Identification | |||||||||||||||||||||
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Name | Gemifloxacin | ||||||||||||||||||||
Accession Number | DB01155 (APRD00053) | ||||||||||||||||||||
Type | small molecule | ||||||||||||||||||||
Description | Gemifloxacin is an oral broad-spectrum quinolone antibacterial agent used in the treatment of acute bacterial exacerbation of chronic bronchitis and mild-to-moderate pneumonia. Gemifloxacin acts by inhibiting DNA synthesis through the inhibition of both DNA gyrase and topoisomerase IV, which are essential for bacterial growth. | ||||||||||||||||||||
Structure |
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Categories (*) | |||||||||||||||||||||
Molecular Weight | 389.3809 | ||||||||||||||||||||
Groups | approved | ||||||||||||||||||||
Monoisotopic Weight | 389.149932358 | ||||||||||||||||||||
Pharmacology | |||||||||||||||||||||
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. | ||||||||||||||||||||
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. | ||||||||||||||||||||
Toxicity | Not Available | ||||||||||||||||||||
Affected organisms |
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Interactions | |||||||||||||||||||||
Drug Interactions |
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Food Interactions |
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DNA topoisomerase 4 subunit A | |
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Name | DNA topoisomerase 4 subunit A |
Gene Name | parC |
Pharmacological action | yes |
Actions | inhibitor |
References |
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DTHybrid score | 0.7501 |
DNA gyrase subunit A | |
Name | DNA gyrase subunit A |
Gene Name | gyrA |
Pharmacological action | yes |
Actions | inhibitor |
References |
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DTHybrid score | 0.7878 |
Id | Partner name | Gene Name | Score |
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6224 | DNA gyrase subunit A | gyrA | 0.7878 |
886 | DNA topoisomerase 4 subunit A | parC | 0.7501 |
6226 | DNA topoisomerase 4 subunit A | parC | 0.7501 |
817 | DNA topoisomerase 2-alpha | TOP2A | 0.3509 |
4200 | Cytochrome P450 1A2 | CYP1A2 | 0.1333 |
118 | Organic cation/carnitine transporter 2 | SLC22A5 | 0.0738 |
1729 | Solute carrier family 22 member 6 | SLC22A6 | 0.0655 |
1735 | Canalicular multispecific organic anion transporter 1 | ABCC2 | 0.0584 |
1588 | Multidrug resistance protein 1 | ABCB1 | 0.0411 |
4512 | Cytochrome P450 3A4 | CYP3A4 | 0.0309 |
833 | Organic cation/carnitine transporter 1 | SLC22A4 | 0.0292 |
862 | Multidrug resistance-associated protein 1 | ABCC1 | 0.024 |
6144 | Solute carrier family 22 member 2 | SLC22A2 | 0.0239 |
6107 | Cytochrome P450 3A7 | CYP3A7 | 0.021 |
4118 | Cytochrome P450 3A5 | CYP3A5 | 0.0197 |
5718 | Cytochrome P450 2A6 | CYP2A6 | 0.0098 |
6024 | Cytochrome P450 1A1 | CYP1A1 | 0.0094 |