Psycho-Babble Medication Thread 1119824

Shown: posts 1 to 12 of 12. This is the beginning of the thread.

 

Oral deprenyl vs bupropion?

Posted by Franz on June 3, 2022, at 11:04:40

Why use bupropion if deprenyl (selegiline) looks similar in that it increases dopamine and norpinephrine (not sure on the last one)?

It seems deprenyl has less side effects like elevated blood pressure from bupropion.

I know deprenyl is a MAOB inhibitor and bupropion a reuptake inhibitor.

Anyone tried both and can compare or elaborate from theory?

Thanks.

 

Re: Oral deprenyl vs bupropion? » Franz

Posted by Jay2112 on June 4, 2022, at 17:52:53

In reply to Oral deprenyl vs bupropion?, posted by Franz on June 3, 2022, at 11:04:40

> Why use bupropion if deprenyl (selegiline) looks similar in that it increases dopamine and norpinephrine (not sure on the last one)?
>
> It seems deprenyl has less side effects like elevated blood pressure from bupropion.
>
> I know deprenyl is a MAOB inhibitor and bupropion a reuptake inhibitor.
>
> Anyone tried both and can compare or elaborate from theory?
>
> Thanks.

I tried oral deprenyl through mail order once, with about a months supply. I personally didn't like the rev'd up feeling. I was only on 1.25mg dose. It was a bit more intense then Wellbutrin/bupropion. But, it's all very individual, as my Dad did excellent on the same dose for years. We don't have the patch here in Canada.

Jay

 

Re: Oral deprenyl vs bupropion?

Posted by undopaminergic on June 6, 2022, at 10:10:32

In reply to Oral deprenyl vs bupropion?, posted by Franz on June 3, 2022, at 11:04:40

> Why use bupropion if deprenyl (selegiline) looks similar in that it increases dopamine and norpinephrine (not sure on the last one)?
>
> It seems deprenyl has less side effects like elevated blood pressure from bupropion.
>
> I know deprenyl is a MAOB inhibitor and bupropion a reuptake inhibitor.
>
> Anyone tried both and can compare or elaborate from theory?
>
> Thanks.

To my knowledge, based on personal experience and a selection of literature I've read, selegiline (l-deprenyl) is the more potent of the two. At first, it had a substantial mood-elevating effect on its own, but this was transient. As a MAO-B inhibitor, it can also be used to potentiate certain other drugs, of which (beta-)phenylethylamine (PEA) is one I have long term experience with. Meanwhile, bupropion (Wellbutrin, Zyban, Voxra) was without effect in my own experience, and I tried doses above those recommended. It does however seem to work for a lot of people, although few of them have tried selegiline.

-undopaminergic

 

Re: Oral deprenyl vs bupropion?

Posted by linkadge on June 6, 2022, at 18:39:45

In reply to Re: Oral deprenyl vs bupropion?, posted by undopaminergic on June 6, 2022, at 10:10:32

Wellbutrin is only a weak dopamine reuptake inhibitor. Also, blocking the nicotine acetylcholine receptors might actually lower dopamine release.

Linkadge

 

Re: Oral deprenyl vs bupropion?

Posted by SLS on June 7, 2022, at 7:28:09

In reply to Re: Oral deprenyl vs bupropion?, posted by linkadge on June 6, 2022, at 18:39:45

Hi.

L-Deprenyl / selegeline / EMSAM is *selective* for MAO-B, but only at low dosages. At higher dosages, selegeline becomes non-selective and MAO-A is also inhibited, Of these two types of MAO enzymes, MAO-A is the the one that is associated with antidepressant effects. The package label for EMSAM is explicit regarding this. Clorgyline is no longer available, but it is an irreversible *specific* inhibitor of MAO-A. It doesn't inhibit MAO-B at all. The NIH had considered it the most powerful antidepressant in the world, but reserved it for their most treatment-resistant cases of treatment-resistant depression - TRD. It left me improved, but they would not allow me to combine it with a tricyclic antidepressant (TCA) like desipramine or nortriptyline, which I had needed to add to Nardil or Parnets in order to respond. Ultimately, they had to discontinue giving clorgyline to their patients because adverse cardiac events were reported.

Moclobemide is another MAOI that is specific for MAO-A. It is a reversible inhibitor of monoamine oxidase (RIMA). Unfortunately, it is reversible rather than irreversible, leaving it an inferior choice. Some people get amazing results in the first week at 300 mg/day. However, dosage escalation is usually inevitable to retain the antidepressant response. The maximum dosage is usually considered to be 1200 mg/day. Still, very few people remain improved indefinitely on moclobemide.

In summary, inhibiting MAO-A is sufficient to yield an improvement in depression.


