Psycho-Babble Medication Thread 208454

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Attn hok: Sublingual Selegiline Trial Results?

Posted by Ron Hill on March 12, 2003, at 13:23:48

HK,

I know it's early in your sublingual Selegiline trial, but what do you think so far?

-- Ron

 

What do you mean by Sublingual? Ron Hill

Posted by Jack Smith on March 12, 2003, at 13:37:34

In reply to Attn hok: Sublingual Selegiline Trial Results?, posted by Ron Hill on March 12, 2003, at 13:23:48

Is that by mouth?

 

Re: What do you mean by Sublingual?

Posted by Dragonslayer on March 12, 2003, at 13:52:01

In reply to What do you mean by Sublingual? Ron Hill, posted by Jack Smith on March 12, 2003, at 13:37:34

Allow to dissolve under your tongue, I believe.

 

Re: What do you mean by Sublingual? Jack Smith

Posted by Ron Hill on March 12, 2003, at 15:00:44

In reply to What do you mean by Sublingual? Ron Hill, posted by Jack Smith on March 12, 2003, at 13:37:34

> Is that by mouth?

Sublingual administration is holding the medication under the tongue which allows a portion of the medication to be transferred directly to the bloodstream by crossing the thin membrane located at the bottom of the mouth under the tongue. One advantage is that this bypasses the gastrointestinal system. Typically a sublingual tablet formulation is used for this type of administration, however in this particular case, Hok is using the liquid form of deprenyl and holding it under his/her tongue. Hok can tell you more about it than I can.

-- Ron

 

Re: Attn hok: Sublingual Selegiline Trial Results? Ron Hill

Posted by hok on March 13, 2003, at 13:31:37

In reply to Attn hok: Sublingual Selegiline Trial Results?, posted by Ron Hill on March 12, 2003, at 13:23:48

Ron,

Sory to hear about your recent trouble with NADH. I had experienced the same tolerance and irritability effects you speak of. It's too bad the initial effects couldn't be kept up.

Yes, the selegiline is still working. I take anywhere from 1-3mg of it per day (usually all together in 1 dose in the AM). It is completely different from the NADH, even though both seem to affect a modulation of tyrosine hydroxylase. The main effect of the selegiline is probably the MAO-B inihibition - something that has helped replace the smokes for now. At the same time, there is no tiredness, irritability, or rebound effect like I experienced on the NADH. It is not as energizing as the NADH (but I keep the dosage low as well). Yet the anti-anhedonic effect seems to be fairly equivalent. I'm convinced selegiline is definitely one of those drugs that you see a very diverse response to. You just don't know how you're going to react to it until you try it.
Initially, I tried 5-10mg per day + DLPA or tyrosine, but once the full effects kicked in, the dose proved to be way too high and I eventually cut out the DLPA/tyrosine altogether. Too much of the selegiline can induce anxiety /tension. I think this is because of the increase of PEA.

I'm convinced there is a fairly big difference between the sublingual version and the oral tablets. The sublingual version acts much quicker, and more importantly, reduces the amount of metabolites which are responsible for all of the bad side effects.

Due to long-standing sleep disruption issues [not associated with the selegiline], I've very recently added remeron to my regimen. I'm unclear what effect this will have on the selegiline, but I'm hoping, if anything, it will increase its effects since remeron's 5HT2A antagonism increases dopaminergic activity.

If you have any specific questions I didn't answer, please let me know.

HK

 

Re: Sublingual Selegiline Trial Results hok

Posted by Ron Hill on March 13, 2003, at 13:49:28

In reply to Re: Attn hok: Sublingual Selegiline Trial Results? Ron Hill, posted by hok on March 13, 2003, at 13:31:37

HK,

> Sorry to hear about your recent trouble with NADH. I had experienced the same tolerance and irritability effects you speak of. It's too bad the initial effects couldn't be kept up.

I haven't given up on Enada NADH yet. I'm still very optimistic that I can titrate downward and find a dose that continues to treat my atypical depression without inducing irritability. Time will tell. If it fails, sublingual deprenyl is high on my list of possible medications to try.

> Yes, the selegiline is still working. I take anywhere from 1-3mg of it per day (usually all together in 1 dose in the AM).

Great!

> If you have any specific questions I didn't answer, please let me know.

