• N&PD Moderators: Skorpio | thegreenhand

Tramadol as an Antidepressant?

Well they both share the 3-chlorophenyl group. I am not necessarily saying this idea will work, or it is destined to failure. However tramadol does induce seizures at doses >400mg. This is a real hefty dose for someone who is using sparingly. But once you develop a tolerance this amount can very easily be digested within a 24hr time frame.
 
There's something they have in common, lowering of the seizure threshold or actually causing seizures. I believe 450 mg / day is the highest recommended dose of bupropion while 400 mg /day is the highest rec. dose of tramadol. I'd like to hear more about your idea.
 
It is just an idea for R&D although I cant say for sure to what extent this infringement on existing work will be a success.

The scope is really open ended but the intent of the project is directed toward enantioselectivity. Enantioselective separation of tramadol has been patented several times already. It seems evident that a racemic mixture works best although the threat of seizure remains.

It could turn out that (S,S)-4-chlorophenyl-tramadol could serve a positive role as a stimulant that shares similarities with cocaine. This idea may not be suitable grounds for a patent but it might be adequate grounds for sale of a potential RC. At this stage in development I just dont know :\
 

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Tramadol surely is a "unique" opioid but I'm curious about the mechanism of action that would give your theoretical (S,S)-4-chlorophenyl-tramadol stimulant properties. Also, could you please elaborate on what similarities it may share with cocaine? I'm just curious as to why you said cocaine as opposed to another stimulant, such as an amphetamine. Are you suggesting that it would have potent stimulant properties and a short duration like cocaine?
 
I'm afraid i'll have to cry wolf on this whole project. It was an idea that occured to me at work. However since I have had time to drag up related patents I have reached the conclusion that this idea does not hold its water.

However, from closer scrutinization of previous work it does appear that appropriately 2-substituted phenyl radicals do possess anti-depressant effects. Find the reference in the above aforementioned patent.

-Smyth
 
Too bad about that not working at as you suspected/hoped Smyth. I'll go check out the info you provided about the "appropriately 2-substituted phenyl radicals" and their A/D effects.
 
I don't think burenorphine has any effect on serotonin reuptake.
 
Nah dont even waste your time with it. Just stick to tramadol if I were you.
 
i love this forum....anyways, buprenorphine might be a safer choice for many people, people with opioid tolerances in particular...plus i dont think there is the risk of seizures at low doses, but i may be wrong. ive used tramadol for pain several times, never bupe, but im very interested in bupe being used as an A/D, i think it would work as good as tramadol, considering they both have lower abuse potentials than most opiates used for pain today. btw, i think its kool how so many people are interested in the use of opioid painkillers as antidepressants. id LOVE to see that happen in my lifetime, but not likely, heh...
 
What about it's kappa effects? Kappa opioid receptor antagonists are also known to be antidepressant in pre-clinical trials... and Bup has that effect... maybe that's why so many people report they like taking it... *shrug*
 
BilZ0r said:
What about it's kappa effects? Kappa opioid receptor antagonists are also known to be antidepressant in pre-clinical trials... and Bup has that effect... maybe that's why so many people report they like taking it... *shrug*

...like taking it for recreational purposes or for depression?
 
For quiting opiates.... people always whinge about taking methadone... but people seem to rave about bup.... even though bup isn't that much more effective.... *shrug* just an idea.
 
people always whine about taking methadone... but people seem to rave about bup.... even though bup isn't that much more effective.... *shrug*

I'm not even sure bupe is more effective. From reading on BL, it seems as though bupe works quite well but methadone still seems to be the "better" option for people with significantly large habits...almost like bupe is only good up to a certain point. But that's just my summary of what I've read here, no personal experience with either.
 
I have no experience with bupe, but plenty with methadone. In my opinion, i found methadone to have worse withdrawal symptoms than oxycodone and H...is bupe any better in that sense?
 
Quite some time ago i had a script for 90 50mg Ultram. They felt pretty good the first 4 days. Then quickly the euphoria diminished into nill.

