity and arrhythmias |
| Quinidine barbiturate | Increased risk of cardiotoxicity and arrhythmias |
| Quinupristin | This combination presents an increased risk of toxicity |
| Sotalol | Increased risk of cardiotoxicity and arrhythmias |
| Sucralfate | Formation of non-absorbable complexes |
| Tacrolimus | Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. |
| Thiethylperazine | Increased risk of cardiotoxicity and arrhythmias |
| Thioridazine | Increased risk of cardiotoxicity and arrhythmias |
| Thiothixene | May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. |
| Toremifene | Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration. |
| Trifluoperazine | Increased risk of cardiotoxicity and arrhythmias |
| Triflupromazine | Increased risk of cardiotoxicity and arrhythmias |
| Trimipramine | Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. |
| Voriconazole | Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). |
| Vorinostat | Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). |
| Warfarin | The quinolone antibiotic, levofloxacin, may increase the anticoagulant effect of warfarin. |
| Zinc | Formation of non-absorbable complexes |
| Ziprasidone | Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated. |
| Zuclopenthixol | Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). |
食物相互作用
- Take without regard to meals. Take with water, drink lliberally. Taking this product with orange juice can result in reduced quinolone plasma levels.
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