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Introduction of a Composite Parameter to the Pharmacokinetics of Venlafaxine and its Active O‐Desmethyl Metabolite
Venlafaxine is a structurally novel, nontricyclic compound that is being evaluated for the treatment of various depressive disorders. A randomized three‐period crossover study was conducted to obtain
Metabolic disposition of 14C-venlafaxine in mouse, rat, dog, rhesus monkey and man.
The metabolic disposition of venlafaxine has been studied in mouse, rat, dog, rhesus monkey and man after oral doses of 14C-venlafxine as the hydrochloride, indicating extensive absorption from the GI tract and renal excretion.
High Performance Liquid Chromatographic Isolation, Spectroscopic Characterization, and Immunosuppressive Activities of Two Rapamycin Degradation Products
Abstract A high performance liquid chromatographic method has been developed for the isolation of two degradation products of rapamycin which is currently under development as an immunosuppressive
Diastereoisomeric glucuronides of oxazepam. Isolation and stereoselective enzymic hydrolysis.
The ready hydrolysis of one of the glucuronides by an enzyme from an intestinal microorganism may play a role in the enterohepatic circulation of oxazepam.
Pharmacokinetics of venlafaxine and O-desmethylvenlafaxine in laboratory animals.
In mouse, rat and dog, exposure to venlafaxine increased more than proportionally with dose, suggesting saturation of elimination, and exposure of animals to the bioactive metabolite, O-desmethylvenlafxine (ODV), was less than that of venl Lafaxine itself.
[14C]7-ethoxycoumarin metabolism by precision-cut rat hepatic slices.
Quantitative comparisons demonstrated that there was approximately two to five times more 7-OHC in the liver slice than in the medium, whereas 7-hydroxycoumarin sulfate, the most abundant metabolite in theMedium, was present only at low levels in the Liver slice, demonstrating that 7- OHC levels are considerably underestimated when only levels inThe medium are considered.
Clinical pharmacokinetics of lorazepam. I. Absorption and disposition of oral 14C-lorazepam.
Biotransformation to a pharmacologically inactive glucuronide metabolite appeared to be the major mechanism of lorazepam clearance and its metabolites in body fluids were determined by appropriate analytic techniques.
The metabolic disposition of 14C-ciramadol in humans.
Only ciramadol and the aryl-O-glucuronide were detected in substantial amounts in plasma, suggesting tubular secretion in addition to glomerular filtration, and more than 90% of the amount recovered in urine was excreted within 24 h after dosing.
Disposition and metabolism of lorazepam in the male rat.
The metabolic disposition of oxazepam in rats.
  • S. Sisenwine, C. Tio
  • Biology, Chemistry
    Drug metabolism and disposition: the biological…
  • 1986
The metabolic fate of oxazepam in the rat is more complex than in larger animal species, and the brain/plasma ratio of approximately 3-5:1 demonstrates that the drug has considerable affinity for that tissue.