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  • BDD Moderators: Keif’ Richards | negrogesic

Why won't opiates work on me?

A

alt 14

Bluelighter
Joined
Jul 20, 2008
Messages
585
Alright well here's what's up with me atm. Let's keep in mind I have NO tolerance (other than natural apparently, but we'll get to that) and do opes less than once a month on avg. Probably more like every 2 or 3 months. I took 55mg of hydrocodone along with a glass of grapefruit after preloading with 400mg cimetidine and maybe 16oz of grapefruit juice 50mins prior in an attempt to potentiate it. Around 5:00 I took 15mg more because I did it a few days earlier with the same potentiation and could tell from what I was feeling I was going to need more. 6:00 comes around and I feel it, but it's extremely mild, so I do a final 15 putting me at a total at 85migs. Now it's 6:30 and I already took 5.5g APAP, plus dosing higher at this point would be a waste anyway. What the fuck is up?

I know hydrocodone is a weak opiate, but I've have the same kinds of things happen to me with other shit like oxy and poppy pods. 45mg of oxy is kind like "ehhhh I guess I can kinda feel it..." Actually of the probably 15 times I've tried opiates in my life I've only nodded once, and don't get me wrong, it was great, but it took 12-15 poppy pods, a total of close to quart of gfj, and 20mg hydrocodone. I know that dose probably sounds reckless for someone who has no built-up tolerance, but I got to those levels after topping up every hour or so for a total of maybe 4 and a half hours of dosing. Thank god pods last so long... I can't seem to get the same high everyone falls in love with.

My question here is - why? Do I have some enzyme deficiency? Is it something in my brain? I have a very high pain threshold if that will somehow explain this phenomenon. Any other BLers experience what I'm talking about? I've yet to try IV heroin (heroin in general actually), but I plan on it in the future. Tbh my hopes aren't very high at this point, but hopefully I'll be wrong. There's really no point in my continuing to use these drugs at this point because of their cost and almost non-existent effect on me.



P.S. I can't comment on their analgesic effects rly either. I got my wisdom teeth removed last friday and was sent home with a script of 30x 10/650 lorcets, and saved them up. I took one the morning I got home for the fuck of it, but didn't really need them for the actual pain. Thanks!
 
Sounds like you just have a high natural tolerance , it takes a lot to get me where I want to be as well.

You really should perform a Cold water extraction on those Hydrocodones if you plan on taking so many. All that APAP is gonna take it's toll on your liver.

I honestly would be careful , having an opiate addiction seriously sucks ass

Your talking about slamming heroin and that's a serious step and a turning point for most drug users

Stay safe my friend <3
 
Stop using grapefruit juice. Despite the idiotic folk "wisdom" loitering about in the drug community that purports that the bergamottin in grapefruit juice potentiates the high, the reverse is actually true. While bergamottin is indeed a CYP3A4 inhibitor - inhibition of which is, I concede, desirable when taking a codinone - it is also a CYP2D6 inhibitor. CYP2D6 is the liver enzyme responsible for the invivo conversion of hydrocodone into hydromorphone (as well as the conversion of any codinone into its corresponding morphinone), which, of all the metabolites of hydrocodone, is the most active at the mu-opioid receptor and thus the most euphoric.

I don't suspect this grapefruit juice bullshit will ever come to an end. People are frustrating in that, once they have accepted an idea, it's very difficult to induce them to relinquish it. Whatever.

If I had hydrocodone and I wanted to get high off of it, I'd do an APAP extraction of some kind, load the hydrocodone-laden liquid into a syringe, and inject it rectally taking into consideration that this route of administration will probably give rise to a higher bioavailability, thus necessitating a lower dose.

If you can find a selective CYP2D6 inducer, great, but they typically also increase CYP3A4. Try some rifampicin.


EDIT: Have you been abusing cocaine, amphetamine, methamphetamine, MDMA, methylphenidate, or dexmethylphenidate or any other such stimulant?
 
Umm not very recently, but maybe 5 days ago I did indulge myself in a gram mephedrone binge. I have this problem all the time though. I'll look into the grape fruit juice thing. Thanks for pointing that out (assuming what you're saying is true). I have taken relatively high doses of pods/oxy/hydro in the past without the tagamet and grapefruit juice and the same thing happened to me - er rather, nothing has happened I guess, lol.

About the APAP, yeah I know, shame shame. To be honest I didn't plan on needing 8.5 pills to catch a buzz. I did 5.2 grams the day before last too which kinda has me worried now. I just didn't want to waste the initial 5.5pills by not taking more and decided the risk for liver damage was worth it. Odds are I'll be fine, yes? I have also taken 400mg of ibuprophen and 2x 220mg naproxen sodium pills this morning and at noon, respectively. I completely forgot I did those... Do I need to rush myself to the ER or will I *probably* be fine? I'm a young, fit male and I know the body is quite resilient. I actually just remembered I took the NSAIDs a few minutes ago... Someone confirm that I will probably be fine so I can use the power of suggestion to enhance my body's healing power.


P.S. Yeah I'm stupid/forgetful. I know. Like I said, I was planning on taking 50-50mg tops. Are there any at-home remedies for mild APAP ODs?
P.P.S. Obviously I'll be taking a break from booze/APAP/drugs that are rough on the liver for a while in case I did do a bit of damage to my liver...
 
STOP taking antihistamines and grapefruit juice, k? You have enzymes like CYP2D6 which o-demethylate about 10% hydrocodone to hydromorphone (which is about 6 times more powerful than morphine). The main idea with grapefruit juice and tagamet and cimetedine is to INHIBIT these enzymes. In this case, that screws up everything. Here, check here: http://en.wikipedia.org/wiki/Cyp2d6. Normally inhibiting enzymes which metabolize a drug is a good thing, but in this case some of the metabolites are ten fold more powerful.

