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Mark G. Papich - One of the best experts on this subject based on the ideXlab platform.

  • Efficacy of Enrofloxacin in a mouse model of sepsis.
    Journal of The American Association for Laboratory Animal Science, 2014
    Co-Authors: Andrea R Slate, Mark G. Papich, Sheila Bandyopadhyay, Kevin P. Francis, Brian Karolewski, Kevin A Prestia
    Abstract:

    We examined the efficacy of Enrofloxacin administered by 2 different routes in a mouse model of sepsis. Male CD1 mice were infected with a bioluminescent strain of enteropathogenic Escherichia coli and treated with Enrofloxacin either by injection or in drinking water. Peak serum levels were evaluated by using HPLC. Mice were monitored for signs of clinical disease, and infections were monitored by using bioluminescence imaging. Serum levels of Enrofloxacin and the active metabolite ciprofloxacin were greater in the group treated by injection than in controls or the groups treated by administration in drinking water. Survival of the group treated with Enrofloxacin injection was greater than that of controls and groups treated with Enrofloxacin in the drinking water. Bioluminescence in the group treated with Enrofloxacin injection was less than that in the groups treated with oral administration at 12 h and in the groups treated orally and the control group at 16 h. According to these findings, we recommend the use of injectable Enrofloxacin at 5 mg/kg SC for mice with systemic infections.

  • stability of three commonly compounded extemporaneous Enrofloxacin suspensions for oral administration to exotic animals
    Javma-journal of The American Veterinary Medical Association, 2013
    Co-Authors: Olivia A Petritz, David Sanchezmigallon Guzman, Valerie J Wiebe, Mark G. Papich
    Abstract:

    Objective—To evaluate the stability of 3 extemporaneous oral suspensions of Enrofloxacin mixed with readily available flavoring vehicles when stored at room temperature (approx 22°C). Design—Evaluation study. Samples—3 commonly compounded oral suspensions of Enrofloxacin. Procedures—On day 0, commercially available Enrofloxacin tablets were compounded with a mixture of distilled water and corn syrup (formulation A) or cherry syrup (formulation B) flavoring vehicles to create suspensions with a nominal Enrofloxacin concentration of 22.95 mg/mL, and 2.27% Enrofloxacin injectable solution was compounded with a liquid sweetener (formulation C) to create a suspension with a nominal Enrofloxacin concentration of 11.35 mg/mL. Preparations were stored in amber-colored vials at room temperature for 56 days. For each preparation, the Enrofloxacin concentration was evaluated with high-performance liquid chromatography at prespecified intervals during the study. The pH, odor, and consistency for all suspensions were ...

  • distribution of Enrofloxacin and its active metabolite using an in vivo ultrafiltration sampling technique after the injection of Enrofloxacin to pigs
    Journal of Veterinary Pharmacology and Therapeutics, 2012
    Co-Authors: Kristen M Messenger, Mark G. Papich, Anthony T Blikslager
    Abstract:

    Messenger, K. M., Papich, M. G., Blikslager, A. T. Distribution of Enrofloxacin and its active metabolite, using an in vivo ultrafiltration sampling technique after the injection of Enrofloxacin to pigs. J. vet. Pharmacol. Therap. 35, 452–459. The objective of this study was to determine the pharmacokinetics (PK) of Enrofloxacin in pigs and compare to the tissue interstitial fluid (ISF). Six healthy, young pigs were administered 7.5 mg/kg Enrofloxacin subcutaneously (SC). Blood and ISF samples were collected from preplaced intravenous catheters and ultrafiltration sampling probes placed in three different tissue sites (intramuscular, subcutaneous, and intrapleural). Enrofloxacin concentrations were measured using high-pressure liquid chromatography with fluorescence detection, PK parameters were analyzed using a one-compartment model, and protein binding was determined using a microcentrifugation system. Concentrations of the active metabolite ciprofloxacin were negligible. The mean ± SD Enrofloxacin plasma half-life, volume of distribution, clearance, and peak concentration were 26.6 ± 6.2 h (harmonic mean), 6.4 ± 1.2 L/kg, 0.18 ± 0.08 L/kg/h, and 1.1 ± 0.3 μg/mL, respectively. The half-life of Enrofloxacin from the tissues was 23.6 h, and the maximum concentration was 1.26 μg/mL. Tissue penetration, as measured by a ratio of area-under-the-curve (AUC), was 139% (±69%). Plasma protein binding was 31.1% and 37.13% for high and low concentrations, respectively. This study demonstrated that the concentration of biologically active Enrofloxacin in tissues exceeds the concentration predicted by the unbound fraction of Enrofloxacin in pig plasma. At a dose of 7.5 mg/kg SC, the high tissue concentrations and long half-life produce an AUC/MIC ratio sufficient for the pathogens that cause respiratory infections in pigs.

