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Pharmacological particulars
ATC Vet Code: QP51AE01
Pharmacological properties
Imidocarb dipropionate is a substituted carbanilide, used as an antiprotozoan treatment for the control of Babesia spp.
Little is known about the mode-of-action of imidocarb dipropionate. It appears that imidocarb acts directly on the parasite, causing alteration in number and size of nuclei and in morphology (vacuolation) of the cytoplasm. The antiprotozoan activity is derived from the carbanilide acting on glycolyis of the parasite. This is the result of this class of drugs giving rise to hypoglycaemia in the host. Babesia as well as many other parasites like trypanosomes depend upon host glucose for aerobic glycolysis. There is also a selective blocking effect on the replication of the quinetoplastic DNA of the parasite.
Pharmacokinetics
Pharmacokinetic studies have been conducted with imidocarb dipropionate and have demonstrated that it has a long duration of activity, a result of it binding to plasma and tissue protein.
Imidocarb dipropionate is poorly absorbed when administered orally. Studies in rats, dogs and monkeys demonstrated that kidney and liver were the target organs, with it having the greatest affinity for kidney in rats and liver in the dog.
A radio-labelled study in lactating and non-lactating cattle, with imidocarb dipropionate being administered subcutaneously at a dose rate of 3 mg/kg body weight, demonstrated that imidocarb dipropionate was slowly excreted so that by 10 days post-dosing less than half the dose had been excreted. Main route of excretion was via the urine. Blood levels peaked at a mean level of 1.3 ppm equivalents 1 hour after injection. Milk levels peaked at a mean 0.37 ppm imidocarb dipropionate equivalents 24 hours post administration, and then depleted with a half-life of about 24 hours. All excreted material was mostly parent compound.
Other work has shown that imidocarb dipropionate can pass the placental barrier.
Studies have been conducted in sheep where imidocarb dipropionate was administered by intravenous injection at a dose rate of 2 mg/kg body weight. This was found to produce a peak level in plasma of 10.8 mg/mL, dropping to 1.9 mg/mL within an hour. It was also found that imidocarb dipropionate binds to plasma proteins, and detectable amounts were found in all major tissues up to four weeks after intramuscular injection.