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Selegiline doses: Transdermal VS Oral.

2CEECS

2CEECS

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Joined
Mar 8, 2007
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Berkeley, CA
Selegiline is pretty amazing stuff. I have a prescription in the form of Emsam®, a transdermal patch for Selegiline. It comes in three varieties: "20mg (6mg/24h)", "30mg (9mg/24h)", and "40mg (12mg/24h)". I used the 20mg variant for two weeks (noticing effects within 20 hours!) before moving up to the 30mg version, which I have been using for about three weeks.

I am curious for an explanation of these dosage numbers, especially in comparison to oral doses. The lowest strength is generally considered to be entirely MAO-B selective, whereas the two higher doses are suspected to cause partial MAO-A inhibition as well. (The company's literature recommends dietary restrictions for people on the stronger doses, but because of the transdermal delivery method, any partial MAO-A inhibition isn't happening in the digestive tract. There is a fair amount of support to the idea that this is unnecessary, and merely an FDA-enforced precaution due to lack of enough clinical trials proving that an MAOI doesn't pose the threat of hypertensive crisis.)

I am also interested in hearing from any other Emsam users on their interaction experiences since starting the routine. I have not yet used any of my chemicals that are metabolized by MAO, -A or -B, because I am unsure the degree of MAO-A inhibition and don't have enough information about, taking, say, a phenethylamine like 2C-E during near-complete MAO-B inhibition (sounds like something that must be done with great care, if at all).

Incidentally, I will be visiting Amsterdam soon, as I am leaving for a tour of Europe on the 9th. While there, I will definitely be evaluating the THC products--but I also want to be prepared to try the mushrooms. For that, I need a better understanding of the level of MAO-A inhibition I am under (if Psilocybin is not metabolized by MAO-A, please correct me).

Thanks!
 
LuxEtVeritas said:
At higher doses selegiline indeed loses its selectivity and will incur MAO-A inhibition
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Indeed--I am trying to find out information about how much MAO-A is inhibited by a given transdermal dose. There are numbers and discussion available for oral doses, such as 5mg remaining entirely MAO-B selective. I'm not sure if the "9mg/24h" number is directly comperable to these oral dose numbers.
 
Are you taking it as an anti-depresant? If you are the dosages are higher because they want to cause MAO-A inhibition. I've taken Selegiline and MAO-B levels and it does nothing for depression at all.
 
selegiline is very poorly absorbed orally so i find it odd that it seems to possibly be indicating that a 40mg patch will express an effect (assumably on brain MAO) similar to administering 12mg of selegiline via oral route (though in a more even level)

as such it appears these patches have a real shitty carrier system and are even more poorly absorbed than via oral route

since it is irreversible and MAOB take a fair amount of time to restore at MAOB selective levels it does not seem to be much of an advantage

perhaps though for depression and the desire to engage MAOA-I it is indeed superior by largely bypassing GI MAO dynamics, though then by losing the selectivity is it really any better than other non-selective MAOIs given by TD route as the point of selegiline is largely its selectivity
 
Broshious said:
Are you taking it as an anti-depresant? If you are the dosages are higher because they want to cause MAO-A inhibition. I've taken Selegiline and MAO-B levels and it does nothing for depression at all.
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Yes, I am using it as an antidepressant. On the 6mg/24hr patch, roughly 20 hours after my first application, the mood lift was so striking as to be undeniable. I couldn't have attributed it to any other current events in my life, either--that day was particularly rough, in fact! I have read similar reviews of Emsam, after the fact, which go so far as to mention feeling the effects by the end of the first patch cycle.

I moved up to 9mg/24hr mostly out of curiosity for how the effects would change as some selectivity was lost, and MAO-B was essentially eliminated. I am still evaluating it, but I believe I prefer the 6mg/24hr level, after noticing emotionally dampening effects presumably attributable to increased serotonin levels. I will not have a chance to change the dosage back until some time after my trip to Europe, so nonetheless, I remain interested in the degree of MAO-A inhibition the 9mg/24hr dosage could be expected to cause.
 