No, I think you covered it. You write well. Please stay in touch regarding the progress of your Selegiline trial.

-- Ron

 

Re: Sublingual Selegiline Trial QUESTION

Posted by Jacob on March 14, 2003, at 20:23:12

In reply to Re: Sublingual Selegiline Trial Results hok, posted by Ron Hill on March 13, 2003, at 13:49:28

Do any of you know if it's safe to use a small dose 1-2mg (drops) of the liquid along with an SSRI (Zoloft)?

Thank you.

 

Re: Sublingual Selegiline Trial QUESTION

Posted by hok on March 15, 2003, at 19:33:14

In reply to Re: Sublingual Selegiline Trial QUESTION, posted by Jacob on March 14, 2003, at 20:23:12

> Do any of you know if it's safe to use a small dose 1-2mg (drops) of the liquid along with an SSRI (Zoloft)?
>
> Thank you.

Yes, you shouldn't have any problem in using the selegiline below a 15mg dose per day (roughly 15 drops).

 

Sublingual Selegiline - more questions hok

Posted by not exactly on March 15, 2003, at 21:20:48

In reply to Re: Attn hok: Sublingual Selegiline Trial Results? Ron Hill, posted by hok on March 13, 2003, at 13:31:37

> I'm convinced there is a fairly big difference between the sublingual version and the oral tablets. The sublingual version acts much quicker, and more importantly, reduces the amount of metabolites which are responsible for all of the bad side effects.

I've tried selegiline in both patch form (worked very well for me) and oral (mixed results). I'm intrigued by the concept of sublingual administration, but I haven't tried it yet. Could you get the same sublingual effect by placing a standard oral tablet (or part of one) under the tongue? How about powder from opening a selegiline cap?

Also, it would seem that regardless of the physical form (liquid, tablet, powder), only some of the medication would be absorbed directly thru the mouth. Doesn't the rest eventually get swallowed and thereby result in the same first-pass metabolism byproducts? Or do you spit it out instead? How long do you leave it under your tongue?

- Bob

 

Re: Sublingual Selegiline - more questions not exactly

Posted by hok on March 15, 2003, at 22:17:35

In reply to Sublingual Selegiline - more questions hok, posted by not exactly on March 15, 2003, at 21:20:48

> I've tried selegiline in both patch form (worked very well for me) and oral (mixed results). I'm intrigued by the concept of sublingual administration, but I haven't tried it yet. Could you get the same sublingual effect by placing a standard oral tablet (or part of one) under the tongue? How about powder from opening a selegiline cap?
>
> Also, it would seem that regardless of the physical form (liquid, tablet, powder), only some of the medication would be absorbed directly thru the mouth. Doesn't the rest eventually get swallowed and thereby result in the same first-pass metabolism byproducts? Or do you spit it out instead? How long do you leave it under your tongue?
>
> - Bob
>

Bob,

You're quite a rare species on this board. It seems not many current posters have had experience with the patch. Do you mind if I pick your brain regarding your trial with the patch in exchange for answers to your own questions? I think we're all curious about what to expect from selegiline in its new form. So here goes...

1) How long ago was the trial that you were in?

2) Was it an open-label trial or was it being tested against something else?

3) Could you give us a brief description of your depressive symptoms (e.g., melancholic, atypical)?

4) Can you provide a subjective rating for the selegiline patch in terms of an antidepressant? In other words, can you compare its efficacy to anything you've been on before?

5) What were the side effects?

6) Was there any issues with being able to tolerate the high dose in patch form (e.g., overstimulation/ increased side effects)? This is more of a personal question because I'm concerned I won't even be able to handle 30 mg in patch form if I can only tolerate 5-10 sublingually. Any thoughts?

7) How much of the oral form have you been taking? My experience with the oral tablets was like taking poison, causing the irritablity of Wellbutrin-like effects times ten.

8) What is your current treatment?


Any other knowledge on the subject would be much appreciated?


As for your questions... I'm quite doubtful you would have an equal effect by placing an oral tablet under your tongue. All the sublignual brands I have come across come suspended in a citrate base to provide better absorption, so I think this aids the process a lot. As for the powder from a capsule...hmmm...it seems likely that this should work. How effectively, who knows though.