  • Plasma and ear tissue concentrations of Enrofloxacin and its metabolite ciprofloxacin in dogs with chronic end‐stage otitis externa after intravenous administration of Enrofloxacin
    Veterinary Dermatology, 2009
    Co-Authors: Lynette K. Cole, Mark G. Papich, Kenneth W. Kwochka, Andrew Hillier, Daniel D. Smeak, Amy Lehman
    Abstract:

    : The purpose of this study was to measure the concentrations of Enrofloxacin and its metabolite ciprofloxacin following intravenous administration of Enrofloxacin in the plasma and ear tissue of dogs with chronic end-stage otitis undergoing a total ear canal ablation and lateral bulla osteotomy. The goals were to determine the relationship between the dose of Enrofloxacin and the concentrations of Enrofloxacin and ciprofloxacin, and determine appropriate doses of Enrofloxacin for treatment of chronic otitis externa and media. Thirty dogs were randomized to an Enrofloxacin-treatment group (5, 10, 15 or 20 mg kg(-1)) or control group (no Enrofloxacin). After surgical removal, ear tissue samples (skin, vertical ear canal, horizontal ear canal, middle ear) and a blood sample were collected. Concentrations of Enrofloxacin and ciprofloxacin in the plasma and ear tissue were measured by high performance liquid chromatography. Repeated measures models were applied to log-transformed data to assess dosing trends and Pearson correlations were calculated to assess concentration associations. Ear tissue concentrations of Enrofloxacin and ciprofloxacin were significantly (P < 0.05) higher than plasma concentrations. Each 5 mg kg(-1 )increase in the dose of Enrofloxacin resulted in a 72% and 37% increase in Enrofloxacin and ciprofloxacin concentrations, respectively. For bacteria with an minimal inhibitory concentration of 0.12-0.15 or less, 0.19-0.24, 0.31-0.39 and 0.51-0.64 microg mL(-1), Enrofloxacin should be dosed at 5, 10, 15 and 20 mg kg(-1), respectively. Treatment with Enrofloxacin would not be recommended for a bacterial organism intermediate or resistant in susceptibility to Enrofloxacin since appropriate levels of Enrofloxacin would not be attained.

  • pharmacokinetics after intravenous subcutaneous and oral administration of Enrofloxacin to alpacas
    American Journal of Veterinary Research, 2005
    Co-Authors: Rae A Gandolf, Mark G. Papich, Amy B Bringardner, Mark W Atkinson
    Abstract:

    OBJECTIVE: To determine plasma concentrations of Enrofloxacin and the active metabolite ciprofloxacin after p.o, s.c., and i.v. administration of Enrofloxacin to alpacas. ANIMALS: 6 adult female alpacas. PROCEDURE: A crossover design was used for administration of 3 single-dose treatments of Enrofloxacin to alpacas, which was followed by an observational 14-day multiple-dose regimen. Single-dose treatments consisted of i.v. and s.c. administration of injectable Enrofloxacin (5 mg/kg) and p.o administration of Enrofloxacin tablets (10 mg/kg) dissolved in grain to form a slurry. Plasma Enrofloxacin concentrations were measured by use of high-performance liquid chromatography. The multiple-dose regimen consisted of feeding a mixture of crushed and moistened Enrofloxacin tablets mixed with grain. Behavior, appetite, and fecal quality were monitored throughout the 14-day treatment regimen and for 71 additional days following treatment. RESULTS: Mean half-life following i.v., s.c., and p.o. administration was 11.2, 8.7, and 16.1 hours, respectively. For s.c. and p.o administration, mean total systemic availability was 90.18% and 29.31%, respectively; mean maximum plasma concentration was 3.79 and 1.81 microg/mL, respectively; and area under the curve (AUC) was 50.05 and 33.97 (microg x h)/mL, respectively. The s.c. or p.o administration of a single dose of Enrofloxacin yielded a ratio for AUC to minimum inhibitory concentration > 100 for many grampositive and gram-negative bacterial pathogens common to camelids. Conclusions and Clinical Relevance-The administration of Enrofloxacin (5 mg/kg, s.c., or 10 mg/kg, p.o) may be appropriate for antimicrobial treatment of alpacas.

Jaroslava Halper - One of the best experts on this subject based on the ideXlab platform.

