The Vespiary

The Hive => Newbee Forum => Topic started by: skanic on July 18, 2004, 08:40:00 PM

Title: codeine administration
Post by: skanic on July 18, 2004, 08:40:00 PM

"Codeine is converted to morphine in the brain"(source : "the codeine faq")
BUT
at contrary, codeine is ALWAYS administered orally because it is demethylated by the cyp450(which is mostly in the LIVERS), to morphine, for analgesia.

THEN my question is :
is codeine active :inhalated(smoked)?
                   or at less, insufflated(snorted) ?

Title: freebase
Post by: methyl_ethyl on July 18, 2004, 09:45:00 PM

Codeine freebase can be smoked.

---

Intranasal codeine, in which I was not aware of..

Patent US6608073 (http://l2.espacenet.com/dips/viewer?PN=US6608073&CY=gb&LG=en&DB=EPD)

Abstract

This invention provides a method of rapidly and reliably delivering codeine, alone or in combination with other compounds, to the systemic circulation by administration via the nasal route to produce rapid onset of beneficial effects in the treatment of pain or cough. The present invention further provides pharmaceutical compositions comprising codeine, and/or pharmaceutically acceptable salts thereof in a variety of unique pharmaceutical dosage forms, with and without other analgesic and/or antitussive compounds.

regards,

m_e

Title: besides this is crossposting!
Post by: jsorex on July 19, 2004, 12:36:00 PM

besides this is crossposting!

Title: But what about conversion to morphine?
Post by: OcoteaCymbarum on July 19, 2004, 05:04:00 PM

If taken intranasally???
10 % of the codeine you ingest is transformed by demethylation to morphine in the liver, not in the brain.
I cant remember what cytochrome does that. Cyp450 means nothing really, as its a class of enzymes, playing an important role to detoxify your organism and make non-polar substances more polar for excretion, mostly by urine.

Which makes me wonder about the potential pain relief you could get from intranasal codeine. I can see the antitussiv properties, but without demethylation and direct access to the brain, what fraction will be transformed into morphine???

Title: Are you thinking that when snorting codeine,...
Post by: jsorex on July 19, 2004, 06:53:00 PM

Are you thinking that when snorting codeine, it will go directly to the brain from your sinuses, passing the BBB, not passing the liver first?

Title: wink, jsorex, i know .
Post by: skanic on July 20, 2004, 11:18:00 AM

wink, jsorex, .
thank you very much for this patent methyl_ethyl.
I have still to solve the problem of that morphine conversion.
Is there cyp2d6 in the brain ,and if yes, is there sufficiently to convert codeine ?
and finally, as already told jsorex, will the codeine cross the bbb ???

It leaves us with a mystery and i think only experiment will be the solution. I'll try and i 'll tell you.

Title: ...
Post by: relic2279 on August 02, 2004, 09:46:00 AM

Title: Codeine readily crosses the BBB
Post by: Rhodium on August 02, 2004, 12:07:00 PM

Codeine certainly does cross the blood-brain barrier, it is only a very bad agonist at opiate receptors compared to morphine, so even if only 10% of ingested codeine is demethylated to morphine, the actions of the latter may account for a significant part of the effects.

Title: and for the demethylation?
Post by: skanic on August 02, 2004, 02:06:00 PM

can codeine demethylation be performed with lithium chloride (or with an other otc reactant) ?
pyridine is nearly impossible to find.

Title: Yes its exactly what I think
Post by: OcoteaCymbarum on August 02, 2004, 05:33:00 PM

A very little fraction will get to the liver, it will distributes itself in the body, and yes it will cross the blood brain barrier easily.
Just like Rhodium said, codeine is not so great on opioid receptors, and need to be demethylated to morphine for its analgésive effects to happen.
As such a dose of codeine for pain relief is about 30mg(of the phosphate), so between 2-3 mg of morphine.

Which is why I wonder about intranasal codeine for pain relief. Who care if its absorbed but not demethylated, unless you want its antitussive properties??

Title: um
Post by: r2e3 on August 03, 2004, 12:16:00 AM

cyp enzymes do make conjugates that are excreted in bile.
conversion of codeine into morphine is preferable(synthetically - meaning the literature is out there) and possible, but into heroin - more troublesome - seems no matter where you live.

if you really wanna pass the bbb - remember 1st pass - stick it up your ass if you that determined, it will by-pass the liver initially

not my bag really but my 2p

Title: swim read somewhere that smoked codeine ...
Post by: skanic on August 03, 2004, 12:22:00 AM

swim read somewhere that smoked codeine freebase is good.
But does the smoke passes trough liver?

as for synthetic conversion if anyone could give me a tip, since pyridine, bbr3, or lselectride aren't availableotc.
can demethylation be done with lithium chloride or aniline ?

Title: smoking
Post by: r2e3 on August 03, 2004, 12:36:00 AM

does miss the liver but hits your heart..

aniline is BAD for you - mess if you want but bladder cancer is common amongst people in the fabric industry that have used it as a dye/preparatory agent.

lithium chloride is a prescription medication - if you can get it - then - maybe  - my knowledge does not extend that far.

OTC, lol - if you are serious then you need to find a way of getting what you through legal means.

try - they can only say no.

if you are in the land of the free - ie the big us of a - then maybe it aint such a good plan.

take a holiday to thailand

feck knows what they use pyridine for

Title: Well..
Post by: relic2279 on August 03, 2004, 11:36:00 AM

I stand corrected. I must have misread it somewhere. (on the net most likely) :P But the point of my post however, was there are many opiates, quite a few actually, which do not. Like Immodium. :)

I had to edit this because I left out the most important part of my post that WASN'T misinforming,

Do not snort freebase codiene!

Title: Anal bioavailability is very often erratic
Post by: OcoteaCymbarum on August 03, 2004, 02:12:00 PM

And some of it will go first pass since it is connected to the portal circulation by anastomosis(2 vein systems connected togeter) Here the hemorroidal plexus is anastomized(is that a word?) with the portal circulation so some codeine would end up in the liver

Title: but is there any otc way to convert codeine to
Post by: skanic on August 03, 2004, 03:31:00 PM

but is there any otc way to convert codeine to morphine without pyridine...
CAN we do it with aniline or lithium chloride?

Title: Skanic: It hasn't been tried yet.
Post by: Rhodium on August 03, 2004, 05:30:00 PM

Skanic: It hasn't been tried yet. Why don't you try it and tell us the results?

Title: hope this helps
Post by: brulaheliko on August 04, 2004, 12:38:00 AM

Maybe im just being redundant, but what about BBr₃or even better, why not catalytically reduce to the 1,4-dihydroxy morhphinones? works, evn in the US, im told by AFOAF. just my 2cents