- Scott

 

Re: Oral deprenyl vs bupropion? - More

Posted by SLS on June 7, 2022, at 7:38:44

In reply to Re: Oral deprenyl vs bupropion?, posted by SLS on June 7, 2022, at 7:28:09

I forgot to mention that taking L-deprenyl / selegiline orally is not terribly effective. I tried sit many years ago. I don't remember the pharmacological reasons for this, but I believe oral administration produces far less circulating selegiline. I think it might be broken down in the gut.

Regarding selegiline and needing dosages high enough to inhibit MAO-A in order to obtain an antidepressant response:

https://pubmed.ncbi.nlm.nih.gov/10418793/


- Scott

 

Re: Oral deprenyl vs bupropion? - More

Posted by undopaminergic on June 7, 2022, at 7:47:04

In reply to Re: Oral deprenyl vs bupropion? - More, posted by SLS on June 7, 2022, at 7:38:44

> I forgot to mention that taking L-deprenyl / selegiline orally is not terribly effective. I tried sit many years ago. I don't remember the pharmacological reasons for this, but I believe oral administration produces far less circulating selegiline. I think it might be broken down in the gut.
>

The first-pass metabolism in the liver converts much of it to l-methamphetamine, l-amphetamine, and desmethylselegiline, but these metabolites are also responsible for some of the pharmacological effects of selegiline. I think the initial mood boost I got from it was due to the amphetamines. Research has revealed that a lot of the neuroprotective properties of selegiline are due to desmethylselegiline, which is also a MAO-B inhibitor.

-undopaminergic

 

Re: Oral deprenyl vs bupropion? - More

Posted by linkadge on June 7, 2022, at 18:40:15

In reply to Re: Oral deprenyl vs bupropion? - More, posted by undopaminergic on June 7, 2022, at 7:47:04

Although, apparently, dopamine agonists are associated with slower Parkinson's progression than selegiline.

Linkadge

 

Re: Oral deprenyl vs bupropion? - More

Posted by SLS on June 7, 2022, at 20:41:03

In reply to Re: Oral deprenyl vs bupropion? - More, posted by undopaminergic on June 7, 2022, at 7:47:04

> > I forgot to mention that taking L-deprenyl / selegiline orally is not terribly effective. I tried sit many years ago. I don't remember the pharmacological reasons for this, but I believe oral administration produces far less circulating selegiline. I think it might be broken down in the gut.
> >
>
> The first-pass metabolism in the liver converts much of it to l-methamphetamine, l-amphetamine, and desmethylselegiline, but these metabolites are also responsible for some of the pharmacological effects of selegiline. I think the initial mood boost I got from it was due to the amphetamines. Research has revealed that a lot of the neuroprotective properties of selegiline are due to desmethylselegiline, which is also a MAO-B inhibitor.
>
> -undopaminergic


Good info, U_D. It has been a long time since I tried EMSAM. I don't remember much about it.

I began studying L-deprenyl in 1983. At the time, I was looking for anything that would boost dopamine. The research clinician who I was seeing at Columbia-Presbyterian laughed at me. Her only comment when I asked her about using bromocriptine was that I would have fun throwing-up all day. At the time, there was only one other publishing author who began to focus on the possible role of dopamine in depression. His name was A. Randrup. He was at the University of Chicago at the time. I was reassured to find someone with letters after his last name coming to the same conclusions.

https://pubmed.ncbi.nlm.nih.gov/408861/


- Scott

 

Re: Oral deprenyl vs bupropion? » SLS

Posted by Jay2112 on June 10, 2022, at 19:28:14

In reply to Re: Oral deprenyl vs bupropion?, posted by SLS on June 7, 2022, at 7:28:09

> Hi.
>
> L-Deprenyl / selegeline / EMSAM is *selective* for MAO-B, but only at low dosages. At higher dosages, selegeline becomes non-selective and MAO-A is also inhibited, Of these two types of MAO enzymes, MAO-A is the the one that is associated with antidepressant effects. The package label for EMSAM is explicit regarding this. Clorgyline is no longer available, but it is an irreversible *specific* inhibitor of MAO-A. It doesn't inhibit MAO-B at all. The NIH had considered it the most powerful antidepressant in the world, but reserved it for their most treatment-resistant cases of treatment-resistant depression - TRD. It left me improved, but they would not allow me to combine it with a tricyclic antidepressant (TCA) like desipramine or nortriptyline, which I had needed to add to Nardil or Parnets in order to respond. Ultimately, they had to discontinue giving clorgyline to their patients because adverse cardiac events were reported.
>
> Moclobemide is another MAOI that is specific for MAO-A. It is a reversible inhibitor of monoamine oxidase (RIMA). Unfortunately, it is reversible rather than irreversible, leaving it an inferior choice. Some people get amazing results in the first week at 300 mg/day. However, dosage escalation is usually inevitable to retain the antidepressant response. The maximum dosage is usually considered to be 1200 mg/day. Still, very few people remain improved indefinitely on moclobemide.
>
> In summary, inhibiting MAO-A is sufficient to yield an improvement in depression.
>
>
> - Scott

