| Identification | Back Directory | [Name]
8-cyano-1-cyclopropyl-7-((1S,6S)-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid | [CAS]
195532-12-8 | [Synonyms]
Pradofloxacin
8-cyano-1-cyclopropyl-7-((1S,6S)-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
8-Cyano-1-cyclopropyl-6-fluoro-1,4-dihydro-7-[(4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid | [Molecular Formula]
C21H21FN4O3 | [MDL Number]
MFCD28127006 | [MOL File]
195532-12-8.mol | [Molecular Weight]
396.415 |
| Chemical Properties | Back Directory | [Melting point ]
246-248°C | [Boiling point ]
664.5±55.0 °C(Predicted) | [density ]
1.50±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
6.38±0.50(Predicted) | [color ]
Light yellow to yellow | [CAS DataBase Reference]
195532-12-8 |
| Hazard Information | Back Directory | [Uses]
Pradofloxacin is a novel fluoroquinolone antibiotic. An antimicrobial agent. | [Indications]
Dogs: Pradofloxacin is a novel third-generation fluoroquinolone currently approved in Europe to treat canine wound infections and superficial and deep pyoderma associated with susceptible strains of Staphylococcus pseudinterme- dius. However, it has shown lower minimal inhibitory concentration (MIC) when compared to various fluoroquinolones for the following organisms: Bordetella, Escherichia coli, Enterococcus, Klebsiella pneumonia, Staphylococcus, Staphy- lococcus pseudintermedius, Streptococcus, Pseudomonas, Proteus, Mycoplasma, Salmonella, and Pasteurella. Moreover, in contrast to other fluoroquinolones, pradofloxacin has shown excellent in-vitro activity against anaerobic bacteria isolated from dogs and cats. Pradofloxacin, concurrently with topical therapy, may also be of benefit for treatment of chronic ear infections, particularly otitis media, caused by susceptible organisms such as Pseudomonas. However, tissue concentration is not known for the external or middle ear, and this indication is controversial with unpredictable efficacy.
Note: The authors do not recommend the use of fluoroquinolones as first-line therapy for pyoderma. Fluoroquinolones should be considered primarily for chronic deep pyodermas associated with extensive scar tissue, because of their excellent tissue penetration. Antibiotic selection, however, should be based on culture and susceptibility results. | [Mechanism of action]
Pradofloxacin is a third-generation fluoroquinolone that inhibits DNA supercoiling and synthesis by inhibition of bacterial DNA gyrase and topoisomerase IV. Because of these two fluoroquinolone targets, development of resistance is less likely than with other fluoroquinolones. Similarly to other fluoroquinolones, pradofloxacin accumulates inside inflammatory cells, in particular in macrophages. | [Side effects]
Dogs: pradofloxacin is generally well tolerated, but it may cause nausea, vomiting, diarrhea, soft stools, lethargy. These signs are typically mild and transient. It can induce seizure when administered at high doses. | [Drug interactions]
Antacids containing divalent or trivalent cations (e.g., Mg++, Al++, Ca++), iron, zinc: decrease pradofloxacin absorption; separate administration of these products and pradofloxacin by at least 2 hours
Aminoglycosides, third-generation cephalosporins, extended spectrum penicillins: drug synergism may occur, especially against Pseudomonas
Digoxin: may increase oral bioavailability of digoxin Cyclosporine: may reduce the metabolism of cyclosporine
Methotrexate, theophylline: may increase the blood levels of these drugs
Nitrofurantoin: may reduce the antimicrobial effect of fluoroquinolones |
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