I typically leave the drops under my tongue for about 10 minutes [seemingly ample time] to provide full absorption. At first, I was actually swallowing the remainder of what was left. But after about a week, when the full effects were kicking in, I found that swallowing the remainder was probably one of the causes of my feeling adverse side effects. I have since spit out any remainder left over after the 10 minute absorption period. Hope this answers your questions. Why not just buy the sublingual form next time to try it out?

-HK

 

Re: Sublingual Selegiline - more questions hok

Posted by not exactly on March 16, 2003, at 8:13:08

In reply to Re: Sublingual Selegiline - more questions not exactly, posted by hok on March 15, 2003, at 22:17:35

HK,

Thanks for the thorough & enlightening answers to my questions. I'll try to give equally thorough (and hopefully somewhat enlightening) answers to your questions.

> 1) How long ago was the trial that you were in?

3 years ago (Dec. 1999 - Mar. 2000).

> 2) Was it an open-label trial or was it being tested against something else?

Open label. All participants started with real selegiline patches; after 3 months, 50% (double-blind random selection) were switched to identical-looking placebo patches. (I unfortunately ended up in the placebo group.)

> 3) Could you give us a brief description of your depressive symptoms (e.g., melancholic, atypical)?

Typical "atypical": mood reactive, poor self-esteem, introverted, low motivation, poor focus/concentration, no long-term goals, anhedonia, hypersomnia. Comorbid ADD, SP, GAD, SAD, OCD, CFS, Asperger's Syndrome.

> 4) Can you provide a subjective rating for the selegiline patch in terms of an antidepressant? In other words, can you compare its efficacy to anything you've been on before?

The best results I ever had from an antidepressant was my very first treatment - Pramipexole (for 1 month in another pre-approval drug study). Complete remission and a fabulous experience (but not manic) - let's call that a 10. Next best was Wellbutrin + Ritalin; I'd give that a 9. Selegiline patch was at least an 8. Wellbutrin by itself, Ritalin by itself, and oral Selegiline were all about 6. Desipramine was a 3, Effexor 2, Paxil 0 (no depression but no motivation either), Amitriptyline -1 (felt poisoned), Remeron -2 (felt VERY poisoned), Prozac -10 (nearly-homicidal agression).

> 5) What were the side effects?

The only significant side effect was local irritation. My skin was red after I removed the patch. Each day, I'd apply a new patch to a different location (as directed), and the redness disappeared after about 3 days. So on any given day, I'd have one patch, one red blotch, and one pink blotch. The irritation was never severe enough to cause pain or itching, and the doctors & nurses that monitored my progress during the study said that the effect was "typical" and "harmless". BTW, this also provided me with confirming evidence that I had been switched to placebo - the phoney patches did not cause redness.

There may have been other temporary side effects at first, but they were so mild and brief that I don't even remember what they were.

> 6) Was there any issues with being able to tolerate the high dose in patch form (e.g., overstimulation/ increased side effects)? This is more of a personal question because I'm concerned I won't even be able to handle 30 mg in patch form if I can only tolerate 5-10 sublingually. Any thoughts?

The 30 mg patch seemed less "speedy" to me than 15 mg/day oral selegiline.

> 7) How much of the oral form have you been taking? My experience with the oral tablets was like taking poison, causing the irritablity of Wellbutrin-like effects times ten.

I never tried more than 20 mg/day, and eventually settled on 15 mg/day as "optimal". More than 15 caused excessive "speedy" side effects and worried me about the possibility of "death by cheese". Less than 15 was unreliable and made me feel almost bipolar - unpredictable and severe mood swings.

Wellbutrin, BTW, never made me irritable. It DID make me feel motivated, and for the first week even DRIVEN. But long term it dulled my emotions - the addition of a bit of Ritalin fixed that problem.

But I'm certainly not immune to drug-induced irritability. Meds that have made me feel irritable include Desipramine (+), Sudafed (++), and Prozac (+++++).

> 8) What is your current treatment?

Right now I'm taking Buspar + Klonopin. This has been very effective for my SP and GAD (no surprise), but it also turns out to be (for me, at least) an excellent antidepressant! I've only been on this combo for 2 weeks, and I'm not sure if the benefit has reached a plateau yet, but I'd give it an 8 so far. It's plausible that it could be improved by dose adjustment or augmentation. In fact, selegiline is one of the meds that I was thinking might enhance the effect.

