Comparison of the pharmacokinetics of penicillin G and ampicillin in the horse

Durr, Amy L.

doi:10.1016/s0034-5288(18)33474-x

Cited by 42 publications

(23 citation statements)

References 13 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…As recently as 1981, statements of the dose rates of procaine penicillin which should provide therapeutically effective blood levels have ignored a number of therapeutic practices (Stover ef ul 1981). It is well established that the activity of penicillins is restricted to the free compound and that penicillin G is 52 to 54 per cent bound to serum proteins in the horse (Durr 1976). Also, it is considered that two to four times the minimum inhibitory concentration is required to ensure bactericidal activity of penicillins (Weinstein 1975a).…”

Section: Discussionmentioning

confidence: 99%

“…However, it is now apparent that although the concentrations were detectable, the levels achieved were unlikely to be therapeutically effective against penicillin sensitive pathogens. More recently, Durr (1976) studied the serum binding and elimination parameters for benzylpenicillin after the intravenous (iv) administration of 35,000 iu benzylpenicillin/ kg body weight (bwt) to horses. He found the binding capacity of serum proteins to be 39.01 f 4.79 p o l / g protein and that the half-life was-53.3 f 4.5 mins.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Serum concentrations of penicillin in the horse after administration of a variety of penicillin preparations

Love

Rose

Martin

et al. 1983

Equine Veterinary Journal

View full text Add to dashboard Cite

Summary Twelve geldings were used to evaluate serum levels of penicillin following the intravenous (iv) and intramuscular (im) injection of benzylpenicillin, im procaine penicillin and im fortified benzathine penicillin, at a variety of dose rates. Blood samples were collected up to 7 h after iv and im benzylpenicillin, up to benzathine penicillin. Results were analysed using an analysis of variance and regression analyses were used to calculate the time taken for the serum penicillin concentration to decline to 0.5 μg/ml. As a result of the experiments the following dosage regimes could be recommended for each drug. Benzylpenicillin should be administered im at a dose rate of 10,000 iu/kg at the commencement of treatment. Procaine penicillin should be injected at a dose rate of 15,000 lu/kg every 12 h or 30,000 iu/kg every 24 h. In serious infections 10,000 iu/kg of benzylpenicillin im should be used concomitantly to begin therapy. Fortified benzathine penicillin appears to have little value for antimicrobial therapy in the horse. Résumé On utilisa 12 chevaux hongres pour évaluer le taux sériques de pénicilline faisant suite à l'injection intraveneuse (iv) ou intramusculaire (im) de benzylpénicilline, im de pénicilline procaïne et im de benzathine pénicilline renforcée suivant des dosages variés. Les échantillons de sang furent prélevés jusqu'à sept heures après l'injection iv ou im de benzylpénicilline; jusqu'à 24 h après injection pour la pénicilline procaine et jusqu'à 96 h après administration de benzathine pénicilline renforcée. Les résultats furent analysés (variance et régression) et l'on calcula le temps nécessaire pour que la concentration se que de pénicilline diminue jusqu'à environ 0.5 μg/ml. A la suite de cette expérimentation, les protocols de dosage suivants peuvent être conseillés pour chaque substance: La benzylpénicilline devraite être administrée im à raison de 10,000 ui/kg en début de traitement. La pénicilline procaîne devrait étre injectée à raison de 15,000 ui/kg toutes les 12 h ou à raison de 30,000 ui/kg toutes les 24 h. Dans les infections sérieux on devrait utiliser la benzylpénicilline im de manière concomitante en début de traitement. La benzathine pénicilline renforcée s'est révéle de peu d'intérêt dans la thérapeutique antibactérienne chez le cheval. Zusammenfassung Zwölf Wallache wurden verwendet zur Bestimmung von Penicillinspiegeln nach intravenöser und intramuskulärer Injektion von Benzylpenicillin, im. Procainpenicillin und im verstärktem Benzathinpenicillin in variierender Dosierung. Die Blutentnahmen erfolgten bis zu 7 h Stunden nach iv und im. Benzylpenicillin, bis zu 24 h nach Procainpenicillin und bis zu 96 h nach Benzathinpenicillin. Die Resultate wurden der Varianzanalyse unterworfen und die Regressionsanalyse wurde zur Berechnung derjenigen Zeit angewendet, in der die Serum‐Penicillinkonzentration um 0.5 μg/ml abnimmt. Als Ergebnis der Versuche wurden die folgenden Dosierungsempfehlungen aufgestellt: Benzylpenicillin sollte intramuskulär in einer Dosis von 10,000 iu/kg...