2CEECS said:
Yes, I am using it as an antidepressant. On the 6mg/24hr patch, roughly 20 hours after my first application, the mood lift was so striking as to be undeniable. I couldn't have attributed it to any other current events in my life, either--that day was particularly rough, in fact! I have read similar reviews of Emsam, after the fact, which go so far as to mention feeling the effects by the end of the first patch cycle.

I moved up to 9mg/24hr mostly out of curiosity for how the effects would change as some selectivity was lost, and MAO-B was essentially eliminated. I am still evaluating it, but I believe I prefer the 6mg/24hr level, after noticing emotionally dampening effects presumably attributable to increased serotonin levels. I will not have a chance to change the dosage back until some time after my trip to Europe, so nonetheless, I remain interested in the degree of MAO-A inhibition the 9mg/24hr dosage could be expected to cause.
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That's interesting. I guess it is absorbed much better transdermally. I imagine you could find the bioavailability of oral Deprenyl online somewhere, and I believe I've read much more about the MAO-A inhibition of oral Deprenyl. So the information of just how much MAO-A it eats is probably out there. Then maybe just assume 100% bioavailability of the transdermal, and wing it? I don't really know anything about this sorta stuff so it's probably so wrong it's retarded, but that's the best I can come up with.
 
I'm 25 and get very noticeable from 1mg oral Deprenyl (selepryl), max 3x a week.

6, 9 and 12mg are very high dosages, especially if absorbption is better transdermal.

Are you 50 + years old? If not, these dosages are very high and might negatively interfere with dompamine neuro-transmettors long term.

Oral deprenyl does MAO-A at 10mg+ they say, but for a youger subjec that might be even lower.

Evidence shows that protective effects of Deprenyl are when taken low dose.
 
jubai said:
I'm 25 and get very noticeable from 1mg oral Deprenyl (selepryl), max 3x a week.

6, 9 and 12mg are very high dosages, especially if absorbption is better transdermal.

Are you 50 + years old? If not, these dosages are very high and might negatively interfere with dompamine neuro-transmettors long term.

Oral deprenyl does MAO-A at 10mg+ they say, but for a youger subjec that might be even lower.

Evidence shows that protective effects of Deprenyl are when taken low dose.
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You say that those are high dosages--but I don't actually know what they can be compared to. For instance, why do the 9mg/24hr patches say "30mg" right above that? But, based on the numbers, I am wondering if the 9mg number might be an adjusted equivalent to 9mg taken orally. The entire thing is very vague, and any help from someone who knows the specifics would be really valuable.

Quite the contrary to 50+; I'm 18. Why do you think that Selegiline will interfere with dopamergic neurons long-term? My understanding is that MAO-B inhibition should go a long way to /protect/ the dopamine pathway, by dramatically reducing the production of free radicals in and around those cells, as caused when dopamine is metabolized by MAO-B. Additionally, the antioxidant-boosting properties of Selegiline (most significantly, Superoxide Dismutase) could help sweep up remaining free radicals.

While I have just recently started Selegiline, it seems to be an ideal "lifestyle drug" that I could take for the rest of my life. If you, or any others, think this is a bad idea to start at my age, do chime in! Given my understanding of the neuroprotective benefits mentioned above, I thought starting it at 18 would be a phenomenal advantage, as my dopamine pathways haven't suffer many decades of attack from oxidizers.
 
If you're wondering about the 30mg vs. 9mg/24hours I would suggest just e-mailing/calling the company that makes the patch. I am positive that they can tell you exactly what it is you want to know.
 
We don't know how safe selegiline is in the long run. It doesn't seem to affect the mortality of PD patients. My guess is that peripheral MAO-B is also inhibited, and you may get some of the negative side effects that you would with levodopa.