> Any other knowledge on the subject would be much appreciated?

I've got lots more stories and opinions. Suggest a topic and I'll babble some more... :-)

> Why not just buy the sublingual form next time to try it out?

1. I assume the sublingual form is not available as a generic, and therefore would be much more expensive. Since I'm currently unemployed, this is a concern.
2. I still have some oral selegiline left from my last prescription, so I was hoping to be able to use it to test the sublingual route and see how well it worked before I tried to convince my pdoc to prescribe it.

- Bob

 

Re: Sublingual Selegiline - more questions not exactly

Posted by hok on March 18, 2003, at 9:55:45

In reply to Re: Sublingual Selegiline - more questions hok, posted by not exactly on March 16, 2003, at 8:13:08

Bob,

thanks for your informative answers. Our symptoms are fairly similar, atypical/anhedonic depression, with concommitant anxiety, SP, SAD, and CFS features.

I'm really surprised the buspar/klonopin combo is working for you. I've found utility in both drugs but only to a limited extent. It's good to hear that a successful tx plan can be so simpilified sometimes. Good luck with the selegiline augmentation. A word of warning though, low doses of selegiline without an AD may induce depression. Hopefully, the buspar will help buffer this effect.

By the way, did you ever have any problems with selegiline and verbal fluency? It seems deprenyl is great for word recall, but I seem to get "caught up" a lot in my conversations. There is some reference in the reserch to a decrease in verbal fluency on selegiline and I was wondering if you ever noticed this while on the patch (or did the MAO-A inhibition help to balance this out).

HK

 

Re: Sublingual Selegiline - more questions hok

Posted by not exactly on March 19, 2003, at 3:04:46

In reply to Re: Sublingual Selegiline - more questions not exactly, posted by hok on March 18, 2003, at 9:55:45

> A word of warning though, low doses of selegiline without an AD may induce depression.

Yes, I've noticed that. As I mentioned before, "Less than 15 [mg/day of oral selegiline] was unreliable and made me feel almost bipolar - unpredictable and severe mood swings."

I found that low-dose selegiline worked well only when I combined it with something else. The three augmentation agents that worked best were phenylalanine, chocolate, and Ritalin. Any of these 3 would turn low-dose selegiline into a consistently effective antidepressant. But none worked so well that they ended my quest for a better solution.

> Hopefully, the buspar will help buffer this effect.

Since Buspar is working well for me as an AD, I was thinking that it too might serve to stabilize the positive effects of selegiline. And hopefully the selegiline will give me a bit more energy and further reduce the anhedonia. There's really only one way to find out for sure. But first, I want to see what the Buspar/Klonopin combo will do with dose optimizing and patiently waiting for the full plateau.

> By the way, did you ever have any problems with selegiline and verbal fluency? It seems deprenyl is great for word recall, but I seem to get "caught up" a lot in my conversations. There is some reference in the reserch to a decrease in verbal fluency on selegiline and I was wondering if you ever noticed this while on the patch (or did the MAO-A inhibition help to balance this out).

I've noticed that my verbal fluency and word recall vary significantly with different meds, but I don't remember selegiline (oral or transdermal) having a negative effect on either capability.

- Bob

 

Re: Sublingual Selegiline - more questions

Posted by fab on October 15, 2003, at 23:17:44

In reply to Re: Sublingual Selegiline - more questions hok, posted by not exactly on March 19, 2003, at 3:04:46

I've taken very low dosages of selegiline with no hint of it causing depression... anyway, who manufactures the new sublingual? I'm interested!!
Thanks!

