Pharmacokinetics of flutoprazepam, a novel benzodiazepine drug, in normal subjects

@article{Barzaghi2010PharmacokineticsOF,
  title={Pharmacokinetics of flutoprazepam, a novel benzodiazepine drug, in normal subjects},
  author={Nicoletta Barzaghi and L. Leone and M Monteleone and G. Tomasini and Emilio Perucca},
  journal={European Journal of Drug Metabolism and Pharmacokinetics},
  year={2010},
  volume={14},
  pages={293-298}
}
  • N. BarzaghiL. Leone E. Perucca
  • Published 1 October 1989
  • Chemistry, Biology, Medicine
  • European Journal of Drug Metabolism and Pharmacokinetics
SummaryThe single dose pharmacokinetics of flutoprazepam and its active N-desalkyl metabolite were determined in 8 normal subjects by using newly developed, highly sensitive, GC-MS and HPLC techniques. Following a 2 mg dose of the drug, the concentrations of unchanged flutoprazepam in serum were extremely low (below 5 ng/ml at 2 h) and declined rapidly to undetectable levels within 6–9 h after dosing. At all sampling times, the serum concentration of the N-dealkylated metabolite (N… 

Propranolol does not alter flutoprazepam kinetics and metabolism in the rat

There was some variability in flutoprazepam disposition, consistent with the concept of an extensive first-pass metabolism of high-extraction drugs, but there was no evidence of any pharmacokinetic interaction between this β-adrenoceptor blocker and flutopsin in the rat.

The physicochemical and pharmacokinetic properties of benzodiazepines appearing as new psychoactive substances

The lipophilicity, the pKa and the plasma protein binding were determined for benzodiazepines appearing as new psychoactive substances and these were compared to theoretical values from software packages and none of the software packages were able to predict parameters to a su_cient degree of accuracy and in vitro data is currently preferable.

The emergence of new psychoactive substance (NPS) benzodiazepines: A review.

This review collates the available information on benzodiazepines and provides a starting point for the further investigation of their pharmacokinetics which is clearly required.

The emergence of new psychoactive substance (NPS) benzodiazepines: A review.

Compound Year patented Year reported to the EMCDDA 3‐hydroxyphenazepam Not reported 2016 [46] [37] 4‐chlorodiazepam (Ro5‐4864) 1964 195 2016 [40] Adinazolam 1980 196 2015 [35] Bromazolam 1979 197

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