Pharmacokinetics of enrofloxacin and its metabolite ciprofloxacin following single-dose subcutaneous injection in black-tailed prairie dogs (Cynomys ludovicianus)

Abstract

OBJECTIVE To determine plasma concentrations of enrofloxacin and its active metabolite ciprofloxacin following single-dose SC administration to black-tailed prairie dogs (Cynomys ludovicianus). ANIMALS 8 captive healthy 6-month-old sexually intact male black-tailed prairie dogs. PROCEDURES Enrofloxacin (20 mg/kg) was administered SC once to 6 prairie dogs and IV once to 2 prairie dogs. A blood sample was collected from each animal immediately before (0 hours) and 0.5, 1, 2, 4, 8, 12, and 24 hours after drug administration to evaluate the pharmacokinetics of enrofloxacin and ciprofloxacin. Plasma enrofloxacin and ciprofloxacin concentrations were quantified with ultraperformance liquid chromatography-mass spectrometry, and noncompartmental pharmacokinetic analysis was performed. RESULTS Enrofloxacin was biotransformed to ciprofloxacin in the prairie dogs used in the study. For total fluoroquinolones (enrofloxacin and ciprofloxacin), the mean (range) of peak plasma concentration, time to maximum plasma concentration, and terminal half-life after SC administration were 4.90 μg/mL (3.44 to 6.08 μg/mL), 1.59 hours (0.5 to 2.00 hours), and 4.63 hours (4.02 to 5.20 hours), respectively. CONCLUSIONS AND CLINICAL RELEVANCE Results indicated that administration of enrofloxacin (20 mg/kg, SC, q 24 h) in black-tailed prairie dogs may be appropriate for treatment of infections with bacteria for which the minimum inhibitory concentration of enrofloxacin is ≤ 0.5 μg/mL. However, clinical studies are needed to determine efficacy of such enrofloxacin treatment.

Longitudinal Surveillance and Risk Assessment of Resistance in Escherichia coli to Enrofloxacin from A Large-Scale Chicken Farm in Hebei, China

“…Significant positive correlation results between ENR and CIP possibly because they belong to the fluoroquinolone antibiotics, and CIP is the main active metabolite when ENR works. After E. coli was resistant to ENR, it developed cross-resistance to CIPs with similar structures and properties [26,27]. Moreover, the metabolism of ENR and CIP in animals is relatively slow, and drug residues are easy to occur, resulting in the increase of drug resistance of pathogens in organisms.…”

Uso das fluoroquinolonas em cães e gatos domésticos

“…Após a incorporação da molécula do flúor, a partir da segunda geração as quinolonas também podem ser denominadas fluoroquinolonas. Em comparação com medicamentos de primeira geração, esses agentes têm aplicações clínicas mais amplas no tratamento de infecções complicadas do trato urinário, pielonefrite, pneumonias, infecções de pele e tecidos moles, infecções por clamídia, prostatite, osteomielite, febres entéricas, cólera e salmonelose, infecções causadas por Pseudomonas aeruginosa, exacerbações agudas de bronquite crônica e pneumonia nosocomial (Eshar, et al, 2018;Kukanich, et al, 2016). Expressam um equilibrado espectro de atividade, com eficácia aumentada contra Streptococcus pneumoniae e menor para P. aeruginosa (Shimizu & Harada, 2017).…”

“…As fluoroquinolonas representam uma das diversas classes de agentes antimicrobianos, que são utilizados em medicina humana e veterinária, no tratamento de uma grande variedade de infecções causadas por micro-organismos. O considerável sucesso desses produtos sintéticos pode ser atribuído ao amplo espectro de atividade, baixa toxicidade, fácil penetração na maioria das células bacterianas e boas propriedades farmacocinéticas (Eshar, et al, 2018). Entretanto, o uso constante e a utilização incorreta, levam a resistência por bactérias patogênicas para o animal e o homem (Cardoso, et al, 2015;Ishii, et al, 2011).…”

“…Os efeitos adversos mais comuns relacionados às fluoroquinolonas são geralmente leves e envolvem o trato gastrointestinal e o sistema nervoso central. As evidências disponíveis sugerem que os efeitos adversos podem ser próprios da classe das fluoroquinolonas, ou podem estar associados a uma porção química particular da estrutura molecular de cada fluoroquinolona, variando assim em frequência, severidade e natureza (Sousa, et al, 2014), ou podem também ocorrer devido a maiores concentrações plasmáticas e aumento da penetração tecidual, como reflexo do maior volume de distribuição (Eshar, et al, 2018).…”

A review article on Ciprofloxacin determination with various analytical techniques.

“…The drug is partially metabolized in the liver, giving four active metabolites; des-ethylene ciprofloxacin, oxo-ciprofloxacin, sulfo-ciprofloxacin and N-acetyl ciprofloxacin, where oxo-Ciprofloxacin is the primary urinary metabolite and sulfo-Ciprofloxacin is the fecal metabolite (Vance-Bryanet al,1990). A large percentage of the drug is excreted unchanged in the urine as well as all four metabolites (Eshar et al,2018). Accounting to the importance and the utmost need for such drug, several studies have employed various analytical techniques in owe of Ciprofloxacin analysis along with its metabolites; due to their major biological activity (Vance-Bryanet al,1990).…”