It might be similar to codeine, which some people don't get anything from- some people are just lacking those enzymes perhaps. I find one thing to make opiates hit very fast and pleasant is to crush up the pills (if there's a lot of pills do a water extraction) and mix them into coffee, with milk so it's not too hot and a lot of sweetener because opiates are quite bitter. This works really well for me- a couple sips into I'll already start feeling fantastic.
 
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I attached a PDF file that some ur you may find interesting.

Hutchinson et al., 2004 M.R. Hutchinson, A. Menelaou, D.J. Foster, J.K. Coller and A.A. Somogyi, CYP2D6 and CYP3A4 involvement in the primary oxidative metabolism of hydrocodone by human liver microsomes, Br J Clin Pharmacol 57 (2004), pp. 287–297. Full Text via CrossRef | View Record in Scopus | Cited By in Scopus (29)

Kaplan et al., 1997 H.L. Kaplan, U.E. Busto, G.J. Baylon, S.W. Cheung, S.V. Otton and G. Somer, Inhibition of cytochrome P450 2D6 metabolism of hydrocodone to hydromorphone does not importantly affect abuse liability, J Pharmacol Exp Ther 281 (1997), pp. 103–108. View Record in Scopus | Cited By in Scopus (23)

Lelas et al., 1999 S. Lelas, S. Wegert, S.V. Otton, E.M. Sellers and C.P. France, Inhibitors of cytochrome P450 differentially modify discriminative-stimulus and antinociceptive effects of hydrocodone and hydromorphone in rhesus monkeys, Drug Alcohol Depend 54 (1999), pp. 239–249. Article | PDF (204 K) | View Record in Scopus | Cited By in Scopus (11)

Poulsen et al., 1996 L. Poulsen, K. Brosen, L. Arendt-Nielsen, L.F. Gram, K. Elbaek and S.H. Sindrup, Codeine and morphine in extensive and poor metabolisers of sparteine: pharmacokinetics, analgesic effects and side effects, Eur J Clin Pharmacol 51 (1996), pp. 289–295. Full Text via CrossRef | View Record in Scopus | Cited By in Scopus (118)

Tomkins et al., 1997 D.M. Tomkins, S.V. Otton, N. Joharchi, N.Y. Li, R.F. Balster and R.F. Tyndale et al., Effect of cytochrome P450 2D1 inhibition on hydrocodone metabolism and its behavioral consequences in rats, J Pharmacol Exp Ther 280 (1997), pp. 1374–1382. View Record in Scopus | Cited By in Scopus (20)
 

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That is interesting... nice read. Doctors should have just given her meperidine or something.

No it's true, while codeine, hydrocodone, and oxycodone are very weak agonists in their own right, a lot of their action is from the ten or more times more powerful demethylated metabolites...

Luckily I have pretty good response to both codeine and hydrocodone... But perhaps these opiates are actually not perfect since their effect varies very much by genetic variability.
 
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chloral hydrate said:
That is interesting... nice read. Doctors should have just given her meperidine or something.

No it's true, while codeine, hydrocodone, and oxycodone are very weak agonists in their own right, a lot of their action is from the ten or more times more powerful demethylated metabolites...

Luckily I have pretty good response to both codeine and hydrocodone... But perhaps these opiates are actually not perfect since their effect varies very much by genetic variability.
Click to expand...

Bull-fucking shit. Most of these metabolites are not in any amounts to be active. Only one that truly needs to be metobolized to have effect here is codeine. People snort oxycontin all the time and get wrecked. Snorting a substance by-passes first pass metabolism so oxycodone does not produce active metobolite's.
 
How about some proof

Dankycodone said:
Bull-fucking shit. Most of these metabolites are not in any amounts to be active. Only one that truly needs to be metobolized to have effect here is codeine. People snort oxycontin all the time and get wrecked. Snorting a substance by-passes first pass metabolism so oxycodone does not produce active metobolite's.
Click to expand...

speculation, would be happy to post more articles if you can give a more researched reply.

BTW insufflation does not bypass first pass

sources jerk-off

give some (not Wikipedia)
 
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Hydrocodone NEVER did anything for me after the first time I took it , and that first time just made me want more.

Maybe that was a warning of how dependent I would be on Opies. That was 5 years ago...

For me , the first time I took a specific opiate it was the best,a glowing experience, and then I would try to repeat the dose and would get greatly diminished effects. This was with every Opiate except morphine and heroin.

Maybe it's a warning. I would stop now. But you probally won't.

-lenses
 
a bit misleading, but thank you for the education

Bob Loblaw said:
Yes it does...
It gets absorbed into the bloodstream via the mucous membranes in the nose, thus avoiding passage into the liver before getting absorbed.
Click to expand...

So much of it just goes down one's throat. I admit I should have looked into that before stating so; but in reality we are probably both half right (of course there are many variables involved so the ratio is different for ever one). For example I can snort mostly pure shit and unless it is P-dope most just ends up down my throat. IMO IV is the only worth while way to bypass first pass, but I strongly suggest not getting into that.
 
Dankycodone, you are an idiot. Snorting oxycodone does avoid first-pass but it still gets to the liver from the bloodstream and metabolized anyways. And only a little gets absorbed via the nose anyways like bell ringer said, a lot of it ends up in the stomach anyways.

Think about it. Hydrocodone is considered to be about 6 times more potent than codeine, just like it's metabolite hydromorphone is considered to be 6 times more potent than codeine's metabolite morphine. Read the literature, those codeinones are very very weak agonists in their own right.
 
Maybe they work but the effects are subtle, and on they note maybe they are not for you? there are plenty other drugs that make you feel good, for that matter working out with weights makes me feel good, I think endorphins are a rec drug in my opinion LOL
 
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