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Super SUPRAtherapeutic doses of racemic Tramadol: Implications?

negrogesic

negrogesic

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For the past few months, when domestic poppy pods were (are) no long available consistently, I have been taking 2.5-3 grams of tramadol, yes 3,000mg of this pro-convulsant crap. Obviously, I have concerns.....

I have had no muscle spasticity, not even a tingle of a petit mal onset. To complicate the matter, I am on 40mg of diazepam which I am trying to taper-off, but there seems to be an inherent battle between the diazepam withdrawal and the tramadol dependence (I hate the stuff, relieves opioid withdrawal), since tramadol reduces the efficacy of the diazepam via some apparent GABA-A antagonist like properties.

When ive gotten ahold of high quality pods, they are able to fully substitute for the opioid withdrawal, and the SNRI withdrawal is moderate but bearable.

However, I am worried about continued use of these molto supra-therapeutic doses, not in regards to seizure, but in the unknown effects of such constistent huge dose, and the complex and rather sketchy non-MOR mediated pharmacology. I am quite aware of the dangerous of hypertensive crises, and avoid anything pro-serotonergic (I take mirtazapine, but it has virtually no affinity for the SERT).

To complicate things further i started take carisopridol to aid in sleep, and found that while it didnt potentiate the tramadol, I feel it has opioidergic properties on its own (I confirmed this when doing some reading, and discovered carisopridol and meprobamate could both be inhibited by naloxone).

The question, any clue as to which drug to switch to in order to get off this shit? Methadone is a headache to get prescribed (I cant do the daily or even bi-daily thing, I am very busy, super-high functioning, at in regards to making money). I am not a fan of buprenorphine, even having taken the DATA waiver through an online 8 hour course hosted by the APA website. It is my opinion that methadone is easier to get off of than buprenorphine, and is far more effective with fewer side-effects.

Also, would cimetidine or other inhibitors of CYP2D6 promote the demethylation of racemic tramadol?


I really enjoyed the o-desmethyltramadol that briefly available, where as tramadol feels very, very different. It would be a bitch to try to use racemic tramadol to try to make M1, or make some substitution to increase potency.
 
I bet that the diazepam is keeping you from having seizures from the tramadol. As such it would be extremely foolish to discontinue the diazepam (an effective and safe anticonvulsant, however addictive it may be) before discontinuing the tramadol!

Consider tapering with tramadol itself. It has a unique mechanism of action and I assume that tram withdrawal is rather different from typical opioid withdrawal.

Ketamine, 4-MeO-PCP, Methoxietamine, or DXM could be helpful in alleviating tramadol withdrawal, though I recommend avoiding the 3-MeO-PCP and 3-MeO-PCE as they seem to cause manic episodes. Also don't take any of the aforementioned while you're still on tramadol; there could be as-yet-unknown, potentially fatal interactions.
 
I have much experience with tramadol dependence and withdrawals, but never at the doses you've taken. However, I can say that, at least in my experience, DXM was definitely a no-no for withdrawals. I only took it at a first plateau dose, but it made me sweaty and extremely floaty, while negating none of the dysphoria or muscle cramps (at the best, it made me fatigued enough for a very short nap). The one thing that definitely makes things a lot better are benzos, and as much as you can handle.

Tapering is easy to do with tramadol, if you have the small pills that break easily into two 25mg portions. The larger, circular pills are a total bitch to break in half, and going down 50mg at a time is too steep for some individuals. Tapering down 25mg a week is pretty easy on the body. 50mg is stretching it. I'm sure this could be rectified if you had some kind of pill cutting device.

Cutting yourself off cold turkey, or tapering too steeply, at that level, could be a bad idea. Tramadol withdrawals cold turkey at normal doses is bearable, if somewhat excruciating, but at that level, the intestinal effects could be extreme. People with much smaller habits cold turkey have gotten serious peptic ulcers that required hospitalization. Tramadol seems to have pretty ridiculous effects on the gastrointestinal system (i.e. constipation), moreso than other opiates, so it's no wonder that the GI disturbances during withdrawal would be exaggerated.
 
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I am not so sure. I have taken 1000mg+ of tramadol at one time when I was on no benzo. The most ive taken was around 2 grams at a time.

Oh, and I went through 5 grams of 0-desmethyltramadol over a few days (intravenous). The high is very good, very sedating, but it didnt have warmth of heroin or some semi-synthetic. It felt very clean, kind of like IV fentanyl, but better. Unfortunately is not easily to find it anymore, and I am not going to synthesize any drug. Closest thing would a biosynth, or something that didnt involve taking out the organic chemistry glassware. Obviously I could extract the racemic product, but from there I dont know, maybe their is some enzyme I can use to prompt o-desmethylation, which would probably be time consuming and yield little.

Once again, I am not worried about seizure risk here, im worried about the unknown effect off such dosages
 
It would be interesting to figure what relative equivalency to other SNRIs (read: venlafaxine)...as far as 2000mg a day goes, that's a lot...personally I think you should be worried about the seizure risk...
 
You know, I`m going to go out on a limb and say the seizure risk might be somewhat exaggerated, especially with regards to dependent users. If you are on a continuous large dose, your brain might have simply adapted to the effects of the tramadol. I could be way off base, but I`ve seen anecdotal reports all over the web about people on habitual doses of around a gram seemingly without issue. Is it possible that the seizure risk is related to people dosing beyond their tolerance level?
 
How about a very slow tapering of everything you are on, starting with the tramadol, then the carisoprol and then the diazepam - but preferably starting to taper diazepam somewhat simultaneously...

Please anyone correct me if I'm wrong, this should probably be consulted with a physician or at least someone who is more experienced than I am (although I am familiar with the pharms).
 
The brain zaps are going to destroy you. You are going to be very uncomfortable. Effexor normally takes 3 months of a fast taper to stop withdrawals (from around 200mg) or 6 months of a gradual taper (the faster is more likely to cause withdrawal symptoms). However switching off of Tramadol to Prozac (fluoxetine) will allow you to start the opiate withdrawal first then deal with the relatively low risk of withdrawals from Prozac later. Prozac has a long half life and your brain will adjust to the lack of it better.
 
It's worth noting that carisoprodol is pro-convulsant. It's odd, surprising, and true.
 
Hammilton said:
It's worth noting that carisoprodol is pro-convulsant. It's odd, surprising, and true.
Click to expand...

What`s the reasoning behind this, out of curiosity? I would think in any case that its GABA agonist properties would override any pro-convulsant activity (excuse my profound pharmacological ignorance).
 
GABA agonist -> Muscimol (Amanita muscaria)
GABA(a) positive allosteric modulator -> Benzodiapines and Carbamates, etc...

But I don't know about the specifics of Carisoprodol being pro-convulsant.
 
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