Slovak J E, Rivera S M, Hwang J K, Court M H, Villarino N F
Program in Individualized Medicine, Department of Veterinary Clinical Sciences, College of Veterinary Medicine, Washington State University, Pullman, WA.
J Vet Intern Med. 2017 Nov;31(6):1827-1832. doi: 10.1111/jvim.14827. Epub 2017 Sep 11.
Mycophenolate mofetil (MMF), the prodrug of mycophenolic acid (MPA), is becoming increasingly popular as an alternative immunosuppressant in feline medicine. Pharmacokinetic information is not available for cats.
The purpose of this study was to determine whether MMF is biotransformed into the active metabolite MPA and to evaluate the disposition of MPA after a 2-hour constant rate intravenous (IV) infusion of MMF in healthy cats.
Healthy cats (n = 6).
This was a prospective pilot study. All cats were administered MMF at 20 mg/kg every 12 hours over a 2-hour constant rate infusion for 1 day. The concentrations of MPA and its derivatives in blood were determined using a validated UHPLC-UV method.
All cats biotransformed MMF into MPA. The mean AUC ranged from 6 to 50 h*mg/L after IV dosing of MMF. Transient large bowel diarrhea was recorded in 2 of 6 cats after medication administration.
The disposition of MPA in plasma was highly variable, which could result in high interindividual variability in the safety and efficacy of treatment with MMF in cats.
霉酚酸酯(MMF)是霉酚酸(MPA)的前体药物,在猫科医学中作为一种替代免疫抑制剂越来越受欢迎。目前尚无猫的药代动力学信息。
本研究的目的是确定MMF是否会生物转化为活性代谢物MPA,并评估在健康猫中以2小时恒速静脉输注MMF后MPA的处置情况。
健康猫(n = 6)。
这是一项前瞻性试点研究。所有猫均以20mg/kg的剂量每12小时进行一次2小时恒速输注,持续1天。使用经过验证的超高效液相色谱-紫外法测定血液中MPA及其衍生物的浓度。
所有猫均将MMF生物转化为MPA。静脉注射MMF后,平均AUC范围为6至50h*mg/L。给药后6只猫中有2只出现短暂的大肠腹泻。
血浆中MPA的处置情况高度可变,这可能导致猫使用MMF治疗的安全性和有效性存在高度个体差异。