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Using opiates without worry of tolerance or withdrawal

 
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daksya
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PostPosted: Fri Oct 27, 2006 1:45 am    Post subject: Using opiates without worry of tolerance or withdrawal Reply with quote

In what could possibly be the biggest advance related to opiates in the last 30-40 years, it has been shown that taking an ultra-low dose (0.5-1 microgram) of an opioid antagonist (like naltrexone) alongwith an opiate (heroin, morphine, codeine, oxycodone..) prevents the tolerance (requirement of increasing doses to maintain effect) and the withdrawal that typically occurs after abruptly stopping prolonged use.

A company called Pain Therapeutics has already conducted Phase III clinical trials with their product OxyTrex which is oxycodone + naltrexone. Their various studies and trials can be found here.

More intriguing is a self-experimentation report in the Journal of Psychoactive Drugs by Jonathan Ott, whom some of you may recognize as an established figure on psychedelic drugs:

Obviation of opioid withdrawal syndrome by concomitant administration of naltrexone in microgram doses: two psychonautic bioassays

Quote:
Two psychonautic bioassays (self-experiments) in stepwise and abrupt cessation of long-term daily oral ingestion habits of 800 mg of codeine phosphate are presented. Concomitant administration of minute doses (about 0.5 mcg) of the opioid antagonist naltrexone with each dose of codeine was found in both cases to obviate the expected opioid withdrawal syndrome, resulting in asymptomatic and uneventful transitions from physical opioid dependency states to exogenous opioid-free metabolism. These experiments are analyzed in the context of a conjectured, rapid, iterative reduction and complete elimination of opioid tolerance, once acquired. It was found that coadministration of naltrexone with codeine phosphate obviated the development of both tolerance and physical dependency over several months of four daily oral doses of 200 mg, allowing abrupt ("cold turkey"), asymptomatic and uneventful withdrawal. This points the way to the biochemical substrate of opioid tolerance itself, and shows that this can easily and inexpensively be blocked, even over months of iterative oral administration of substantial doses of opioid analgesics. Finally, it suggests the opioid withdrawal syndrome is directly related to the physiology of opioid tolerance, and can be prevented by blocking tolerance itself. Even when tolerance has been acquired, this can be reduced stepwise over a matter of days, with no symptoms of opioid withdrawal syndrome.


The Ott study is important because he tackles the aspect of euphoria in humans, which is unlikely to be tackled by government or industry, and who would have, or still may, point blank claim that this method is not suitable for treating street addicts, or "worse", not an argument for considering regulated opiate availability. He confirms that analgesia and euphoria are retained. Most dramatic is the observation that he was able to induce euphoric effects out of 96 mg codeine (+ naltrexone), which had been true for him, 30 years prior when he first took opiates, but not since, due to tolerance.
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