Ampicillin and its congener prodrugs in the horse.

Ampicillin is an antibiotic commonly administered to horses by both the intramuscular (i.m.) and the intravenous (i.v.) route. Its physicochemical properties restrict its absorption after oral administration and explain its rapid elimination from the body. To prolong the effects of ampicillin in the horse, attempts have been made to alter its elimination and absorption rates. The alteration of urinary pH did not change the plasma disposition of the antibiotic but when probenecid was administered concurrently with ampicillin, a significant reduction of total body clearance was achieved. Ampicillin may also be maintained in the equine body, for a prolonged period of time when administered as an i.v. infusion. However, the practical difficulties associated with this route of administration and the limited potential advantage over conventional routes such as i.m. injection restrict its application to the critically ill animal and the perioperative period. When bacampicillin and pivampicillin (two ampicillin prodrugs) were administered to horses, high oral bioavailability was obtained, and the use of prodrugs commands the need for further investigation. The use of ampicillin might be limited in the future as an increase in the number of resistant equine bacterial strains emerge and it may be prudent to restrict its use according to the principles of good clinical pharmacological practice.