Ok strange info

[PantyShot9]

I knew hydrocodone turned into hydromorphone but I just read this off wiki about another drug. Dihydrocodeinone enol acetate's analgesic (http://en.wikipedia.org/wiki/Analgesic) and antitussive potency is slightly higher than that of its parent compound hydrocodone (http://en.wikipedia.org/wiki/Hydrocodone). Like all of its chemical relatives in this therapeutic class (codeine-based narcotic antitussives and midrange analgesics), thebacon exerts some of its effect by being a prodrug (http://en.wikipedia.org/wiki/Prodrug) for a stronger opioid, namely hydromorphone (http://en.wikipedia.org/wiki/Hydromorphone), which is formed in the liver by the Cytochrome P450 II-D-6 enzyme pathway, meaning that effectiveness of a given dose will vary amongst patients and other drugs taken at the same time can antagonise or potentiate thebacon. Does anyone know any drugs that would potentiate thebaine (thebacon)? I've tried tagamet for the cytochrome part and I didn't feel much more.

[resorcinol]

Thebaine and thebacon (hydrocodone enol acetate) aren't the same thing.

If you've got thebaine, you're not gonna feel much -- only somebody who's opioid naive might feel some opioid effects from thebaine's active metabolite oripavine (which is a mu opioid agonist). Thebaine itself is inactive.

If you've got thebacon (hydrocodone enol acetate), well that's a different story. Thebacon is probably between hydrocodone and oxycodone in potency, so if you take enough you should feel some opiate effects. If cyp2d6 is what metabolizes thebacon into hydromorphone, and you want more to be turned into hydromorphone, you wouldn't want to take cimetadine. Cimetadine inhibits cyp2d6 and would inhibit hydromorphone formation. You'd need a cyp2d6 inducer liek glutethiamide (sp?) to increase hydromorphone formation. But glutethiamide is a controlled substance, a downer similar to barbiturates (ie difficult to acquire, and probably not worth it).

But if you've really got thebacon, I wouldn't worry about hydromorphone formation too much. It's not really a prodrug. Sure, hydromorphone's binding affinity for mu opioid recepts is a lot higher than thebacon's, but thebacon is an active mu opioid agonist itself. If you take enough you should get high. If you really have thebacon (where'd you get it?), figure out how much hydrocodone you'd need to get buzzed and then take maybe 3/4 that amount of thebacon.

[nick]

Any drug with bacon in its name has got to be good.Hell,I've never had bad bacon.

[PantyShot9]

Thebaine and thebacon (hydrocodone enol acetate) aren't the same thing.

If you've got thebaine, you're not gonna feel much -- only somebody who's opioid naive might feel some opioid effects from thebaine's active metabolite oripavine (which is a mu opioid agonist). Thebaine itself is inactive.

If you've got thebacon (hydrocodone enol acetate), well that's a different story. Thebacon is probably between hydrocodone and oxycodone in potency, so if you take enough you should feel some opiate effects. If cyp2d6 is what metabolizes thebacon into hydromorphone, and you want more to be turned into hydromorphone, you wouldn't want to take cimetadine. Cimetadine inhibits cyp2d6 and would inhibit hydromorphone formation. You'd need a cyp2d6 inducer liek glutethiamide (sp?) to increase hydromorphone formation. But glutethiamide is a controlled substance, a downer similar to barbiturates (ie difficult to acquire, and probably not worth it).

But if you've really got thebacon, I wouldn't worry about hydromorphone formation too much. It's not really a prodrug. Sure, hydromorphone's binding affinity for mu opioid recepts is a lot higher than thebacon's, but thebacon is an active mu opioid agonist itself. If you take enough you should get high. If you really have thebacon (where'd you get it?), figure out how much hydrocodone you'd need to get buzzed and then take maybe 3/4 that amount of thebacon.


I didn't get thebacon I read this on wiki my main question was what could convert more hydrocodone to hydromorphone glutetimide is the only one?

[resorcinol]

I didn't get thebacon I read this on wiki my main question was what could convert more hydrocodone to hydromorphone glutetimide is the only one?

http://en.wikipedia.org/wiki/CYP2D6

Look under inducers.

Honestly though, with hydrocodone this isn't nearly as much of an issue as with codeine. It's such a big deal with codeine b/c codeine is pretty much totally inactive as a mu opioid agonist. Hydrocodone one the other hand is active as a mu opioid agonist.

