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ask K5: codeine phosphate

By zombie HollyHopDrive in zombie HollyHopDrive's Diary
Mon Dec 12, 2005 at 12:58:00 AM EST
Tags: User Diary (all tags)
User Diary

hoping there are some arm-chair chemists who can answer a few questions about codeine for me.


I rarely take pain-killers containing codeine. Literally only a couple of times in the past 10 years I've taken Panadeine forte

I found it to be extremely effective as a pain-killer, but with strong side affects. Both times when I took it, I was quite sedated within 30 minutes - to the point that walking around was out of the question (in danger of falling over) let along driving a car.

I just figured I was more susceptible to the side effects and avoided it as a pain killer.

I've got a bad cold at the moment with quite a sore throat, so this morning I thought I'd give my old friend codeine phosphate a try in the form of some cold-and-flu tablets. The dosage of codeine was much less than panadeine forte, so I assumed I wouldn't really notice it...I took two tablets, for a total of:

pseudoephedrine HCI 60mg
paracetamol 1000mg
codeine phosphate 12mg

Note that the amount of codeine phosphate was only about 20% of what I'd previously taken for toothache, and was not as strong, yet there was a marked affect - I felt quite sleepy and disconnected with reality, sort of like dreaming while awake. It was difficult to stay awake. Like previously, I must confess it was an extremely pleasant effect.

So I wasn't surprised when googling it to find that euphoria and drowsiness are common side effects. What I can't seem to find though is:
- how common is it to experience such strong side effects from low doses?
- Why aren't there more warnings of the side effects? The tablets with codeine were the "Day" tablets, so it's like the assumption is they won't have these effects on the average person
- Anyone else have these experiences? If so, were you tempted to take codeine more often just for the euphoric effect?

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ask K5: codeine phosphate | 26 comments (26 topical, editorial, 0 hidden)
You're a lightweight... (none / 1) (#1)
by bighappyface on Mon Dec 12, 2005 at 01:00:07 AM EST

...most people need like 300-400mg codeine to get high, if codeine even really gets them high anymore.

I guess that's a good thing for you. I'm also surprised the pseudoephedrine didn't cancel it out.

But whatever.

yeah, codeine will get you high (none / 0) (#3)
by Blarney on Mon Dec 12, 2005 at 01:10:05 AM EST

It's a great painkiller, in my experience. But it will get you high. Don't drive. And yeah, it can build dependency. I've found myself craving more on a couple occasions. Never, though, have I bothered to go get more, even though I used to live a mere 30 minute's drive from the Canadian border where such delightful pills may be purchased OTC. So I'd say it's habit forming, far more so than pot, even a bit worse than alcohol, but nowhere near as bad as cigarettes. Could be different for you, though.

Important Note (none / 1) (#16)
by brain in a jar on Mon Dec 12, 2005 at 05:36:14 AM EST

Pretty much all over the counter medication containing codeine also contains paracetamol/acetaminophen.

This means that altough at low doses it is a safe and effective painkiller, exceeding the stated dose by a significant amount is likely to lead to acute liver failure and death due to the paracetamol/acetaminophen.

In fact overdoses (accidental or deliberate) of medication containing paracetamol/acetaminophen are the most common cause of acute liver failure in the US.

So, by all means use this effective painkiller, (though possibly not while driving or operating machinery due to the opiate nature of codeine), but don't even think about doing it for fun, overdoses kill.


Life is too important, to be taken entirely seriously.

Codeine :) (none / 1) (#17)
by Have A Nice Day on Mon Dec 12, 2005 at 09:21:35 AM EST

Where to begin....

12mg is a little low but 16 gives me a nice drowsy buzz. Luckily 16 is in a recommended dose of most OTC codeine meds here in the UK. As people say below, most copdeine medication also has either paracetamol (acetominophen) or aspirin in it to try to stop people using it recreationally - take too much and it will poison you.

HOOWEVER - there are various ways around this. The least effort is to find a chemist who will sell you codeine linctus. Basically a cough syrup type product with only one active ingredient. You can also get "Benilyn with Codeine" cough syrup which contains a kicker of diphenhydramine hydrochloride - an anticholinergic that can induce psychedelic responses in high doses.

