QuickView for Gatifloxacin (compound)

Summary
General Info

PubChem

PubChem Compound 1150508

Name:	gatifloxacin
PubChem Compound ID:	1150508
Molecular formula:	C₁₉H₂₂FN₃O₄
Molecular weight:	375.394 g/mol

DrugBank

Identification

Name:	gatifloxacin
Name (isomeric):	DB01044
Drug Type:	small molecule
Brand:	Zymar, Tequin
Category:	Anti-Infective Agents, Quinolones, Antibiotics
CAS number:	112811-59-3

Pharmacology

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
Pharmacology:	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. Not... show more » 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. show less «
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%
Protein binding:	20%
Biotransformation:	Gatifloxacin undergoes limited biotransformation in humans with less than 1% of the dose excreted in the urine as ethylenediamine and methylethylenediamine metabolites
Half Life:	7-14 hours
Affected organisms:	Enteric bacteria and other eubacteria

Interactions

Food interaction:

Drink liberally.

Absorption does not seem to be affected by milk or calcium carbonate, however, gatifloxacin bioavailability appears significantly reduced when combined with Ensure™ (C_max is reduced by about 50% while total drug exposure (AUC) is reduced by about 25%).

Take without regard to meals.

Drug interaction:

Disopyramide	Increased risk of cardiotoxicity and arrhythmias
Promazine	Increased risk of cardiotoxicity and arrhythmias
Triflupromazine	Increased risk of cardiotoxicity and arrhythmias
Iron	Formation of non-absorbable complexes
Chlorpromazine	Increased risk of cardiotoxicity and arrhythmias

Disopyramide	Increased risk of cardiotoxicity and arrhythmias
Promazine	Increased risk of cardiotoxicity and arrhythmias
Triflupromazine	Increased risk of cardiotoxicity and arrhythmias
Iron	Formation of non-absorbable complexes
Chlorpromazine	Increased risk of cardiotoxicity and arrhythmias
Magnesium oxide	Formation of non-absorbable complexes
Bretylium	Increased risk of cardiotoxicity and arrhythmias
Zinc	Formation of non-absorbable complexes
Magnesium salicylate	Formation of non-absorbable complexes
Sucralfate	Formation of non-absorbable complexes
Digoxin	Gatifloxacin increases the effect of digoxin
Thiethylperazine	Increased risk of cardiotoxicity and arrhythmias
Magnesium	Formation of non-absorbable complexes
Dihydroquinidine barbiturate	Increased risk of cardiotoxicity and arrhythmias
Promethazine	Increased risk of cardiotoxicity and arrhythmias
Perphenazine	Increased risk of cardiotoxicity and arrhythmias
Methotrimeprazine	Increased risk of cardiotoxicity and arrhythmias
Sotalol	Increased risk of cardiotoxicity and arrhythmias
Mesoridazine	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.
Aluminium	Formation of non-absorbable complexes
Thioridazine	Increased risk of cardiotoxicity and arrhythmias
Vorinostat	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Bepridil	Increased risk of cardiotoxicity and arrhythmias
Prochlorperazine	Increased risk of cardiotoxicity and arrhythmias
Propiomazine	Increased risk of cardiotoxicity and arrhythmias
Quinidine barbiturate	Increased risk of cardiotoxicity and arrhythmias
Ziprasidone	Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
Quinupristin	This combination presents an increased risk of toxicity
Tacrolimus	Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Amiodarone	Increased risk of cardiotoxicity and arrhythmias
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.
Quinidine	Increased risk of cardiotoxicity and arrhythmias
Iron Dextran	Formation of non-absorbable complexes
Fluphenazine	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.
Trifluoperazine	Increased risk of cardiotoxicity and arrhythmias
Voriconazole	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).

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Targets

DNA gyrase subunit A

DNA gyrase subunit B

DNA topoisomerase 4 subunit A

DNA topoisomerase 4 subunit B

Carriers

Serum albumin