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Opioids The Ultimate Opiate Potentiation Thread

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^VERY good question. i have been wondering the same thing thorought this whole thread but couldnt quite figure out how to word it.

i REALLY hope some of the more serious contributors chime in on this.

thanks.
 
Fail Fighter said:
So can you see my predicament? I can potentiate the Oxy with DXM by decreasing NMDA activity. Or I can potentiate the Oxy with Tagamet by inhibiting the 2d6 enzyme and slowing the Oxy breakdown. But I can't take them both at once, because the DXM needs the 2d6 enzyme to convert to DXO


Decisions decisions...

I guess just try both and report back, make sure you have a day or so break between the two.
 
For what it's worth, I tried the DXM route. 60mg DXM Hbr an hour before the oxy. All it seemed to do was make me more "spacey" and drunk feeling. I didn't like it. I'll try the Tagamet next time.
 
^^^
I have a zero DXM tolerance. I took 120mg of DXM in combination with 100mg of cimetidine, a half hour before dosing hydrocodone. I felt stronger effects and longer duration or the medication. So I guess try doing more DXM and throw some cimetidine in the mix.
 
william1985 said:
^^^
I have a zero DXM tolerance. I took 120mg of DXM in combination with 100mg of cimetidine, a half hour before dosing hydrocodone. I felt stronger effects and longer duration or the medication. So I guess try doing more DXM and throw some cimetidine in the mix.


The Tagamet prevents the DXM from metabolizing into DXO, so you're counteracting your efforts. And actually, for hydrocodone, you should be using grapefruit juice instead of Tagamet anyway. Reasons:

1. Hydrocodone is metabolized into nor-hydrocodone via enzyme 3A4
2. Hydrocodone is metabolized into hydromorphone via enzyme 2D6
3. DXM is metabolized into DXO via enzyme 2D6

So the better choice is clearly inhibiting 2D6 which will lead to increased DXO and hydromorphone levels, while still slowing the breakdown of the hydrocodone. This is accomplished by taking grapefruit juice, not Tagamet.
 
^^^
So your stating that DXM isnt active on its own, without its metabolites? I dont like grapefruit juice, so im not doing that. Hydrocodone isnt the only opiate i use anyways. As far as the hydrocodone to hydromorphone conversion, hydrocodone is active without having to be converted. Even when the conversion occurs, the hydromorphone levels are so low.
 
william1985 said:
^^^
So your stating that DXM isnt active on its own, without its metabolites?

Not really. DXM is primarily a sigma agonist. Here is what wiki has to say about sigma receptors:

wiki said:
Physiologic effects (what happens to the human body) when the sigma receptor is activated include hypertonia (increased muscle tension), tachycardia (increase in heart rate), tachypnea (increase in rate of breathing), and mydriasis (increase in the size of the pupils, similar to what occurs in conditions of low light). Some sigma receptor agonists--such as cocaine, a weak sigma agonist--exert convulsant effects in animals. Behavioral reactions to sigma agonists are rather heterogeneous: some individuals find sigma receptor agonists euphoric with significant anti-depressive effects. Other individuals, however, experience dysphoria and often report feelings of malaise or anxiety.

So who knows about that. Doesn't sound at all beneficial to me. DXO, however, is a strong NMDA antagonist, which is what we want for euphoria potentiation.


william1985 said:
I dont like grapefruit juice, so im not doing that.

I can't stand it either, but it's a sacrifice I'm willing to make %)


william1985 said:
As far as the hydrocodone to hydromorphone conversion, hydrocodone is active without having to be converted.

It doesn't really matter. I'm just pointing out that you aren't inhibiting the correct hepatic enzyme!

william1985 said:
Even when the conversion occurs, the hydromorphone levels are so low.

...which is why it behooves you to inhibit the 3A4 enzyme as opposed to the 2D6 enzyme. Would you rather have MORE hydromorphone is you or LESS hydromorphone in you? With Tagamet, you're choosing LESS. With grapefruit juice, you're choosing MORE.
 
sp0r said:
I just want to warn you guys that drugs such as promethazine and compazine can be very dangerous. Make sure you check with your pharmacist to ensure you are not on any drugs that can react for those types of drugs have about 100 different ways to kill you.

