Comparison of fluoroquinolone pharmacokinetic parameters after treatment with marbofloxacin, enrofloxacin, and difloxacin in dogs

Frazier, Donita L.; Thompson, Leslie; Trettien, A.; Evans, E. I.

doi:10.1046/j.1365-2885.2000.00285.x

Cited by 55 publications

(33 citation statements)

References 34 publications

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“…Difloxacin is rapidly absorbed and has high systemic bioavailabilities following oral administration in chickens, pigs (Inui et al, 1998) and dogs (Frazier et al, 2000) as well as i.m. administration in rabbits (Abd el Aty et al, 2005).…”

Section: Introductionmentioning

confidence: 99%

Disposition Kinetics of Difloxacin After Intravenous, Intramuscular and Subcutaneous Administration in Calves

Ismail

2006

Vet Res Commun

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The pharmacokinetics of difloxacin (Dicural) was studied in a crossover study using three groups (n = 4) of male and female Friesian calves after intravenous (i.v.), intramuscular (i.m.) and subcutaneous (s.c.) administrations of 5 mg/kg body weight. Drug concentration in plasma was determined by high-performance liquid chromatography using fluorescence detection. The plasma concentration-time data following i.v. administration were best fitted to a two-compartment open model and those following i.m. and s.c. routes were best fitted using one-compartment open model. The collected data were subjected to a computerized kinetic analysis. The mean i.v., i.m. and s.c. elimination half-lives (t(1/2beta)) were 5.56 +/- 0.33 h, 6.12 +/- 0.42 h and 7.26 +/- 0.6 h, respectively. The steady-state volume of distribution (V(dss)) was 1.12 +/- 0.09 L/kg and total body clearance (Cl(B)) was 2.19 +/- 0.1 ml/(min x kg). The absorption half lives (t(1/2ab)) were 0.38 +/- 0.027 h and 2.1 +/- 0.09 h, with systemic bioavailabilities (F) of 96.5% +/- 6.4% and 84% +/- 5.5% after i.m. and s.c. administration, respectively. After i.m. and s.c. dosing, peak plasma concentrations (C(max)) of 3.38 +/- 0.13 microg/ml and 2.18 +/- 0.12 microg/ml were attained after (t(max)) 1.22 +/- 0.20 h and 3.7 +/- 0.52 h. The MIC90 of difloxacin for Mannheimia haemolytica was 0.29 +/- 0.04 microg/ml. The AUC/MIC90 and C(max)/MIC90 ratios for difloxacin following i.m. administration were 120 and 11.65, respectively and following s.c. administration were 97.58 and 7.51, respectively. Difloxacin was 31.7-36.8% bound to calf plasma protein. Since fluoroquinolones display concentration-dependent activities, the doses of difloxacin used in this study are likely to involve better pharmacodynamic characteristics that are associated with greater clinical efficacy following i.m. administration than following s.c. administration.

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Section: Introductionmentioning

confidence: 99%

Disposition Kinetics of Difloxacin After Intravenous, Intramuscular and Subcutaneous Administration in Calves

Ismail

2006

Vet Res Commun

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“…El t½β obtenido excede los hallados con enrofloxacina, difloxacina y orbifloxacina (11)(12)(13)(14)(15)(16). Se informaron valores de t½β para la vía oral de 9,07 ± 1,9 h (16), de 10,89 ± 0,84 h (11) y de 14,0 ± 4,9 h (17); de 8,08 ± 6,25 h (15) y de 12,4 ± 2,6 h (17), para la vía endovenosa, y de 7,51 ± 3,7 (15), para la aplicación intramuscular.…”

Section: Introductionunclassified

“…El 35-40 % de fármaco se elimina por orina sin modificaciones (2,17); por aplicación oral de 2,75 mg/kg se detectaron niveles urinarios de 18,08 y 13,9 µg/ml a las 2 y 24 h, respectivamente (11).…”

Section: Introductionunclassified

Evaluation of the contribution of gyrA mutation and efflux pumps to fluoroquinolone and multidrug resistance in pathogenic Escherichia coli isolates from dogs and cats