I guess you could call hydrocodone a quasi pro-drug, because hydromorphone metabolite no doubt contributes moderately to the effects of hydrocodone... and hydrocodone would be weaker if it didn't have hydromorphone as one of its metabolites, but only a little weaker. Honestly, hydrocodone really isn't a prodrug like codeine is. Saturating that double bond and oxidizing the hydroxy group at position 6 of codeine (inactive, pretty much), results in a compound with significant mu receptor affinity (hydrocodone).

[PantyShot9]

http://en.wikipedia.org/wiki/CYP2D6

Look under inducers.

Honestly though, with hydrocodone this isn't nearly as much of an issue as with codeine. It's such a big deal with codeine b/c codeine is pretty much totally inactive as a mu opioid agonist. Hydrocodone one the other hand is active as a mu opioid agonist.

I guess you could call hydrocodone a quasi pro-drug, because hydromorphone metabolite no doubt contributes moderately to the effects of hydrocodone... and hydrocodone would be weaker if it didn't have hydromorphone as one of its metabolites, but only a little weaker. Honestly, hydrocodone really isn't a prodrug like codeine is. Saturating that double bond and oxidizing the hydroxy group at position 6 of codeine (inactive, pretty much), results in a compound with significant mu receptor affinity (hydrocodone).


But would it feel more like hydromorphone if u used a CYP2D6 inhibitor. I always heard if u used it with codeine it doesn't work is that false?

[Seedy]

Any drug with bacon in its name has got to be good.Hell,I've never had bad bacon.

and this stuff is thebacon!

[upstate_007]

Any drug with bacon in its name has got to be good.Hell,I've never had bad bacon.

Reading this thread has made me hungry.

[longduckdong]

Any drug with bacon in its name has got to be good.Hell,I've never had bad bacon.

You sure Nick??? I thought you were in UK.... That shit over there aint bacon I'll tell you that.

I'll never forget my first morning in London for breakfast when I visited. Going to the breakfast bar in the hotel, and seeing what they called bacon and eggs just wasn't for me.

[Woody Bear]

But would it feel more like hydromorphone if u used a CYP2D6 inhibitor. I always heard if u used it with codeine it doesn't work is that false?
If you block off the CYP26D enzyme from working by taking an CYP2D6 inhibitor, then codeine won't get changed into morphine, and hydrocodone won't get changed into hydromorphone. So you'd get no effect from the codeine, and limited effect from the hydrocodone.

If you enhance the CYP26D enzyme into working overtime by taking an CYP2D6 enhancer, then a lot more codeine then usual will get changed into morphine, and a lot more hydrocodone then usual will get changed into hydromorphone. So you'd get better effects from both the codeine and hydrocodone.

But even if you took an CYP2D6 enhancer and hydrocodone, it would still take time for the hydrocodone to get converted into hydromorphone. So the hydrocodone would feel more like oral hydromorphone, but nothing but IV or plugging hydromorphone itself would have the unique rush that hydromorphone is famous for.

[bigNasty]

so what is tagamet? is it an inhibitor or enhancer?

[alowishus]

Personly anything I read from Wiki I take w/ a grain of salt, it aint like it's write by PHD's; it's writen by people like you and me for fucks sake.

[Woody Bear]

Tagamet is the brand name for Cimetidine.
Cimetidine is a known inhibitor of many isozymes of the cytochrome P450 enzyme system (specifically CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4).

Grapefruit juice, and grapefruit in general, is a potent inhibitor of the intestinal cytochrome P450 enzyme CYP3A4.

Codeine is converted into morphine by CYP2D6.
Morphine is deactivated by CYP3A4.

So if you've taken Cimetidine, then codeine will have no effect, because Cimetidine inhibits CYP2D6 which prevents the codeine being changed into morphine. But if you've taken morphine, then the Cimetidine will slow down the break down of morphine, and enhance the effect.

Grapefruit juice inhibites CYP3A4, but not CYP2D6, so it slows down the breakdown of morphine, and does nothing to the enzyme that converts codeine to morphine. So if you have the CYP2D6 enzyme then taking grapefruit juice increases the effect from taking codeine.

[bigNasty]

so cimetidine+hydrocodone=not good? I thought i've read on here before that people take tagamet an hour before the 'codones. Is it better to use it with the 'morphones?

[Woody Bear]

Cimetidine is the better inhibitor to take with morphine and hydromorphone, while grapefruit is the better inhibitor to take with codeine and hydrocodone.