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

Abstract

BackgroundStudies 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.MethodsA 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.ResultsThe 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 %.ConclusionImidacloprid 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.

The Biology and Ecology of Cat Fleas and Advancements in Their Pest Management: A Review

“…A soft chewable tablet containing imidacloprid given to puppies and adult dogs provided 96% kill of fleas at 4 h [ 368 ].…”

“…Within 2 weeks, 81–88% of the dogs were flea free. In a pharmacokinetic study, a soft chewable tablet containing imidacloprid given daily for 14 days provided 98% kill of adult fleas [ 368 ].…”

Systemic insecticides used in dogs: potential candidates for phlebotomine vector control?

“…The only study published about this commercial product used dogs from different clinics and different breeds. At the oral dose of 0.75 mg/kg BW, the study reported no adverse effect in the 118 dogs treated, and 95% efficacy at controlling fleas infestations . Studies of rodents fed on diets with imidacloprid concentrations of 250 mg/kg reported sand fly mortality after blood fed on treated rodents > 85% for at least 3 days post‐treatment .…”

Effectiveness of the immidacloprid/ivermectin combination for external application (“MEGA STOP” for cats)

“…Імідоклоприд використовується у багатьох галузях та комбінаціях як інсектицидна діюча речовина, що й обумовлює ефективність застосування при блошиній інвазії (Huang & Lien, 2013;Qureshi et al, 2015).…”