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Metabolizing & Bioavailability of Tramadol {Urgent}

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Unlucky

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Apr 26, 2007
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Metabolizing & Bioavailability of Tramadol

(I am currently having a bad reaction hence the {urgent} title, but im choosing to ride this one out)
Currently I am experiencing bad reactions to 60mg of tramadol like overheating (38.1c), muscle spasm and twitching in mainly in chest and upper jaw, feeling tight and constricted in my throat, shallow breathing feel like im not getting enough oxygen, confusion and itchy all over so I would apreciate any quick responses or tell me if these effect are within safe limits.

This is my second thread on this topic, unfortunately the last one I made during another adverse reaction bout 2 weeks ago it was moved to the "other drugs" section shortly after I posted it and all the responses I got in there were off topic and totally irrelevant to my post. This topic is extremely important for me and it is very important that I get answers for the sake of my well being.

I use Tramadol for a chronic detereorating joint condition. To make matters complex I have a neurological disorder and an extreme chemical sensitivity. I am one of the very few, if any people in the world who suffers from a thermoregulatory dysfunction where I constantly overheat. My body reacts in unpredictable ways. I have had adverse reaction to morphine and oxycodone so I can not use them for my pain.

I can barely tolerate the Tramadol and have very unpredictable reactions to it. I can not take anymore than one 50mg tramadol a day anymore than 1 have resulted in trips to the E.R.
I have looked for alternatives but most were not avaliable in Australia or too expensive or too risky for me to try, so I would prefer to better understand tramadol.

For me Tramadol takes up to 5 hours to metobilise or feel any effects, any additional dose i take after the 5 hours ends up doubling and increasing the bioavaliabilty onto the first dose and causing adverse reaction. I have found that if I devide a 50mg capsule into 4 parts of 12.5mg and take it at 1 - 2 hour intervals my body ends up feeling more wired and intense then if I had just taken the one 50mg in 1 go.

It seems that I have a reaction to the actual process involved in metobolizing tramadol to an active form. So as long as my body is busy processing it dosent matter how small of a dose I take I end up having intense reactions as I am experiencing currently. My temperature at the moment is 38.1 and I'm overheating more so than usual and this is just from one 60mg devided into 5 parts and taken at 1 hour intervals.

I dont understand how can this be, can anyone explain or verify this for me please if the act of metobolising at a continuos rate from administered small doses cause an overload and if the function involved in metobolizing effect a person in odd ways other than just the tramdol itself and if the the dose I took today is still being influenced by yesterdays dose from 15 hours ago as my metobolism of tramdol seems to be ver slow yet intense. Thanks.
 
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60mg is fine.

Just allow it to play itself out. Drink plenty of water if feeling hot flushes and dry mouth.

The first time i EVER had tramadol, it was a 100mg XR, and I also had an adverse reaction.

It took several weeks of low doses before my brain worked out what it is about and I felt safe to increase my dosage. Then even after a period of abstinence, it seems like my mind has retained the information about how to 'deal' with this drug. It should be speedy onset, opioid fuzzyness, but then some hot flashes at night because of the serotonergic affinity. What it felt like when I first starting taking it is NOTHING like what it feels like after you develop a tolerance.
 
Thanks for the tip. Despite how unwell I feel the the only reason I havent gone to the ER is because its only 60mg. I keep telling myself that its only 60 mg and nothings serious can happen but my reaction is intense, especially the constant feeling of like im not getting enough air, inside it feels weird sorta and numb and tight and my hearts pretty slow but its ocassionally keeps fluttering. Also u seaid it should be speedy onset but with me it takes up to 5 hours to feel anything. I think its me im not reacting to it as healthy people do.
 
I also just found this article now , its about the CYP2D6 ENZYME that is responsible in how people metobolize and react to tramadol apparently Patients with different CYP2D6 genotypes may respond differently to tramadol in terms of pain relief and adverse events. I already have defects in certain genes due to my rare neurological condition. Seeng this article made a lot of sense to me why it takes me so long to metobolize and why I react so differently to it, perhaps my CYP2D6 enzyme is also effected. I have also been using tramadol for about 2 months now and each time my reaction is different depending on the state of my body. Instead of gaining tolerance somedays I have a adverse and odd reaction to smaller doses than usual.

http://www.ingentaconnect.com/content/adis/mdt/2007/00000011/00000003/art00006

http://mb.rxlist.com/rxboard/ultram.pl?noframes;read=2684
 
Would concomitantly taking an antipyretic (anti-fever) drug like simple aspirin help any?
 
Just keep taking 25mg per day for a good two weeks, then double the dose every 2 weeks until you hit the 400mg mark, then taper back to baseline again.
 
You can find the answers to everything you've asked about by searching here. Questions like these don't really even belong at BL- we're not doctors, and those of us who are sure as hell can't tell you what to do online. I'm pretty sure that if you look through the BLUA or somewhere in the rules you'll see where it says that "emergency" threads don't belong on here.

This is something you should see a doctor about. And stop taking tramadol. If you're this sensitive to it, you shouldn't take it. You had an adverse reaction that caused you to make an "urgent" thread in OD two weeks ago? Why the hell are you still taking it?

