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Doxylamine and Cytochrome P450 2D6 Activity

Jktm

Bluelighter
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May 19, 2012
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I recently found out that Diphenhydramine is an inhibitor of the liver enzyme CYP2D6, and, being that I'm prescribed tramadol, which, as most of you probably know, is activated by this enzyme through demethylation, am now in search of a different sleep aid (hell, I was already having to take 200+mg of the shit anyway). I've used Doxylamine in the past (with mixed results) when I felt the need to take a break from the DPH because of increasing required doses. My question is, does doxylamine have similar effects on this enzyme? I realize ADD isn't the place to ask individualized questions, but, seeing as about 25% of drugs are affected in some way by this enzyme, felt this thread merited some post value.
 
First, stop taking diphenhydramine - it is know to be toxic, long -term use can fuck up your enzyme levels, and there is no way antihistamines can make you sleep better, yeah it can knock you down faster, but quality of sleep is dimiinished. The doses you are taking are huge. Tramadol by itself is good at making falling asleep easier. There are many different drugs that can be used as sleeping aids - Trazodone is good, Melatonin is good, Z-drugs are good in short-term.
Second doxylamie is not good for you body, it is known that it can produce rhabdomyolosis, and i suggest if you have huge tolerance to DPH you will need the same or bigger amount of doxylamine.

off-topic:
i'm usign tramadol IM daily for a two month, doses from 100 to 200 mg, sometimes i just swalloow pills, but sometimes I have only vials, today I tried addding 20 mg chloropheniramine and made 100mg tramadol/20mg CPH IV injection. The next hour I felt dizzzy, stupid, but not sleepy, so to say, antihistamines do not potentiate tramadol in a good way.
 
I can normally get away with 100mg of doxylamine. And my quality of sleep is already in the shitter. I've tried melatonin in combination with valerian root and passion flower-didn't do fuck-all. Used to use trazadone a couple years ago, but had to take doses of 200mg to achieve sleep, and I can't take it now, as tricyclic antidepressants are contraindicated for use with tramadol (added seizure risk). I've tried zolpidem, up to 60mg before, and it doesn't help at all (I have a pretty stout benzo tolerance though). And I've been taking 400mg of tramadol daily for the past 16 months and really, in truth, have made the really risky choice in the past of taking 500mg of it in one dose and it doesn't provide me with adequate pain relief, so it's not gonna help me sleep lol. To be perfectly honest I need some triazolam or temazepam for sleep, but my doc won't prescribe me anything for sleep because I'm prescribed phentermine (and my sleep-habits are unchanged since starting it) for weight-loss (the zolpidem I tried wasn't mine). I've never had (S)-zopiclone but don't see it being more effective than zolpidem.

And as far as using anti-histamines with opioids, they've never really done anything for me other than help the itch a little bit lol (however, I've never had hydroxyzine, so that maybe a different story lol).
 
there is no way antihistamines can make you sleep better, yeah it can knock you down faster, but quality of sleep is dimiinished.

cyproheptadine is actually good for sleep architecture.


Also, antihistamines are great for short-term use in lower doses. And where on earth does evidence suggest they are toxic?
 
I guess no one knows or cares to answer my question? lmao
 
Doxylamine
succinate caused marked induction of CYP2B enzymes, as demonstrated by a
large increase in the O-dealkylation of 7-pentoxyresorufin (up to 38-fold) and in the
16β-hydroxylation of testosterone (up to 6.9-fold). In addition, treatment resulted in a
modest induction of CYP3A and CYP2A and a 50% increase in thyroxine glucuronosyltransferase
activity. No induction of CYP1A, CYP2E or CYP4A was found.

So the answer seems to be, no doxyalime doesn't inhibit CYP2D.
 
yea but in the amounts he takes of Diphenhydramine the effect should be quiet strong
 
TY for the answers...should I worry about the induction of the other enzymes seeing as how more tramadol would go through those and make more inactive metabolites? Or is it only processed through CYP3A4 and 2D6?
 
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