Development of advantus™(imidacloprid) soft chewable tablets for the treatment of Ctenocephalides felis infestations on dogs

Background: studies reported here were conducted to evaluate the safety and effectiveness of advantus™ (imidacloprid) soft chewable tablets for the treatment of flea (ctenocephalides felis) infestations on dogs and puppies 10 weeks of age or older and weighing 4 pounds or greater. methods: a pharmacokinetic study was conducted to evaluate parameters of orally administered imidacloprid. a dose confirmation study was conducted to confirm the efficacy of 0.75 mg/kg at 8,12 or 24 hours post-treatment. a knockdown and speed of kill study was conducted to confirm the efficacy of 0.75 mg/kg dose at 0.5,1,4 or 24 hours post-treatment. the safety of a daily dose administered for six months at approximately 1,3,and 5 times the maximum exposure dose of 3.75 mg/kg was evaluated in puppies. a field study was conducted to evaluate the safety and efficacy of a daily oral dose of 0.75 mg/kg for 14 days in client-owned dogs. results: the pharmacokinetic parameters of the final imidacloprid oral formulation were; tmax 1.31 hours,cmax 690.0 ng/ml,auc 2615.5 h∗ng/ml and half-life was 2.2 hours. the efficacy of 0.75 mg/kg bw was 98.6 %,99.9 % and 100 % at 8,12 and 24 hours post-treatment,respectively. the live flea counts were significantly different (p < 0.0001) and the treatment was well tolerated. the flea counts at 1 hour post-treatment were significantly lower in the treated group and the speed of kill efficacy was 96.6 % at 4 hours post-treatment in the knockdown and speed of kill study. the target animal safety study showed that the advantus™ soft chewable tablets administered orally to 10-week-old puppies once daily for 6 months at approximately 1,3 and 5 times the maximum dose of 3.75 mg/kg was well tolerated and did not produce clinically relevant findings in beagles. in the field study,efficacy of the soft chewable tablets administered daily for 14 days to flea-infested dogs was 98.2 %. conclusion: imidacloprid administered orally as a soft chewable tablet for the treatment of fleas on dogs was safe and highly effective with a rapid knockdown effect and rapid elimination. © 2015 qureshi et al.