  • The effects of Enrofloxacin on decorin and glycosaminoglycans in avian tendon cell cultures
    Archives of Toxicology, 2004
    Co-Authors: Jung Hae Yoon, Randolph L. Brooks, Jian Zeng Zhao, David Isaacs, Jaroslava Halper
    Abstract:

    Tendonitis and tendon rupture have been reported to occur during or following therapy with fluoroquinolone antibiotics. Though the pathogenesis is unknown, several studies suggest that fluoroquinolone antibiotics alter proteoglycan content in soft tissues, including tendons, and thereby alter collagen fibrillogenesis. To better understand the mechanism of action of fluoroquinolones, we studied the effects of Enrofloxacin, a widely used fluoroquinolone in veterinary medicine, on avian tendon cell cultures established from gastrocnemius tendons from 18-day-old chicken embryos. We found that cell proliferation was progressively inhibited with increasing concentrations of Enrofloxacin. This was accompanied by changes in morphology, extracellular matrix content and collagen fibril formation as detected by electron microscopy. We also observed a 35% decrease in the content of total monosaccharides in Enrofloxacin-treated cells. The ratio of individual monosaccharides was also altered in Enrofloxacin-treated cells. Enrofloxacin also induced the synthesis of small amounts of keratan sulfate in tendon cells. Moreover we observed Enrofloxacin-induced changes in glycosylation of decorin, the most abundant tendon proteoglycan, resulting in the emergence of multiple lower molecular bands that were identifiable as decorin after chondroitinase ABC and N -glycanase treatment of extracts from Enrofloxacin-treated cells. Medium conditioned by Enrofloxacin-treated cells contained less decorin than did medium conditioned by control cells. We hypothesize that Enrofloxacin induces either changes in the number of N -linked oligosaccharides attached to the core protein of decorin or changes in decorin degradation process. In conclusion, our data suggest that Enrofloxacin affects cell proliferation and extracellular matrix through changes in glycosylation.

Jung Hae Yoon - One of the best experts on this subject based on the ideXlab platform.

  • The effects of Enrofloxacin on decorin and glycosaminoglycans in avian tendon cell cultures
    Archives of Toxicology, 2004
    Co-Authors: Jung Hae Yoon, Randolph L. Brooks, Jian Zeng Zhao, David Isaacs, Jaroslava Halper
    Abstract:

    Tendonitis and tendon rupture have been reported to occur during or following therapy with fluoroquinolone antibiotics. Though the pathogenesis is unknown, several studies suggest that fluoroquinolone antibiotics alter proteoglycan content in soft tissues, including tendons, and thereby alter collagen fibrillogenesis. To better understand the mechanism of action of fluoroquinolones, we studied the effects of Enrofloxacin, a widely used fluoroquinolone in veterinary medicine, on avian tendon cell cultures established from gastrocnemius tendons from 18-day-old chicken embryos. We found that cell proliferation was progressively inhibited with increasing concentrations of Enrofloxacin. This was accompanied by changes in morphology, extracellular matrix content and collagen fibril formation as detected by electron microscopy. We also observed a 35% decrease in the content of total monosaccharides in Enrofloxacin-treated cells. The ratio of individual monosaccharides was also altered in Enrofloxacin-treated cells. Enrofloxacin also induced the synthesis of small amounts of keratan sulfate in tendon cells. Moreover we observed Enrofloxacin-induced changes in glycosylation of decorin, the most abundant tendon proteoglycan, resulting in the emergence of multiple lower molecular bands that were identifiable as decorin after chondroitinase ABC and N -glycanase treatment of extracts from Enrofloxacin-treated cells. Medium conditioned by Enrofloxacin-treated cells contained less decorin than did medium conditioned by control cells. We hypothesize that Enrofloxacin induces either changes in the number of N -linked oligosaccharides attached to the core protein of decorin or changes in decorin degradation process. In conclusion, our data suggest that Enrofloxacin affects cell proliferation and extracellular matrix through changes in glycosylation.

J.k. Malik - One of the best experts on this subject based on the ideXlab platform.

