Hansson H, Bergvall K, Bondesson U, Hedeland M, Törneke K
Department of Small Animal Clinical Sciences, Box 7037, Swedish University of Agricultural Sciences, S-750 07 Uppsala, Sweden.
Vet Dermatol. 2004 Jun;15(3):152-8. doi: 10.1111/j.1365-3164.2004.00367.x.
The pharmacokinetic properties of clemastine were investigated in six healthy dogs and compared with the effect of the drug recorded as inhibition of wheal formation induced by intradermal injections of histamine. Clemastine clearance was high (median: 2.1 L h(-1) kg(-1)) and the volume of distribution large (13.4 L kg(-1)). The half-life after intravenous administration was 3.8 h and the plasma protein binding level in vitro was 98%. After oral administration, the bioavailability was only 3%. Given intravenously, clemastine (0.1 mg kg(-1)) inhibited wheal formation completely for 7 h, whereas the effect after oral administration (0.5 mg kg(-1)) was minor. The data show that most dosage regimens suggested in the literature for the oral administration of clemastine to dogs are likely to give too low a systemic exposure of the drug to allow effective therapy.
在6只健康犬中研究了氯马斯汀的药代动力学特性，并将其与该药物对皮内注射组胺引起的风团形成的抑制作用进行比较。氯马斯汀清除率高（中位数：2.1 L h⁻¹ kg⁻¹），分布容积大（13.4 L kg⁻¹）。静脉给药后的半衰期为3.8小时，体外血浆蛋白结合率为98%。口服给药后，生物利用度仅为3%。静脉注射氯马斯汀（0.1 mg kg⁻¹）可完全抑制风团形成7小时，而口服给药（0.5 mg kg⁻¹）后的作用较小。数据表明，文献中建议的大多数给犬口服氯马斯汀的给药方案可能会使药物的全身暴露量过低，从而无法进行有效的治疗。