The other way is to do a cold water extraction on the tablets. I've done this myself a few times but if you're making a high dose you have to really trust the technique and your own skills as otherwise you may ingest way too much of something bad.

At this point I would like to point out a little list of perils associated with recreational codeine use:
  • Drinking too much Benilyn with codeine will give you the raging shits
  • Getting a cold water extraction wrong could cost your life or at least do some serious liver damage.
  • In contrast to the first point - repeated use of codeine will make you constipated
  • Repeated use of codeine will make you addicted - it's an opiate, it's metabolised to something similar to morphine by the time it hits your brain.
  • Repeated use of codeine (and codeine containing medications) can have other odd effects. A friend of mine who had a serious habit ended up with skin so sensitive that if you touched her you would leave hand marks.

if you stick to occasional use and 12mg does it for you then there's no real harm, but be careful.

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Have A Nice Day has left the building.
The psuedoephedrine (none / 0) (#18)
by daani on Mon Dec 12, 2005 at 09:28:07 AM EST

is keeping you awake. So your body and parts of your mind are very very drowsy, but you don't feel it because of the psuedoephedrine. I'm guessing a bit of course. A pharmacist once told me that drug addicts like to take psuedoephedrine because it helps them stay awake and enjoy the high (I asked why you need to give your name to purchase it once).

I felt pretty darn good taking cold & flu tablets last year (I think 20 mg codeine per 2-tablet dosage). By the end of the 3 or 4 days that had worn off a bit though.

As others have said, the dangerous part of these pills is the paracetamol. I've been told a paracetamol overdose is a fucking horrible thing to do to yourself. Any wasters out there, the golden rule is that if it's illegal it's almost certainly better for you. :)

Also on a couple of your questions (none / 0) (#19)
by Have A Nice Day on Mon Dec 12, 2005 at 09:34:22 AM EST

A little nbausea on a high dose is common, codeine irritates the stomach, maybe you are just very sensitive to codeine.

If it had that strong an effect on you may I ask if you had been drinking grapefruit juice? There is something in grapefruit juice that knocks out one of the enzymes in your liver that metabolises the codeine into inactive metabolites, leaving more to be metabolised by the other enzyme (it is thought there are two that work on codeine) which metabolises it to a morphine-like substance.



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Have A Nice Day has left the building.
Codeine (3.00 / 2) (#21)
by Sgt York on Mon Dec 12, 2005 at 10:59:47 AM EST

Codeine is metabolized away in the body by two processes: glucoronidation and O-demethylation. The latter is the one we are concerned with; Codeine is just an O-demethylation away from being morphine. In the body, the amount of the codeine you ingest that is converted into morphine depends on the ratio of the speed of these two pathways. The pathways compete for the codeine, making you produce more of the active (O-demethylation) or inactive (glucoronidation) forms.

O-demethylation is carried out by the enzyme CYP2D6. There are several dozen genetic variants of CYP2D6, and the activity of the enzyme varies widely among the variants. Most of the work has been done looking at the -3 and -4 family of variants; these are inactive enzymes. If you have one copy of one of these alleles, most of the codeine undergoes glucorinudation (the "other pathway"), leaving little or no morphine production. If you have two copies, you get no morphine. It is nearly impossible to get a person with CYP2D6-3 or -4 addicted to codeine; codeine alone simply isn't strong enough. It has to be converted to morphine.

Anywhere from 20-60% of the population has one of these inactive forms, depending on your ethnicity (whites=20%, asians=60%, IIRC). However, there are also hyperactive forms. Which variant it is escapes me, but IIRC it's present in less than 10% of the US population as a whole.

If you have one of these forms, the majority of the codeine you ingest is converted to morphine, and that's why you can't walk. You're a lightweight. Sorry, it's just your genes.

There is a reason for everything. Sometimes, that reason just sucks.

ask K5: codeine phosphate | 26 comments (26 topical, 0 editorial, 0 hidden)
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