  • Pharmacokinetic disposition of subcutaneously administered Enrofloxacin in goats.
    Veterinary Research Communications, 2002
    Co-Authors: S. Ramesh, J.k. Malik
    Abstract:

    The pharmacokinetic disposition of Enrofloxacin was studied in goats after subcutaneous (s.c.) administration at a single dose of 7.5 mg/kg body weight. Blood samples were drawn from a jugular vein into heparinized tubes at predetermined time intervals after administration of the drug and the plasma was separated by centrifugation. The concentrations of Enrofloxacin in the plasma were determined by a microbiological assay using Escherichia coli as the test organism. The plasma concentration–time data were analysed by non-compartmental methods. Enrofloxacin was rapidly absorbed, an appreciable concentration of the drug (0.30±0.13 μg/ml) being present in the plasma by 5 min after s.c. administration. The maximum plasma concentration of Enrofloxacin and the time to reach that maximum were 2.91±0.39 μg/ml and 2.9±0.51 h, respectively. A detectable concentration of Enrofloxacin persisted in the plasma for 12 h. The elimination half-life and mean residence time of Enrofloxacin were 2.84±0.57 and 5.74±0.28 h, respectively. It is suggested that Enrofloxacin given subcutaneously may be useful in the treatment of susceptible bacterial infections in goats.

  • Pharmacokinetics of Enrofloxacin and its metabolite ciprofloxacin in goats given Enrofloxacin alone and in combination with probenecid.
    Veterinary Journal, 2002
    Co-Authors: S. Ramesh, A. H. Ahmad, H.c. Tripathi, L.d. Sharma, J.k. Malik
    Abstract:

    Abstract The pharmacokinetics of Enrofloxacin and its active metabolite ciprofloxacin were investigated in goats given Enrofloxacin alone or in combination with probenecid. Enrofloxacin was administered i.m. at a dosage of 5 mg.kg−1 alone or in conjunction with probenecid (40 mg.kg−1, i.v.). Blood samples were drawn from the jugular vein at predetermined time intervals after drug injection. Plasma was separated and analysed simultaneously for Enrofloxacin and ciprofloxacin by reverse-phase high performance liquid chromatography. The plasma concentration-time data for both Enrofloxacin and ciprofloxacin were best described by a one-compartment open pharmacokinetic model. The elimination half-life (t1/2β), area under the plasma concentration-time curve (AUC), volume of distribution (Vd(area)), mean residence time (MRT) and total systemic clearance (ClB) were 1.39 h, 7.82 μg.h.mL, 1.52 L.kg−1, 2.37 h and 802.9 mL.h−1.kg−1, respectively. Enrofloxacin was metabolized to ciprofloxacin in goats and the ratio between the AUCs of ciprofloxacin and Enrofloxacin was 0.34. The t1/2β, AUC and MRT of ciprofloxacin were 1.82 h, 2.55 μg.h.mL and 3.59 h, respectively. Following combined administration of probenecid and Enrofloxacin in goats, the sum of concentrations of Enrofloxacin and ciprofloxacin levels ≥0.1 μg.mL−1 persisted in plasma up to 12 h.Co-administration of probenecid did not affect the t1/2β, AUC, Vd (area) and ClB of Enrofloxacin, whereas the values of t1/2β (3.85 h), AUC (6.29 μg.h.mL), MRT (7.34 h) and metabolite ratio (0.86) of ciprofloxacin were significantly increased. The sum of both Enrofloxacin and ciprofloxacin levels was ≥0.1 μ.mL−1 and was maintained in plasma up to 8 h in goats after i.m. administration of Enrofloxacin alone. These dataindicate that a 12 h dosing regime may be appropriate for use in goats.

  • Disposition kinetics of Enrofloxacin and ciprofloxacin following intravenous administration of Enrofloxacin in goats
    Small Ruminant Research, 2002
    Co-Authors: S. Ramesh, A. H. Ahmad, H.c. Tripathi, L.d. Sharma, J.k. Malik
    Abstract:

    Abstract Pharmacokinetic properties of the antimicrobial fluoroquinolone, Enrofloxacin, were studied in female goats. Enrofloxacin was given to goats in a single dose of 2.5 mg kg −1 body weight by intravenous (i.v.) route. Blood samples were collected via jugular venipuncture into heparinized tubes at predetermined times after drug administration. Plasma concentrations of Enrofloxacin and its active metabolite ciprofloxacin were simultaneously determined by reversed-phase high performance liquid chromatography. The decline of Enrofloxacin concentrations in plasma after the drug administration was best described by a biexponential equation. A rapid distribution phase was followed by the slower elimination phase with a half-life ( t 1/2 β ) of 0.73±0.047 h. The volume of distribution ( V d(area) ), total systemic clearance (Cl B ), and mean residence time (MRT) of Enrofloxacin were 1.38±0.045 l kg −1 , 1331±93.64 ml h −1  kg −1 and 0.97±0.051 h, respectively. The ratio between the area under the plasma concentration–time curves (AUCs) of ciprofloxacin and Enrofloxacin was 0.24. The AUC, t 1/2 β and MRT of ciprofloxacin were 0.44±0.02 μg h ml −1 , 0.92±0.13 and 1.93±0.19 h, respectively. The combined Enrofloxacin and ciprofloxacin concentrations in plasma (≥0.1 μg ml −1 ) were maintained up to 3 h after Enrofloxacin administration. It appears that Enrofloxacin can be useful for the treatment of goat diseases associated with pathogens that are sensitive to the drug.

