Beta‐lactam Antibiotics

Prescott, John F.

doi:10.1002/9781118675014.ch9

Cited by 34 publications

(43 citation statements)

References 66 publications

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“…8,11,13 Cephalothin is partially metabolized to desacetylcephalothin in the liver and, the parent drug and the metabolite are excreted through the kidneys by glomerular filtration and tubular secretion. 2,12 Extension of metabolism varies with the species, being of 5-15% in humans, 14 and greater in rabbits, dogs and horses. 5,9,11 The antibacterial activity of desacetylcephalothin is only one-half to onesixteenth that of cephalothin, the lowest value corresponding to Bacillus subtilis ATCC 6633.…”

Section: Introductionmentioning

confidence: 99%

“…Also, parenteral first generation cephalosporins might be used to establish high tissue levels rapidly before using an oral cephalosporin. 2 For surgical prophylaxis they should be administered intravenously around 30 minutes prior to the first tissue incision (to allow achieving therapeutic concentrations at tissue level when the incision is performed) only once. Administration can be repeated 90 minutes later in long lasting surgeries or when significant blood loss occurs.…”

Section: Introductionmentioning

confidence: 99%

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Plasma pharmacokinetics, tissue concentrations and urine elimination after cephalothin intravenous administration to cats under surgical conditions

et al. 2015

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Pharmacokinetic profile, tissue concentrations and urine elimination of cephalothin in cats under surgical conditions after a single intravenous dose (30 mg/kg) were studied. . Tissue/plasma concentrations rate was in a range of 0.04 (testicle) to 0.21 (uterus). Cephalothin urine elimination was 66.49% in the first 6 hours after administration. Cephalothin plasma concentrations remained above a minimum inhibitory concentration (MIC)≥1 µg/mL up to 5.5 hours in all the studied cats. However, for MIC≥8 µg/mL (MIC breakpoint) this time is reduced to 2.5 hours. This suggests that proper perioperative prophylactic use of cephalothin in cats requires a dose interval not longer than 2 hours.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Plasma pharmacokinetics, tissue concentrations and urine elimination after cephalothin intravenous administration to cats under surgical conditions

et al. 2015

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“…Cephalexin is a first generation cephalosporin with high activity against Gram-positive cocci (staphylococci, streptococci) including many beta-lactamaseproducing strains, some Gram-negative Enterobacteriaceae and anaerobes (Prescott, 2006). Cephalexin is, due to its high efficacy against Pasteurella multocida and Staphylococcus aureus, commonly used in rabbit for the treatment of respiratory infections (Rougier et al, 2006).…”

Section: Introductionmentioning

confidence: 99%

“…The reported minimum inhibitory concentration (MIC) for most gram-positive organisms and Pasteurella multocida is ≤1.0 μg/mL, while for susceptible gramnegative organisms (E. coli, and Klebsiella pneumoniae) it may be as high as 8 μg/ml (Prescott, 2006).…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of Cephalexin after Intravenous and Single and Multiple Intramuscular Administration to Rabbit

Meneses¹,

Albarellos²,

Landoni³

2014

IJVMR

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Cephalexin is a first generation cephalosporin widely used in rabbits. Its spectrum includes Pasteurella multocida and Staphylococcus aureus. These bacteria, together with Bordetella bronchiseptica, are the main cause of respiratory infections. Although many textbooks on rabbit therapeutics report the use of cephalexin, including administration schedules, there are not published papers on the pharmacokinetics of cephalexin after IV and IM administration to rabbit. Therefore, the objective of the present study was to describe cephalexin disposition in rabbits after intravenous and single and multiple intramuscular administrations. Three administration schedules were studied: single IV administration (10 mg/kg), single IM administration (10 mg/kg) and multiple IM administration (2.5 mg/kg/6). Serial blood samples were collected over a 24 h period. Cephalexin plasma concentrations were determined by microbiological method using Kocuria rhizophila ATCC 9341 as microorganism test. No statistical differences were observed between routes of administration for any of the estimated PK parameters. The unique difference was observed on bioavailability between intramuscular administration schedules. Elimination half-life was 1.45, 1.09 and 1.91 h for the single IV, single IM and multiple IM administration, respectively. Bioavailability after single and multiple IM administration was 47 and 97.5%, respectively. After multiple IM administration maximum and minimum plasma concentration at steady state were 2.77 and 0.34 µg/ml, while Cmax after single IM administration was 9. 22 µg/ml.Considering that for betalactams the PK/PD breakpoint recommended for efficacy (T > MIC) should be 50-80% and that the reported MIC for most gram-positive organisms and Pasteurella multocida is ≤1.0 μg/ml, the present study demonstrates that a single IM dose of 10 mg/kg/24 h is enough to maintain therapeutic concentrations for a 24 hours period. When a 2.5mg/kg dose is used administration every 6 hours is recommended.

