Pharmacokinetics of enrofloxacin and the rate of formation of its metabolite ciprofloxacin following intravenous and intramuscular single dose administration to male buffalo calves

Sharma, Pradeep; Ahmad, A. H.; Sharma, Lalita; Varma, Rachna

doi:10.1016/s1090-0233(02)00261-7

Cited by 13 publications

(16 citation statements)

References 6 publications

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“…The distribution half‐life (0.16 ± 0.04 h) of enrofloxacin in the present study indicated an easy and efficient distribution of enrofloxacin in the body tissues and fluids of sheep as in buffalo calves (7.73 min, Sharma et al. , 2003), while much shorter distribution half‐life has been reported in goats ( t 1/2 α 0.073 h, Rao et al.…”

Section: Pharmacokinetic Parameters Of Enrofloxacin and Ciprofloxacisupporting

confidence: 60%

Pharmacokinetics of enrofloxacin in sheep following intravenous and subcutaneous administration

Rahal

Kumar

Ahmad

et al. 2006

Vet Pharm & Therapeutics

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Enrofloxacin is a synthetic antibacterial agent of the flouroquinolone group developed exclusively for veterinary use (Altreuher, 1987). The important characteristics of the antimicrobial agent includes low host toxicity, high bioavailability, excellent tissue penetration, long serum half-life and a wide spectrum of activity against G-ve bacteria, intracellular organisms and lesser activity against G+ve organisms (Brown, 1996). It is mainly indicated for gastrointestinal, urogenital, skin and respiratory tract infections in various domestic animal species (Nielsen & Gyrd-Hansen, 1997).Flouroquinolones possess good oral bioavailability in all monogastric animals (up to 80%) but poor in ruminants (approximately 10%), which necessitates the use of parenteral routes of administration (Jenkins, 1990). The pharmacokinetics of enrofloxacin has been described in a variety of domestic animal species, but little is known about its kinetic behaviour following the subcutaneous administration in sheep, which forms an important component of Indian livestock population.The objective of this study was to determine the plasma concentrations and pharmacokinetics of enrofloxacin and its active metabolite, ciprofloxacin following the single dose intravenous and subcutaneous administration in sheep.Six crossbred healthy female sheep (weighing 25-30 kg) were quarantined for 2 weeks for use in the study. They were dewormed and maintained on concentrate, green fodder and were provided water ad libitum. The animals used for the pharmacokinetic study following intravenous administration were reused for the study following subcutaneous administration after observing a minimum washout period of 15 days.Pure technical grade enrofloxacin and ciprofloxacin were generously gifted by Intas Pharmaceuticals, Ahmedabad and Aurobindo Pharmaceutical, Chennai, respectively. Enrofloxacin (Quintas 10%; Intas Pharmaceuticals, Ahmedabad, India) was injected (5 mg/kg) in the jugular vein and in the flank region for i.v. and s.c. study, respectively. Blood samples (3 mL each) were collected by jugular indwelling catheter into heparinized glass tubes at predetermined time intervals, i.e. 0, 2, 5, 10, 15, 30, 45 min and 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24 and 36 h after drug administration. Blood samples were centrifuged to harvest plasma, which was stored at )20°C until assayed. The concentrations of enrofloxacin and ciprofloxacin in plasma were simultaneously extracted (Nielsen & Gyrd-Hansen, 1997) and determined using HPLC system (Model SPD-10A, LC-10AT; Shimadzu Corporation, Kyoto, Japan) (Kung et al., 1993). Peak areas were used for quantification of the compounds. External standards were used to prepare calibration curves and determine the assay precision and recovery. Assay precision was determined by analysing two samples four times each day for intra-day assay and on four occasions 24 h apart for inter-day assay.The calibration curves prepared by spiking external standards in the pooled drug free sheep plasma were linear in the range of 0.02-3.2 ...

