Bioavailability and disposition of sodium and procaine penicillin G (benzylpenicillin) administered orally with milk to calves

Musser, Jeffrey M.B.; Anderson, Kevin L.

doi:10.1046/j.1365-2885.2001.00325.x

Cited by 5 publications

(4 citation statements)

References 27 publications

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“…Ranheim et al reported that the clearance of penicillin was lower in 1-week-old piglets than in adult pigs (7,51). Musser et al found that the volume of distribution at steady state (V ss ) of the calf was significantly higher than that of adult cattle (5,30). The use of adult data only may not be able to describe all of the PK characteristics of penicillin G. Thus, we combined data from a wide range of weights and ages by adding them as covariates in order to illustrate their relationships with the basic PK parameters.…”

Section: Discussionmentioning

confidence: 99%

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Interspecies Mixed-Effect Pharmacokinetic Modeling of Penicillin G in Cattle and Swine

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et al. 2014

Antimicrob Agents Chemother

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c Extralabel drug use of penicillin G in food-producing animals may cause an excess of residues in tissue which will have the potential to damage human health. Of all the antibiotics, penicillin G may have the greatest potential for producing allergic responses to the consumer of food animal products. There are, however, no population pharmacokinetic studies of penicillin G for food animals. The objective of this study was to develop a population pharmacokinetic model to describe the time-concentration data profile of penicillin G across two species. Data were collected from previously published pharmacokinetic studies in which several formulations of penicillin G were administered to diverse populations of cattle and swine. Liver, kidney, and muscle residue data were also used in this study. Compartmental models with first-order absorption and elimination were fit to plasma and tissue concentrations using a nonlinear mixed-effect modeling approach. A 3-compartment model with extra tissue compartments was selected to describe the pharmacokinetics of penicillin G. Typical population parameter estimates (interindividual variability) were central volumes of distribution of 3.45 liters (12%) and 3.05 liters (8.8%) and central clearance of 105 liters/h (32%) and 16.9 liters/h (14%) for cattle and swine, respectively, with peripheral clearance of 24.8 liters/h (13%) and 9.65 liters/h (23%) for cattle and 13.7 liters/h (85%) and 0.52 liters/h (40%) for swine. Body weight and age were the covariates in the final pharmacokinetic models. This study established a robust model of penicillin for a large and diverse population of food-producing animals which could be applied to other antibiotics and species in future analyses.

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Section: Discussionmentioning

confidence: 99%

“…or intramuscular (i.m.) (5,6), while penicillin G procaine is approved for use via intramuscular and subcutaneous (s.c.) administration for cattle and swine (7).…”

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confidence: 99%

Interspecies Mixed-Effect Pharmacokinetic Modeling of Penicillin G in Cattle and Swine

Gehring

Tell

et al. 2014

Antimicrob Agents Chemother

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“…In a study using experimental animals, administration of high dose of penicillin G is required for seizure induction (Stankiewicz et al, 1995). Additionally, the oral bioavailability of penicillin G in mammals is low (Poschet et al, 1999;Musser and Anderson, 2001). In the present study, no deaths in zebrafish larvae were observed and general symptoms were good.…”

Section: Discussionmentioning

confidence: 41%

Establishment of a novel experimental protocol for drug-induced seizure liability screening based on a locomotor activity assay in zebrafish

et al. 2014

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-As drug-induced seizures have severe impact on drug development, evaluating seizure induction potential of candidate drugs at the early stages of drug discovery is important. A novel assay system using zebrafish has attracted interest as a high throughput toxicological in vivo assay system, and we tried to establish an experimental method for drug-induced seizure liability on the basis of locomotor activity in zebrafish. We monitored locomotor activity at high-speed movement (> 20 mm/sec) for 60 min immediately after exposure, and assessed seizure liability potential in some drugs using locomotor activity. However this experimental procedure was not sufficient for predicting seizures because the potential of several drugs with demonstrated seizure potential in mammals was not detected. We, therefore, added other parameters for locomotor activity such as extending exposure time or conducting flashlight stimulation (10 Hz) which is a known seizure induction stimulus, and these additional parameters improved seizure potential detection in some drugs. The validation study using the improved methodology was used to assess 52 commercially available drugs, and the prediction rate was approximately 70%. The experimental protocol established in this present study is considered useful for seizure potential screening during early stages of drug discovery.Key words: Zebrafish, Locomotor activity, Seizure, Extending exposure time, Flashlight stimulation Correspondence: Naoteru Koseki (E-mail: naoteru-koseki@ds-pharma.co.jp) Original ArticleThe Journal of Toxicological Sciences (J. Toxicol. Sci.) Vol.39, No.4, 579-600, 2014 Vol. 39 No. 4 579 through the blood-brain barrier (BBB). Since such assays are conducted with a focus on specific neural networks or cells associated with seizures, performing an evaluation using above alternative methods is direct and limited. On the basis of the aforementioned findings, a test system that can take pharmacokinetic effects into account and can be used to perform an evaluation under conditions closer to whole body is considered desirable. As such, an in vivo evaluation system using Caenorhabditis elegans (C. elegans), which is one of the nematodes with gamma-aminobutyratergic (GABAergic) neurons related to seizures, has been reported (Locke et al., 2006;Pandey et al., 2010), and an evaluation using behavioral assessment of such organism is expected. However, nematodes are very different from mammals in terms of the anatomical structure of central nervous system (CNS) or pharmacokinetics. Therefore, performing an assessment which approximates the evaluation of a conventional study using rodents is considered to be difficult.Zebrafish is a vertebrate and its genomic homology to humans is approximately 70% (Howe et al., 2013). In addition, zebrafish can be utilized in early stage drug screening in recent decades. For these reasons, an evaluation using zebrafish has recently been given attention as a novel in vivo evaluation system for safety assessment. Since zebrafish have tele...

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“…The efficacy of penicillin against Sarcina is unknown, but it may be effective locally, and penicillin is safe. 2 The decision for surgery was considered to be the best option for this calf, although no studies have proven whether surgical or medical management is better for calves with abomasitis.…”

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Postanesthetic Poliomyelopathy in a 7-Day-Old Calf

Gold

Divers

Lahunta

2005

Journal of Veterinary Internal Medicine

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Bioavailability and disposition of sodium and procaine penicillin G (benzylpenicillin) administered orally with milk to calves

Cited by 5 publications

References 27 publications

Interspecies Mixed-Effect Pharmacokinetic Modeling of Penicillin G in Cattle and Swine

Interspecies Mixed-Effect Pharmacokinetic Modeling of Penicillin G in Cattle and Swine

Establishment of a novel experimental protocol for drug-induced seizure liability screening based on a locomotor activity assay in zebrafish

Postanesthetic Poliomyelopathy in a 7-Day-Old Calf

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