is the ceiling dose of codeine for codeine or codeine phosphate

[Anon54]

I just found this from another BL thread while helping another person answer a qestions about one of the codeine salts

I just found this, the equivalence between 4 Codeine salts:

From the stronger to the weaker:
-20mg Codeine Hydrochloride = 17,1mg Codeine
-20mg Codeine Phosphate Hemihydrate = 15,6mg Codeine
-20mg Codeine Phosphate = 14,7mg Codeine
-20mg Codeine Camsilate = 11,9mg Codeine

(I found that on a very reliable site)

So does this mean u have to drink u would hve to drink 600mg of codeine phosphate to acheive the ceiling codeine 450mg dose.

Im pretty sure the ceiling dose is for codeine phosphate. but just checking

sorry should have put this thread in BDD

 

[Seith]

I just found this from another BL thread while helping another person answer a qestions about one of the codeine salts




So does this mean u have to drink u would hve to drink 600mg of codeine phosphate to acheive the ceiling codeine 450mg dose.

Im pretty sure the ceiling dose is for codeine phosphate. but just checking

sorry should have put this thread in BDD

450mg wouldn't do anything for me, 800mg would be mild and 1.6g is what I need now. codeine phosphate is what I use.

Can you explain why this is if the ceiling dose is only 450mg (Or 600mg if you are correct)?

Also any first time readers reading this do not take any of these amounts on your first try.

 

[debaser]

No, the ceiling dose is for codeine base.

 

[Mr Blonde]

Interesting question! I'm not sure about that one actually, and a quick search to try and find information just turns up a lot of forums talking about how they think the ceiling dose is a myth and there aren't any good sources discussing it. All I've managed to find really is sources talking about saturation of CYP2D6 with other substances, for example paroxetine, and how that influences it's kinetics.

I imagine that it quite possibly could be listed as the ceiling dose for a particular salt, as codeine freebase you don't see much in medicine.

Also that conversion chart seems a little off... Why would codeine phosphate hemihydrate be worth more freebase codeine then codeine phosphate? Given that the former has extra 'filling' in there in the form of water of crystallization.

ETA:

450mg wouldn't do anything for me, 800mg would be mild and 1.6g is what I need now. codeine phosphate is what I use.

Can you explain why this is if the ceiling dose is only 450mg (Or 600mg if you are correct)?

Also any first time readers reading this do not take any of these amounts on your first try.

Because not everyone has the same ceiling dose; as we know, there are those who can barely metabolize codeine into morphine at all and then those like you and I who can metabolize it extensively. My tolerance is sitting at 2.2 grams of codeine phosphate, give or take.

450-600mg seems to be the average from what I have read.

 

[misk]

so for those that can't metabolize it as well, is it a case of needing more to feel the effects, or is the ceiling dose much lower and thats that?

 

[Seith]

Because not everyone has the same ceiling dose; as we know, there are those who can barely metabolize codeine into morphine at all and then those like you and I who can metabolize it extensively. My tolerance is sitting at 2.2 grams of codeine phosphate, give or take.

450-600mg seems to be the average from what I have read.

Which is why I always ask them about the ceiling dose. Someone probably theorised it which just seemed to spread all over now. I would like them to show me where they are getting their information from.

A month back my mind was in a rough place and I tried to OD on codeine (was suicidal) and also slash my wrists if I didn't think it would work, I took 3.2g worth minus what was lost in a quick extraction and that was a really intense feeling, first time I have felt itchy, was sweating which I've never done on codeine and was really out of it. I forgot about the razors I had and after a while everything felt too good to go through with it.

There is certainly a difference between ~2g to ~3g for me.

so for those that can't metabolize it as well, is it a case of needing more to feel the effects, or is the ceiling dose much lower and thats that?

I've also wondered this, when I first started I used 300mg and it wasn't much. I was taking 600mg+ within the first few weeks (using only once or twice a week). No opiate tolerance.

 

[misk]

yeah im the same, first time i did it, 150mg reminded me of when i had morphine last in a hospital several years earlier in the way that i felt a slight sedation, euphoria but also a strange stimulant feeling also, but was very faint and very short. after that, i've never felt the euphoria or sedation (any of the good codeine traits) from anything upto 500mg i think might have been the highest i've done and never more than once or twice a month with several months break between in alot of cases.

i've never looking into attempting such a higher dose (1g+) because i had heard about the ceiling dose and also didn't want to test if my reaction to the histamine effect increased with a dose of say 1g lol.

even after reading about it, i can never figure out how the low metabolism of codeine effects the 'ceiling dose'

 

[titstypedthis]

most intense effects ive ever got from codiene and the only time i've spewed from opies was like 300mg phosphate CWE and about 10 nurofen+ 12.5's.


felt like i dunno bout 90-100 odd mg of morphine orally.. which was a nod dose of morphine for me.

 

[Jabberwocky]

Which is why I always ask them about the ceiling dose. Someone probably theorised it which just seemed to spread all over now. I would like them to show me where they are getting their information from.

