Evaluation of a Tasteless Enrofloxacin Pharmaceutical Preparation for Cats. Naive Pooled-Sample Approach to Study Its Pharmacokinetics

Available pharmaceutical preparations of enrofloxacin injected SC or IM to cats are likely to cause adverse tissue reactions in the injection sites (pH of the drug preparations is ≥10.4). Tablets often induce abundant ptyalism and vomiting, casting doubt on the efficacy of the drug administration ma...

Full description

Bibliographic Details
Main Authors: Lilia Gutierrez, Graciela Tapia, Eduardo Gutierrez, Hector Sumano
Format: Article
Language:English
Published: MDPI AG 2021-08-01
Series:Animals
Subjects:
Online Access:https://www.mdpi.com/2076-2615/11/8/2312
_version_ 1797524910148419584
author Lilia Gutierrez
Graciela Tapia
Eduardo Gutierrez
Hector Sumano
author_facet Lilia Gutierrez
Graciela Tapia
Eduardo Gutierrez
Hector Sumano
author_sort Lilia Gutierrez
collection DOAJ
description Available pharmaceutical preparations of enrofloxacin injected SC or IM to cats are likely to cause adverse tissue reactions in the injection sites (pH of the drug preparations is ≥10.4). Tablets often induce abundant ptyalism and vomiting, casting doubt on the efficacy of the drug administration maneuver. In addition, the reported oral bioavailability is very low. In this trial, the oral pharmacokinetics of dried alginate beads of enrofloxacin (DABE) administered by concealing them in the cat’s moist food or morsels, is described. A naïve polled sampling approach was chosen with fourteen adult healthy cats. Neither their housing nor their feeding habits were altered. A single pharmacokinetic profile was obtained with 5 samples per designated bleeding time, sampling each cat 2–3 times only. None of the cats rejected their medicated food or morsels. Plasma profile of enrofloxacin exhibited an AUC<sub>0–24</sub> value of 12.4 µg·h/mL and an AUC<sub>0–∞</sub> value of 19.2 µg·h/mL, which are comparatively greater than values previously referred for kittens. In contrast, λ and elimination t½ were almost identical (0.12 1/h and 6.1 h). Pharmacokinetics/pharmacodynamics ratios taking the breakpoint of <i>Staphylococcus epidermidis</i> as a surrogate (0.5 µg/mL), can be regarded as borderline or low, but perhaps adequate in cats, as higher concentrations may be linked to toxicity (AUC<sub>0–24</sub>/MIC = 24.8; Cmax/MIC = 4.6).
first_indexed 2024-03-10T09:04:20Z
format Article
id doaj.art-6d8d0ac2488e4c8bbf7deeaf17c71016
institution Directory Open Access Journal
issn 2076-2615
language English
last_indexed 2024-03-10T09:04:20Z
publishDate 2021-08-01
publisher MDPI AG
record_format Article
series Animals
spelling doaj.art-6d8d0ac2488e4c8bbf7deeaf17c710162023-11-22T06:30:18ZengMDPI AGAnimals2076-26152021-08-01118231210.3390/ani11082312Evaluation of a Tasteless Enrofloxacin Pharmaceutical Preparation for Cats. Naive Pooled-Sample Approach to Study Its PharmacokineticsLilia Gutierrez0Graciela Tapia1Eduardo Gutierrez2Hector Sumano3Departamento de Fisiología y Farmacología, Facultad de Medicina Veterinaria y Zootecnia, Universidad Nacional Autónoma de México, Avenida Universidad 3000, Coyoacán 04510, MexicoDepartamento de Genética y Bioestadística, Facultad de Medicina Veterinaria y Zootecnia, Universidad Nacional Autónoma de México, Avenida Universidad 3000, Coyoacán 04510, MexicoDepartamento de Fisiología y Farmacología, Facultad de Medicina Veterinaria y Zootecnia, Universidad Nacional Autónoma de México, Avenida Universidad 3000, Coyoacán 04510, MexicoDepartamento de Fisiología