Posted by Kon-shuss on September 18, 2003, at 3:00:41
In reply to Re: OpioidsDepression:TheKey2LockTolerance:NALTRE » Liligoth, posted by craig allen on September 17, 2003, at 19:18:53
...yep, that gal sure knows her stuff ;)
... so as Britt pointed out in her last quirey, "...in the future when one takes OxyTrex, how would we know if the psychological effect can keep up to par with the analgesic effects?" Well, if you ask me, I'am totally convinced they go HAND-IN-HAND,.... that is 2 say......: if the analgesic [physiological] tolerance properties are stabilized in use of OxyTrex, then the psychological [antidepressant] tolerance properties MUST be stabilized as well. (Narcotics* are antidepressants BECAUSE of their unique analgesic mechanisms'/pathways in the body)
* =Meaning, Full-Opiate Agonist(s)
I really cant be that surprised to find out that the ONLY medication (out of a long list of failed) I have responded to, with marked antidepressant effects, is that of the full-opiate agonists (morphine, oxycodone, hyrocodone, ect.)..... I mean, to really describe the true disabling, even 'life threatening', symptoms of my Severe [treatment-resistant/refrectory] Depression, is as simply as: chronic mental/emotional pain. Pain in one sense is not merely that different than that of the other sense. Prescription pain medication is what i responded to(unfortunately), becuase 'pain' is what i deal with on a chronic level. I say "unfortunatelly" fittingly, because I wish I'd responded to the traditional and orthodox meds over the years.
Also, ... in case someone has not read all the threads previous: The above references to "analgesics/narcotics/Full-Opiate Agonists" and "antidepressant", IT IS TO SAY, Opiate agonists [such as morphine, hydrocodone, oxycodone, ect] can and have a pronounced antidepressant effect upon a small percentage of people suffering from: Severe [Treatment-Resistant/Refractory] Depression....BUT THE LAST BIT OF INFO I WANNA SHARE WITH YA'LL, is some more in-depth evidence on exactly how *SMALL DOSES* of the 'full-opiate ''Antagonist'' -NALTREXONE- stabilizes the tolerance of long/short term use of the 'full-opiate ''Agonist'' - OXYCODONE.
So; from what i have read and know,... the main reason [full]Opiate agonists **-aka-:narcotics: morphine, oxycodone, hydrocodone, hydromorphine, fenatyl, dimorphine[heroin], ect.-** build tolerace in the user MUCH FASTER than compared to other non-narc CNS depressants and CNS stimulants is this: Not only do Opiates/Opioids react the body into producing less of its own, natural opiates (endorphins/enkalphins) over duration and dose-intensity, THEY also react the body into producing MORE opiate receptors. And that's the 'key difference' right there.....; 'that' production of "More opiate receptors", combined with the under-production of endorphins/enkalphins IS what really makes the body's tolerance climb fast and high...(all relative to dose-intensity and duration, of course). And here's the real "kicker": those newly-produced receptors are actually "pseudo-receptors", meaning: they don't work.......they just have opiate-receptor affinity, and that's all. They just allow an opiate/opioid or endorphin/enkalphin to bind there (with no cell action) other then to keep 'em there. THAT IS THE KEY DIFFERENCE in terms of tolerance build-up when compared to other non-narc CNS depressants and CNS stimulants. (With benzo's and barbituates, tolerance is created when the body starts to under-produce it's natural GABA ((and an increase of some more enzymes)).)(With cocaine and meth/amphetamine, tolerance is created when the body starts to under-produce it's natural Dopamine and Norepinephrine ((and an increase of some more enzymes)).) AND ALSO, IT MUST BE NOTED, & generally speaking, that tolerance with ANY SUBSTANCE (least of which NARCOTICS) is also the result -to some degree- of the substances' respected enzyme being produced increasingly, of which alcohol tolerance results especially and completely in this "enzyme category"."wssshhhhhheewww"....
NOW,... this is where low doses of NALTREXONE comes into play when stabilizing tolerance to Opiates and/or Opioids (ie: morphine; oxycodone):............ We'll, first of which should be understood of Naltrexone, is that it is a full-opiate receptor antagonist, meaning, if taken at a full dose (say, 50mg) with the body having a full dose of Opiates/Opioids on it, Naltrexone binds to the Opiate/Opioid receptors, "kicking out" the Opiate/Opioid substance and completely REVERSING the previous 'narcotic' effects. Contrary to what was shown on the movie "Pulp Fiction";... the scene where the woman overdoses on some high-grade heroin and in return they "antidote" her with a IV shot of adrenaline directly into the heart. Come on(!)... ...you're talkin' about some serious 'speedballin'. A full dose IV shot of Naltrexone is the true overdose antidote,...and not in the heart, either. That's why it was made in the first place;... ...Naltrexone (or Noxolone) reverses the effects of narcotics, as said before;... a true narcotic antidote, not only made for OD's, but for use during detox programs.
THAT BEING SAID, concerning what a full dose of Naltrexone demonstrates in the presence of narcotics (Opiates/Opioids)... ... there is the issue of the recently found properties [and now, benefits] of LOW DOSES of Naltrexone with full doses of Opiate/Opioid narcotics [ie: morphine and oxycodone, respectively].
*****The recently found property upon giving low doses of Naltrexone with full doses of an Opioid narcotic [example: 2.5mg/day Naltrexone WITH 60mg/day Oxycontin(time-releaseOxycodone)] IS: TOLERANCE TO THE OXYCONTIN WAS STABILIZED.
This pheonomena of low-dose Naltrexone to stabilize the tolerance of powerfull narcotics, shows the great benefit of making the long-term use of powerfull time-released Opioids CONSIDERABLY SAFER(!), by many times fold. Because before (and still present), people who need long-trem use of narcotics are having to take several 160mg time-release oxycodone's per day(!) due to the unstabilized tolerance that continues to climb after only over a year or so of use;... ... ... Outrageous amounts of narcotics being consumed that it definately 'opens the gate up' on drug-costs, side effects, and most importantly, SAFETY! Now imagine that tolerance has been stabilized, and that the same person need only AT MOST 80mg/day Oxycontin and retain all the same pain-relieving effects for years.SO HOW DOES LOW DOSES OF NALTREXONE DO THIS?.....this ability to stabilize one's tolerance to narcotics?
: current evidence shows that the low-doses of Naltrexone simply seems to INHIBIT the formation of those "pseudo"opiate-receptors... ...the one's that form normally when full-opiate agonist narcotics are taken WITHOUT low dose full-opiate antagonists [Naltrexone; Naloxone].
Man(!)....the evidence really shows, that if the formation of those extra, 'fake' opiate-receptors can be stopped, tolerance stops signifigantly with it.
OK...that was a lot....but i had 2 share that with ya'll and those who might stumble-upon it in the near future.
And as BrittPark stated before, those people at Pain Theraputics know of the benefits, too.....they're not too far off from releasing their two-in-one pill on the market... with a fitting name to suit it: "OxyTrex": Oxycodone(time-release)w/ low-dose Naltrexone.
Thankx 'Britt' 4 the company name so I could see their website: www.PainTheraputics.netAlso, BrittPark....where did you find the info on the MS Contin/Naltrexone pill.?....i couldn't find any info on the time-release morphine-sulphate w/Naltrexone type medication. Only OxyTrex info I could find at Pain Theraputics. hmmmmmm?
Peace>>>>"(Kon)-shuss"
poster:Kon-shuss
thread:120871
URL: http://www.dr-bob.org/babble/20030917/msgs/261264.html