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Emsam Selegeline skin patch approved


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Bristol-Myers Squibb Co. and a joint venture including Corona-based drug maker Watson Pharmaceuticals Inc. won final U.S. approval Tuesday for the first skin patch to deliver antidepressant medication.

This being the MAOI that in lower doses will not require strict dietary restrictions (but still will in larger doses).

Here's the link to the full article in the March 1, 2006 edition of the Los Angeles Times.

It's always good to have another arrow in the quiver.

Greeny

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i find this really exciting for some reason.  i really wanted to try this about a year ago and was bummed it wasn't approved yet.  now i'm stable, so don't need it, but i still think it's pretty damn cool that people can eat cheese and have an maoi.  (i really like cheese)

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Heya,

Yah, good news for MI and also for Parkinson's patients, who might *also* like cheese.

Or red wine.

Plus, MAOIs are just a *really really good drug.*

Cutting the s/e is *good.*  Very.

Interesting.

--ncc--

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Aha. Found the PI sheet here

It comes in three dosages: 6 mg/24 hours, 9 mgs/24 hours, & 12 mgs/24 hours.

Only the lowest dosage does not come with the standard MAOI dietary restrictions.

Nevertheless, the restricted diet is less restricted now than it was years ago.

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Only the lowest dosage does not come with the standard MAOI dietary restrictions.

I was almost optimistic about my friend cheese until here. The only reason I'd consider any change at all would be the food restrictions. And probably not even then -- I'm just doing too well right now.

Nevertheless, the restricted diet is less restricted now than it was years ago.

<{POST_SNAPBACK}>

Yes! Very much less restricted, thankfully.

Fiona

(stay away from Parnate and you won't get hurt)

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Aha. Found the PI sheet here

It comes in three dosages: 6 mg/24 hours, 9 mgs/24 hours, & 12 mgs/24 hours.

Only the lowest dosage does not come with the standard MAOI dietary restrictions.

Nevertheless, the restricted diet is less restricted now than it was years ago.

<{POST_SNAPBACK}>

I don't quite understand why 12mg requires a restriction, or even the 9mg. I was taking 12.5 of selegiline by the time I quit it, and my doctor never recommeded any restriction. He did say that if I went up to 15mg that I would need to, but that was it.

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Does anyone know if it carries any risk to the liver, such as increased liver enzmes? Does anyome know if it is going to produce the same confusion side effect caused by the oral version?

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Does anyone know if it carries any risk to the liver, such as increased liver enzmes? Does anyome know if it is going to produce the same confusion side effect caused by the oral version?

<{POST_SNAPBACK}>

It appears to be metabolized by the liver (abstract), but I'd be surprised if it were a heavy load on it. ( Not that that means much! )

As to side effects... it's still selegiline. The delivery method should even out side

effects from blood levels going up and down during the day though.

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  • 3 weeks later...

As to side effects... it's still selegiline. The delivery method should even out side

effects from blood levels going up and down during the day though.

<{POST_SNAPBACK}>

There will definitely be more evenness to the dose. But I think that the key with the transdermal delivery system is that you get a lot more of the selegiline, and less of the metabolites. See page 3 of the PI sheet. This is good because there are substantial levo-amphetamine metabolites to the oral, which can be the source of anxiety and other unpleasant side effects.

Best,

cache-monkey

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I don't quite understand why 12mg requires a restriction, or even the 9mg. I was taking 12.5 of selegiline by the time I quit it, and my doctor never recommeded any restriction. He did say that if I went up to 15mg that I would need to, but that was it.

<{POST_SNAPBACK}>

I think this has to do with the fact that there's actually far more selegilne in your system with the patch form. In the

PI sheet, it looks like a 6 mg/24 patch is bio-equivalent to about 100 mg of the oral, after single dosing. This is in terms of cumulative exposure; if it's peak concentrations that matters it ends up being more like a factor of two (based on a PPT presentation by an FDA person).

So there's a lot more MAO inhibition going on, and it would look like you'd need dietary restrictions even with the 6 mg patch. Balancing against that is that the transdermal bypasses the gut, which is where the problem with MAO-A inhibition and the tyramine effect lies.

