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QuickView for Gemifloxacin (compound)


PubChem
Name: gemifloxacin
PubChem Compound ID: 11352253
Molecular formula: C19H24FN5O7S
Molecular weight: 487.48 g/mol
DrugBank
Identification
Name: gemifloxacin
Name (isomeric): DB01155
Drug Type: small molecule
Synonyms:
Gemifloxacin mesilate; gemifloxacin mesylate
Brand: Factive
Category: Anti-Bacterial Agents, Quinolones
CAS number: 175463-14-6
Pharmacology
Indication: For the treatment of bacterial infection caused by susceptible strains such as <i>S. pneumoniae</i>, <i>H. influenzae</i>, <i>H. parainfluenzae</i>, or <i>M. catarrhalis</i>, <i>S. pneumoniae</i> (including multi-drug resistant strains [MDRSP]), <i>M. pneumoniae</i>, <i>C. pneumoniae</i>, or <i>K. pneumoniae</i>.
Pharmacology:
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 D...
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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%.
Protein binding: 60-70%
Biotransformation: 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 (± SD) of 61 ± 9.5% of the dose was excreted in the feces and 36 ± 9.3% in the urine as unchanged drug and metabolites. The mean (± SD) renal clearance following repeat doses of 320 mg was approximately 11.6 ± 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: renal cl=11.6+/- 3.9 L/hr [Healthy subjects receiving repeat doses of 320 mg orally]
Affected organisms: Enteric bacteria and other eubacteria
Interactions
Food interaction:
Take without regard to meals.
Drug interaction:
Calcium AcetateCalcium salts such as calcium acetate may decrease the absorption of quinolone antibiotics such as gemifloxacin. Of concern only with oral administration of both agents. Interactions can be minimized by administering oral quinolone at least 2 hours before, or 6 hours after, the dose of an oral calcium supplement. Monitor for decreased therapeutic effects of oral quinolones if administered with oral calcium supplements.
MagnesiumFormation of non-absorbable complexes
AluminiumFormation of non-absorbable complexes
Iron DextranFormation of non-absorbable complexes
IronFormation of non-absorbable complexes
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Targets