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Section: Pharmacokinetic Parameters Of Enrofloxacin and Ciprofloxacisupporting

confidence: 60%

Pharmacokinetics of enrofloxacin in sheep following intravenous and subcutaneous administration

Rahal

Kumar

Ahmad

et al. 2006

Vet Pharm & Therapeutics

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“…The mean ratio in AUC 0→∞ of ciprofloxacin/enrofloxacin after the first dose found here was 12.3%. This was significantly lower than reported in 8-month-old buffalo calves (27%) and adult cattle (29.9%) [ 6 ]. In newborn and one-week-old calves the ciprofloxacin/enrofloxacin ratio can range from 10 to 27%.…”

Section: Resultscontrasting

confidence: 67%

Influence of systemic fluoroquinolone administration on the presence of Pasteurella multocida in the upper respiratory tract of clinically healthy calves

et al. 2008

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The influence of enrofloxacin administration (5 mg/kg) for five consecutive days on the occurrence of Pasteurella multocida in the upper respiratory tract of two healthy calves was monitored over a 10-day period. From nasal swabs of two additional healthy control calves, which received a placebo saline administration, P. multocida was isolated throughout the study period. In the enrofloxacin treated calves, P. multocida was not demonstrated in the nasopharynx from 48 h after the first injection until two days after the last administration, when P. multocida reappeared and proved to be clonal in nature to the original isolates. During the experiment, no change in minimal inhibitory concentration for enrofloxacin of the P. multocida isolates was detected (MIC ≤ 0.015 μg/mL). Enrofloxacin concentrations were determined in the plasma by a high-performance liquid chromatography method with fluorescence detection. The PK/PD indices AUC/MIC and C max /MIC ratio were calculated and found to be 1157.7 and 129.8, respectively. Remarkably, the respiratory pathogen Arcanobacterium pyogenes became the predominant recovered organism in the nasopharynx of one animal following enrofloxacin therapy throughout the remaining of the experiment. FindingsIn calves, enrofloxacin is frequently used to treat pneumonic pasteurellosis, a disease mostly due to Pasteurella multocida [1]. P. multocida is a common inhabitant of the upper respiratory tract of calves. To better understand the epidemiology of pneumonic pasteurellosis and the occur-

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“…About 40% of the radioactivity was recovered from the bile, which contained mainly the unchanged parent molecule. In various food animal species, the metabolism pathway of enrofloxacin has been well documented by many earlier investigators (Bergan et al, 1988;Tyczkowska et al, 1989;Anadon et al, 1995;Kaartinen et al, 1997;Rao et al, 2001;Sharma et al, 2003). This drug induces inhibition of cytochrome P450 isoenzymes (Vancutsem and Babish, 1996;Vaccaro et al, 2003).…”

Section: Discussionmentioning

confidence: 97%

Nonlinear toxicokinetics of enrofloxacin in rats

Shin

Cho

et al. 2010

Arch. Pharm. Res.

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The dose-dependent toxicokinetics of enrofloxacin were studied by administering various single subcutaneous doses (5, 10, 20, 40, 70, 100, 150, 200, 300 and 400 mg/kg) in male Sprague-Dawley rats. The blood samples were collected from the tail veins, and the plasma concentration of enrofloxacin was determined by an HPLC-fluorescence detection (FLD) method. The time-concentration profiles of enrofloxacin were well fitted by an one-compartmental model with first order elimination. The absorption half-lives (t₁(/)₂(abs)) ranged from 0.2-0.8 h, and the mean time to maximum plasma concentration (T(max)) ranged from 0.6-1.8 h. On the other hand, marked disproportionate increases of the area under the curve (AUC) and elimination half-lives (t₁(/)₂) were observed from the increase of the doses. This result indicates that the elimination of enrofloxacin has nonlinear pharmacokinetic properties with increasing doses. Therefore, we need to take into consideration the possible occurrence of side effects resulting from greater systemic exposure from high dose therapies.

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Pharmacokinetics of enrofloxacin and the rate of formation of its metabolite ciprofloxacin following intravenous and intramuscular single dose administration to male buffalo calves

Cited by 13 publications

References 6 publications

Pharmacokinetics of enrofloxacin in sheep following intravenous and subcutaneous administration

Pharmacokinetics of enrofloxacin in sheep following intravenous and subcutaneous administration

Influence of systemic fluoroquinolone administration on the presence of Pasteurella multocida in the upper respiratory tract of clinically healthy calves

Nonlinear toxicokinetics of enrofloxacin in rats

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