A month back my mind was in a rough place and I tried to OD on codeine (was suicidal) and also slash my wrists if I didn't think it would work, I took 3.2g worth minus what was lost in a quick extraction and that was a really intense feeling, first time I have felt itchy, was sweating which I've never done on codeine and was really out of it. I forgot about the razors I had and after a while everything felt too good to go through with it.

There is certainly a difference between ~2g to ~3g for me.



I've also wondered this, when I first started I used 300mg and it wasn't much. I was taking 600mg+ within the first few weeks (using only once or twice a week). No opiate tolerance.

look after yourself, brother. there's plenty of your ausdd brethren to talk to at times of distress. i hate to hear another of us feeling like this.

pm me anytime you like, dude i'll be an ear to listen and give any advice i can

stay safe

 

[Anon54]

Seith. u honestly dose 1.6g of codeine phosphate?
really? & its stronger than 400mg?
I was convinced fom many sources than the max dose the codeine could be converted to morphine is around 450mg.

Ive fairly reguarly takin 400mg codeine phosphate for quite a while & get no nausia, itchiness or anything like that. just a high which i wish was stronger.

this could be a good if I could dose 1.6g of codeine & get 4 times as high. this sounds to good to be true. Some sources say the LD50 for codeine is between 0.8 & 1.3 grams. So im not really game to take any more than 600mg

I do remember doing cwe on a pack of panadeine forte (600mg codeine) & getting a much stronger effect than my usualy 360, or 400mg)

so what now. are ppl saying the 450mg dose is a myth. because according to seith if he's telling the truth than it is a myth & we could all be getting more out of codeine.

If all 1.6g of codeine is metabalizes into morphine, than codeine would actually be pretty good opiate. its only the ceiling effect that that doesnt make it as good as morphine itself.

infact with some of codeine other metabolites. i think hydromorphone & nor codeine comes to mind than it would potentially be better than morphine (if used orrally)

sounds like BS to me. to good to be true.

can someone help me find evednce on the internet (not just a cwe site) where tests have proven the averag dose where supposingly the liver is saturated with codeine & cannon convert more to morphine?

oh & mods this thread should really be in BDD

 

[Anon54]

Wikipedia claims there is not ceiling dose to codeine:

A dose of approximately 200 mg (oral) of codeine must be administered to give analgesia approximately equivalent to 30 mg (oral) of morphine (Rossi, 2004). However, codeine is, in general, not used in single doses of greater than 60 mg (and no more than 240 mg in 24 hours).[5] When analgesia beyond this is required, stronger opioids such as hydrocodone or oxycodone are favored.

Codeine is metabolized to C6G by uridine diphosphate glucuronosyl transferase UGT2B7, and, since only about 5% of codeine is metabolized by cytochrome P450 CYP2D6, the current evidence is that C6G is the primary active compound.[6] Claims about the supposed "ceiling effect" of codeine doses seemed to rest on the assumption that high doses of codeine saturated CYP2D6, which prevented further conversion of codeine to morphine, which is simply incorrect.[citation needed] There is also no evidence that CYP2D6 inhibition is useful in treating codeine dependence,[7] though the metabolism of codeine to morphine (and hence further metabolism to glucuronide morphine conjugates) does have an effect on the abuse potential of codeine.[8] However, CYP2D6 has been implicated in the toxicity and death of neonates when administered to lactating mothers, particularly those with increased 2D6 activity ("ultra-rapid" metabolisers).

 

[Mr Blonde]

^ Citation needed.

so for those that can't metabolize it as well, is it a case of needing more to feel the effects, or is the ceiling dose much lower and thats that?

I believe that it's just lower and that's it. For a prodrug, the rate limiting factor is the process that converts it into the active form and if that factor is deficient then you need to boost it (there are substances that release and increase formation of microsomal enzymes like CYP2D6).

In the case of a genetic deficiency of an enzyme though, I'm not sure how well the CYP2D6 inducers will work. On Tuesday I should have access to more information and I will see what sources I can provide.

ETA: That wikipedia article is really poorly written, I seem to remember it being a lot better once.

 

[drug_mentor]

I am pretty sure that the ceiling is for codeine and that is why it tends to vary between 400-600mg when quoted. Because most (possibly all?) OTC codeine in Australia is codeine phosphate that makes the ceiling dose up near 600mg to be the same as 400mg of codeine.

 

[Mr Blonde]

^ Yeah that would make sense actually. And I think you're right it's all the phosphate salt here, I've never seen any other form.

 

[amapola]

Before anybody get too deep into a debate on a possible ceiling dose, I think one needs to better clarify codeine's complete mechanism of action. This will also require separating the different effects. Something like codeine itself for histamine release itching and heat, morphine for euphoria, and c-6-g for analgesia is a good start I would guess. Though of course there can be a lot of cross over between them all and it will be different for everybody.

