| 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 |
|
| 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 (± 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]
|
| Toxicity |
Not Available |
