Opioids Tramadol rectal

[WaywardSon70]

I am on Tramadol for legit pain, I have built up a tolerance to my dose and wanted to take it rectal administration due to having read this bypasses the liver and makes it potentially more effective. My question would be if someone did this would they have to lower the dose to avoid too much onset first time?

 

[Skorpio]

I am on Tramadol for legit pain, I have built up a tolerance to my dose and wanted to take it rectal administration due to having read this bypasses the liver and makes it potentially more effective. My question would be if someone did this would they have to lower the dose to avoid too much onset first time?

As a fan of boofing, I am going to reccomend not doing that with Tramadol.

It is a prodrug for O-desmethyl tramadol, which is a much stronger opioid agonist. This conversion is actuated by the liver enzyme CYP2D6 (just like codeine demethylation to morphine is).

Therefore, you actually want first pass metabolism to occur for the greatest effects.

 

[Deleted member 593549]

not worth it imo.

Rectal administration of tramadol has bioavailability of approximately 77%, which is slightly higher than the 68–75% observed with oral administration.

and this is with an optimal rectal administration (bowels fully cleared out)

 

[HealingEnergy14]

One thing that always worked to potentiate my Tramadol was to stagger the dosage. So instead of taking, for example, 200mg at once, you take 50mg every half hour for 2 hours.

Easily made me twice as high. Although once you really build up a tolerance to Tramadol (or any drug...) getting the original feeling you are looking for back is very hard.

 

[WaywardSon70]

As a fan of boofing, I am going to reccomend not doing that with Tramadol.

It is a prodrug for O-desmethyl tramadol, which is a much stronger opioid agonist. This conversion is actuated by the liver enzyme CYP2D6 (just like codeine demethylation to morphine is).

Therefore, you actually want first pass metabolism to occur for the greatest effects.

Is there any validity to b vitamins helping ? I read an article in the Oxford Journal but was interested in someone with first hand knowledge.

 

[Chaurus]

As a fan of boofing, I am going to reccomend not doing that with Tramadol.

It is a prodrug for O-desmethyl tramadol, which is a much stronger opioid agonist. This conversion is actuated by the liver enzyme CYP2D6 (just like codeine demethylation to morphine is).

Therefore, you actually want first pass metabolism to occur for the greatest effects.

Would boofing O-DSMT work better than oral?

 

[Skorpio]

Is there any validity to b vitamins helping ? I read an article in the Oxford Journal but was interested in someone with first hand knowledge.

I’ve never heard of this. The only enzyme inducers for cyp2d6 that aren’t harsh drugs like rifampin are things like glutethimide (and some barbiturates to a minor extent).

Would boofing O-DSMT work better than oral?

I believe so, but don’t have any evidence beyond the fact that any hepatic metabolism of O-DSMT will render it inactive, so there is an incentive to avoid first-pass metabolism.

 

[Chaurus]

One thing that always worked to potentiate my Tramadol was to stagger the dosage. So instead of taking, for example, 200mg at once, you take 50mg every half hour for 2 hours.

Easily made me twice as high. Although once you really build up a tolerance to Tramadol (or any drug...) getting the original feeling you are looking for back is very hard.

Interesting! Any thoughts on why this happens?

I believe so, but don’t have any evidence beyond the fact that any hepatic metabolism of O-DSMT will render it inactive, so there is an incentive to avoid first-pass metabolism.

That settles it! My last two O-DSMT pills are going up my ass! (Not necessarily whole).

 

[HealingEnergy14]

Interesting! Any thoughts on why this happens?

Once read that after the first dose of tramadol is in your system, your liver will metabolize further ingested tramadol more readily to O-desmethyltramadol; thus increasing the opioid effects.

 

[Skorpio]

Interesting! Any thoughts on why this happens?

First pass metabolism in this step can be viewed as a rate limiting step towards making the active metabolite (just as gabapentin uptake is a rate limited step). Staggering doses will overwhelm the pathway less and you will get more ODSMT and less of other metabolites that you don’t want (because drug metabolism almost never relies on a single enzyme; once one pathway saturates, the metabolism is shunted to another pathway).