Disposition of venlafaxine enantiomers in rats with hepatic encephalopathy after chronic drug treatment.

Forskningsoutput: TidskriftsbidragArtikel i vetenskaplig tidskrift

Abstract

Portacaval shunted (PCS) rats, a model of hepatic encephalopathy, and control animals were administered racemic venlafaxine for 14 days (10 mg/kg). The levels of the S- and R-enantiomers and the S/R-enantiomer ratios of venlafaxine and its metabolites were assessed by an enantiomer-selective chromatographic assay in serum, brain parenchyma, and brain dialysate of both groups. Higher levels of the S- and R-enantiomers of venlafaxine were found in serum and brain of PCS vs. normal rats (median values of S- and R-venlafaxine in serum: 290 and 201 nM in PCS; 97 and 66 nM in normal rats; median values of S- and R-venlafaxine in cortex: 956 and 939 nM in PCS; 357 and 318 nM in normal rats). Interestingly, similar S/R-venlafaxine ratios were observed in PCS and normal rats both in serum (S/R = 1.4) and brain compartments (S/R = l.0-1.1). These findings may have clinical relevance for the safety of venlafaxine in chronic hepatic encephalopathy.

Detaljer

Författare
  • Cecilia Wikell
  • Chin B Eap
  • Martin Josefsson
  • Gustav Apelqvist
  • Johan Ahlner
  • Pierre Baumann
  • Finn Bengtsson
Enheter & grupper
Forskningsområden

Ämnesklassifikation (UKÄ) – OBLIGATORISK

  • Läkemedelskemi
  • Farmakologi och toxikologi

Nyckelord

Originalspråkengelska
Sidor (från-till)347-350
TidskriftChirality
Volym14
Utgivningsnummer4
StatusPublished - 2002
PublikationskategoriForskning
Peer review utfördJa