Boeckh A, Boothe D, Wilkie S, Jones S
Department of Veterinary Physiology and Pharmacology, College of Veterinary Medicine, Texas A&M University, College Station, TX 77843-4466, USA.
Vet Ther. 2001 Fall;2(4):334-44.
The accumulation of fluoroquinolones in peripheral leukocytes is well established for several members of this family of drugs. This study documented accumulation of enrofloxacin and its active metabolite, ciprofloxacin, in canine peripheral leukocytes after oral administration at 7.5, 10, or 20 mg/kg, doses that are within the currently approved label of Baytril (Bayer Corporation Animal Health, Shawnee Mission, KS) in the United States. Accumulation index, as defined by C(max) in white blood cells (WBCs) divided by C(max) in plasma at the same time points, ranged from 47-fold to 63-fold for enrofloxacin and 28- to 35-fold for ciprofloxacin. Time course of both enrofloxacin and ciprofloxacin in WBCs paralleled the time course in plasma. Disappearance half-life of ciprofloxacin from WBCs was significantly (P = .001) longer than was enrofloxacin (P= .015) for all doses studied. The accumulation of enrofloxacin in peripheral leukocytes may contribute to the antimicrobial efficacy of this compound.
氟喹诺酮类药物在几种该类药物成员中外周血白细胞中的蓄积现象已得到充分证实。本研究记录了恩诺沙星及其活性代谢产物环丙沙星在犬外周血白细胞中的蓄积情况,这些犬口服剂量分别为7.5、10或20mg/kg,这些剂量均在美国目前批准的拜有利(拜耳公司动物保健部,堪萨斯州肖尼使命)标签范围内。蓄积指数定义为同一时间点白细胞(WBC)中的C(max)除以血浆中的C(max),恩诺沙星的蓄积指数范围为47倍至63倍,环丙沙星为28倍至35倍。恩诺沙星和环丙沙星在白细胞中的时间进程与血浆中的时间进程平行。在所研究的所有剂量下,环丙沙星从白细胞中的消除半衰期均显著长于恩诺沙星(恩诺沙星P = 0.015,环丙沙星P = 0.001)。恩诺沙星在外周血白细胞中的蓄积可能有助于该化合物的抗菌效果。