• Neuroscience & Pharmacology Discussion Welcome Guest
    Posting Rules Bluelight Rules
    Recent Journal Articles Chemistry Mega-Thread
    FREE Chemistry Databases! Self-Education Guide

  • N&PD Moderators: Skorpio

Tramadol used as anti-depressant: Neurotoxic?

K

Kudos

Bluelighter
Joined
May 3, 2007
Messages
172
Is there any consensus on the neurotoxicity of Tramadol when used long-term as an anti-depressant? It seems extremely effective, but the serotonin-releasing mechanism and opiod-agonism makes me nervous.
 
It doesnt release serotonin, its a reuptake inhibitor of serotonin and norepinephrine - same as SNRI anti-depressants - and the opioid agonism is not going to cause neurotoxicity either. The only concern of long term use would be dependence

And be careful with tramadol, it lowers the seizure threshold
 
It's my understanding that there's some controversy over whether tramadol accords mild 5ht release or simply acts as a reuptake inhibitor, but insofar as it does act as a releaser, this release is limited in amount (so there isn't mdma-like transporter reversal). While tramadol has not likely been tested extensively for neurotoxicity, there's no reason to believe it would be.

ebola
 
the only problem with tramadol is that seizures occurred in individuals using below the supposed 400mg dose threshold. however, many people use way beyond that limit and never have a seizure. just to be safe, find another route.
 
But aren't there long term brain "changes", if not damage per se, that results from extended opioid agonism?
 
Well, there is damage to synaptic plasticity because opioids mess with reward so strongly.
 
I doubt tramadol in neurotoxic (in reasonable doses) given how long its been on the market and the FDA's reluctance to approve anything that hasn't been exhaustively tested with regards to toxicology. Given it's structural and mechanistic similarity to venlafaxine (Effexor), chronic use would likely result in downregulation of postsynaptic 5-HT/NE/mu-opioid receptor/system downregulation etc... Anecdotal evidence clearly demonstrates that long-term use results in physical dependence via alterations in (primarily) these three NT systems.

As withdrawal from effexor ((SNRI)) alone is purportedly hellacious, combining that with opioid w/d (albeit mild) would not be fun. In terms of neurotox, I doubt there's anything to worry about....after all it is not a very potent 5-HT reuptake inhibitor/releasing agent, which would be of the most concern for neurotox in this case.
 
alkap555 said:
I doubt tramadol in neurotoxic (in reasonable doses) given how long its been on the market and the FDA's reluctance to approve anything that hasn't been exhaustively tested with regards to toxicology. Given it's structural and mechanistic similarity to venlafaxine (Effexor), chronic use would likely result in downregulation of postsynaptic 5-HT/NE/mu-opioid receptor/system downregulation etc... Anecdotal evidence clearly demonstrates that long-term use results in physical dependence via alterations in (primarily) these three NT systems.

As withdrawal from effexor ((SNRI)) alone is purportedly hellacious, combining that with opioid w/d (albeit mild) would not be fun. In terms of neurotox, I doubt there's anything to worry about....after all it is not a very potent 5-HT reuptake inhibitor/releasing agent, which would be of the most concern for neurotox in this case.
Click to expand...

its not that similar to effexor
 
You must log in or register to reply here.
Top