Pharmacokinetics and distribution in interstitial and pulmonary epithelial lining fluid of danofloxacin in ruminant and preruminant calves

Mzyk, Danielle A.; Baynes, Ronald E.; Messenger, Kristen M.; Martinez, Marilyn N.; Smith, Geof W.

doi:10.1111/jvp.12346

Cited by 11 publications

(17 citation statements)

References 51 publications

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“…The lower distribution of ENR was previously reported for 4-to 5-month-old calves (Davis et al, 2007). The V dss value for DNX in premature calves (4.45 L/ kg) is higher than that previously reported in six-month-old calves (3.12 L/kg; Aliabadi & Lees, 2003); however, it is similar to that previously reported in 2-to 3-week-old calves (4.12 L/kg; Mzyk, TA B L E 1 Mean (± SD) pharmacokinetic parameters of ENR (10 mg/kg, IV and IM administration), ciprofloxacin, and danofloxacin (8 mg/ kg, IV and IM administration) in premature calves (n = 6) Baynes, Messenger, Martinez, & Smith, 2017). The V dss is affected by age-related changes, such as the ratio of binding to plasma proteins, the body fat-water composition, hemodynamic parameters, and the physicochemical properties of the drugs (Mangoni & Jackson, 2004).…”

Section: Discussionsupporting

confidence: 85%

Pharmacokinetics of enrofloxacin and danofloxacin in premature calves

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et al. 2019

Vet Pharm & Therapeutics

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The aim of this study was to determine the pharmacokinetics/pharmacodynamics of enrofloxacin (ENR) and danofloxacin (DNX) following intravenous (IV) and intramuscular (IM) administrations in premature calves. The study was performed on twenty‐four calves that were determined to be premature by anamnesis and general clinical examination. Premature calves were randomly divided into four groups (six premature calves/group) according to a parallel pharmacokinetic (PK) design as follows: ENR‐IV (10 mg/kg, IV), ENR‐IM (10 mg/kg, IM), DNX‐IV (8 mg/kg, IV), and DNX‐IM (8 mg/kg, IM). Plasma samples were collected for the determination of tested drugs by high‐pressure liquid chromatography with UV detector and analyzed by noncompartmental methods. Mean PK parameters of ENR and DNX following IV administration were as follows: elimination half‐life (t1/2λz) 11.16 and 17.47 hr, area under the plasma concentration–time curve (AUC0‐48) 139.75 and 38.90 hr*µg/ml, and volume of distribution at steady‐state 1.06 and 4.45 L/kg, respectively. Total body clearance of ENR and DNX was 0.07 and 0.18 L hr−1 kg−1, respectively. The PK parameters of ENR and DNX following IM injection were t1/2λz 21.10 and 28.41 hr, AUC0‐48 164.34 and 48.32 hr*µg/ml, respectively. The bioavailability (F) of ENR and DNX was determined to be 118% and 124%, respectively. The mean AUC0‐48CPR/AUC0‐48ENR ratio was 0.20 and 0.16 after IV and IM administration, respectively, in premature calves. The results showed that ENR (10 mg/kg) and DNX (8 mg/kg) following IV and IM administration produced sufficient plasma concentration for AUC0‐24/minimum inhibitory concentration (MIC) and maximum concentration (Cmax)/MIC ratios for susceptible bacteria, with the MIC90 of 0.5 and 0.03 μg/ml, respectively. These findings may be helpful in planning the dosage regimen for ENR and DNX, but there is a need for further study in naturally infected premature calves.

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Section: Discussionsupporting

confidence: 85%

Pharmacokinetics of enrofloxacin and danofloxacin in premature calves

Çorum

Altan

Yıldız

et al. 2019

Vet Pharm & Therapeutics

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“…It is best to assess the clinical efficacy of macrolides at the site of infection [ 7 ]. According to previous studies, intrapulmonary pharmacokinetic examination had been performed by collecting the BAL from larger mammals using a sterilised catheter [ 7 , 38 , 43 , 62 ]. However, the target tissue should be plasma but not PELF for the calculation of CO PD for macrolides.…”

Section: Discussionmentioning

confidence: 99%

“…The urea dilution method was used to estimate the volume of PELF in the BAL fluid, as previously described method [ 17 , 41 – 43 ]. The concentration of urea in plasma and BAL were determined by the urea glutamate dehydrogenase enzymatic method, measured using an automatic dry-type biochemical analyser (DRI-CHEM NX500iVC, FUJIFILM (China) Investment Co., Ltd.) at the National Reference Laboratory of Veterinary Drug Residues (Wuhan, China).…”