Shaheen¹,

Boothe²,

Oyarzábal³

et al. 2011

ajvr

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ResumenSe estudió la disposición plasmática y urinaria de marbofloxacina en caninos (n = 6) tras la aplicación intramuscular de 2 mg/kg. En distintos tiempos posadministración se tomaron muestras de sangre hasta las 24 h, y de orina solo en los caninos machos (n = 4) a las 4, 8, 12 y 24 h. Se realizó una extracción líquido-líquido del analito con agua, metanol y centrifugado a 13.500 r. p. m. a 4 °C. La separación y cuantificación se realizó por HPLC mediante la elusión isocrática en fase reversa, utilizando columna C-18, detector de fluorescencia a 295 nm de excitación y 490 nm de emisión y fase móvil compuesta por agua, acetonitrilo y trietilamina. Las concentraciones plasmáticas temporales se analizaron con el software no compartimental PK Solution 2.0. Los resultados conseguidos indican pronta absorción, rápida y amplia distribución. El Cl y los valores conseguidos de t½β y TMR indican lenta depuración y prolongada permanencia. El ensayo determinó concentraciones plasmáticas perdurables hasta 24 h, y que exceden la CMI de patógenos relevantes. El cociente ABC/ CMI indica eficacia frente a microorganismos con CMI ≤ 0,15 μg/ml. Las concentraciones urinarias de marbofloxacina son más significativas que las plasmáticas. No obstante, se requieren nuevos estudios que avalen su empleo con la dosis y vía de aplicación ensayada.Palabras clave: caninos, farmacocinética, marbofloxacina, plasma, orina. Plasma and urine pharmacokinetics of intramuscular marbofloxacin in canines AbstractPlasma and urinary disposition of marbofloxacin was studied in canines (n = 6) after intramuscular administration of 2 mg/kg. At different times post-administration, blood samples were collected until 24 h, and urine samples, only from male dogs (n = 4) at 4; 8; 12, and 24 h. Liquid-liquid extraction of analyte with water, methanol, and centrifugation at 13500 rpm at 4 °C were performed. Separation and quantification were made using HPLC by reverse phase isocratic elution with a C18 column, fluorescence detector at 295 nm excitation and 490 nm emission, and a mobile phase consisting of water, acetonitrile, and triethylamine. Temporary plasma concentrations were analyzed with non-compartmental PK Solution 2.0 software.

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“…Further optimisation of the ultrafiltration probe placement technique may reduce morbidity. Care should be taken when interpreting pharmaceutical concentrations in ultrafiltrate from infected lamellar probes as infection may affect drug concentrations (Cars and Ogren 1985;Frazier et al 2000).…”

Section: Discussionmentioning

confidence: 99%

“…The vasodilation and increased vascular permeability that accompany inflammation can cause an increase in drug delivery to the tissue, but viscosity is also increased, slowing diffusion (Barza and Cuchural 1985). Generally the low level of inflammation compared to infected tissue is a concern in antimicrobial pharmacokinetic studies using ultrafiltration (Frazier et al 2000;Bidgood and Papich 2003), as it is preferable to measure drug concentrations in tissue conditions similar to the diseased state. Laminitis development involves inflammation (Visser 2009 The median collection rate of ultrafiltrate in this study (55 µL/h) was similar to, but slightly lower than, collection rates previously reported from the subcutaneous tissues of horses using 3-12 membrane length ultrafiltration probes (68-82 µL/h) (Davis et al 2005;Davis et al 2006).…”

Section: Discussionmentioning

confidence: 99%

Drug delivery to equine digital lamellar tissue

Underwood¹

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Laminitis, a serious and debilitating disease of the equine foot, is a significant cause of wastage in the equine industry. There is no scientifically validated treatment and laminitis prophylaxis is currently limited to digital cryotherapy. Several key steps in laminitis pathophysiology have been elucidated, resulting in identification of drugs that may prevent laminitis (anti-laminitis drugs (ALDs)). Many of these pharmaceuticals are not suitable for systemic delivery but may be amenable to either local or nanoparticle delivery mechanisms.The aim of this thesis was to evaluate local, systemic and nanoparticle delivery mechanisms, using the matrix metalloproteinase (MMP) inhibitor marimastat, to establish a method of drug delivery that yields sustained therapeutic lamellar concentrations for experimental and potential clinical use. In order to establish marimastat concentrations necessary for inhibition of lamellar MMPs, zymography was performed using lamellar homogenates incubated in increasing concentrations of marimastat. Based on this assay, target marimastat concentrations of 177 ng/mL were set (the concentration necessary to inhibit 90% of lamellar MMP-2 and MMP-9).

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Comparison of fluoroquinolone pharmacokinetic parameters after treatment with marbofloxacin, enrofloxacin, and difloxacin in dogs

Cited by 55 publications

References 34 publications

Disposition Kinetics of Difloxacin After Intravenous, Intramuscular and Subcutaneous Administration in Calves

Disposition Kinetics of Difloxacin After Intravenous, Intramuscular and Subcutaneous Administration in Calves

Evaluation of the contribution of gyrA mutation and efflux pumps to fluoroquinolone and multidrug resistance in pathogenic Escherichia coli isolates from dogs and cats

Drug delivery to equine digital lamellar tissue

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