Pharmacokinetics of Levofloxacin Following Intravenous and Subcutaneous Administration in Sheep

Patel, Urvesh D.; Patel, Jatin H.; Bhavsar, Shailesh K.; Thaker, Aswin M.

doi:10.3923/ajava.2012.85.93

Cited by 12 publications

(18 citation statements)

References 26 publications

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“…The volume of drug distribution at a steady-state after I/V administration of 1.37 L/kg suggests moderate penetration of the drug through the biological membranes of the body. This value is within the range reported in avian and mammalian species, 0.92 L/kg in sheep and 2.88-3.25 L/kg in broiler chickens [15,16,35].…”

Section: Discussionsupporting

confidence: 87%

“…The average plasma clearance of levofloxacin was 0.6 mL/g*h with some variability among the experimental animals. This is the highest clearance rate thus far reported in all previous mammalian and avian species studied, except sheep, which had similar reported clearance (0.55 mL/g*h [35] vs. 0.6 mL/g*h in rabbits) and half-life of elimination (2.38 h vs. 2.06 h in rabbits) values. However, another study in sheep [14] showed a lower clearance of 0.2 mL/g*h and a longer elimination half-life (3.3 h), but that study was performed using sheep with a body mass almost twice as large, possibly, resulting in slower drug elimination.…”

Section: Pharmacokinetics Of Levofloxacin In Healthy Rabbitssupporting

confidence: 70%

“…These similarities in PKs suggest that the same drug efficacy should be expected for all 3 routes of administration when levofloxacin is given at a dose of 5 mg/kg. Moreover, previous studies of other fluoroquinolones in rabbits [33,34] and of levofloxacin in other animal species [11,16,35] showed very similar PK profiles after different routes of administration. The levofloxacin terminal plasma half-life appeared to be one of the shortest among the species tested (1.8-2.06 h, depending on the route of parenteral administration).…”

Section: Discussionmentioning

confidence: 61%

“…In food-producing animals, the levofloxacin extraction rate is also low. Based on data provided by Goudah and Abo-El-Sooud [13], Goudah and Hasabelnaby [14], and Patel et al [35], the authors have calculated average extraction levels for goats, sheep, and camels of 3.2%, 3.9%, and 9.5%. The estimated extraction ratio values in all of the animal species investigated indicate similar drug elimination abilities among the species.…”

Section: Pharmacokinetics Of Levofloxacin In Healthy Rabbitsmentioning

confidence: 99%

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Pharmacokinetic profiles of levofloxacin after intravenous, intramuscular and subcutaneous administration to rabbits (Oryctolagus cuniculus)

et al. 2020

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Levofloxacin pharmacokinetic profiles were evaluated in 6 healthy female rabbits after intravenous (I/V), intramuscular (I/M), or subcutaneous (S/C) administration routes at a single dose of 5 mg/kg in a 3 × 3 cross-over study. Plasma levofloxacin concentrations were detected using a validated Ultra Performance Liquid Chromatography method with a fluorescence detector. Levofloxacin was quantifiable up to 10 h post-drug administration. Mean AUC 0-last values of 9.03 ± 2.66, 9.07 ± 1.80, and 9.28 ± 1.56 mg/h*L were obtained via I/V, I/M, and S/C, respectively. Plasma clearance was 0.6 mL/g*h after I/V administration. Peak plasma concentrations using the I/M and S/C routes were 3.33 ± 0.39 and 2.91 ± 0.56 µg/mL. Bioavailability values, after extravascular administration were complete, -105% ± 27% (I/M) and 118% ± 40% (S/C). Average extraction ratio of levofloxacin after I/V administration was 7%. Additionally, levofloxacin administration effects on tear production and osmolarity were evaluated. Tear osmolarity decreased within 48 h post-drug administration. All 3 levofloxacin administration routes produced similar pharmacokinetic profiles. The studied dose is unlikely to be effective in rabbits; however, it was calculated that a daily dose of 29 mg/kg appears effective for I/V administration for pathogens with MIC < 0.5 µg/mL.

