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Selegiline bioavailability and MAO-A inhibition

mitragyna

mitragyna

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Dec 7, 2006
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I was pondering about Selegiline and MAO-A inhibition. Many say Selegiline starts to inhibit MAO-A at doses >10 mg. But most are talking about the oral form of Selegiline when on this discussion, and the oral form has a pretty low bioavailability. This made me think, if one was to use Selegiline transdermally wouldn't MAO-A inhibition occur at a lesser dosage since this form is much more bioavailable?

The reason I'm asking is because I was recently prescribed Emsam 9 mg and need to know this for safety reasons. Thanks in advance for your replies.
 
Oral selegiline? Isn't it supposed to be used sublingually?
I'd imagine that triple bond would get ruined quick-smart in 1st-pass metabolism...

So yeah if you're right about the oral selegiline then you're most probably right on the second point too. But, it wouldn't make sense that a transdermal patch would be created in a high enough dose that appreciable MAO-A inhibition would occur, no? That's kinda the point of using Selegiline in the first place, avoiding that very thing.
 
^^
I'm not sure about the sublingual thing, I wouldn't be surprised.

That's a good point about the patch and MAO-A inhibition. But maybe doctors prescribe it in those higher doses for that very fact that both MAO-A and B are inhibited. Almost like turning it into the older non-selective MAOI's like Nardil and Parnate. Maybe some people tolerate higher doses of Selegiline better than the old school hydrazine-derived MAOI's. Just an idea, that's an interesting question though. I'll have to ask my psychiatrist tomorrow about that.
 
Selegiline is prescribed oral, sublingual and transdermal.

Oral bioavailability is extremely low unless consumed with lipids. Transdermal often inhibits non-selectively (MAO-A) with the patches above 6 mg. You could very likely have non-selective MAO inhibition at 9 mg.

You could have found these answers using the search engine.

UTFSE regarding selegiline. It's ridiculous how many questions are reiterated.
 
^^
Umm, as a matter of fact I haven't seen one thread regarding transdermal selegiline and mao-a inhibition.
 
a simple google search would yield more than a dozen studies on the deprenyl transdermal patch
 
the transdermal selegiline systems is designed to inhibit both mao-a and mao-b fully in the brain. however it avoids the GI system so you can eat whatever food you want.
 
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