The Department of Veterinary Clinical Medicine, College of Veterinary Medicine, University of Illinois Urbana-Champaign, Urbana, Illinois, USA.
The Metabolomics Lab, Roy J. Carver Biotechnology Center, University of Illinois Urbana-Champaign, Urbana, Illinois, USA.
J Vet Pharmacol Ther. 2023 Jan;46(1):17-24. doi: 10.1111/jvp.13104. Epub 2022 Nov 10.
Telmisartan is an angiotensin II receptor blocker that has great potential to improve the treatment of hypertension, proteinuria, and cardiovascular disease in dogs. A feline-approved telmisartan oral solution (TOS) is available, but this formulation has not been evaluated in dogs. The aims of this study were to establish the pharmacokinetics of telmisartan administered as TOS and determine the effect of feeding on drug absorption in dogs. In a cross-over design, seven healthy dogs received 1 mg/kg telmisartan orally as TOS with or without food and underwent serial measurement of plasma telmisartan concentrations over 24 h. Bioequivalence of TOS administered with vs. without food was assessed by the 90% confidence interval method for maximum concentration (C ), and the observed and extrapolated areas under the curve (AUC and AUC ). The mean ratios of these parameters were 0.97 (CI 0.74-1.27), 0.92 (0.81-1.03), and 0.90 (0.82-1.00), respectively. Feeding methods were not bioequivalent based on C due to interindividual variation. These results suggest that TOS can be given to dogs with or without food but should be administered in the same way consistently. Additional pharmacokinetic and pharmacodynamic studies are warranted to confirm this recommendation and establish the therapeutic targets for telmisartan in dogs.
替米沙坦是一种血管紧张素 II 受体阻滞剂，具有很大的潜力改善高血压、蛋白尿和犬心血管疾病的治疗效果。目前有一种已批准用于猫的替米沙坦口服溶液（TOS），但尚未在犬中进行评估。本研究的目的是确定 TOS 给予犬时的药代动力学，并确定进食对药物吸收的影响。在一项交叉设计中，7 只健康犬口服 1mg/kg 的替米沙坦 TOS，同时或不进食，并在 24 小时内连续测量血浆替米沙坦浓度。通过最大浓度（C ）的 90%置信区间法评估 TOS 与进食同时给药与不进食给药的生物等效性，以及观察到的和外推的曲线下面积（AUC 和 AUC ）。这些参数的平均比值分别为 0.97（CI 0.74-1.27）、0.92（0.81-1.03）和 0.90（0.82-1.00）。由于个体间的差异，基于 C ，进食方法不是生物等效的。这些结果表明，TOS 可以在犬进食或不进食时给予，但应始终以相同的方式给予。需要进行额外的药代动力学和药效学研究来证实这一建议，并确定替米沙坦在犬中的治疗目标。