For me to potentiate
1hr before: cimetidine
10 minute before: 50mg hydroxyzine and 25mg diphenhydramine (too much diphen will put you to sleep)
Then dose. You dont want too many drugs in your body you wont even know what you are high on. This method works best on oxycodone, hydrocodone, and heroin. The way codeine works is much different than other opiates and should probably be looked at in another thread.
Flexaril btw is a very strong anticholinergic, and really potentiates for me. Also, dont be active, lay down and watch tv, being active you wont feel much unless its heroin.

Bon apetit
sp0r
(bluelighter)
where do u get hydroxyzine from and cimetidine like what each used for i never heard of them in australia. Are they OTC
 
sp0r said:
Another amazing potentiator is dextromethorphan. (in small doses, high doses will make u trip). Take about 50mgs dxm 30minutes before you dose. Or if you feel like tripping off dxm, trust me when u are comming down off your trip, if you do an opiod such as heroin, you are in for a HUGE suprise. Trust me.

sp0r

Yeah DXM definately does something i nearly OD'ed a few times using it with opiates. Been hardly breathing and cold as no responsive. But thats that but be careful. It also meant to repair and fix opiate receptors or something. They use it in rehab. Wasn't DXM created for the reson of a better alternative to opiates and PCP or something to stop coughing.
 
Binge Artist said:
I don't really understand the science of opiod receptors, but I have this theory that I've been waiting to try out.

Say you take a bunch of Immodium and wait a couple hours. Then take your DOC. My guess is that the "anti-shits" receptors will be taken over by the immodium, and so the molecules from your DOC that would have normally gone to the "anti-shits" receptors will now be rerouted to the "fuck-you-up" receptors, thereby increasing your buzz.

really? i don't think it does anything i had large dose's. you have to have it with some emulsifier or something to get high.
 
^ He's not saying that his theory would make loperamide centrally active, he's saying that it could possibly lead to more of the other drug you take being active in the brain as opposed to the gut.

I don't know about this, it would depend on the affinities that loperamide and your opioid of choice have for the receptors.
 
Fail Fighter said:
Hopefully someone here can answer this. Which would be the better potentiator for Oxycodone: DXM or Tagamet/Cimetidine?

Fact 1: Oxycodone is metabolized by the 2d6 enzyme, so we want to inhibit that.
Fact 2: We want to decrease NMDA activity, and DXM is an NMDA antagonist.
Fact 3: DXM is only a WEAK NMDA antagonist; its metabolite (DXO) is a more potent NMDA antagonist.
Fact 4: DXM is metabolized by the 2d6 enzyme into DXO.


So can you see my predicament? I can potentiate the Oxy with DXM by decreasing NMDA activity. Or I can potentiate the Oxy with Tagamet by inhibiting the 2d6 enzyme and slowing the Oxy breakdown. But I can't take them both at once, because the DXM needs the 2d6 enzyme to convert to DXO


Decisions decisions...

I am somewhat confused about this because I thought that cyp3a4 inhibitors were also suppose to potentiate dxm. ????. So couldn't you use DXM to decrease the NMDA activity and use cimetidine or grapefruit juice to potentiate the opiate/oid and then DXM? Or am I not understanding this right?

Also, Bergamottin is the natural chemical in grapefruit juice that inhibits the cyp3a4 enzyme. Apparently It is also naturally occuring in Bergamot oil (Who would have thought by the names?). Bergamot oil is what they use as the flavoring agent in Earl Grey Tea. As to how much Bergamottin is present in Earl Grey, I am unsure but it seems, in theory, Earl Grey would work as well. Maybe I will try adding it to my pod tea next time.
 
sp0r said:
I just want to warn you guys that drugs such as promethazine and compazine can be very dangerous. Make sure you check with your pharmacist to ensure you are not on any drugs that can react for those types of drugs have about 100 different ways to kill you.

Interesting, what kinds of drugs can interact with promethazine that will kill you?

enoughorangejuice? said:
GFJ
temazepam (10-30mg)
diazepam (5-30mg)
diphenhydramine (10-15mg)

Just watch out if you are benzo naive, that could leave you as a stiff if you have a decent opiate dose.
 