Moclobomide was, personally, a super-interesting drug. Yes, it has a super short half-life...of 2-3 hours. But, being a rapid metabolizer of drugs, I took smaller doses, like a 150mg dose split in half to a 75mg dose, and I spaced it one of those every 4-5 hours, 4x a day. And boy, it's antidepressant effects are felt immediately! It works more for apathetic, slow, tiring depression, than anxiety..at least at first. I remember so clearly, taking the 75mg dose on a day where I felt deflated by life, and WOW..I was a tad manic, but felt productive.It also has a pro-testosterone effect too. Sex with this stuff was f'ing increadible!! After years of chronic SRI use, just...WOW. So, I keep it in the back of my mind as an emergency drug when all others run out!

And...apparently it works even MUCH better with lithium..in fact I know of a number of individuals at university who are on this combo, and have been in remission for years. I would add, a STRONG GABA drug, like Lyrica, or a strong benzo, really help cool off the stimulating effects of this drug in the evening.

FWIW...IMHO...etc...

Jay

 

Re: Oral deprenyl vs bupropion? » Jay2112

Posted by SLS on June 11, 2022, at 8:35:24

In reply to Re: Oral deprenyl vs bupropion? » SLS, posted by Jay2112 on June 10, 2022, at 19:28:14

Hi, Jay.

Thanks for your valuable contribution of describing the phenomenology of moclobemide, and how you responded to it. Why did you stop taking it?

Regarding your use of moclobemide as an "emergency" drug, I would suggest that the most important role of moclobemide *might* be to knock enough bricks out of the wall of complete resistance to allow other drugs to regain their efficacies as antidepressants.

I like to think that this is possible.


- Scott

> > Hi.
> >
> > L-Deprenyl / selegeline / EMSAM is *selective* for MAO-B, but only at low dosages. At higher dosages, selegeline becomes non-selective and MAO-A is also inhibited, Of these two types of MAO enzymes, MAO-A is the the one that is associated with antidepressant effects. The package label for EMSAM is explicit regarding this. Clorgyline is no longer available, but it is an irreversible *specific* inhibitor of MAO-A. It doesn't inhibit MAO-B at all. The NIH had considered it the most powerful antidepressant in the world, but reserved it for their most treatment-resistant cases of treatment-resistant depression - TRD. It left me improved, but they would not allow me to combine it with a tricyclic antidepressant (TCA) like desipramine or nortriptyline, which I had needed to add to Nardil or Parnets in order to respond. Ultimately, they had to discontinue giving clorgyline to their patients because adverse cardiac events were reported.
> >
> > Moclobemide is another MAOI that is specific for MAO-A. It is a reversible inhibitor of monoamine oxidase (RIMA). Unfortunately, it is reversible rather than irreversible, leaving it an inferior choice. Some people get amazing results in the first week at 300 mg/day. However, dosage escalation is usually inevitable to retain the antidepressant response. The maximum dosage is usually considered to be 1200 mg/day. Still, very few people remain improved indefinitely on moclobemide.
> >
> > In summary, inhibiting MAO-A is sufficient to yield an improvement in depression.
> >
> >
> > - Scott



> Moclobomide was, personally, a super-interesting drug. Yes, it has a super short half-life...of 2-3 hours. But, being a rapid metabolizer of drugs, I took smaller doses, like a 150mg dose split in half to a 75mg dose, and I spaced it one of those every 4-5 hours, 4x a day. And boy, it's antidepressant effects are felt immediately! It works more for apathetic, slow, tiring depression, than anxiety..at least at first. I remember so clearly, taking the 75mg dose on a day where I felt deflated by life, and WOW..I was a tad manic, but felt productive.It also has a pro-testosterone effect too. Sex with this stuff was f'ing increadible!! After years of chronic SRI use, just...WOW. So, I keep it in the back of my mind as an emergency drug when all others run out!
>
> And...apparently it works even MUCH better with lithium..in fact I know of a number of individuals at university who are on this combo, and have been in remission for years. I would add, a STRONG GABA drug, like Lyrica, or a strong benzo, really help cool off the stimulating effects of this drug in the evening.
>
> FWIW...IMHO...etc...
>
> Jay

 

Thanks to ALL! (nm)

Posted by Franz on June 12, 2022, at 8:56:19

In reply to Oral deprenyl vs bupropion?, posted by Franz on June 3, 2022, at 11:04:40


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