Tobacco smoke inhibits MAO-B, but not to the extent that Deprenyl does. A regimen of 2 x 5 mg daily of selegiline daily irreversibly inhibits over 90% of MAO-B in the basal ganglia. Cigarettes inhibit roughly 40% of MAO-B in the brain, iirc.
 
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I realize this is digging up an old thread. But I figured having the final, real word in here would help now that all the fda paperwork is there.

http://www.drugs.com/pro/emsam.html

Read under Pharmacokinetics . The potency as measured in blood concentration of the 6mg patch is 10x higher than taking 10mg of selegiline orally. WOW!


Edit:

Note: This would indicate substantial MAO-A inhibition at even the 6mg patch dose, of which i suspected as much. Whoever thought up emsam really had a great idea to expand on an already great drug. Moving beyond selegiline's MAO-B selectivity opens up an entirely new realm of positive effects, which would be for all practical purposes unattainable with the oral dosage form due to side effects and metabolites.
 
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permastoned said:
I was under the impression that vendors in Amsterdam are no longer allowed to sell mushrooms, and only those who are citizens of Amsterdam are allowed to buy the weed. Due to some new douchebag in charge of the place.
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This post doesnt make any sense at all in relation to the thread
 
Newmoonrecord said:
This post doesnt make any sense at all in relation to the thread
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2CEECS said:
Incidentally, I will be visiting Amsterdam soon, as I am leaving for a tour of Europe on the 9th. While there, I will definitely be evaluating the THC products--but I also want to be prepared to try the mushrooms. For that, I need a better understanding of the level of MAO-A inhibition I am under (if Psilocybin is not metabolized by MAO-A, please correct me).
Click to expand...

Next time, read the whole post by the OP before attempting to label my information redundant, douchebag. You may gain a sliver of respect from me if your name is in reference to the Elliott Smith album. Just a sliver, because you have already displayed such prominent douche baggery.
 
I started taking Emsam 6mg in July 2012 and I noticed a mood improvement literally overnight. Within ten days not only did I have sustained improvement but all my fibromyalgia dramatically improved. (Aside: I attribute this to dopamine, which is also why it helps RLS, Parkinson's, and other neuromuscular conditions. When the medical community starts treating fibro as the neurological condition it is, instead of rheumatic, then we'll have improvement.)
These other symptoms include: parasthesia, tender points, myalgia, stiffness, anxiety, depression, irritability, brain fog, problems with word recall, vision issues, and overwhelming and unrelenting fatigue. I did have some middle insomnia but I didn't care because I was jumping out of bed after 6 hours of sleep feeling motivated and happy instead of feeling like a zombie as I had since my fibro onset. My libido came back after three years, as well!
I stayed at 6 mg until now, mid-October 2012 when suddenly, overnight, I woke up with my old fibro pain. Wondering if it was transient, hormonal, weather-related, or otherwise, I waited it out for ten days. I am definitely not getting the same benefit as when I started.
Today I saw my psychiatrist and my internist. We all wondered about tachyphylaxis, which scares the heck out of me. I do NOT want to go up to 9mg, only to go up to 12mg, only to have to scrap the whole thing in six months and feel miserable again. Another option we discussed was cutting a 9mg or 6mg patch in half to reduce the dose, give my body a chance to "reboot", and go back to 6mg. Not sure if this is realistic or if you can even cut a patch and get the same rate of release.
One more option my internist suggested was similar to hypothyroid therapy. If you start someone at the "real" dose they need, it won't work right. You instead need to titrate up. Perhaps three months at 6mg was a titration period and 9mg is actually my therapeutic dose. I'm not sure this is the case since when I first started 6mg, I felt sometimes it was too strong and I was really buzzy. I felt great otherwise so I really didn't care. Over time, that burst of energy settled into a comfortable, functional energy level. Now I'm back to feeling completely miserable.
Anyone have any experiences they can relate to mine?
 
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