• N&PD Moderators: Skorpio | thegreenhand

Venlafaxine (Effexor) similar in structure to Tramadol

Yeah fits like a glove - which explains why effexor and escitalopram are both serotonin reuptake inhibitors. Not sure why tramadol isn't - i suspect it might be, i'll have a hunt around on medline or something.

I dont get the last bit though - why is this an example of drawbacks of SAR?
 
Just because two compounds fit the same "binding pocket" doesn't mean they're both active there.
 
Yeah ofcourse, i have no idea why i wrote that. Anyway, its been a pleasure conversing with you sekio and i'll be sure to watch out for more of your posts.
 
effexors opiate receptor affinity is little to none, and the withdrawals from effexor aren't like opiate withdrawals, i know from experience. it's also very similar in structure to PCP! it actually can cause a false positive on a drug test for PCP.
 
That's interesting about the PCP connection - tramadol is an NMDA receptor antagonist too, albeit a light one, not sure about effexor.
As for the opiate activity of venlafixine, i've never taken it and so have no subjective data to lean me either way and the literature seems to say it doesn't. What's interesting is that tramadol doesnt really either. Its the major metabolite o-desmethyl tramadol that is responsible for nearly all its opiate activity. Now venlafaxine is also mostly converted to o-desmethyl venlafaxine (70 % of its effects come from the metabolite). Whether or not o-desmethyl venlafaxine has opiate activity or not is probably the best thing to focus on in terms of the opiate question.
 
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It doesn't.

desvenlafaxine (1 µM or greater) possessed no significant affinity for dopamine D2, muscarinic, α1-adrenergic, histamine H1, mu-opioid, 5-HT2 or 5-HT1
 
This is an amazing thread... holy cow. I clicked in because Effexor is one of the drugs I have to memorize for Pharm Tech training. Then I got my pill book and read about Venlafaxine. I found out that Cymbalta, my drug, is in this family. My book says that unlike other antidepressants, these work by inhibiting the ability of nerve endings in the brain to absorb serotonin, norepinephrine and to a lesser extent, dopamine. The book also says they shouldn't be combined with certain other drugs, tramadol being one, because of the risk of serotonin syndrome. I did not know that. I have taken trammies with my Cymbalta. I learned something very valuable from your discussion and my reading. (The Pill Book 15th edition) I won't do that anymore. Harm Reduction rewards for each of you.

The book states that Tramadol is a synthetic compound and explains what it does but says "the exact way in which this drug works is unknown."

WTF? I did not think a drug like that would be released to the public...
I'm fascinated by your discussions and I hope I don't seem like a hopeless n00b, but the science behind all the meds in my house, and all the meds I'm memorizing for the state exam, that is brand new information.

I'm tremendously impressed with the advanced drug forum. The more I read, the more I want to read. Keep on discussing.

sekio: you're a fukkn boss.
 
Tramadol's mode of action is far from "unknown". It functions through a combination of mu-opioid agonism, serotonin-norepinephrine reuptake inhibition, and NMDA antagonism.

Three pain killing properties in one make for a good drug.
 
sekio... why am I being taught something that isn't true, from a book. It's not like I'm reading wiki. Why would they say they don't know it works if they do? What is the point of that?

I wish you were my teacher. Your aren't full of shit.
 
Well, to be fair, The Pill Book is a "consumer's guide", so for all they care they could put that tramadol kills pain by feeding magical unicorns tiny molecular tacos to make them happier. If you can manage to wade through the big words and sometimes confusing conclusions fo medical papers, it's probably worthwhile consulting PubMed for information on drugs and their effects, (or even Wikipedia!) before a paper book.

Even sticking to those refrences made for medical students and doctors is better than "consumer's guides". The more authors, the better.

Some people seem to have an issue with wikipedia being publically editable, but almost every one of the drug/chemical info pages has at least a few reliable, on-line sources that you can verify the facts with. And since it's publically editible, there's a squadron of individuals who read PubMed/medical journal articles seemingly for fun and come up with all the content for the wierd and wacky effects of pharmaceuticals almost immediately, rather than watiting on one man and his editorial squad.
 
There is some serotonin reuptake inhibition with tramadol. As others have eloquently pointed out, Effexor is no opioid...
 
Well, to be fair, The Pill Book is a "consumer's guide", so for all they care they could put that tramadol kills pain by feeding magical unicorns tiny molecular tacos to make them happier. If you can manage to wade through the big words and sometimes confusing conclusions fo medical papers, it's probably worthwhile consulting PubMed for information on drugs and their effects, (or even Wikipedia!) before a paper book.
Me lol'ing my ass off aside he's right, they more focus on ends rather than mechanisms.

And since it's publically editible, there's a squadron of individuals who read PubMed/medical journal articles seemingly for fun and come up with all the content for the wierd and wacky effects of pharmaceuticals almost immediately, rather than watiting on one man and his editorial squad.
Don't judge me :p
 
Well, to be fair, The Pill Book is a "consumer's guide", so for all they care they could put that tramadol kills pain by feeding magical unicorns tiny molecular tacos to make them happier. If you can manage to wade through the big words and sometimes confusing conclusions fo medical papers, it's probably worthwhile consulting PubMed for information on drugs and their effects, (or even Wikipedia!) before a paper book.

OMG you are a comedian too? I laughed like I'd lost my mind when I read this.


Me lol'ing my ass off aside he's right, they more focus on ends rather than mechanisms.

Right, Ep? sekio is gonna need a fukkn fan club at this rate!
 
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