6533b838fe1ef96bd12a3c9c
RESEARCH PRODUCT
The role of cytochrome P450 2D6 in the metabolism of moclobemide.
Sebastian HärtterD. BaierGismar ZieglerChristoph HiemkeJ. Dingemansesubject
AdultMaleCYP2D6Monoamine Oxidase InhibitorsMoclobemidePharmacologydigestive systemIsozymeAbsorptionchemistry.chemical_compoundPharmacokineticsCytochrome P-450 Enzyme SystemMoclobemidemedicineHumansPharmacology (medical)skin and connective tissue diseasesBiological PsychiatryPharmacologyChemistryDextromethorphanMetabolismPsychiatry and Mental healthNeurologyDebrisoquineCytochrome P-450 CYP2D6BenzamidesFemaleNeurology (clinical)Drug metabolismmedicine.drugdescription
The metabolic fate of moclobemide (Ro 11-1163), a new reversible and selective inhibitor of monoamine oxidase type A (MAO-A), has been assessed in a pilot study in 2 debrisoquine poor metabolizers (PM) and 4 extensive metabolizers (EM) after multiple oral dosings of moclobemide with and without co-medication of dextromethorphan. Absorption and disposition parameters were not different between PM and EM. Concurrent application of dextromethorphan, a selective substrate of CYP2D6, did not affect the pharmacokinetics of moclobemide. These results indicate that the cytochromal isoenzyme CYP2D6 does not play a major role in the metabolic degradation of moclobemide. Limited CYP2D6 activities because of a genetic defect or co-medications with CYP2D6 substrates should therefore not give rise to elevated moclobemide blood levels.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1996-08-01 | European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology |