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Opioids BA%, T1/2, Tmax-duration superthread by Lorne???

^ I meant the best you can do is post ?relative? affinities- like morphine being ~5x of Oxycodone off the top of my head, and that paper implies 15x higher than hydrocodone, though another source says 8x higher; or say they are relative, based on method(and different animal studies)

Yeah, a disclaimer would work, though it is complicated; scientifically they were still recently trying to figure out what made Oxycodone so effective, relative to it?s low Mu binding affinity (Kappa affinity notwithstanding, as that is debatable though reasonable)

Nice though

Thanks to all

(Will post references for Tmax values, and diamorphine?s higher P.O BA% etc.)

Soon we will have a purge(or whatever you call it) to honor an occasion
 
Ah yes that makes sense. I was missing context :\

Correct me if I'm wrong (I researched this a bit a while back and don't remember details) but I thought some of the early studies on oxycodone efficacy had some misrepresented data? I know that oxycontin should have never been approved as a 12 hour pain medication, but I also thought it wasn't that much more efficacious in terms of analgesia as other opioids that are routinely prescribed
 
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^ Yep.

It is similar in effectiveness to morphine, the question they asked about oxy in general was ?what makes this more potent than it?s experimental properties would suggest

Yeah, they sued; think it was biggest pharmaceutical lawsuit at the time

They claimed ?less addictive? or something, yet a thorough study/experiment demonstrated that crushed OxyContin 40mg tablets snorted by users(crushed of course) yielded a BA of ~75%;

Am weary of many CR formulations, personally; not saying they don?t have there place, just it seems evergreening atp, and some just do not wok, at least as intended; do not trust 24hr formulations of medications that normally clear the body rapidly(2-3hr, like morphine, or a lipophillic like hydromorphone)
 
Good afternoon Pacific, gentlemen. Since it's considerably safer dumping into a new thread anyway, I figure I'll wait until our esteemed researcher Dr. Lorne feels there's enough additional editing before I try to undo my unsticky and go to v2; that's not a delay tactic, I mean, like hopefully only a couple days max, right Lorne? I just can't risk single line-edits. Everything's backed up, but it's easy to lose traceability.

(Vbulletin erased half of the original table just in switching out of WYSIWYG mode and erased all the slashB from the bottom (which is good, cause that was dumb anyway). And it's only a third the length of the original.)

Bear in mind this is just a raw info sheet, it's not very readable or helpful in its current form and will be changed.
 
Is that the cue for me to update?

It has been a while, you should get some sleep, Lorne, really. Have you talked to your doctor about a type of drug known as a ben - zo - diaz - uh-peen? They can help you get to sleep.
 
Reminder to me: include a CYP2D6 inhibitor list, plus a para on when a potentiator becomes an inhibitor.

Ie. codeine, di-H codeine, and tramadol.
 
^ Wouldn't worry about Dihydrocodiene so much, though I concur

And there are a lot of Codeine derivatives that are pro drugs-ethyl or nicocodiene, it is noteworthy; also Wellbutrin is a completely different drug when it is not converted properly, although abusing Wellbutrin, well...
 
Sounds like there's no end to possible derivatives. But we need a cap somewhere, like 1% of people on this board have actually encountered said drug in any capacity.

Somewhere out there a guy is working on 2-trifluoromethoxy N-Isopropyl amphetamine, but we don't need to include it in the stims table yet. By June, though . . . .


And when not converted properly, Welbutrin becomes . . . Welbutrin! A potent dopamine reuptake inhibitor.
 
Wellbutrin is a prodrug for two different metabolites, is what was meant. You knew what I meant! (Yiu are a nind reader/ninja, right?)
mThat is why some crazy people snort it(have witnessed Wellbutrin abuse, and the pharmacy handed out like a 90 day supply per month; said person developed epilepsy

Of course we cannot go into every derivative, just making an observation: perhaps a blanket statement for the few that more than 1-2% may have encountered or is available otc in a populous place
 
Joke being that bupropion taken PO means not one molecule of actual bupropion gets into your brain. So it's rumored DAT inhibition is void as prescribed (first pass metabolism, plus actual scans of DAT occupancy show no Welbutrin to be found).

Also, dosage is not based on actual therapeutic benefit; like tramadol it's about the acceptable seizure risk set by the FDA. The drugs might actually work for depression if you could take the proper dose without seizing and dying.

So kids at home, you can get some of that dopamine action with Welbutrin up your nose, but it'd be worse than you get with regular old Ritalin . . . before your friends run screaming and forget to call the ambulance as you seize up on them.
 
https://www.ncbi.nlm.nih.gov/m/pubmed/14534521/?i=2&from=/11073290/related

Oral Diamorphine BA 67%; it needs to be updated, it is far higher than 35% with doses that people are actually using

An earlier post has a more detailed study, with 50-70% BA for high dose diamorphine

PO (could) actually viable, with decent dope, if you aren't an injector and don't snort

https://www.ncbi.nlm.nih.gov/m/pubmed/18945270/?i=3&from=/14534521/related

Another link demonstrating variability in morphine classic and H and the specifics (the Swiss study)

Hopefully Tommorow is another day, and can progress this thing- today had to do BK interviews (wait, what?)
 
Are you the subject or the object to that gerund, "interviewing"?

One is a bit excrutiating, the other the most hopeless feeling man can experience. I've faced them both.
 
^ They wouldn’t let me in the front door ;) or back

Interviews will fail because of Diazepam/liquid-solid/dextofisopam/jealously of former SMB3 skills conspiracy

Sorry Scrofula, FWR
 
https://www.ncbi.nlm.nih.gov/m/pubmed/8159633/

Lipophillicity figures for opioids, as well; morphine is low, Fentanly the highest(along with bupe in the above study)

Makes sense since fentanly hits hard and fast, yet lasts all of like 40 minutes

Buprenorphine is complicated because of slow receptor dissociation and long receptor t1/2, and very high binding affinity

Oxycodone has a modest lipophillicity, better than morphine, though lower than the morphinones, with hydromorphone being 10x(?) more lipophillic than morphine if not mistaken

Anyway this shall also bump the thread :)

https://www.ncbi.nlm.nih.gov/m/pubmed/2458208/?i=3&from=/17472518/related

Relates to sublingual absorption; it should be noted fentanly had a sublingual ba% of ~50~, and with ph adjusted methadone 75%; However, morphine was less than 10%
 
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