Section: Methodsmentioning

confidence: 99%

The pharmacokinetic-pharmacodynamic modeling and cut-off values of tildipirosin against Haemophilus parasuis

et al. 2017

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The goal of this study was to establish the epidemiological, pharmacodynamic cut-off values, optimal dose regimens for tildipirosin against Haemophilus parasuis. The minimum inhibitory concentrations (MIC) of 164 HPS isolates were determined and SH0165 whose MIC (2 μg/ml ) were selected for PD analysis. The ex vivo MIC in plasma of SH0165 was 0.25 μg/ml which was 8 times lower than that in TSB. The bacteriostatic, bactericidal and elimination activity (AUC24h/MIC) in serum were 26.35, 52.27 and 73.29 h based on the inhibitory sigmoid Emax modeling. The present study demonstrates that 97.9% of the wild-type (WT) isolates were covered when the epidemiological cut-off value (ECV) was set at 8 μg/ml. The parameters including AUC24h, AUC, T1/2, Cmax, CLb and MRT in PELF were 19.56, 60.41, 2.32, 4.02, 56.6, and 2.63 times than those in plasma, respectively. Regarding the Monte Carlo simulation, the COPD was defined as 0.5 μg/ml in vitro, and the optimal doses to achieve bacteriostatic, bactericidal and elimination effect were 1.85, 3.67 and 5.16 mg/kg for 50% target, respectively, and 2.07, 4.17 and 5.78 mg/kg for 90% target, respectively. The results of this study offer a more optimised alternative for clinical use and demonstrated that 4.17 mg/kg of tildipirosin by intramuscular injection could have an effect on bactericidal activity against HPS. These values are of great significance for the effective treatment of HPS infections, but it also be deserved to be validated in clinical practice in the future research.

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“…The ISF was injected directly onto the HPLC/UPLC. Danofloxacin was extracted from plasma and BAL supernatant using a modified enrofloxacin extraction method described previously [19]. For tulathromycin, plasma samples for UPLC-MS/MS analysis were pretreated by mixing 500-μL of plasma with 500-μL of 4% phosphoric acid, and vortexing for 10 seconds.…”

Section: Methodsmentioning

confidence: 99%

Impact of bovine respiratory disease on the pharmacokinetics of danofloxacin and tulathromycin in different ages of calves

et al. 2019

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Pneumonia is one of the most economically important respiratory diseases of calves and knowledge of the impact of clinical disease on pharmacokinetics (PK) in young calves is limited. This study was undertaken to investigate the efficacy and PK of two antibiotics, tulathromycin and danofloxacin, in two age groups of calves experimentally infected with Pasteurella multocida . Both danofloxacin, a fluoroquinolone antibiotic, and tulathromycin, a macrolide antibiotic is approved for the treatment of bovine respiratory disease (BRD). To evaluate potential influences of age and disease on drug distribution and elimination in calves, plasma, interstitial fluid (ISF), and pulmonary epithelial lining fluid (PELF) were analyzed for drug concentrations. Concentrations for both drugs in the PELF were estimated by a urea dilution assay of the collected bronchoalveolar lavage fluids. Age was determined to be a significant covariate for calves administered danofloxacin and tulathromycin for plasma PK parameters. For calves administered danofloxacin, the area under the curve (AUC) in the plasma was lower in 6-month old calves (18.9 ± 12.6 hr* μg/mL) vs. 3-week old calves (32.0 ± 8.2 hr* μg/mL). Clearance (CL/F) of danofloxacin was higher in 6-month old calves. In contrast, tulathromycin plasma concentrations were higher in 6 month old calves and CL/F was higher in 3-week old calves. Age did not significantly influence the ISF concentrations of danofloxacin or tulathromycin in calves with respiratory disease, unlike previous studies which reported higher ISF concentrations of danofloxacin and tulathromycin in 6-month old calves when compared to younger calves. PELF concentrations were higher than plasma and ISF for both danofloxacin and tulathromycin, but did not differ between age groups. Potential reasons for age-related differences on plasma concentration–time profiles and the impact of disease on the partitioning of the drug from the blood to the lungs and ISF as a function of age are explored.

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Pharmacokinetics and distribution in interstitial and pulmonary epithelial lining fluid of danofloxacin in ruminant and preruminant calves

Cited by 11 publications

References 51 publications

Pharmacokinetics of enrofloxacin and danofloxacin in premature calves

Pharmacokinetics of enrofloxacin and danofloxacin in premature calves

The pharmacokinetic-pharmacodynamic modeling and cut-off values of tildipirosin against Haemophilus parasuis

Impact of bovine respiratory disease on the pharmacokinetics of danofloxacin and tulathromycin in different ages of calves

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