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Oxy - Stimulating, Heroin - Sedating, Why?

Gaz_hmmmm

Gaz_hmmmm

Bluelighter
Joined
Nov 27, 2002
Messages
4,137
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England, UK
Why is it that they work on the same receptors yet one's slightly stimulating and the other's more so sedating? :\
 
well different alkaloids of the papavar poppy plant produce different effects. i know that morphine is a very sedating drug. when making h, morphine is extracted from the raw opium (morphine is responsible for roughly 10% of the weight), and then converted to heroin (diacetylmorphine).

oxycodone is formed by the oxidation of codeine to codeinone, and then a few other steps which finally produce oxycodone. codeine in nature is a very stimulating drug too.
 
Oxycodone is a more pure mu agonist where morphine is spread prety evenly.. Mu agonism gives euphoria and analgesia and really has nothing to do with sedation.. Kappa agonism(double check that) results in sedation and the deadly side effects, mainly because those receptors are located in the brainstem and spine, which happens to control your autnomic functions.. The mu are in the cerebrum and limbic system which is the upper brain, which controls sensation and perception... So it makes sense that a mu would cause euphoric effects, while kappa cause somatic, due to the fact that their location in the brain gives way to what effect they have.

Both oxycodone and heroin are potent mu agonists, but heroin is a much more potent kappa agonist... So while 40mg of oxy and 18mg of H may give the same mental high(becasue both oxy and H have roughly equal amounts of molecules binding to mu), the H is going to knock your ass down merely because more of its molecules are binding to kappa than oxy.

There are other factors to take into consideration, like the fact that kappa still will produce some euphoria, and add to the mental high. Also, either A.mu stimulation causes sedation, or B. Oxy is a partial kappa agonist because obviously enough of it will kill you. If mu agonism causes no sedation, and oxy is a pure mu agonist, then it would seem as though you would just get high without ever recieving sedative effects.. Not true.. Im assuming when people say oxy is a pure mu agonist, they are talking in terms of agonism/antagonism, not in terms of which receptors, seeing as oxy will give you constipation, a side effect caused by delta stimulation..

Given the fact that oxy eventually is sedating, one could say that it feels stimulating merely because the user is feeling the euphoria, but not the sedation typically associated with that euphoria, which prolly comes from past experiences with a different opiate.

Mu agonism results in an increase in dopamine in the limbic system, which typically causes a stimulating effect in itsself. Its only when the side effects of the opiate override it that a user does not feel stimulated.. I know myself, that lower doses of morphine, an impure agonist, will make me feel stimulated, if only in a mental/social sense.

*Note - I may have gotten the effects of kappa/delta agonism reversed. Same principle applies.
 
adradmin said:

oxycodone is formed by the oxidation of codeine to codeinone, and then a few other steps which finally produce oxycodone.
Click to expand...

I thought oxycodone was an analoug of thebaine... :\
 
vicodelicious said:
I thought oxycodone was an analoug of thebaine... :\
Click to expand...

Codiene is produced from thebaine so possibly oxycodone is just one more step from that?
 
^^Codeine is produced from codeine. It's a naturally occuring substance found in the opium poppy plant, along with morphine, thebaine and some other alkaloids.
 
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yep, codeine is codeine, no conversions...Oxycodone comes from thebaine, thebaine is used to make semi-syntehtic narcotics(oxycodone, hydrocodone, Dilaudid, oxymorphone)...Thebaine is known to have more stimulant qualities than morphine, which explains probably why oxycodone has more a speedy type opiate feel and not that knockout nod morphine/heroin type feel...although quite a good nod can come from oxy, most definatly...
 
^^Actually, Hydrocodone and Hydromorphone are synthesized from codeine. The name Vicodin actually comes from V-codeine, for Five-Codeine, which is basically the chemical name of hydrocodone. Anyway, the V-codeine is where they got the brand name from. Hydromorphone is simply a further synthesized version of Hydrocodone.

As for Oxycodone, yes it is derived from Thebaine, as is Oxymorphone. The same Codone to Morphone principal applies, as Oxymorphone is simply a further synthesized Oxycodone. And yes, thebaine, a natural opium alkaloid, has stimulating properties on its own, which seem to be present to a lesser extent in the Oxy- substances.