show abstract

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Serum concentrations of penicillin in the horse after administration of a variety of penicillin preparations

Love

Rose

Martin

et al. 1983

Equine Veterinary Journal

View full text Add to dashboard Cite

show abstract

“…As plasma protein binding is less than 8% for ampicillin in horses (Durr, 1976), it was assumed that total ampicillin concentration measured was representative of the antimicrobial activity.…”

Section: Discussionmentioning

confidence: 99%

Intramuscular dosing strategy for ampicillin sodium in horses, based on its distribution into tissue chambers before and after induction of inflammation

Hoven¹,

Hierweck²,

Dobretsberger

et al. 2003

Vet Pharm & Therapeutics

View full text Add to dashboard Cite

The Pharmacokinetics (PK) and distribution into tissue chamber fluid (TCF) of intramuscularly (i.m.) administered ampicillin sodium were examined in horses in order to design adequate dosing strategies. Concentration-time curves of ampicillin in plasma and TCF were determined in six horses following administration of 15 mg/kg ampicillin sodium, before and after the induction of local inflammation with 0.5% carrageenan. The calculated parameters were used to simulate various dosage-dosing interval combinations. Ampicillin was absorbed very rapidly following i.m. administration. Plasma concentrations were maximual between 18 and 21 min after administration. None of the plasma PK parameters were affected significantly by local (TC) inflammation. Penetration of ampicillin into and elimination from the TCF were affected significantly by inflammation and the half-life of elimination from the tissue fluid t1/2(d) was significantly shorter in inflammation. In the simulated dosage-dosing interval scenarios, only a dosage of 15 mg ampicillin/kg four times daily would successfully treat all ampicillin-susceptible bacterial isolates in well vascularized tissues. However a dosage as low as 10 mg/kg twice daily, would, in theory, treat all ampicillin-susceptible isolates in the inflamed poorly vascularized tissues. Decreasing the dosage results in loss of efficacy that cannot be completely compensated for by increasing the frequency of dosing.

show abstract

“…In a study in which sodium penicillin was injected im, there were no apparent differences between serum penicillin concentrations in foals and adults (Doll and Dimock 1946). Following intravenous (iv) administration of sodium penicillin G to horses, Durr (1976) reported an elimination half-life of 0.9 h. Knudsen (1960) estimated renal clearance of penicillin at 8.29 ml/min/kg after iv administration of its sodium salt to horses.…”

Section: Introductionmentioning

confidence: 99%

Aqueous procaine penicillin G in foals: Serum concentrations and pharmacokinetics after a single intramuscular dose

Brown

Gronwall

Боос³

et al. 1984

Equine Veterinary Journal

View full text Add to dashboard Cite

Comparison of the pharmacokinetics of penicillin G and ampicillin in the horse

Cited by 42 publications

References 13 publications

Serum concentrations of penicillin in the horse after administration of a variety of penicillin preparations

Serum concentrations of penicillin in the horse after administration of a variety of penicillin preparations

Intramuscular dosing strategy for ampicillin sodium in horses, based on its distribution into tissue chambers before and after induction of inflammation

Aqueous procaine penicillin G in foals: Serum concentrations and pharmacokinetics after a single intramuscular dose

Contact Info

Product

Resources

About