Is Proglumide useful to combat opiate addiction?

[Alfa]

I was just wondering this. It seems to counter tolerance. Any views on this?

[Paracelsus]

What would be the connection between lowering tolerance and combating addiction? I know that DXM seems to reverse tolerance to opiates and to be useful to combat opiate addiction aswell, although the mechanisms are most likely two different ones.

[atemeles5]

Swy will try soon proglumide. Look this:


from Tolerance, Addiction, and Effective Pain Management
by K. Trout
Originally Published at Opioids.com

Proglumide is a nonselective CCK inhibitor that was formerly employed as an anti-ulcer medication (Hahne et al. 1981). It shows NO analgesic effects of its own.

Although proglumide is now considered to be an obsolete pharmaceutical due to changes in our understandings of ulcer etiology, it has already seen extensive pharmacological and toxicological testing proving its safety and has been approved for use in humans.

It has largely fallen into disuse but is still available in bulk via chemical houses or as a pharmaceutical in Europe and Africa sold under the trade name Milid and Milide.

Other CCK inhibitors show similar properties. However, beyond simply having seen previous use in humans, proglumide is both inexpensive and nontoxic. (Ott 1999)

Proglumide is not some sort of magic bullet for completely eliminating the risk of tolerance development and addiction as its effects are only effective for a limited duration before tolerance to IT begins to develop. (After 8 days its effectiveness begins to wane) The work of Kellstein & Mayer 1990 suggests that successful therapeutic/maintenance applications will probably require its discontinuation for a week after each week of use. More work is needed to better define the precise parameters of its effective use for this purpose.

Despite this, proglumide has already demonstrated itself to be of value both in pain management and as an adjunct to maintaining a narcotic addiction within a larger program of harm reduction.

What is fascinating is how few drug educators, drug treatment facilities or even drug users are aware of this despite it being readily available information for nearly 20 years.

[I've removed references from this for "cut and paste" reasons - Dickon]

[Dickon]

1. Watkins LR, Kinscheck IB, Mayer DJ. Potentiation of opiate analgesia and apparent reversal of morphine tolerance by proglumide. Science. 1984 Apr 27;224(4647):395-6.
2. ^ Tang J, Chou J, Iadarola M, Yang HY, Costa E. Proglumide prevents and curtails acute tolerance to morphine in rats. Neuropharmacology. 1984 Jun;23(6):715-8.

Alpha, I'm not speaking from personal experience, but the titles of the two above papers seem to suggest that in animal models at least it does. An interesting theory occurs to me [Dr D is 76 hours from finishing tapering off of 225mg methadone daily, so his mind is working thusly..]

Let's say Mr X is an opiate addict, for sake of argument he is addicted to 100mg methadone a day, but is stable on that dose. Then, assuming this Proglumide does as it says on the tin, Mr X takes it for the requisite number of days to reduce his tollerance, then as Mr X's tolerance is reduced he is now happy on say, 80mg of methadone a day. For it genuinely to reduce tolerance it must of course keep tolerance down once it is dicontinued otherwise the reduction would only be chimeral. Mr X now is on 80mg methadone / day and taking no Proglumide. Leaving a suitable interval (again as determined experimentally. This is purely hypothetical), he takes proglumide again (and assuming the 20% reduction in tolerance is roughly stable over all dose ranges) Mr X is now on 64mg methadone /day. You see where I am going with this. If this theory were correct it would provide a painless taper down to an arbitrarily small daily dose of Methadone. Wouldn't that be a Pip? lol

Dr D.

Dickon added 1 Minutes and 21 Seconds later...

Ooopps forgot to mention that the above is all lies or might be.....

[fiveleggedrat]

Coming from Mr. Opioid Tolerance, in studies and in theory, yes, it is.

Swim would GLADLY test under controlled settings. Swim has permanent tolerance that won't go away.

Now, the problem is sourcing it