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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 20 of 20. This is the beginning of the thread.
Posted by crabwalk on July 12, 2006, at 15:15:11
Wondering if anyone can answer this for me. I've been using 1/2 of a patch for 6-8 weeks now because I wanted to get a primarily dopaminergic effect. It's actually been better than a full patch in terms of my overall wellbeing. However, my goal with any med now is to try to undo the long-lasting damage ssri's caused to my emotional and sexual responses. So far I haven't really come close. If 1/2 a patch is still inhibiting mao-a then I'm thinking that it could be hindering rather than helping my recovery. People have discussed the pharmacokinetics of the patch here before--I know that the 6mg patch is equivalent to 40mg dose of selegiline.
Does anyone know if 1/2 a patch would still strongly raise serotonin? It sure feels like it sometimes, but that could very well just be me still screwed up from prozac.
Posted by linkadge on July 12, 2006, at 15:37:52
In reply to 1/2 an emsam patch - both types of mao inhibition?, posted by crabwalk on July 12, 2006, at 15:15:11
The problem is that serotonin is involved in sexual response. If you push it too low, then you can sexual problems in its own right.
The 5-ht1a receptor is important in sexual response. This may be why ginkgo helps. You could try buspar.
Its hard to say, since I am in the same boat.
Linkadge
Posted by SLS on July 12, 2006, at 16:08:49
In reply to 1/2 an emsam patch - both types of mao inhibition?, posted by crabwalk on July 12, 2006, at 15:15:11
> I know that the 6mg patch is equivalent to 40mg dose of selegiline.
Where can I find more information on this?
- Scott
Posted by Phillipa on July 12, 2006, at 22:05:46
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by SLS on July 12, 2006, at 16:08:49
Who's that Doctor that developed the patch that you can E-mail? Two people here have E-mailed him that I know of. I may have the name in my Robert David file. He's e-mailed him and he e-mails back quickly. Love Phillipa
Posted by Jost on July 13, 2006, at 10:28:57
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by SLS on July 12, 2006, at 16:08:49
I was under the impression that the 6 mg patch was equal to 20 mg oral selegiline; the 9 mg patch equaled 30 mg oral s.; and the 12 mg patch was 40 mg.
One reason I think this is that the box says 20mg-6/24h, 30mg-9/24h, and 40 mg-12/24h.
Can' think of any interpretation of this other than that the 6 mg patch for 24 hours gives you same as 20 mg oral selegiline, etc.
I was also under the impression that since the selegiline from the patch goes directly to the brain and intestine, and not through the liver, there was some, but much less mao-a inhibition (in the intestine). There would be some, but fairly insignificant.
One reason is, if you look at the company's charts, mao-a inhibition in the intestine continues to rise, after the pass through the liver, rather than levelling off. See: www.fda.gov/ohrms/dockets/ac/05/slides/2005-4186S2_03_Somerset-EMSAM.ppt
Jost
Posted by SLS on July 13, 2006, at 11:40:19
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by Jost on July 13, 2006, at 10:28:57
> I was under the impression that the 6 mg patch was equal to 20 mg oral selegiline; the 9 mg patch equaled 30 mg oral s.; and the 12 mg patch was 40 mg.
>
> One reason I think this is that the box says 20mg-6/24h, 30mg-9/24h, and 40 mg-12/24h.
>
> Can' think of any interpretation of this other than that the 6 mg patch for 24 hours gives you same as 20 mg oral selegiline, etc.
>
> I was also under the impression that since the selegiline from the patch goes directly to the brain and intestine, and not through the liver, there was some, but much less mao-a inhibition (in the intestine). There would be some, but fairly insignificant.
>
> One reason is, if you look at the company's charts, mao-a inhibition in the intestine continues to rise, after the pass through the liver, rather than levelling off. See: www.fda.gov/ohrms/dockets/ac/05/slides/2005-4186S2_03_Somerset-EMSAM.ppt
>
> Jost
The labelling indicates 20mg/20cm2 or 30mg/30cm2 or 40/40cm2These represent the total amount of drug contained in each patch, not some sort of pharmacokinetic bioequivalency representative of an oral dose.
- Scott
Posted by crabwalk on July 13, 2006, at 11:57:46
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by Jost on July 13, 2006, at 10:28:57
I was confused by this for awhile...
The 20mg patch contains 20 mg of selegiline on it, but only slightly less than a third (30%) of it gets delivered through the skin in 24 hrs. The same with the other patches, so 20 delivers 6, 30 delivers 9, 40 delivers 12.
But, I remember someone posting that they had talked to a researcher involved in the testing or development, and he'd said wearing the 20 mg patch was the same as taking 40mg of oral selegiline daily. I guess that'd be because it bypasses the liver, so 40mg oral would actually be a good deal less once it reached the brain. Also the oral dose is all at once while the patch is spread out over 24 hrs, so I guess the average concentration ends up being the same? I'm not exactly sure.
