Effects - Oral Heroin, and MS Contin. The same?

[WrtngCocaineTutorial]

SWIM has been reading on wikipedia lately about herion. And, as SWIM understands it, if someone were to take Heroin orally, it would have to undergo first-pass metabolism, which makes the drug into morphine before it reaches the brain...

And SWIM has been checking out the ingredient in MS Contin; Morphine.

Does anyone know if taking Herion orally, and taking MS Contin orally would give equal effects?

[Tony Williams]

I think it would be a little better than morphine still. I believe when you shoot H, it crosses the BBB 2-3 times quicker and the brain turns it into morphine.

So I think the liver/intestine MAO would do the same living more morphine than morphine, maybe.

[davestate]

Acetlyated opiates are broken down by the body when consumed orally very quickly, resulting in very low bioavailability. I'm sure I can dig up journals confirming this. Plug it rectally

[WrtngCocaineTutorial]

How did that go? Guess it gives a different high than taking it orally. More like a herion high than a morphine high.

[jon-q]

When Morphine is acetylated it becomes Diacetylmorphine (Heroin); Heroin is approx 1.5 times more potent than Morphine.
Heroin enters the brain much faster than morphine, where it undergoes (Deacetylation) this reaction produces Monoacetylmorphine (6-MAM) and Morphine.
When a drug is taken orally it undergoes (First pass effect) reducing the amount of drug that’s available (Bioavailability)
Both Heroin and morphine have a low Bioavailability <35%, Heroin also undergoes (Deacetylation) in the liver, effectively turning it back into Morphine, this is a simplified version of current understanding anyway?

So to answer the question, on a mg-mg basis Heroin would be approx 1.5 times stronger than Morphine when injected or when taken orally, all things being equal.
Because your question asks about MS-Contin, things wouldn’t be equal. MS-Contin is a continuous release tablet; this means the morphine will be released over a period of time rather than one single hit.
Q
New research disputes these findings in chronic opiate users. BJP Aug 2008 66,6

[samuraigecko]

Heroin is metabolized into Morphine and 6-Monoacetyl-morphine (not just morphine alone) 6MAM is a lot stronger than both Morphine and Heroin.

Taking oral Heroin (Diamorphine SR) is much better than taking MScontin (Morphine Sulfate Continuous Release).

Peace

Reputation Comments on this post:

Second tree to the left. - That's funny. Especially when thinking about people who are paranoid from tweeking

[jon-q]

Thanks for correcting me samurai
Of course one swallow dosen't make a summer. But this study if true casts a lot of doubt on current thinking towards oral use of Heroin.

Published 15th Aug 2008 British journals of clinical pharmacology.
Issue 66,6

WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT
• Venosclerosis prevents many opioid addicts in heroin substitution programmes from injecting intravenously, which makes consideration of other routes of administration necessary.
• Even high doses of oral diacetylmorphine are completely converted to morphine presystemically.
• Morphine bioavailability in heroin addicts after high-dose oral diacetylmorphine administration is considerably higher than expected based on prior data obtained with relatively low oral diacetylmorphine or morphine doses in healthy subjects or patients receiving treatment for pain (64–72% vs. 20–25%).
WHAT THIS STUDY ADDS
• Morphine influx into systemic circulation is more rapid after oral diacetylmorphine than after oral morphine, resulting in earlier and more than double maximal concentrations.
• In opioid-dependent people, bioavailability of morphine from oral doses of diacetylmorphine is also 37% higher than that of oral morphine.
• Morphine bioavailability is two and 1.5 times higher in chronic users than in opioid-naive subjects after low oral doses of diacetylmorphine or morphine, respectively.
• Oral absorption of morphine from diacetylmorphine is dose dependent, i.e. bioavailability increases with diacetylmorphine dose.

AIMS

In the Swiss heroin substitution trials, patients are treated with self-administered diacetylmorphine (heroin). Intravenous administration is not possible in patients that have venosclerosis. Earlier studies have demonstrated that oral diacetylmorphine may be used, although it is completely converted to morphine presystemically. Morphine bioavailability after high-dose oral diacetylmorphine is considerably higher than would be predicted from low-dose trials. The aim was to investigate whether the unexpectedly high bioavailability is due to a difference in the drug examined, and whether it depends on previous exposure or on dose.

METHODS

Opioid-naive healthy volunteers and dependent patients from the Swiss heroin trials (n = 8 per group) received low doses of intravenous and oral deuterium-labelled morphine and diacetylmorphine, respectively. Patients also received a high oral diacetylmorphine dose.

RESULTS

The maximum plasma concentration (Cmax) of morphine was twofold higher after oral diacetylmorphine than after morphine administration in both groups. However, morphine bioavailability was considerably higher in chronic users [diacetylmorphine 45.6% (95% confidence interval 40.0, 51.3), morphine 37.2% (30.1, 44.3)] than in naive subjects [diacetylmorphine 22.9% (16.4, 29.4), morphine 23.9% (16.5, 31.2)] after low oral doses (48.5 µmol) of either diacetylmorphine or morphine. Morphine clearance was similar in both groups. Moreover, oral absorption of morphine from diacetylmorphine was found to be dose dependent, with bioavailability reaching 64.2% (55.3, 73.1) for high diacetylmorphine doses (1601 µmol).

CONCLUSIONS

Oral absorption of opioids is substance-, dose- and patient collective-dependent, suggesting that there may be a saturation of first-pass processes, the exact mechanism of which is not yet understood.
Received
1 June 2008
Accepted
10 August 2008

DIGITAL OBJECT IDENTIFIER (DOI)
10.1111/j.1365-2125.2008.03286.x

Reputation Comments on this post:

Great info! Thanks for digging it up