There was a lot of back and forth with between the manufacturer and the FDA about the restrictions. The manufacturer didn't want them at all since there were no "cheese reactions" in the 2500 people enrolled in the various clinicals. The FDA wanted restrictions at all doseages. (See the FDA's summary on the issue in the PPT presentation I linked to above.) This ended up being the kind of wierd compromise.

Best,

cache-monkey

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As to side effects... it's still selegiline. The delivery method should even out side

effects from blood levels going up and down during the day though.

There will definitely be more evenness to the dose. But I think that the key with the transdermal delivery system is that you get a lot more of the selegiline, and less of the metabolites. See page 3 of the PI sheet. This is good because there are substantial levo-amphetamine metabolites to the oral, which can be the source of anxiety and other unpleasant side effects.

Best,

cache-monkey

Drat.  I was kinda curious if it would help with ADD at all or not and that makes me think more in the not direction.

It still might potentate the effect of stimulants though.

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It still might potentate the effect of stimulants though.

VE.  Stimulants are strongly contraindicated with MAO meds THey're one of the agents or foods that can precipitate a hypertensive crisis!    Sinee my functioning (tho not morale) is much improved with ADD meds, this is the main reason I'm not giving ENSAM a whirl.

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  • 2 weeks later...

So, is the patch form less likely to cause anxiety?  I think selegeline is more MAOI B specific than MAOI A specific so you don't get much affect on serotonin, unfortunately.

Do you think someone with fairly severe anxiety could use the patch, or would it still be overstimulating?

Also, selegeline metabolizes to AMPHETAMINE(?)  Won't that mean that you could burn out, develope tolerance on this drug?  Did they do any long term studies to test for this?

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So, is the patch form less likely to cause anxiety? [...] Do you think someone with fairly severe anxiety could use the patch, or would it still be overstimulating? [...] Also, selegeline metabolizes to AMPHETAMINE(?)  Won't that mean that you could burn out, develope tolerance on this drug?  Did they do any long term studies to test for this?

<{POST_SNAPBACK}>

The l-amphetamine and l-methamphetamine metabolites are supposed to be negligable in the pill form, but some people seem to still react strongly.[*] They're supposed to be virtually irrelevant in the patch.

I've read posts a person involved in the clinical trial that they didn't find it to be that anxiogenic. Granted, this was someone without a predisposition, but he found the pill form (which he took after the clinical) to be pretty anxiety-provoking. You can read his posts on psychobabble. Actually, here's a link to a google search for his posts on selegiline.

It also looks like there is someone in that group who just started selegiline a few days ago. Here's a link to his thread. It looks like the guy is a long-time GAD/SP-type and hasn't seen an increase in anxiety, through 4 days. He's also on Klonopin, but his pdoc seems to think that (because of the MAO-A inhibition that you get in the patch) he will eventually be able to reduce/discontinue the K.

So, the short answer is that there will be a lot fewer anxiogenic/activating (alliterative) amphetamine metabolites with the patch. It seems that selegiline itself migth no be so overstimulating.

~cache-monkey

[*] I suspect this is due to deficient activity in CYP-2D6, which is the liver enzyme that (I think) clears most of the amphetamine metabolites of selegiline. This happens in about 10% of the population. There's a blood test for your genotypic CYP-2D6 capacity. I think it's a good thing to get because quite a few psycho-active meds are cleared by that enzyme. It costs about $250, which is a not a small amount, but it can save a lot of adverse effects.

My insurance actually covered it after I convinced my pdoc to order it. (This was based on Sherlock-Holmesing some of my bad drug reactions to infer that it might be the case.) Based on the test, I'm a genotypically "intermediate" CYP-2D6 metabolizer, which is a lot closer to poor than normal. Even though I need low doses with most drugs, it's nice to know that I should be especially careful with certain ones. (E.g. OTC cough syrup, which always left me content but super out-of-it at normal doses... DXM is the main ingrediant and is used recriationally in larger doses to get looped.) [/rambling proselytization]

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Thanks c-monkey!  I am following the guys trial on psychobabble but he seems to have more mental anxiety than extreme physical anxiety.  I, unfortunately, have very physical anxiety as well as mental torture.  Also hard to say how well he would fair without Klonopin.

I will look at the link to those older posts you mentioned.  Should be informative.

Thanks so much for taking the time to respond! K

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