Talk:Norbuprenorphine
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So does this have no inverse-agonist properties that Buprenorphine has, making it a pure mu-receptor agonist? Nagelfar (talk) 18:41, 22 July 2010 (UTC)
The Emperor is partially clothed ;)
The highly political claim that buprenorphine acts primarily as a partial agonist is only part of the true picture, but it makes for a nice cure for the over moralistic harm maximization crusaders' need to believe that patients given buprenorphine wont enjoy it. look at what china uses, Dihydroetorphine! their leaders are not under the same delusions. ironically buprenorphine is effective because its primarily metabolite is a full mu agonist. but this is never mentioned. it all depends how you look at it, buprenorphine could more authentically be described as a prodrug. actually the slow buffered self tapering does result in part from the equilibrium between bupe, norbupe and possibly naloxone which is 10% bioavailable, which in suboxone is high enough that a dose of 16mg bup:4mg naloxone yields .4mg naloxone to the brain which is enough to 1) significantly shift the slow rates of metabolic conversion of bup->norbup due to competition for the same enzymes (cyp 3a4), and 2) causing a direct effect of naloxone in patients who ostensibly would not choose to take naloxone otherwise, and so this is forced upon the patient in a variety of ways.
Who would voluntarily accept the side effects of naloxone such as; suicidal ideation, asthenia (weakness), inability to sleep, chills, malaise, akathisia, and a large reduction in the time span between dosing without resulting in marked discomfort!
Ultimately if it was purely about diversion why not change the formulation into either a small volume of liquid which could be administered buccally and absorb much more quickly or the listerine like strips which are being developed but only containing suboxone! the pathological codependency between the opioid dependent and the highly profitable medical syndicate which 'treats' them is exploitation on a billion dollar scale. —Preceding unsigned comment added by 220.101.92.34 (talk) 09:16, 21 April 2011 (UTC)
The above poster is insane
It has been proven that nalaxone has NO CLINICAL effect in people, making suboxone and subutex literally the same drug. But you did have some good points...