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Pharmacokinetics, metabolism and renal clearance of flumequine in veal calves
Author(s) -
MEVIUS D.J.,
BREUKINK H.J.,
GUELEN P. J. M.,
JANSEN T.,
GRÈVE B.
Publication year - 1990
Publication title -
journal of veterinary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.527
H-Index - 60
eISSN - 1365-2885
pISSN - 0140-7783
DOI - 10.1111/j.1365-2885.1990.tb00764.x
Subject(s) - flumequine , pharmacokinetics , chemistry , glucuronide , oral administration , zoology , absorption (acoustics) , urine , pharmacology , medicine , antibiotics , biochemistry , biology , physics , enrofloxacin , ciprofloxacin , acoustics
Mevius, D.J., Breukink, H.J., Guelen, P.J.M., Jansen, T. & de Grève, B. Pharmacokinetics, metabolism and renal clearance of flumequine in veal calves. J. vet. Pharmacol. Therap. 13, 159–169. The pharmacokinetics of flumequine was studied in 1‐, 5‐and 18‐week‐old veal calves. A two‐compartment model was used to fit the plasma concentration‐time curve of flumequine after the intravenous injection of 10 mg/kg of a 10% solution. The elimination half‐life (t 1/2 ß ) of the drug ranged from 6 to 7 h. The V d ß and Cl B of 1‐week‐old calves (1.07 1/kg, 1.78 ml/min/kg) were significantly lower than those of 5‐week‐old (1.89 1/kg, 3.23 ml/min/kg) and 18‐week‐old calves (1.57 1/kg, 3.10 ml/min/kg). After the oral administration of 10 mg/kg of a 2% flumequine formulation mixed with milk replacer, the C max was highest in 1‐week‐old (9.27 μg/ml) and lowest in 18‐week‐old calves (4.47 μg/ml). The absorption was rapid (T max of approximately 3 h) and complete. When flumequine itself and a formulation containing 2% flumequine and 20 times 10 6 iu of colistin sulphate were mixed with milk replacer and administered at the same dose rate, absorption was incomplete and C max was lower. The main urinary metabolite of flumequine was the glucuronide conjugate (approximately 40% recovery within 48 h of intravenous injection) and the second most important metabolite was 7‐hydroxy‐flumequine (approximately 3% recovery within 12 h of intravenous injection). Only 3.2–6.5% was excreted in the urine unchanged. After oral administration a ‘first‐pass’ effect was observed, with a significant increase in the excretion of conjugated drug. For 1‐week‐old calves it is recommended that the 2% formulation should be administered at a dose rate of 8 mg/kg every 24 h or 4 mg/kg every 12 h; for calves over 6 weeks old, the dose should be increased to 15 mg/kg every 24 h or 7.5 mg/kg every 12 h. The formulation containing colistin sulphate should be administered to 1‐week‐old calves at a flumequine dose of 12 mg/kg every 24 h or 6 mg/kg every 12 h. Dr D. J. Mevius, Department of Large Animal Medicine and Nutrition, Yalelaan 16, 3508 TD Utrecht, the Netherlands.