Besifloxacin
- Atc Codes:S01AX23
- CAS Codes:405165-61-9
- PHARMGKB ID:405165-61-9
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
North America
Canada: Besivance; USA: Besivance.
Drug combinations
Chemistry
Besifloxacin Hydrochloride: C~19~H~22~Cl~2~FN~3~O~3~. Mw: 430.30. 7-[(3R)-3-aminoazepan-1-yl]-8-chloro-1-cyclopropyl-6-fluoro-4-oxoquinoline-3-carboxylic acid hydrochloride. CAS-405165-61-9.
Pharmacologic Category
EENT Preparations; Antibacterials; Quinolones. (ATC-Code: S01AX23).
Mechanism of action
Besifloxacin is an 8-chloro fluoroquinolone with a N-1 cyclopropyl group. The compound has activity against Gram-positive and Gram-negative bacteria due to the inhibition of both bacterial DNA gyrase and topoisomerase IV. Besifloxacin is bactericidal with minimum bactericidal concentrations generally within one dilution of the minimum inhibitory concentrations. The mechanism of action of fluoroquinolones, including besifloxacin, is different from that of aminoglycoside, macrolide, and β-lactam antibiotics. Therefore, besifloxacin may be active against pathogens that are resistant to these antibiotics and these antibiotics may be active against pathogens that are resistant to besifloxacin. In vitro studies demonstrated cross-resistance between besifloxacin and some fluoroquinolones.
Therapeutic use
Treatment of bacterial conjunctivitis caused by susceptible isolates of the following bacteria: CDC coryneform group G Corynebacterium pseudodiphtheriticum*, Corynebacterium striatum*, Haemophilus influenzae, Moraxella lacunata*, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus hominis*, Staphylococcus lugdunensis*, Streptococcus mitis group, Streptococcus oralis, Streptococcus pneumoniae, Streptococcus salivarius*.
*Efficacy for this organism was studied in fewer than 10 infections.
Pregnancy and lactiation implications
Use in pregnancy only when clearly needed. Besifloxacin has not been measured in human milk, although it can be presumed to be excreted in human milk. Caution should be exercised when administered to nursing women.
Unlabeled use
Contraindications
None known to date.
Warnings and precautions
Topical ophthalmic use only. Growth of resistant organisms with prolonged use. Contact lenses should be avoided if patient has signs or symptoms of bacterial conjunctivitis or during the course of the therapy.