dopetalk
Core Topics => Opiates & Opioids => Drugs => Heroin => Topic started by: Griffin on September 29, 2015, 07:29:36 AM
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I was just wondering what the high would be like from oral heroin if it were made into a pill for pain control and what the oral and intranasal bioavailability would be. Would it be similar to morphine or would there be any rush like there is with oxycodone. From the studies I read it basically said that the main reason for pain control was from the morphine that it converted into so morphine was a better alternative and there was no need to make it a pill. I never got a rush from smoking it and I have very little IV experience mainly because of my shaky hands and the amount of cheap(comparitively) 30 mg oxy and the generic opana that I was getting prescribed.
I always daydream about having a few kilos of pure powder heroin and the things I would do. Also a few kilos of opium from the huge poppy farm that I find myself at in my dreams. That is what got me wondering about if I compounded it into a pill with a press and what it would be like as a pill, and also what it would be like if i just tried the powder orally. I am sure the information is out there on oral bioavailability. I just figured you guys would know and it would be easier to ask than to search and read a bunch of studies or read other forums of people that I have no faith in their knowledge of opiates.
Will I just have to get better at IV in my dreams or is there a future in pharmaceutical heroin for a good ol first time trying opiates type of rush? If there isn't I guess I will just have to study up on my chemistry to make all the good pharms when I become a billionaire and find myself on that poppy farm isolated from thoughts of incarceration.
Griffin
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well, there would be no rush IF it worked orally but i believe that our digestive acids will render the benefits from Morphine's acetylation useless.
i could be completely wrong but that's my un-googled best guess.
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It just hydrolyzes back into morphine in the presence of HCl (stomach acid).
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the body metabolizes heroin into morphine in 7-15 min after you ingest it. Oral heroin would turn into morphine before it passes through the blood brain barrier. basically, oral heroin would be just like oral morphine.
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the body metabolizes heroin into morphine in 7-15 min after you ingest it. Oral heroin would turn into morphine before it passes through the blood brain barrier. basically, oral heroin would be just like oral morphine.
I believe the quote your looking for is saying something has that has a BA 23 %or 24% is a long long from it active at all.
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Although in the days of patent medicines, there were medicine with heroin for oral use (notably Glyco-Heroin cough syrup), it does indeed revert quickly to morphine in the gut.
Think about going through the conversion process for the syrup, only to have it become morphine again.
You would have to have a different ROA to get the increased efficacy: smoking, injection, maybe even rectal.
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Yes, a good portion of the heroin would be hydrolyzed to morphine in stomach acid, and also by various enzymes in the liver and blood, but the 3-phenolic ester would be preferentially hydrolyzed (as it's harder to make a phenolic ester than an ester with a 2° alcohol) creating a certain amount of 6-monoacetylmorphine.
There would be an equilibrium reached where a certain portion of the heroin would be present as 6-MAM for some time, instead of total conversion to morphine, depending on the gastric pH and metabolic status of the individual.
6-MAM is more lipophilic than morphine per se and thus would find its way into the CNS more readily.
So, bottom line, you might see a slightly increased potency of oral heroin over oral morphine, but not by much.
As someone else has noted, there were some oral heroin products available and in use back in the "good ol' days." Bayer's "sedative of choice for coughs" was Glyco-Heroin (not sure what the "glyco" part in the name was about - probably just to make it sound fancy).
LOVE ME SOME HEROIN!