y Farmacología, Facultad de Medicina Veterinaria y Zootecnia, Universidad Nacional Autónoma de México, Avenida Universidad 3000, Coyoacán 04510, MexicoAvailable pharmaceutical preparations of enrofloxacin injected SC or IM to cats are likely to cause adverse tissue reactions in the injection sites (pH of the drug preparations is ≥10.4). Tablets often induce abundant ptyalism and vomiting, casting doubt on the efficacy of the drug administration maneuver. In addition, the reported oral bioavailability is very low. In this trial, the oral pharmacokinetics of dried alginate beads of enrofloxacin (DABE) administered by concealing them in the cat’s moist food or morsels, is described. A naïve polled sampling approach was chosen with fourteen adult healthy cats. Neither their housing nor their feeding habits were altered. A single pharmacokinetic profile was obtained with 5 samples per designated bleeding time, sampling each cat 2–3 times only. None of the cats rejected their medicated food or morsels. Plasma profile of enrofloxacin exhibited an AUC<sub>0–24</sub> value of 12.4 µg·h/mL and an AUC<sub>0–∞</sub> value of 19.2 µg·h/mL, which are comparatively greater than values previously referred for kittens. In contrast, λ and elimination t½ were almost identical (0.12 1/h and 6.1 h). Pharmacokinetics/pharmacodynamics ratios taking the breakpoint of <i>Staphylococcus epidermidis</i> as a surrogate (0.5 µg/mL), can be regarded as borderline or low, but perhaps adequate in cats, as higher concentrations may be linked to toxicity (AUC<sub>0–24</sub>/MIC = 24.8; Cmax/MIC = 4.6).https://www.mdpi.com/2076-2615/11/8/2312enrofloxacin-alginatepharmacokineticscatsnaïve pooled sampling
spellingShingle Lilia Gutierrez
Graciela Tapia
Eduardo Gutierrez
Hector Sumano
Evaluation of a Tasteless Enrofloxacin Pharmaceutical Preparation for Cats. Naive Pooled-Sample Approach to Study Its Pharmacokinetics
Animals
enrofloxacin-alginate
pharmacokinetics
cats
naïve pooled sampling
title Evaluation of a Tasteless Enrofloxacin Pharmaceutical Preparation for Cats. Naive Pooled-Sample Approach to Study Its Pharmacokinetics
title_full Evaluation of a Tasteless Enrofloxacin Pharmaceutical Preparation for Cats. Naive Pooled-Sample Approach to Study Its Pharmacokinetics
title_fullStr Evaluation of a Tasteless Enrofloxacin Pharmaceutical Preparation for Cats. Naive Pooled-Sample Approach to Study Its Pharmacokinetics
title_full_unstemmed Evaluation of a Tasteless Enrofloxacin Pharmaceutical Preparation for Cats. Naive Pooled-Sample Approach to Study Its Pharmacokinetics
title_short Evaluation of a Tasteless Enrofloxacin Pharmaceutical Preparation for Cats. Naive Pooled-Sample Approach to Study Its Pharmacokinetics
title_sort evaluation of a tasteless enrofloxacin pharmaceutical preparation for cats naive pooled sample approach to study its pharmacokinetics
topic enrofloxacin-alginate
pharmacokinetics
cats
naïve pooled sampling
url https://www.mdpi.com/2076-2615/11/8/2312
work_keys_str_mv AT liliagutierrez evaluationofatastelessenrofloxacinpharmaceuticalpreparationforcatsnaivepooledsampleapproachtostudyitspharmacokinetics
AT gracielatapia evaluationofatastelessenrofloxacinpharmaceuticalpreparationforcatsnaivepooledsampleapproachtostudyitspharmacokinetics
AT eduardogutierrez evaluationofatastelessenrofloxacinpharmaceuticalpreparationforcatsnaivepooledsampleapproachtostudyitspharmacokinetics
AT hectorsumano evaluationofatastelessenrofloxacinpharmaceuticalpreparationforcatsnaivepooledsampleapproachtostudyitspharmacokinetics