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Re: MAOI's

Posted by Adam on November 3, 1999, at 18:25:08

In reply to Re: MAOI's, posted by Adam on November 3, 1999, at 18:15:20

Oops. Sorry, I think it's phenylethylamine, not methylethylamine. That stuff in chocolate, whatever it is. (Don't know how I got methyl- screwed up with phenyl-...)

Um, Dr. Bob? Could we have a correction feature? My memory ain't so good these days...

> I have heard that brofaromine also seems to be a bit less robust than the irreversible and nonselective inhibitors of MAO. Check out this reference:
> Neuropsychopharmacology 1999 Mar;20(3):226-47
> Meta-analysis of the reversible inhibitors of monoamine oxidase type A moclobemide and
> brofaromine for the treatment of depression.
> Lotufo-Neto F, Trivedi M, Thase ME
> Instituto de Psiquiatria da Faculdade de Medicina da Universidade de Sao Paulo, Brazil.
> I wonder if there is any work being done on an irreversible inhibitor of MAO-A. Since MAO-B metabolism of tyramine is sufficient to protect against the
> pressor effect of tyramine (of any severity), what's so great about reversibility? Is it not possible to design a molecule such that it covalently binds
> MAO-A but has little or no affinity for MAO-B? Maybe not. I've just wondered if moc.'s lackluster performance for some patients is due to the fact that
> it is "reversible" in its binding to MAO-A, or to its lesser effect on MAO-B (and thus dopamine and methylelthylamine).
> Also, can tyramine not displace moc. from MAO-A at all? Just curious.
> > > Hi James. You probably already know this, but Selegiline at 15mg or less (+ -) is void of the cheeze reaction. The reversible MAOI is Moclobemide. There is another similar one too. The name escapes me. Both are in other countries. Not USA. Moclobemide seems to be the most popular reversible MAOI. No cheeze reaction.
> >
> > Two others that are available in some places (though less widely) are toloxatone and brofaromine. What I have heard about moclobemide mostly suggests that it's very hit-or-miss and that it just doesn't work as well as the irreversible, nonselective MAOIs, in general. This is why I haven't bothered trying it (too much hassle for something that might not even be worth it).
> >
> > Reversibility just means that the MAO can be "recaptured" -- it's not effectively destroyed by moclobemide. When a molecule of phenelzine, say, hits MAO, they interact in such a way as to turn the MAO into something completely different that will no longer function as an enzyme.
> >
> > > Moclobemide primary inhibits MAOs of serotonin and NE, with about 30% inhibition of dopamine MAO.
> >
> > The more common names for these two are MAO-A and MAO-B. Tyramine is an MAO-B substrate; because moclobemide only has a modest affinity for MAO-B, it's easily displaced by tyramine.
> >
> > > Don't know if it's available in Mexico.
> >
> > It might be, under the brand name Aurorix.




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