MA0-A is not just in the gut, it's in the cortex as well where it breaks down serotonin and norepinephrine and less so dopamine. The patch mostly bypasses the gut where mao-a is needed to break down tyramine, making sure only cortical mao-a is destroyed.
So my original question was what exactly does 1/2 a patch (10mg - 3 delivered) do in terms of mao inhibition? If the 20mg patch is like 40mg oral, is 10mg like 20 oral? If so there should still be mao-a inhibition, but it may not work that way. Anybody have that email address?
Posted by SLS on July 13, 2006, at 12:07:22
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by crabwalk on July 13, 2006, at 11:57:46
> But, I remember someone posting that they had talked to a researcher involved in the testing or development, and he'd said wearing the 20 mg patch was the same as taking 40mg of oral selegiline daily.
That sounds very plausible.
- Scott
Posted by Last Chance on July 13, 2006, at 22:25:29
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by SLS on July 13, 2006, at 12:07:22
Hi - I have tried higher doses, 9mg 24/7, but it made me feel worse. For a couple of weeks I have been on 1/2 a 6mg patch, and I take it off a few hrs. before bed. I take .25 klonapin in the morning, and again at night. I sleep pretty well, not great - depression seems to be under control - I am more social, spontaneous - so for whatever reason this small dose works for me. So I am back to thinking Emsam is pretty good - the negative sexual side effects are also gone.
Posted by Phillipa on July 13, 2006, at 22:34:46
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by Last Chance on July 13, 2006, at 22:25:29
Thats great. Someone just suggested to me 1/3 of a 6mg patch. Love Phillipa
Posted by mayzee on July 13, 2006, at 23:22:49
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by Last Chance on July 13, 2006, at 22:25:29
Having heard that several people were doing better on 1/2 a patch --while I was still feeling worse after 6 weeks on the whole 6mg patch-- I asked 2 pdocs what they thought about my trying 1/2 rather than increasing to 9mg. Both said it didn't make any sense that going to a lower dose could be better for me. Neither pdoc has much experience with MAOIs.
Is it just a matter of "everybody reacts differently"? Or is there some rationale for why the lower dose might work when the higher one made me feel more depressed? (e.g., something specific to MAOIs?) I am really a novice with this. If someone with more expertise has any thoughts to share, I will greatly appreciate it.
Posted by KayeBaby on July 14, 2006, at 14:54:47
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by mayzee on July 13, 2006, at 23:22:49
> Having heard that several people were doing better on 1/2 a patch --while I was still feeling worse after 6 weeks on the whole 6mg patch-- I asked 2 pdocs what they thought about my trying 1/2 rather than increasing to 9mg. Both said it didn't make any sense that going to a lower dose could be better for me. Neither pdoc has much experience with MAOIs.
>
> Is it just a matter of "everybody reacts differently"? Or is there some rationale for why the lower dose might work when the higher one made me feel more depressed? (e.g., something specific to MAOIs?) I am really a novice with this. If someone with more expertise has any thoughts to share, I will greatly appreciate it.
I know that "too much" Wellbutrin made me despondant in a way I have never known. Flat. Just...nothing had meaning. The world seemed less deminsional. More plastic. I cried all day. This is totally unlike the usual depression I might feel.
150 mg was fine and helpful. 300mg made me just numb and despondant.I have the same problem with ritalin. I can only tolerate a tiny amount. I normal dosage will make me into a drooling zombie. I will sit and stare at the wall.
A very similar effect with strattera. When I got close to the standard adult dose I could barely move.
Less is more with NA and DA-I guess. I really need that little bit though or I am pretty much worthless.
I am not sure why this is.
Peace,
Kaye
Posted by Jost on July 14, 2006, at 18:52:44
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by SLS on July 13, 2006, at 11:40:19
Posted by Donna Louise on July 17, 2006, at 5:50:15
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by SLS on July 12, 2006, at 16:08:49
> > I know that the 6mg patch is equivalent to 40mg dose of selegiline.
>
> Where can I find more information on this?
>
>
> - ScottScott, it is all in the whatchacallit that comes in the package with the drug. PI sheet? There is a graph too. I don't know where the idea that 6mg =40mg. According to this package info, transdermally you get about 3 1/2 times the amount you get orally. So, 6mg orally=20mg transdermally. 9mg=30 and 12mg=40. This is why I didn't get the most relief until 12 mg patch as it takes 40mg for me to get enough MAOI A deanimation.
donna
Posted by SLS on July 17, 2006, at 9:56:39
In reply to Re: 1/2 an emsam patch - both types of mao inhibit » SLS, posted by Donna Louise on July 17, 2006, at 5:50:15
> > > I know that the 6mg patch is equivalent to 40mg dose of selegiline.
> >
> > Where can I find more information on this?
