Effect of oral co-administration of frozen-dried grapefruit juice on pharmacokinetics of tramadol in dogs

نویسندگان

  • G. Saccomanni Department of Pharmaceutical Sciences, Via Bonanno 6, 56126 Pisa, Italy;
  • H. I. Yun Institute of Veterinary Science, College of Veterinary Medicine, Chungnam National University, Daejeon 305-764, South Korea
  • M. Giorgi Veterinary Teaching Hospital 24 h, Department of Veterinary Clinics, University of Pisa, Via Livornese (lato monte) 1 San Piero a Grado, 56010 Pisa, Italy
  • M. MacCheroni Veterinary Teaching Hospital 24 h, Department of Veterinary Clinics, University of Pisa, Via Livornese (lato monte) 1 San Piero a Grado, 56010 Pisa, Italy; Department of Pharmaceutical Sciences, Via Bonanno 6, 56126 Pisa, Italy
  • S. Del Carlo Department of Pharmaceutical Sciences, Via Bonanno 6, 56126 Pisa, Italy
چکیده مقاله:

Tramadol is a centrally acting analgesic drug extensively metabolized in animal species. Its clinicalresponse is mainly due to the M1 metabolite, poorly produced in dogs. Grapefruit-juice can inhibit themetabolism of different drugs in animals and humans. The aim of the present study was to evaluate thepharmacokinetics of tramadol and its major metabolites after co-administration of tramadol and frozen-dried grapefruit-juice. A balanced cross-over study was used involving six male Beagle dogs. They were administered with tramadol alone (5 mg/kg) or with tramadol (5 mg/kg) plus frozen-dried grapefruit-juice (10 g). The plasma concentration vs time curves showed significant differences during the first 4 h following drug administration. Tmax was at 1.33 and 1.70 h following tramadol and tramadol plus frozen-dried grapefruit-juice treatment, respectively. Significant differences were also shown in Cmax (490 vs 270 ng/ml) and AUC (11,610 vs 5,890 h·h·ng/ml). Significant differences between the treatments were shown in all the M1 parameters reported. M2 and M5 did not show significant differences after both administrations. In conclusion, the frozen-dried grapefruit-juice was shown to affect the plasma concentrations of M1, despite them being well below those reported in humans.

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effect of oral co-administration of frozen-dried grapefruit juice on pharmacokinetics of tramadol in dogs

tramadol is a centrally acting analgesic drug extensively metabolized in animal species. its clinicalresponse is mainly due to the m1 metabolite, poorly produced in dogs. grapefruit-juice can inhibit themetabolism of different drugs in animals and humans. the aim of the present study was to evaluate thepharmacokinetics of tramadol and its major metabolites after co-administration of tramadol an...

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عنوان ژورنال

دوره 12  شماره 1

صفحات  8- 15

تاریخ انتشار 2011-03-20

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