健常犬におけるテルミサルタンの血中動態解析と薬用量の決定

抄録

At present, the appropriateness and proper dosage of telmisartan for canine cardiovascular diseases have not been evaluated or determined. Thus, in our report, we evaluate the internal pharmacokinetics of telmisartan in dogs and determine its proper dose by orally administering the drug in healthy beagle canines. At 3.6 hours after the oral administration, the highest blood concentration observed was 0.588±0.074 μg/mL; the average absorption time was 7.34±2.45 h; and the bioavailability was 28.2±0.1%. The area under the drug concentration–time curve (AUC) was 6.53±0.97 μg-h/mL; the steady-state volume of distribution was 1.80± 0.30 L/kg; and the elimination half-life was 9.9± 2.21 h. Finally, the plasma protein binding rate was 99.5±0.073%. This kinetic profile was similar to that of previously reported human kinetic profiles of the drug, and after comparing the AUCs of canines and humans, The appropriate oral dose of telmisartan for dogs was considered to be 1.0–2.0 mg/kg once daily. However, the data in this study were obtained from healthy dogs. Therefore, when using telmisartan in clinical cases, it is necessary to start with a lower dose and adjust the dose while confirming the effects.