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Section: Discussionsupporting

confidence: 87%

Section: Pharmacokinetics Of Levofloxacin In Healthy Rabbitssupporting

confidence: 70%

Section: Discussionmentioning

confidence: 61%

Section: Pharmacokinetics Of Levofloxacin In Healthy Rabbitsmentioning

confidence: 99%

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Pharmacokinetic profiles of levofloxacin after intravenous, intramuscular and subcutaneous administration to rabbits (Oryctolagus cuniculus)

et al. 2020

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“…The MRT was 4.01 ± 0.33 h which was similar to cefepime in goats 4.89 h [8], while being shorter than cefepime in sheep 6.89 h [13]. These differences are relatively common and are frequently related to interspecies variation, assay methods used, the amount of time between blood samplings and/or the health status, and age of the animal [22].…”

Section: Discussionmentioning

confidence: 99%

Influence of Flunixin on the Disposition Kinetic of Cefepime in Goats

El-Hewaity

2014

Advances in Pharmacological Sciences

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The pharmacokinetic profile of cefepime (10 mg/kg b.w.) was studied following intravenous and intramuscular administration of cefepime alone and coadministered with flunixin (2.2 mg/kg b.w.) in goats. Cefepime concentrations in serum were determined by microbiological assay technique using Escherichia coli (MTCC 443) as test organism. Following intravenous injection of cefepime alone and in combination with flunixin, there are no significant changes in the pharmacokinetic parameters. Following intramuscular injection of cefepime alone and in combination with flunixin, the maximum serum concentration was significantly increased in flunixin coadministered group compared with cefepime alone. However, no significant changes were reported in other pharmacokinetic parameters. The result of in vitro protein binding study indicated that 15.62% of cefepime was bound to goat's serum protein. The mean bioavailability was 92.66% and 95.27% in cefepime alone and coadministered with flunixin, respectively. The results generated from the present study suggest that cefepime may be coadministered with flunixin without change in dose regimen. Cefepime may be given intramuscularly at 12 h intervals to combat susceptible bacterial infections.

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Ex vivo antibacterial activity of levofloxacin against Escherichia coli and its pharmacokinetic profile following intravenous and oral administrations in broilers

Lee

DeVito

Vercelli

et al. 2017

Research in Veterinary Science

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The use of antibiotics is necessary to treat bacterial diseases. Determination of optimal dosage in the target animals is increasingly being recognized as vital for maximizing efficacy and minimizing the risk of resistance, so this study aimed to evaluate the pharmacokinetics/pharmacodynamics (PK/PD) of levofloxacin in broilers. Using a parallel study design, each group of animals (n=20) received 5mg/kg of levofloxacin intravenously (IV) and orally (PO). Plasma, serum and tissues were collected for PK and PD studies. Plasma concentrations of levofloxacin were determined by HPLC. Minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) were determined against E. coli, isolated in clinical broilers. Ex vivo antibacterial activity was evaluated using the time killing method. Mean values of terminal half-life for IV and PO groups were 6.93 and 8.09h, respectively. Following oral administration, the peak plasma concentration was achieved at 0.88h (T). Mean value of oral bioavailability was 123.25%. Levofloxacin residues were found in all the tissues tested (muscle, liver, kidney and lung). Plasma concentration above 8× MIC lead to eradication of E. coli (incubation period of 24h). The results of ex vivo growth inhibition curves were consistent with the in vitro time-kill study. Levofloxacin showed dependent plasma concentration antibacterial activity against a clinical isolate of E. coli. According to the assessment of PK/PD relationship, administration of 5mg/kg of levofloxacin seems to be effective in killing E. coli. Also, simulated optimal dose based on the ex vivo PK/PD approach was 2.9mg/kg/day (bactericidal) to 4.3mg/kg/day (eradication) PO against E. coli (MIC=0.125μg/ml).

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Pharmacokinetics of Levofloxacin Following Intravenous and Subcutaneous Administration in Sheep

Cited by 12 publications

References 26 publications

Pharmacokinetic profiles of levofloxacin after intravenous, intramuscular and subcutaneous administration to rabbits (Oryctolagus cuniculus)

Pharmacokinetic profiles of levofloxacin after intravenous, intramuscular and subcutaneous administration to rabbits (Oryctolagus cuniculus)

Influence of Flunixin on the Disposition Kinetic of Cefepime in Goats

Ex vivo antibacterial activity of levofloxacin against Escherichia coli and its pharmacokinetic profile following intravenous and oral administrations in broilers

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