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  • Author or Editor: Quintin A. McKellar x
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SUMMARY

Bacampicillin hydrochloride is an ester prodrug that is hydrolyzed to ampicillin after its absorption from the gastrointestinal tract. It was administered intragastrically at a dose rate of 13.5 mg/kg of body weight to ponies and horses, and was highly bioavailable (F = 41.0%), compared with other penicillins in adult horses. The high peak ampicillin plasma concentration of 6,1 ± 0,5 µg/ml achieved and persistence of the antibiotic at concentration of 0.3 ± 0.1 µg/ml 6 hours after its intragastric administration, suggest that bacampicillin hydrochloride may reach suitable bactericidal concentrations for treatment of infections caused by susceptible microorganisms.

In a separate experiment, dichlorvos, an organo-phosphate compound that inhibits some of the esterase activity in plasma, was administered orally to the same animals at a dose rate of 40 mg/kg, followed by intragastric administration of bacampicillin hydrochloride at a dose of 13.5 mg/kg. Plasma pseudocholines-terase and erythrocyte acetylcholinesterase activities were reduced to < 5% of reference (predichlorvos) values after dichlorvos administration. However, rate of hydrolysis of bacampicillin into ampicillin was not affected. Consequently, the disposition and fate of bacampicillin when administered intragastrically 1 day after dichlorvos administration were similar to the values obtained after administration of bacampicillin alone.

Intragastric coadministration of probenecid at a dose rate of 75 mg/kg and bacampicillin at 13.5 mg/ kg limited absorption of the antibiotic from the gastrointestinal tract. This suggests existence of a common transport mechanism for bacampicillin and probenecid in the gastrointestinal wall, and precludes use of this combination for treatment. The bioavailable fraction of ampicillin after combination treatment indicated prolonged residence time in the plasma, presumably as a consequence of reduced renal tubular secretion.

Free access
in American Journal of Veterinary Research

Abstract

Objective—To assess anti-inflammatory effects of carprofen (CPF), CPF enantiomers, and NG-nitro-L-arginine methyl ester (L-NAME) in sheep.

Animals—8 sheep.

Procedure—Sheep with SC tissue cages were used. After intracaveal injection of 1% carrageenan, sheep were given single doses of racemic (Rac; 50:50 mixture of S[+] and R[–] enantiomers)-CPF (4.0 mg/kg), R(–)CPF (2.0 mg/kg), S(+)CPF (2.0 mg/kg), L-NAME (25 mg/kg), and placebo (PLB) IV in a crossover design.

Results—Rac-CPF and S(+)CPF inhibited serum thromboxane2 (TXB2) and exudate prostaglandin (PG)E2 generation significantly for 32 hours. Maximal inhibitory effect for serum TXB2 was 79 ± 3% for Rac- CPF and 68 ± 6% for S(+)CPF. The Rac-CPF and S(+)CPF induced 50 to 98% reversible inhibitory effect for exudate PGE2 generation during a 4- to 32- hour period. The R(–)CPF and L-NAME attenuated serum TXB2 generation significantly. The R(–)CPF did not affect exudate PGE2 production, whereas L-NAME potentiated exudate, PGE2 generation by 30% during 4 to 32 hours. The S(+)CPF and L-NAME increased leukotriene B4 generation and WBC recruitment in exudate although significance was achieved only at a few time points. Increase in skin temperature over inflammatory cages was effectively inhibited by Rac- CPF and S(+)CPF but not by R(–)CPF.

Conclusion and Clinical Relevance—Carprofen is a potent cyclooxygenase inhibitor in vivo in sheep, and its anti-inflammatory effects are attributable only to S(+)CPF in Rac-CPF. Nitric oxide may enhance eicosanoid production and accelerate the acute inflammatory process. (Am J Vet Res 2002;63: 782–788)

Full access
in American Journal of Veterinary Research

Summary

The effect of urine pH on plasma disposition of ampicillin sodium was evaluated. A single dose of 10 mg/kg of body weight was administered iv to Thoroughbreds with alkaline (pH > 8.0) or acidic (pH < 4.5) urine. Urine alkalinity was achieved and maintained by oral administration of up to 400 mg of sodium bicarbonate/kg/d, and acidity was achieved and maintained by oral administration of up to 400 mg of ammonium chloride/kg/d.

Ampicillin sodium was measured in the plasma of horses by use of an agar diffusion microbiological assay with Bacillus subtilis as the test organism. The plasma disposition kinetics of ampicillin sodium best fitted a 2-exponential decay pattern, and statistically significant differences were not evident in elimination half-life, area under the plasma concentration time curve, volume of distribution, or body clearance rate between horses with alkaline or acidic urine.

Results indicate that changes in urine pH over a range encountered in clinically normal horses are unlikely to affect plasma pharmacokinetic variables of ampicillin sodium after iv administration of the drug.

Free access
in American Journal of Veterinary Research