q35;BALOFLOXACIN;Barlow of sand;BALOFLOXACIN 98.5%;Balofloxacin425.46;Balofloxacin, >=99%;Balofloxacin hydrate;Balofloxacin USP/EP/BP;Cypermethrin Impurity 4;BALOFLOXACIN 98.5% EXTRA PURE
Balofloxacin, a novel orally-active fluoroquinolone antibiotic, was introduced in South
Korea for the treatment of urinary tract infections (UTI). It can be synthetized by reaction of
3-(methylamino)piperidine with the classical 4-quinolone-3-carboxylic acid template. In
vitro antibacterial activity of balofloxacin against gram-positive bacteria (Staphylococcus
aureus including methicillin-resistant S. aureus, Staphylococcus epidermis, Streptococcus
pneumonia, Streptococcus pyrogenes) was almost equal to that of sparfloxacin or
tosufloxacin, in contrast its activity against gram-negative bacteria was 2 times or more
lower. In clinical trials, balofloxacin was well tolerated and showed comparable efficacy to
ofloxacin in patients with UTls. After oral administration, balofloxacin was well absorbed,
and was primarily eliminated unchanged in the urine with an elimination half-life of
approximately 8 h. In animal studies, balofloxacin did not exhibit any phototoxicity.
화학적 성질
Crystalline Solid
용도
Balofloxacin is quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.
Pharmaceutical Applications
A 6-fluoro-8-methoxy quinolone derivative. It has good antistaphylococcal activity (MIC 0.4–4 mg/L), but is inactive against methicillin-resistant Staph. aureus (MRSA) and quinolone-resistant Staph. aureus; Str. pneumoniae is inhibited by 0.4 mg/L. It has good activity against Enterobacteriaceae, but is inactive against Ps. aeruginosa (MIC 8–16 mg/L). After a 200 mg oral dose a peak level of 1.7 mg/L is reached in 1 h. The apparent elimination halflife is about 8 h, rising to 13 h in elderly subjects. Plasma protein binding is about 16%. It was withdrawn from the market in Japan because of adverse events, but is available in China.
