Opioids Using Naltrexone to sleep after Tramadol

[YoPanda]

So I'm one of the "lucky" few who gets an immense amount of pleasure from tramadol (more than oxycodone or morphine strangely!) and so on the weekend I like to pop a pill or two with some weed as my drugs of choice (been doing this for years). However tramadol really messes with my sleep. Usually I'll take a benzo to knock me out but that messes with my memory which I need as I'm in grad school right now. I had the idea of popping a naltrexone at the end of the night to kick out the tramadol from my system so I can sleep. Does this seem like a good strategy or am I overlooking something? As I am usually dosing between 50mg-150mg once a week I figured I shouldn't go into an uncomfortable withdrawal experience. I'd love your thoughts!

 

[Skorpio]

That doesn’t seem like a good idea. You may likely experience precipitated withdrawals, which are not in themselves conducive to sleep. Second the naltrexone would not abrogate the SNRI effects of the tramadol, which might be a significant contributor to sleeplessness.

I’ve always been sensitive enough to antihistamines for sleep that those are my go to options (if I can get away with it I take one or two pills of certirazine as it is one of the most selective H1 blockers, but it’s not super potent as a hypnotic).

 

[WellTram]

Don't use tramadol every day and stay under 300 mg. Use low dose for light lift and relief and higher doses for serious lift and relief on the level of morphine spiked with some kind of stimulant.

This substance is potent for many of us and i taking now after 15 years, still. Just not 2000mg daily but 150mg three times per day.

M1 binds very effectively to opioid receptors with enough affinity to produce real, dose-dependent / tolerance dependent opioid effects. Than there is stimulant part - too strong in heavy doses ( need of anticonvulsants )

 

[Helpmeescapethis]

You won’t get PWD from taking the naltrexone, since you’re not physically dependent on opioids. But it will do NOTHING for the sleep factor, either.

Tramadol is barely an opioid, it’s got more SNRI activity than opioid action. Only like 30% of the dose gets metabolized into O-desmethyltramadol, and that’s the part responsible for opioid effects.

The SNRI activity is what keeps you up, and what makes Tramadol so enjoyable for you.

 

[WellTram]

You won’t get PWD from taking the naltrexone, since you’re not physically dependent on opioids. But it will do NOTHING for the sleep factor, either.

Tramadol is barely an opioid, it’s got more SNRI activity than opioid action. Only like 30% of the dose gets metabolized into O-desmethyltramadol, and that’s the part responsible for opioid effects.

The SNRI activity is what keeps you up, and what makes Tramadol so enjoyable for you.

O-DSMT binds to mu-opioid receptors VERY strongly, 3 times more strongly than buprenorphine for example. In dose of 300mg it Is serious and 9hour lasting opioid. ( If u are good cyp2d6 metabolizer than 1000mg tramadol with anticonvulsants Is HEAVY )

 

[Helpmeescapethis]

O-DSMT binds to mu-opioid receptors VERY strongly, 3 times more strongly than buprenorphine for example. In dose of 300mg it Is serious and 9hour lasting opioid. ( If u are good cyp2d6 metabolizer than 1000mg tramadol with anticonvulsants Is HEAVY )

This is patently untrue. It seems you misunderstand the measurements for binding affinity. The *lower* the value is, the HIGHER the binding affinity is.

O-DSMT: 3.4 Ki nM
Buprenorphine: 0.22 - 1.5 Ki nM, with most research showing 0.22 Ki nM

Binding affinity is also essentially totally irrelevant to efficacy as a painkiller, how much euphoria it gives, how much respiratory depression it causes, how much tolerance increases, etc..

Binding affinities are just one of very many characteristics that drugs possess.

Everything I said in my previous post is still true. I’m well experienced with O-DSMT as a compound itself, and I wouldn’t call Tramadol or O-DSMT a “serious opioid” at all. The only seriousness comes from the seizure risk of Tramadol.

 

[WellTram]

This is patently untrue. It seems you misunderstand the measurements for binding affinity. The *lower* the value is, the HIGHER the binding affinity is.

O-DSMT: 3.4 Ki nM
Buprenorphine: 0.22 - 1.5 Ki nM, with most research showing 0.22 Ki nM

Binding affinity is also essentially totally irrelevant to efficacy as a painkiller, how much euphoria it gives, how much respiratory depression it causes, how much tolerance increases, etc..

Binding affinities are just one of very many characteristics that drugs possess.

Everything I said in my previous post is still true. I’m well experienced with O-DSMT as a compound itself, and I wouldn’t call Tramadol or O-DSMT a “serious opioid” at all. The only seriousness comes from the seizure risk of Tramadol.

I wasn't speaking about binding affinity. I was speaking about how efficiently it binds to the receptors.

 

[Helpmeescapethis]

I wasn't speaking about binding affinity. I was speaking about how efficiently it binds to the receptors.

Hmm… You said “binds 3x more strongly than buprenorphine” which is exactly what a misunderstanding of the values for their respective binding affinities would lead someone to say.

Not to mention that your own specific verbiage applies to speaking of binding affinity.

Drug-receptor binding efficiency is
determined by affinity (how strongly/tightly a drug binds) and intrinsic efficacy (how effectively it activates the receptor). This is *the* definition of the idea of “binding efficiency”.

Perhaps you meant “intrinsic efficacy”. But even if you did mean to speak PURELY of intrinsic efficacy, buprenorphine is still superior in that metric as well.

 

[Syntherize]

Hmm… You said “binds 3x more strongly than buprenorphine” which is exactly what a misunderstanding of the values for their respective binding affinities would lead someone to say.

Not to mention that your own specific verbiage applies to speaking of binding affinity.

Drug-receptor binding efficiency is
determined by affinity (how strongly/tightly a drug binds) and intrinsic efficacy (how effectively it activates the receptor). This is *the* definition of the idea of “binding efficiency”.

Perhaps you meant “intrinsic efficacy”. But even if you did mean to speak PURELY of intrinsic efficacy, buprenorphine is still superior in that metric as well.

Thanks for dishing out the facts, but this person clearly doesn’t know what they’re talking about, and the fact that they think Tramadol is a “heavy” opioid says it all. They’re gonna have fun waking up on the floor after a seizure without knowing what has happened to them…smfh