> >
> >
> > - Scott
>
> Scott, it is all in the whatchacallit that comes in the package with the drug. PI sheet? There is a graph too. I don't know where the idea that 6mg =40mg. According to this package info, transdermally you get about 3 1/2 times the amount you get orally. So, 6mg orally=20mg transdermally. 9mg=30 and 12mg=40. This is why I didn't get the most relief until 12 mg patch as it takes 40mg for me to get enough MAOI A deanimation.
I looked at the drug monograph PDF from BMS and on rxlist.com, and couldn't find anything that addressed my question. This issue is really bugging me. I am getting the impression that the 12mg/24hr patch is giving you a plasma level of selegiline that is quite a bit higher than that you would receive from taking a 40mg oral dose.You would think that you could find a bunch of stuff on Medline stating quite simply what the relative pharmacokinetics are between the two preparations, but you can't.
- Scott
Posted by Phillipa on July 17, 2006, at 21:05:34
In reply to Re: 1/2 an emsam patch - both types of mao inhibit » Donna Louise, posted by SLS on July 17, 2006, at 9:56:39
Scott would that explain why so many EMSAM users are having horrendous insomnia problems? Love Phillipa
Posted by SLS on July 17, 2006, at 22:13:50
In reply to Re: 1/2 an emsam patch - both types of mao inhibit » SLS, posted by Phillipa on July 17, 2006, at 21:05:34
> Scott would that explain why so many EMSAM users are having horrendous insomnia problems? Love Phillipa
That's a good thought. Probably.
- Scott
Posted by Jost on July 18, 2006, at 19:50:07
In reply to Re: 1/2 an emsam patch - both types of mao inhibit » Donna Louise, posted by SLS on July 17, 2006, at 9:56:39
> > > > I know that the 6mg patch is equivalent to 40mg dose of selegiline.
> > >
> > > Where can I find more information on this?
> > >
> > >
> > > - Scott
> >
> > Scott, it is all in the whatchacallit that comes in the package with the drug. PI sheet? There is a graph too. I don't know where the idea that 6mg =40mg. According to this package info, transdermally you get about 3 1/2 times the amount you get orally. So, 6mg orally=20mg transdermally. 9mg=30 and 12mg=40. This is why I didn't get the most relief until 12 mg patch as it takes 40mg for me to get enough MAOI A deanimation.
>
>
> I looked at the drug monograph PDF from BMS and on rxlist.com, and couldn't find anything that addressed my question. This issue is really bugging me. I am getting the impression that the 12mg/24hr patch is giving you a plasma level of selegiline that is quite a bit higher than that you would receive from taking a 40mg oral dose.
>
> You would think that you could find a bunch of stuff on Medline stating quite simply what the relative pharmacokinetics are between the two preparations, but you can't.
>
>
> - ScottI thought about posting to the effect that I'm pretty sure, in retrospect, that my pdoc said something about doing the math and coming up with 40 mg in the 6/20 mg patch. But I can't figure out how he got that, after reading through the materials, which are really confusing.
Is it possible they really don't want to commit about how much you're getting compared to oral selegiline? If so, I can't figure out if it could be because the drug seems to be metabolized, and or to have effects that aren't precisely in proportion to what you would think, based solely on the amount in the patch. Or, if it's because there's so much variation in how individuals metabolize it, and there's all this controversy about maoi food effects, that they don't want to go on record with a number, even though they've shown that it's safe, in effect, by the use of tyramine challenges.
But the 40 mg figure really does ring a bell--
Jost
Posted by crabwalk on July 19, 2006, at 11:46:21
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by Jost on July 18, 2006, at 19:50:07
It might be a moot question anyway because of individual variation, for instance some people are sensitive to less than 5mg of prozac. But my thinking was a) oral selegiline goes through much more metabolism before reaching the cortex than does transdermal, and b) oral doses are taken once or twice a day while transdermal is essentially a drip-feed or a very stable controlled-release, and this surely affects the stability of plasma and cortical levels of the drug. I have no idea if either/which of these makes the substantial difference, but it could work out that a lot of oral selegiline=not much transdermal.
Posted by Donna Louise on July 19, 2006, at 16:13:52
In reply to Re: 1/2 an emsam patch - both types of mao inhibit, posted by crabwalk on July 19, 2006, at 11:46:21
> It might be a moot question anyway because of individual variation, for instance some people are sensitive to less than 5mg of prozac. But my thinking was a) oral selegiline goes through much more metabolism before reaching the cortex than does transdermal, and b) oral doses are taken once or twice a day while transdermal is essentially a drip-feed or a very stable controlled-release, and this surely affects the stability of plasma and cortical levels of the drug. I have no idea if either/which of these makes the substantial difference, but it could work out that a lot of oral selegiline=not much transdermal.
I think it means that their is more selegiline transdermally and less metabolites than orally. By bypassing the liver, not as much of the originally drug is broken down into its amphetamine metablolites and more parent drug is available directly to the bloodstream and therefore the brain.
donna
This is the end of the thread.
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