ADME of fluoroquinolones 单次口 药物服剂量 生物利半衰期最高峰浓度分布容积肾排泄率”蛋白结合率 用度%小时 m gL % g 诺氟沙星400 35~45 3~4 1.6 >100 33-38 10 环丙沙星 500 60~803.5~5.41.2~2.8 307 40 ~60 14-25 依诺沙星 400 80 3.8~5.82.8~3.6 175 52 35 「氧氟沙星40085-955.0~7035-5.39070~90 25 左氧氟沙星20090~1004.0~6.02.0 119 85-90 30~40 氟罗沙星40090~10011.04.4~6.8 110 50~65 32 洛美沙星 400 90~100 6.33.71127 70 14~25 培氟沙星 40 90-1007.5-10.03.8-5.6 139 11 20~30 托氟沙星 300 4.7 1.9 45 37 司氟沙星 200 77 16~20.0 0.62 160 12 37-42 尿中排出原形占给药量的百分数(%)
ADME of fluoroquinolones
Clinical Uses Urinary tract infections Gl and abdominal infections Respiratory tract infections Bone, joint and soft tissues infections, Osteomyelitis Meningitis STD: Neisseria gonorrhea(奈瑟氏淋球 菌) and chlamydia(衣原体, Quinolone resistance in gonorrhea increasing)
• Urinary tract infections. • GI and abdominal infections. • Respiratory tract infections. • Bone, joint and soft tissues infections, Osteomyelitis. • Meningitis • STD: Neisseria gonorrhea (奈瑟氏淋球 菌)and Chlamydia (衣原体，Quinolone resistance in gonorrhea increasing) Clinical Uses
Adverse reactions Gastrointestinal effects oCNS side effects .Allergic reaction Hepatotoxicity, nephrotoxicity jOint/cartilage toxicity, Tendinopathy Achilles tendon rupture Limited FDa approval for children
•Gastrointestinal effects. •CNS side effects. •Allergic reaction. •Hepatotoxicity, nephrotoxicity. •Joint/cartilage toxicity, Tendinopathy –Achilles tendon rupture –Limited FDA approval for children Adverse reactions
Fluoroquinolones agents Norfloxacin(诺氟沙星) Ciprofloxacin(环丙沙星) Ofloxacin(氧氟沙星) Levofloxacin(左氧氟沙星) Lomefloxacin(洛美沙星) Fleroxacin(氟罗沙星) Sparfloxacin(司帕沙星) Clinafloxacin(克林沙星) Gatifloxacin (加替沙星)
• Norfloxacin (诺氟沙星) • Ciprofloxacin (环丙沙星) • Ofloxacin (氧氟沙星) • Levofloxacin (左氧氟沙星) • Lomefloxacin (洛美沙星) • Fleroxacin (氟罗沙星) • Sparfloxacin (司帕沙星) • Clinafloxacin (克林沙星) • Gatifloxacin (加替沙星) Fluoroquinolones agents
Contents Quinolones(喳诺酮粪) Sulfonamides(磺胺类) Other Synthetic antimicrobial Trimethoprim(甲氧苄咬) Nitrofurans(硝基央喃类)
• Quinolones ( 喹诺酮类) • Sulfonamides ( 磺胺类) • Other Synthetic antimicrobial Trimethoprim (甲氧苄啶) Nitrofurans (硝基呋喃类) Contents