RE: > > A word of warning though, low doses of selegiline without an AD may induce depression.
>
> Yes, I've noticed that. As I mentioned before, "Less than 15 [mg/day of oral selegiline] was unreliable and made me feel almost bipolar - unpredictable and severe mood swings."
>
> I found that low-dose selegiline worked well only when I combined it with something else. The three augmentation agents that worked best were phenylalanine, chocolate, and Ritalin. Any of these 3 would turn low-dose selegiline into a consistently effective antidepressant. But none worked so well that they ended my quest for a better solution.
>
> > Hopefully, the buspar will help buffer this effect.
>
> Since Buspar is working well for me as an AD, I was thinking that it too might serve to stabilize the positive effects of selegiline. And hopefully the selegiline will give me a bit more energy and further reduce the anhedonia. There's really only one way to find out for sure. But first, I want to see what the Buspar/Klonopin combo will do with dose optimizing and patiently waiting for the full plateau.
>
> > By the way, did you ever have any problems with selegiline and verbal fluency? It seems deprenyl is great for word recall, but I seem to get "caught up" a lot in my conversations. There is some reference in the reserch to a decrease in verbal fluency on selegiline and I was wondering if you ever noticed this while on the patch (or did the MAO-A inhibition help to balance this out).
>
> I've noticed that my verbal fluency and word recall vary significantly with different meds, but I don't remember selegiline (oral or transdermal) having a negative effect on either capability.
>
> - Bob
>

 

Is Selegiline an antidepressant below 15 mg?

Posted by sb417 on October 16, 2003, at 1:37:14

In reply to Re: Sublingual Selegiline - more questions, posted by fab on October 15, 2003, at 23:17:44

Does Selegiline have antidepressant properties at low (1-15mg) dosages? Is it an antidepressant at any dosage?

 

Sublingual Selegiline - more qs - more effective?

Posted by btnd on October 17, 2003, at 7:47:33

In reply to Re: Sublingual Selegiline - more questions, posted by fab on October 15, 2003, at 23:17:44

> I've taken very low dosages of selegiline with no hint of it causing depression... anyway, who manufactures the new sublingual? I'm interested!!


Why do you care about special sublingual brand of selegiline? Can't someone just crush Jumex/Deprenyl/Segan (selegiline 5mg) pills to powder and put them under the tongue? I do that with Klonopin and it works so much faster.
Does anyone know if using selegiline sublingually would be more effective or have less side-effects?
What's the story on sublingual selegiline VS normal selegiline - what are the differences? Also I've heard about selegiline in a patch - would this be the best method of administration? Hmm I'm a little confused on the subject of taking selegiline - I will be trying it in short future for my dopaminal-motivation problems and just want to know what would be the best way to use selegiline.

 

Re: Sublingual Selegiline - more qs - more effective?

Posted by elleff on October 19, 2003, at 19:16:46

In reply to Sublingual Selegiline - more qs - more effective?, posted by btnd on October 17, 2003, at 7:47:33

> Why do you care about special sublingual brand of selegiline? Can't someone just crush Jumex/Deprenyl/Segan (selegiline 5mg) pills to powder and put them under the tongue?

In my experience putting one tablet under the tongue and allowing it to disolve and absorb is quite effective if you can stand the bitter taste.

> Does anyone know if using selegiline sublingually would be more effective or have less side-effects?

I don't think there is any concrete evidence here, but my guess is that because selegiline has such a short half-life (less than 30 mins) and a high rate of first pass metabolism (into desmethyl selegiline and l-methamphetamine), the SL route simply puts more of the parent compound into your brain. As 2.5 - 5mg per day of selegiline will completely inhibit MAOI-B, one 5mg tablet per day SL should be all that is required, which conforms with my experience.

The clinical trial data suggests that 30-60mg of oral selegiline, or 20mg per day of transcutaneous selegiline is an effective antidepressant dose (the patch is soon likely to get FDA approval). At the above oral dose selegiline is nonselective and is quite similar to tranylcypramine (Parnate).

Other trial data suggests that 10mg per day of Selegiline plus 250mg - 1,000mg per day of DL-phenylalanine is an effective antidepressant combination.

My experiences is that 5mg of Selegiline SL in the morning, plus 500mg DL-phenylalanine + 200mcg of Chromium chelate + a Vit B6 & Vit C containing multivitamin morning and afternoon is pretty effective for ADD and dysthymic symptoms. The chromium probably works via an insulin augmenting action which increases transport of branch-chain and aromatic amino acids across the blood brain barrier. Presumably the combination increases the amount of endogenous PEA (phenylethylamine) quite substantially and probably also increases dopamine levels. PEA is only one methyl group short of dexamphetamine, which presumably works as a high-powered exogenous version of the former.

For best absorption and BBB penetration DL-phenylalanine should be taken on an empty stomach.

regards

elleff


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