Pharmacokinetic/pharmacodynamic modeling of the antinociceptive effects of (+)-tramadol in the rat: role of cytochrome P450 2D activity.

@article{Garrido2003PharmacokineticpharmacodynamicMO,
  title={Pharmacokinetic/pharmacodynamic modeling of the antinociceptive effects of (+)-tramadol in the rat: role of cytochrome P450 2D activity.},
  author={Mar{\'i}a Jes{\'u}s Garrido and Onintza Sayar and Cristina Segura and Javier Rapado and Mar{\'i}a del Carmen Dios-Vi{\'e}itez and Mar{\'i}a Jes{\'u}s Renedo and I{\~n}aki F. Troc{\'o}niz},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2003},
  volume={305 2},
  pages={710-8}
}
In this study the role of cytochrome P450 2D (CYP2D) in the pharmacokinetic/pharmacodynamic relationship of (+)-tramadol [(+)-T] has been explored in rats. Male Wistar rats were infused with (+)-T in the absence of and during pretreatment with a reversible CYP2D inhibitor quinine (Q), determining plasma concentrations of Q, (+)-T, and (+)-O-demethyltramadol [(+)-M1], and measuring antinociception. Pharmacokinetics of (+)-M1, but not (+)-T, was affected by Q pretreatment: early after the start… CONTINUE READING

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