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Opioids Help with codeine?

doubleheadedeagle

doubleheadedeagle

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May 17, 2015
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In my long lasting journey to find something to get the best out of codeine, in my mind came across an idea...

What if we take meds that use cyp3a4 metabolites right before taking codeine so the enzymes are busy and may metabolize less morphine into inactive compounds?

I have available Pantoprazole and Simvastatin and their main metabolites are CYP3A4?

And what about grapefruit juice, Is it any good?

And about the ceiling dose of codeine I am currently taking 450mg and am afraid of taking more because it may get wasted, what is the case about this as I search I come across many contradictions.
 
GFJ is trash when it comes opiate potentiation. In my experience, it kills the high. I've read numerous reports regarding the issue with the same results as mine. It's mostly people with little opiate experience and little tolerances are the ones claiming it helps with anything.

I don't know about those other meds, but I think Simvastin(lol) will be useless.

The only true potentiator, in my experience, is 800mg of Cimetidine taken an hour after your opiate. A lot of people will tell you to take 800mg an hour before and an hour after, but in my experience taking it before provides no increase in effect.
 
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doubleheadedeagle said:
I am having trouble finding true anti-histamines like cimetidine and promethazine so I am trying to find something different
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Cimetedine is OTC in US. Usually can be found in Walmart or Walgreens.

Promethazine, btw, also kills the high for me the same way GFJ does.
 
I live in south east europe, to be exact in Kosovo, here codeine phosphate tablets are OTC but it would be ironic for cimetedine not to be so. I have to look it up. EDIT: I have ranitidine available it works the same as cimetedine, doesn't it?

By the way what is the thing about the ceiling dose? is it true or a myth?
 
Is promethazine not OTC in your country? As far as I'm aware it's only a prescription drug in the US. In the UK it's OTC, I assumed the same would be true in most of Europe.
 
doubleheadedeagle said:
I live in south east europe, to be exact in Kosovo, here codeine phosphate tablets are OTC but it would be ironic for cimetedine not to be so. I have to look it up. EDIT: I have ranitidine available it works the same as cimetedine, doesn't it?

By the way what is the thing about the ceiling dose? is it true or a myth?
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Ranitidine, unfortunately, does nothing.

I never had much experience with Codeine, kind of went with Hydrocodone in the beginning of my opiate addiction. According to what I read here, there is a ceiling effect.
 
I have no idea, I must ask my pharmacist. But btw what is the mechanism of action of promethazine is it H1 antihistamine antagonist? D1ahp suggested a H2 antihistamine antagonist?
 
From Wikipedia:

Promethazine, a phenothiazine derivative, is structurally different from the neuroleptic phenothiazines, with similar but different effects.[1] It acts primarily as a strong antagonist of the H1 receptor (antihistamine) and a moderate mACh receptor antagonist (anticholinergic),[1] and also has weak to moderate affinity for the 5-HT2A,[10] 5-HT2C,[10] D2,[11][12] and α1-adrenergic receptors,[13] where it acts as an antagonist at all sites, as well.
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Promethazine is also unique in that it actually metabolises more of your codeine into morphine. You want to take it about an hour before the codeine so you get this effect. It definitely makes a difference in my experience. Without promethazine I can barely feel codeine, but with it I am nicely chilled out.
 
15mg if you just want the codeine to be stronger, 25mg if you want a lot of sedation.

No idea about cimetidine.
 
"Codeine is metabolized to codeine-6-glucuronide (C6G) by uridine diphosphate glucuronosyl transferase UGT2B7, and, since only about 5% of codeine is metabolized by cytochrome P450CYP2D6, the current evidence is that C6G is the primary active compound."

Promethazine inhibits CYP2D6, which has little to no effect on the codeine saturation via blood levels. It only introduces sedation.
 
doubleheadedeagle said:
Btw should I take it before or after codeine? sorry for the separate questions but you understand our brains don't process things as fast lol
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About an hour before.

d1ahp said:
"Codeine is metabolized to codeine-6-glucuronide (C6G) by uridine diphosphate glucuronosyl transferase UGT2B7, and, since only about 5% of codeine is metabolized by cytochrome P450CYP2D6, the current evidence is that C6G is the primary active compound."

Promethazine inhibits CYP2D6, which has little to no effect on the codeine saturation via blood levels. It only introduces sedation.
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While all sedating antihistamines will potentiate the effects of codeine, enzyme induction leading to greater hepatic conversion of codeine to morphine is the reason for both the clinical and recreational use of promethazine with codeine.

https://en.wikipedia.org/wiki/Codeine
 
Wilson Wilson said:
About an hour before.



While all sedating antihistamines will potentiate the effects of codeine, enzyme induction leading to greater hepatic conversion of codeine to morphine is the reason for both the clinical and recreational use of promethazine with codeine.

https://en.wikipedia.org/wiki/Codeine
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Actually, judging by that page. There's evidence both ways.

One thing is that C6G plays a way bigger role than was thought for decades.

I don't have irrefutable proof that what I'm saying is universal truth.

There's a study with people who lack the CYP2D6(conversion to morphine) enzyme and those who don't claiming that there's no difference in action. Which would make Promethazine mostly useless. However, there are also things that state Promethazine's effectiveness in that article as well.

I do have a high tolerance and Promethazine always ruins the high while Cimetidine works for anything from Codeine to Hydrocodone to Oxycodone to Methadone.
 
I guess that I should see which one of them is more easily available, if both I shall try them and see which one increases the high, as judging from your statements it seems that it is subjective as which has more potential to increase the conversion of codeine to morphine.
 
doubleheadedeagle said:
I guess that I should see which one of them is more easily available, if both I shall try them and see which one increases the high, as judging from your statements it seems that it is subjective as which has more potential to increase the conversion of codeine to morphine.
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You should be able to find it online. It's still available in the US, but doctors rarely prescribe it because of its many interactions with other drugs.
 
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