  • Pharmacokinetics of Enrofloxacin and its metabolite ciprofloxacin after intramuscular administration of Enrofloxacin in goats.
    Veterinary Research Communications, 2001
    Co-Authors: S. Ramesh, A. H. Ahmad, H.c. Tripathi, L.d. Sharma, J.k. Malik
    Abstract:

    The pharmacokinetics of Enrofloxacin and its active metabolite ciprofloxacin were investigated in goats after a single intramuscular administration of Enrofloxacin at 2.5 mg/kg body weight. The plasma concentrations of Enrofloxacin and ciprofloxacin were determined simultaneously by a HPLC method. The peak concentrations (Cmax) of Enrofloxacin (1.13 μg/ml) and ciprofloxacin (0.24 μg/ml) were observed at 0.8 and 1.2 h, respectively. The elimination half-life (t1/2β), volume of distribution (Vd(area)), total body clearance (ClB) and mean residence time (MRT) of Enrofloxacin were 0.74 h, 1.42 L/kg, 1329 ml/h per kg and 1.54 h, respectively. The t1/2β, area under the plasma concentration–time curve (AUC) and the MRT of ciprofloxacin were 1.38 h, 0.74 μg h/ml and 2.73 h, respectively. The metabolic conversion of Enrofloxacin to ciprofloxacin was appreciable (36%) and the sum of the plasma concentrations of Enrofloxacin and ciprofloxacin was maintained at or above 0.1 μg/ml for up to 4 h. Enrofloxacin appears to be useful for the treatment of goat diseases associated with pathogens sensitive to this drug.

  • Effects of endotoxin-induced fever and probenecid on disposition of Enrofloxacin and its metabolite ciprofloxacin after intravascular administration of Enrofloxacin in goats
    Journal of Veterinary Pharmacology and Therapeutics, 2000
    Co-Authors: S. Ramesh, A. H. Ahmad, H.c. Tripathi, L.d. Sharma, J.k. Malik
    Abstract:

    : Pharmacokinetics of Enrofloxacin and its active metabolite ciprofloxacin were investigated in normal, febrile and probenecid-treated adult goats after single intravenous (i.v.) administration of Enrofloxacin (5 mg/kg). Pharmacokinetic evaluation of the plasma concentration-time data of Enrofloxacin and ciprofloxacin was performed using two- and one-compartment open models, respectively. Plasma Enrofloxacin concentrations were significantly higher in febrile (0.75-7 h) and probenecid-treated (5-7 h) goats than in normal goats. The sum of Enrofloxacin and ciprofloxacin concentrations in plasma > or =0.1 microg /mL was maintained up to 7 and 8 h in normal and febrile or probenecid-treated goats, respectively. The t1/2beta, AUC, MRT and ClB of Enrofloxacin in normal animals were determined to be 1.14 h, 6.71 microg .h/mL, 1.5 h and 807 mL/h/kg, respectively. The fraction of Enrofloxacin metabolized to ciprofloxacin was 28.8%. The Cmax., t1/2beta, AUC and MRT of ciprofloxacin in normal goats were 0.45 microg /mL, 1.79 h, 1.84 microg .h/mL and 3.34 h, respectively. As compared with normal goats, the values of t1/2beta (1.83 h), AUC (11.68 microg ? h/mL) and MRT (2.13 h) of Enrofloxacin were significantly higher, whereas its ClB (430 mL/h/kg) and metabolite conversion to ciprofloxacin (8.5%) were lower in febrile goats. The Cmax. (0.18 microg /mL) and AUC (0.99 microg .h/mL) of ciprofloxacin were significantly decreased, whereas its t1/2beta (2.75 h) and MRT (4.58 h) were prolonged in febrile than in normal goats. Concomitant administration of probenecid (40 mg/kg, i.v.) with Enrofloxacin did not significantly alter any of the pharmacokinetic variables of either Enrofloxacin or ciprofloxacin in goats.

B. K. Park - One of the best experts on this subject based on the ideXlab platform.