Good luck on all of that and finding studies which don't just say it is unfeasible and to move up to a stronger opioid...

 

[Jabberwocky]

^ Yeah that would make sense actually. And I think you're right it's all the phosphate salt here, I've never seen any other form.

neither have i fwiw

 

[Anon54]

Ive doses 480mg (cwe of pack of panadeine forte) before & it was realy strong. for 20 minutes i was really sedative & had a pleasent effect. better than what I get out of codeine now with a 24pack of panadeine xtra strength which is 360mg codeine.
but its been because ive been using it fairly reguarly lately & it's because Ive got a mild tolerance to it probably becaayse then i had the panadeine forte i hadnt had any codeine for like a year or something. back when the Nurofen + tablets were splttable.
I think the best way to get results from codeine is when ya already relaxed & havnt had any got a long time.
I personally dont think there is a ceiling dose to codeine I dont rekon 600mg if twice as strong as 300mg if u know what i mean but higher doses would make it stronger but ud probably start to get side effects if ya took over 400mg.

 

[Mr Blonde]

^ N+ hasn't been splittable for a long time now.

And yeah the increase of side effects is the worst part; whenever I up my dosage with codeine I make sure to have antihistamines because I know that the histamine reaction will kick my ass otherwise. Same if I take a break for a couple of weeks.

 

[Davevanza]

Seith. u honestly dose 1.6g of codeine phosphate?
really? & its stronger than 400mg?
I was convinced fom many sources than the max dose the codeine could be converted to morphine is around 450mg.

Ive fairly reguarly takin 400mg codeine phosphate for quite a while & get no nausia, itchiness or anything like that. just a high which i wish was stronger.

this could be a good if I could dose 1.6g of codeine & get 4 times as high. this sounds to good to be true. Some sources say the LD50 for codeine is between 0.8 & 1.3 grams. So im not really game to take any more than 600mg

I do remember doing cwe on a pack of panadeine forte (600mg codeine) & getting a much stronger effect than my usualy 360, or 400mg)

so what now. are ppl saying the 450mg dose is a myth. because according to seith if he's telling the truth than it is a myth & we could all be getting more out of codeine.

If all 1.6g of codeine is metabalizes into morphine, than codeine would actually be pretty good opiate. its only the ceiling effect that that doesnt make it as good as morphine itself.

infact with some of codeine other metabolites. i think hydromorphone & nor codeine comes to mind than it would potentially be better than morphine (if used orrally)

sounds like BS to me. to good to be true.

can someone help me find evednce on the internet (not just a cwe site) where tests have proven the averag dose where supposingly the liver is saturated with codeine & cannon convert more to morphine?

oh & mods this thread should really be in BDD

I read a couple of yrs back, that, initially Codeine at any dose, taken in one day, would be converted to Morphine ( 10 % ).
But it needs our liver enzyme called CYP 450 2D6 to convert it. In this case, the first dose, Codeine acts as a substrate.

If a second dose is taken ( any amount of codeine) within the same day, then, Codeine becomes an Inhibitor of CYP 450 2D6. So, conversion to Morphine is reduced. That's why, when I take a second dose within the same day, I don't feel the same "Kick" as the first dose.

As far as I know, Codeine, unlike Pentazocine and buprenorphine, is a pure Agonist, so as long as our liver could produce the isoenzyme CYP 450 2D6, there is no ceiling effect. ( I read, Glutethimide, a sleeping agent,and Dexamethasone,a corticosteroid, actually the only 2 drugs that boost this CYP 450 2D6, making Codeine being metabolised into Morphine ). So , theoretically, if Codeine at any dose is taken with any of these 2 drugs, it will be all metabolised to Morphine.

I tried Pentazocine, it's a partial Agonist, and its effect is no difference like taking Mersyndol, an OTC analgesic combo. I read before abt Buprenorphine, it has a ceiling effect at 12mg, being antagonist at "mu" receptor ( This is where we get the high and analgesia, but still retains being agonist at "kappa" and "delta" receptor).

 

[slortaone]

years ago, i started at 200mg and slowly worked my way up to around 800mg of codeine. it was awesome, i got really high but i decided id slowly taper my dose down to 400mg because tolerance is a bitch. i always wanted to add a few more pills and i knew before long id have to go to too many chemists, and also my tolerance would be sky high. i still dose 400mg and maybe once a month 500mg. theres always temptation to add more but i dont, i dont want to ruin it... i am a fan of it, been using it reguarly for long enough to feel ill effects on the days i dont have it though. i dose once every three days at the moment which is more than i like, i have to control it more. i dont believe in the codeine ceiling dose theory, the few people i know that do codeine wouldnt feel much off 400mg but would feel effects from, say 600mg.

are alot of you guys reliant on codeine? i just ask because for alot of you, thats a shitload of codeine to come up with, especially with smaller boxes these days. i dont know how you guys do it.

id be careful getting your tolerance that high, but i suppose its better than going to a stronger opiate. stay safe guys.