I hope that clears the issue up a bit more, though there is still further to go as far as the technical terms for everything, and why exactly the effects that occur, occur.
 
Its very simple, oxycodone has some of the characteristics of thebaine, from which it is derived, which includes CNS-stimulation.....

Heroin is made from morphine, and its effects are similar.

But it also has to do with fact that morphine has a greater affinity for more opiate receptors than oxycodone, which is more of a pure mu agonist. Mu is the euphoria receptor, and the Kappa is associated with sedation (and dissociation), so morphine is more sedative because it effects both mu and kappa, whereas oxycodone is more of a mu agonist.
 
goldenbrown said:
^^Actually, Hydrocodone and Hydromorphone are synthesized from codeine. The name Vicodin actually comes from V-codeine, for Five-Codeine, which is basically the chemical name of hydrocodone. Anyway, the V-codeine is where they got the brand name from. Hydromorphone is simply a further synthesized version of Hydrocodone.

As for Oxycodone, yes it is derived from Thebaine, as is Oxymorphone. The same Codone to Morphone principal applies, as Oxymorphone is simply a further synthesized Oxycodone. And yes, thebaine, a natural opium alkaloid, has stimulating properties on its own, which seem to be present to a lesser extent in the Oxy- substances.

I hope that clears the issue up a bit more, though there is still further to go as far as the technical terms for everything, and why exactly the effects that occur, occur.
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Hmmm, didnt know that..i thought thebaine was responsible for all the codone semi synth products..interesting, are you sure such a powerful narcotic like Dilaudid is from codeine though and not thebaine?...God how Id love to try IV oxymorphone, hard to get your hands on those (numorphan)...Id really like to see how it compares to heroin....IV dilaudid is nice, cooked up the generic 4mg yellow pill(with the E on them)..good rush, but i think the H rush is alot better opposed to popular belief...
 
goldenbrown said:
^^Actually, Hydrocodone and Hydromorphone are synthesized from codeine. The name Vicodin actually comes from V-codeine, for Five-Codeine, which is basically the chemical name of hydrocodone. Anyway, the V-codeine is where they got the brand name from.
Click to expand...

I thought the name Vicodin came from:

Hydrocodone is 6 (VI roman numeral) times more potent (5mg hydro = 30mg codeine) than codeine, VIcodine... Vicodin...

I read somewhere that is how vicodin came about.. I don't remeber where though. Hmmm. Makes sense though huh? :\
 
Yeah, I originally posted that here, Vico. I read it on a site regarding opioids. Now I'm going to have to go and dig it up as reference. It's the analgesic potency 6 x's codeine (VI) codeine = vicodin.

At least that's what I read. And, it was on an authoritative site. I will have to look through my shit. Ugh.
 
Weird... that drug salvia works as a kappa opioid agonist and no way have i ever noticed similarities between that and stuff like oxy .
 
Well kappa is responsible for dissociation, and salvia is definately dissociative. Just because it may have an affinity towards the kappa receptor, doesnt mean it would necessarily feel opiate like, which it definately does not. I believe that salvia also may have an affinity towards the sigma and delta receptor, which can cause dysphoria, hallucinations.....
 
vicodelicious said:
I thought the name Vicodin came from:

Hydrocodone is 6 (VI roman numeral) times more potent (5mg hydro = 30mg codeine) than codeine, VIcodine... Vicodin...

I read somewhere that is how vicodin came about.. I don't remeber where though. Hmmm. Makes sense though huh? :\
Click to expand...

Yeah you are right. I just remembered it had something to do with Roman Numerals. Thanks for clearing that up.

As for the other information, I may be wrong. Since it isn't a health sensitive issue, I didn't do all of my research. I'll check up on my facts tonight.
 
negrogesic said:
Its very simple, oxycodone has some of the characteristics of thebaine, from which it is derived, which includes CNS-stimulation.....

Heroin is made from morphine, and its effects are similar.

But it also has to do with fact that morphine has a greater affinity for more opiate receptors than oxycodone, which is more of a pure mu agonist. Mu is the euphoria receptor, and the Kappa is associated with sedation (and dissociation), so morphine is more sedative because it effects both mu and kappa, whereas oxycodone is more of a mu agonist.
Click to expand...

yes I got one right! ;)
 
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