As far as methadone goes, i know for a fact that Grapefruit juice greatly increases both peak values and half-life of the drug. I was even told this by my methadone clinic doctor. Cimetidine does the same for methadone.
Another note is using two kinds of opiates at the same time: bad idea. Eventhough they both are mu opioid receptor agonists, the small difference in chemical structure only allows one of them to activate the receptor, they cant both fit onto it, so you create a "competition" between the two and the one with a higher affinity or a greater amount will win and basically block and "waste" the other opiate you took. This is especially true when mixing tramadol with other opiates or methadone with other opiates.
Codeine, which is worthless in my book anyway, is a strange drug mecause it is metabolised to morphine, heroin also is quickly converted to morphine and so for these drugs that are ultimatley just changed to morphine in the body, might not have the same reaction to grapefruit juice and cimetidine. They both work great for benzos too. But remember, be very carefull, they can increace plasma levels by as much as 50% so you could eisily overdose playing with these two things. Also they inhibit the metabolism of common other high blood pressure and antidepressant drugs ans countless others. So if you're on other meds you could be manipulating thier levels too. Grapfruit juice is dangerous to toy with when it comes to drugs, you'd be surprised at how many drugs are metabolised by the enzyme that it inhibits. Many prescription bottles say "do not drink grapefruit juice while taking this medication".
On another note, In my opinion and experience, things like diphenhydramine (benadryl) and promethazine (phenergan), just ruin an opiates high. Instead of the crystal clear euphoric fuzz, its transformed into this shitty, groggy, detached, foggy headed feeling. For me, an opiate lover, I just want to increase the pure opiate feeling, not add other impure effects to it with things like the above mentioned or benzos or weed or alcohol. that's why I stick to GF juice and cimetidine (Tagamet). I hate it when a doctor in the E.R. comes in and says I'll get you a shot off demerol and phenergan to control its neusea, I make up the excuse that I'm allergic to phenergan just to get the pure demerol, it's so much better.
 
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animalman said:
Another note is using two kinds of opiates at the same time: bad idea. Eventhough they both are mu opioid receptor agonists, the small difference in chemical structure only allows one of them to activate the receptor, they cant both fit onto it, so you create a "competition" between the two and the one with a higher affinity or a greater amount will win and basically block and "waste" the other opiate you took. .
I dont think this is exactly true. If two or more agonists are taken at the same time, as long as the levels of one arent ridiculously higher than the other, your receptors should be able to handle both(all). Many doctors prescribe multiple opioid medications to be taken simultaneously by the patient, usually one long acting and one quick-acting for breakthrough pain. I as well as many people I know have greater success combining opiate/opioids, rather than just taking a single medication, whether for pain or for pleasure.
 
^ It should be remembered that a drug does not lock into a receptor and stay there for a long time. To put it into non-scientific terms, drugs float around, hit a receptor, leave, float around more, hit another receptor, etc (by hit I mean agonize). The difference being a partial agonist like suboxone, which spends more time in the receptor, hence the "blocking" effect. Thats essentially the only time you have to worry about receptor affinity. If you're talking about taking two comparable mu agonists at once, say hydrocodone and oxycodone, neither blocks the other out, they both float around agonizing receptors and working concurrently.
 
^ Very good point. Well put. Plasma levels can vary due to many different factors;ie diet, hydration, other drugs taken, etc.
 
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I had some promethazine (50mg) and fresh grapefruit juice (4 whole in a juicer). Tasted fine but about 20mins later it made me projectile vomit, feel really sick and get a headache. As soon as it all came up I felt much better so I doubt it was a coincidence.

This ever happened to anyone else ?
 
^ Nope not for me.

One thing I keep forgetting to mention in this thread is cigarettes. I can't say that they make the experience stronger or last longer but I have noticed that they always seem to kick in opiates for me. I guess this could just be coincidental but almost every time I take an opiate the first familiar signs begin to manifest when I smoke a cig.
I'll have to check around on the web and see if I can't find any factual information.
 
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