Moclobemide treatment causes a substantial rise in the sparteine metabolic ratio. Danish University Antidepressant Group.
A sparteine test was carried out immediately before (n = 37) and during (n = 33) moclobemide treatment (200 mg twice daily) in 37 patients participating in a controlled clinical trial. The sparteine metabolic ratio (MR) did not correlate with the plasma concentration of moclobemide and/or its oxidized metabolite Ro 12-8095, and four sparteine poor metabolisers (PM, MR > 20) had plasma moclobemide concentrations similar to those in extensive metabolisers (EM, MR < 20). The Ro 12-8095/moclobemide ratio tended to correlate negatively with the sparteine MR before and during treatment (rs = -0.32, -0.37). During moclobemide treatment the sparteine MR rose substantially by a factor of 1-103 (median 4.7), and two EM became phenotypically PM. In the PM subjects as well as in one EM patient on cimetidine during both tests, no change in sparteine MR occurred.
Gram
L F
LF
Department of Clinical Pharmacology, Odense University, Denmark.
Brøsen
K
K
D000328:Adult; D000368:Aged; D001549:Benzamides / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology*; D002927:Cimetidine / Q000494:pharmacology; D019389:Cytochrome P-450 CYP2D6; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D003647:Debrisoquin / Q000378:metabolism; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D006899:Mixed Function Oxygenases / Q000378:metabolism; D020912:Moclobemide; D008996:Monoamine Oxidase Inhibitors / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology*; D009025:Morpholines / Q000097:blood; D010084:Oxidation-Reduction; D010641:Phenotype; D011110:Polymorphism, Genetic; D016037:Single-Blind Method; D013034:Sparteine / Q000378:metabolism*
D001549:Benzamides; D008996:Monoamine Oxidase Inhibitors; D009025:Morpholines; D013034:Sparteine; D002927:Cimetidine; D003577:Cytochrome P-450 Enzyme System; C062937:Ro 12-8095; D006899:Mixed Function Oxygenases; D019389:Cytochrome P-450 CYP2D6; D020912:Moclobemide; D003647:Debrisoquin