Ketamine: A Review of Clinical Pharmacokinetics and Pharmacodynamics in Anesthesia and Pain Therapy

@article{Peltoniemi2016KetamineAR,
  title={Ketamine: A Review of Clinical Pharmacokinetics and Pharmacodynamics in Anesthesia and Pain Therapy},
  author={Marko Peltoniemi and Nora Hagelberg and Klaus T. Olkkola and Teijo I. Saari},
  journal={Clinical Pharmacokinetics},
  year={2016},
  volume={55},
  pages={1059-1077}
}
Ketamine is a phencyclidine derivative, which functions primarily as an antagonist of the N-methyl-d-aspartate receptor. It has no affinity for gamma-aminobutyric acid receptors in the central nervous system. Ketamine shows a chiral structure consisting of two optical isomers. It undergoes oxidative metabolism, mainly to norketamine by cytochrome P450 (CYP) 3A and CYP2B6 enzymes. The use of S-ketamine is increasing worldwide, since the S(+)-enantiomer has been postulated to be a four times more… Expand
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TLDR
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TLDR
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TLDR
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Simulations suggested that after oral dosing, norketamine AUC at steady state is 16.5 times higher than that of S-ketamine, a feasible alternative to repeated intravenous dosing in the setting of chronic pain. Expand
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