For me Tramadol takes up to 5 hours to metobilise or feel any effects, any additional dose i take after the 5 hours ends up doubling and increasing the bioavaliabilty onto the first dose and causing adverse reaction.
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Tramadol *is* the active form. The o-desmethyl provides opiodergic activity, but tramadol is an active drug that provides pain relief (and considering how long it takes to build up an effective dose of the metabolite, probably the majority of the pain relief).

Just keep taking 25mg per day for a good two weeks, then double the dose every 2 weeks until you hit the 400mg mark, then taper back to baseline again.
Click to expand...

That's not good advice at all. He's been taking it for a while, right? At least two weeks. He's sensitive to opioids (morphine and oxycodone). He's not taking it to get high (at least that's the impression I got), so increasing to 400mg is neither warranted nor advisable.

No competent doctor would ever advise him to continue taking the drug (at all) that has caused such adverse effects.
 
Wow, congenital hyperthermia...that is fucking scary. Be sure to never take an amphetamine or any type of serotonergic drug. Since tramadol has some serotonergic action (the (+)-enantiomer inhibits SERT at around 1 uM), I would think that it would be a bad drug for pain considering your other medical conditions. I would talk to your doctor about switching to a different type of opioid pain medication altogether: if you are allergic to morphine/morphinians and tramadol, then perhaps low-dose methadone would work better for chronic pain?
 
Methadone is actually a really good idea in this situation. I think hypersensitivity to it is pretty rare.
 
The problem is that tramadol, including enantiomers and metabolites, has four (significant) pharmacologically active forms, so saying that carbamazepine "accelerates clearance" is ambiguous. Clearance of what?

The reuptake blocking effect is in one enantiomer, while the opioid effect is in the other. The reuptake blocking effect is so weak that it's really stretching things to say that it contributes to the analgesia. Even strong reuptake blockers (e.g., protriptyline) are pretty much bullshit for pain.

I'd be nice if it wasn't supplied as the racemate. Of course, then it would be controlled. It'd be nicer still if they just sold O-desmethyltramadol. I wonder if you can get it from some chemical supply house?
 
Bondmaker said:
Would concomitantly taking an antipyretic (anti-fever) drug like simple aspirin help any?
Click to expand...

That was one of the first thing my specialists tried for my temperature problems me but it didnt help, impressive to see your thinking along those same lines.
 
Ham-milton said:
You had an adverse reaction that caused you to make an "urgent" thread in OD two weeks ago? Why the hell are you still taking it?
Click to expand...

My pain is quite severe and when i havent been given any other options to deal with it I end up taking the risks with Tramadol. But i will make another trip to my Doctor to see if he can send me to someone who know other alternatives because I have already shown my Doctor a list of alternatives I found on these forums such as....

-piperidine derivateves
-benzomorphons
-darvocet
-gabba derivateves
-Phenazocine
-Pentazocine
-Dihydrocodeine
-Dextropropoxyphene -digesic
-Fentanyl

But they were either unavaliable here or too expensive or too risky like the fentanyl patches that need to build up in your system first.


Ham-milton said:
He's not taking it to get high (at least that's the impression I got),
Click to expand...

Thats exactly right, since developing the neurological disorder and chemical sensitivity I lost my right to get high off any substance.
 
Riemann Zeta said:
Wow, congenital hyperthermia...that is fucking scary. Be sure to never take an amphetamine.
Click to expand...

I wish I had listened to that before I developed chronic hyperthermia and a neurological condition following an overdose.
 
Ham-milton said:
No competent doctor would ever advise him to continue taking the drug (at all) that has caused such adverse effects.
Click to expand...

When he made that "urgent!" thread a few weeks back, I gave him the only answer that makes sense:

SWITCH FUCKING MEDICATIONS!
 
^^^ Thats not as easy as it sounds. If you had read through my threads you would have seen that I actually tried switching medication, I have asked 4 different pharmacists to find out what other painrelif is avaliable after my Dr was unable prescribe anything else as he is also unsure on what to do about this. Most of the ones yous have mentioned on the forums here are not avaliable and I dont know what else to fucking take!!!

Through the 8 years I had this neurological condition I have switched so many Dr's looking for someone who can understand me. I have tried and discarded many and finally I have found a Dr who is able to show some acceptance and undesratnding but the only thing is he feels as helpless as I do and just like all my specialists he also tells me Im a difficult case to manage due to my sensitivities and Im tired of switching Dr's and the stupid pain managment clinic has a fucking 1 year waiting list so for now theres not much I can do!!!
 
Messing around with a serotonergic drug that obviously messes with your ability to regulate your body temp is a really fucking bad idea, though.

Keep taking tramadol and you're gonna put yourself into an early grave. Stick to NSAIDs, they shouldn't kill you.
 
Well detropropoxyphene is a complete waste of time as an analgesic (codeine is more effective as an analgesic) & pentazocine is unpleasant enough to put a fair few people off continuing to use it (the confusion factor with pentazocine makes salvia seem clear-headed in comparison!); actually that holds true for most of the benzonorphans to some degree (even with phenzocine and metazocine which are the best of the bunch).

If it's (the pain) neuropathic in origin then most conventional opioid anagesics will be pretty useless (I;;ve had a range for phantom limb pain & even Diconal was ineffective); best opioid for neuropathic pain is methadone as it has some NMDA antagonist activity.

For my pain, I've found either cannabis or ketamine the best controlling options, cannabis being the best if you need to remain functional (if you use ket to control it, forgwet being able to do anything other than sit and drool! =D)
 
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