I find it important to point out that tramadol can cause seizures in certain people. I've never had a seizure in my life until i took tramadol. It was a mild one, but a seizure non the less. I kept taking them until i ran out, cause they are addictive. Throughout the time i had them i would get violent tremors or occasional sharp twitches. My whole body would just jolt then come back to normal.
It also fucked with my reality. I was watching a show on life inside a maximum security prison, and i half way passed out, but then thought i was in the jail. I went completely delerious for a good 10 minutes. I had some very strange dreams during my use as well.

I abuse opiates heavily, and tramadol is the only drug that has done these things to me.
 
I'm not sure if this has been covered before. So please excuse me. This article made me think further of the possibilities of using opiates as A/D. But not just any opiate. The natural precusor that exists in your body.

"Several persistent researchers finally have proof for a theory they have held for more than a decade, despite dissent from the larger scientific community: Morphine occurs naturally in the human brain.

Most scientists have been skeptical of the claim, saying previously studied samples were likely contaminated with morphine molecules. But a paper published in the Sept. 21 issue of the Proceedings of the National Academy of Sciences seems to put the question to rest.
Meinhart Zenk and his colleagues at Martin-Luther-University Halle-Wittenberg in Germany found that human cells grown in a dish synthesized morphine.

"Without doubt, human cells can produce the alkaloid morphine," Zenk wrote in the paper. "The studies presented here serve as a platform for the exploration of the function of 'endogenous morphine' in the neurosciences and immunosciences."

In other studies, researchers had found trace amounts of morphine in human and other animal tissues, but only a handful of believers thought morphine occurred naturally in the brain. Most assumed it came from foods like hay, lettuce, milk and rabbit feed that contain the chemical.

If Zenk's paper finally convinces scientists that morphine is as natural a presence in the brain as serotonin or dopamine, it will open new doors for looking at the treatment of pain, addiction and other health issues, said George Stefano, director of the Neuroscience Research Institute at the State University of New York at Old Westbury.

Stefano also has a paper coming out in the Oct. 5 Neuroendocrinology Letters showing that animal neural tissue can synthesize morphine.

Instead of pumping patients full of morphine, Stefano said, doctors could instead give a morphine precursor -- a molecule that would set off a chain reaction eventually resulting in increased morphine production in the brain. Stefano, who has championed the existence of morphine in the brain for years, published proof of such a precursor, called reticuline, in the journal Molecular Brain Research in 2003.

The approach could circumvent dependency because it would increase an individual's own morphine levels instead of replacing natural morphine with a synthetic version. Similarly, a drug called levodopa, a precursor to dopamine, is commonly used to treat Parkinson's disease.

The discovery could also explain why some people are more susceptible to addiction -- they may have a morphine deficiency.

"All of a sudden," Stefano said, "(morphine-deficient individuals) take this compound (and) it really makes them feel not only good but normal."

A morphine deficiency could also be the cause of some chronic pain, Stefano said.

The researchers believe morphine is created by neurons in the brain, but much about the production remains mysterious. They found morphine in the limbic center, which is involved with emotions.

"That puts this new signaling molecule in a very crucial part of the brain," Stefano said. "If morphine's there, it's involved with subjective thinking."

Stefano hopes that the realization that morphine is endogenous (meaning it's produced within an organism) will lessen morphine's association with abuse, and increase the amount of research on naturally occurring morphine. With only about 15 scientists concentrating on endogenous morphine, progress is slow going.

"In science, painstaking trial and error are big part of your life," he said. "But it's much harder when most people don't believe you.""


Perhaps people that abuse opiates have a natural deficiancy of this particular precur. Perhaps, and this is a big PERHAPS, people that have this deficiancy are more likely to be depressed or have anxiety.
 
why would your body need to synthesize morphine? when it can just naturally increase the amount of dopamine in the synapse when needed, like when you are in pain. if seems like if the body was to actually synthesize morphine, it would be a long way of doing something, because morphine would cause increase of dopamine anyway. i dunno much tho, may be wrong.
 
Organisms make a huge bunch of chemicals... the question is whether any of them are of any use... They fact that when most people take opioid antagonists they don't really notice it, indicates that endogenous opioids have little importance in day to day activity. And yes, I know it causes dysphoria in some people, but so do opioids.
 
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