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药品详细

Gatifloxacin (加替沙星 )

化学结构式图
中文名
加替沙星
英文名
Gatifloxacin
分子式
Not Available
化学名
1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
分子量
Average: 375.3941
Monoisotopic: 375.159434412
CAS号
112811-59-3
ATC分类
J01M 未知;S01A 抗感染药
药物类型
small molecule
阶段
商品名
Tequin;Zymar;
同义名
gatifloxacin;
基本介绍

Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Bristol-Myers Squibb introduced Gatifloxacin in 1999 under the proprietary name Tequin庐 for the treatment of respiratory tract infections, having licensed the medication from Kyorin Pharmaceutical Company of Japan. Allergan produces an eye-drop formulation called Zymar庐. Gatifloxacin is available as tablets and in various aqueous solutions for intravenous therapy. [Wikipedia]

生产厂家
  • Allergan
  • Allergan inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Park-Wyllie LY, Juurlink DN, Kopp A, Shah BR, Stukel TA, Stumpo C, Dresser L, Low DE, Mamdani MM: Outpatient gatifloxacin therapy and dysglycemia in older adults. N Engl J Med. 2006 Mar 30;354(13):1352-61. Epub 2006 Mar 1. Pubmed
  2. Gurwitz JH: Serious adverse drug effects—seeing the trees through the forest. N Engl J Med. 2006 Mar 30;354(13):1413-5. Epub 2006 Mar 1. Pubmed
剂型
Form Route Strength
Solution Ophthalmic
规格
Unit description Cost Unit
Zymar 0.3% Solution 5ml Bottle 87.53 USD bottle
Zymar 0.3% eye drops 16.75 USD ml
化合物类型
Type small molecule
Classes
  • Fluoroquinolones and Quinolones
  • Aminoquinolines and Derivatives
  • Hydroxyquinolines
Substructures
  • Hydroxy Compounds
  • Acetates
  • Aliphatic and Aryl Amines
  • Phenols and Derivatives
  • Pyridines and Derivatives
  • Piperazines
  • Fluoroquinolones and Quinolones
  • Cyclopropane and Derivatives
  • Ethers
  • Benzene and Derivatives
  • Aminoquinolines and Derivatives
  • Carboxylic Acids and Derivatives
  • Hydroxyquinolines
  • Halobenzenes
  • Heterocyclic compounds
  • Aromatic compounds
  • Anisoles
  • (Iso)quinolines and Derivatives
  • Aryl Halides
  • Phenyl Esters
  • Anilines
适应症
antibacterials 抗细菌;
药理
Indication For the treatment of bronchitis, sinusitis, community-acquired pneumonia, and skin infections (abscesses, wounds) caused by S. pneumoniae, H. influenzae, S. aureus, M. pneumoniae, C. pneumoniae, L. pneumophila, S. pyogenes
Pharmacodynamics Gatifloxacin is a synthetic broad-spectrum 8-methoxyfluoroquinolone antibacterial agent for oral or intravenous administration. 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. Gatifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
Mechanism of action The bactericidal action of Gatifloxacin 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 Well absorbed from the gastrointestinal tract after oral administration with absolute bioavailability of gatifloxacin is 96%
Volume of distribution Not Available
Protein binding 20%
Metabolism

Gatifloxacin undergoes limited biotransformation in humans with less than 1% of the dose excreted in the urine as ethylenediamine and methylethylenediamine metabolites
Route of elimination Not Available
Half life 7-14 hours
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Enteric bacteria and other eubacteria
Pathways Not Available
理化性质
Properties
State solid
Melting point 182-185 oC
Experimental Properties
Property Value Source
water solubility 60 mg/mL (at pH 4) PhysProp
logP 2.6 PhysProp
Predicted Properties
Property Value Source
water solubility 6.31e-01 g/l ALOGPS
logP -0.23 ALOGPS
logP -1.24 ChemAxon Molconvert
logS -2.77 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 7 ChemAxon Molconvert
hydrogen donor count 2 ChemAxon Molconvert
polar surface area 82.11 ChemAxon Molconvert
rotatable bond count 4 ChemAxon Molconvert
refractivity 98.82 ChemAxon Molconvert
polarizability 38.29 ChemAxon Molconvert
药物相互作用
Drug Interaction
Aluminium Formation of non-absorbable complexes
Amiodarone Increased risk of cardiotoxicity and arrhythmias
Bepridil Increased risk of cardiotoxicity and arrhythmias
Bretylium Increased risk of cardiotoxicity and arrhythmias
Chlorpromazine Increased risk of cardiotoxicity and arrhythmias
Digoxin Gatifloxacin increases the effect of digoxin
Dihydroquinidine barbiturate Increased risk of cardiotoxicity and arrhythmias
Disopyramide 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
Magnesium Formation of non-absorbable complexes
Magnesium oxide Formation of non-absorbable complexes
Magnesium salicylate 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
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).
Zinc Formation of non-absorbable complexes
Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
食物相互作用
  • Absorption does not seem to be affected by milk or calcium carbonate, however, gatifloxacin bioavailability appears significantly reduced when combined with Ensure™ (Cmax is reduced by about 50% while total drug exposure (AUC) is reduced by about 25%).
  • Drink liberally.
  • Take without regard to meals.

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