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“…No son sensibles Klebsiella sp. y Pseudomonas aeruginosa (Prescott, 2006). La actividad de la ampicilina es tiempodependiente, esto es, la muerte de las bacterias está estrechamente vinculada a la concentración de la droga y a la duración de la exposición de la bacteria a ésta (Craig 1998, Drusano 2004.…”

Section: Introductionunclassified

Farmacocinética comparativa de una dosis única de ampicilina en llamas luego de la administración intravenosa, intramuscular y subcutánea

et al. 2014

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SUMMARYSix healthy, adult llamas (Lama glama) received a single intravenous (i.v.), intramuscular (i.m.) and subcutaneous (s.c.) administration of ampicillin at a dosage of 20.0 mg/kg body weight. Venous blood samples were collected, and ampicillin plasma concentrations were determined by microbiological assay. Kinetic calculations were done using noncompartmental analysis. The period of time that plasma concentrations spent above the minimum inhibitory concentration (T > MIC) was graphically determined. Following the i.v. administration, mean pharmacokinetic parameters (± SD) were as follows: terminal elimination half-life (t ½λ ) 0.52 ± 0.1 h, total body clearance (Cl t ) 10.3 ± 1.3 ml/kg·min, volume of distribution at steady state (V ss ) 0.35 ± 0.07 l/kg. Following the i.m. and the s.c. administration, significant differences were determined for peak concentrations (34.1± 6.2 and 18.6 ± 6.3 µg/ml, respectively), time to peak concentrations (0.26 ± 0.08 and 0.6 ± 0.2 h, respectively); t ½λ (0.83 ± 0.17 and 1.66 ± 0.6 h, respectively); mean residence time (1.3 ± 0.3 and 2.7 ± 1.0 h, respectively), and mean absorption time (0.72 ± 0.2 and 2.1 ± 0.9 h, respectively). T > MIC values suggest that different ampicillin s.c. and i.m. dosing should be used in llamas, as s.c. injection provides therapeutically effective plasma concentrations for a longer duration.Key words: camelids, pharmacokinetics, antibiotics, ampicillin. RESUMENLos objetivos de este estudio fueron describir y comparar la farmacocinética y biodisponibilidad de la ampicilina administrada por las vías intravenosa (i.v.), intramuscular (i.m.) y subcutánea (s.c.) a llamas (Lama glama) adultas sanas, y calcular los correspondientes tiempos sobre la CIM (T > CIM) a fin de proveer una base farmacológica para la terapia antimicrobiana racional en esta especie. Seis llamas recibieron una dosis de ampicilina por las vías i.v., i.m. y s.c. Se extrajo sangre a tiempos predeterminados y se calculó las concentraciones plasmáticas utilizando el método microbiológico. Los parámetros farmacocinéticos se calcularon de las curvas de disposición correspondientes. El T > CIM se calculó gráficamente. Los parámetros medios luego de la administración i.v. ( ± DE) fueron: vida media de eliminación (t ½λ ) 0,52 ± 0,1 h, clearance (Cl t ) 10,3 ± 1,3 ml/kg·min, volumen de distribución al estado estacionario (V ss ) 0,35 ± 0,07 l/kg. Luego de las administraciones i.m. y s.c., se encontraron diferencias significativas para las concentraciones máximas (34,1± 6,2 y 18,6 ± 6,3 µg/ml, respectivamente), tiempo a la concentración máxima (0,26 ± 0,08 y 06 ± 0,2 h, respectivamente); t ½λ (0,83 ± 0,17 y 1,66 ± 0,6 h, respectivamente); tiempo medio de residencia (1,3 ± 0,3 y 2,7 ± 1,0 h, respectivamente), y de absorción (0,72 ± 0,2 y 2,1 ± 0,9 h, respectivamente). Los valores de T > CIM sugieren que en llamas deberían usarse diferentes dosificaciones cuando se administra la ampicilina por vía i.m. o s.c., ya que la inyección s.c. provee concentraciones plasmáticas terapéuticamente efecti...

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Beta‐lactam Antibiotics

Cited by 34 publications

References 66 publications

Plasma pharmacokinetics, tissue concentrations and urine elimination after cephalothin intravenous administration to cats under surgical conditions

Plasma pharmacokinetics, tissue concentrations and urine elimination after cephalothin intravenous administration to cats under surgical conditions

Pharmacokinetics of Cephalexin after Intravenous and Single and Multiple Intramuscular Administration to Rabbit

Farmacocinética comparativa de una dosis única de ampicilina en llamas luego de la administración intravenosa, intramuscular y subcutánea

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