Posted by cisco on March 31, 2002, at 21:15:24
The answer was here all along....
I found this old Psycho-Babble post during a Google search for Buprenorphine Kappa Antagonism:"The mu receptor is most commonly associated with euphoria and pain relief. The kappa receptor is most commonly associated with sedation (nodding often seen in Heroin addicts).
Underproduction or over-removal (severe re-uptake) of these endogenous opioids can be the cause of many psychiatric disorders ranging from Bipolar Personality disorders to major depressive disorders that often times manifest themselves in severe drug abuse.
Unbeknownst to them, these patients use Opioid medications either illicit or pharmaceutical because they are compelled to attempt to replace the endorphins, dynorphins, and enkephalins (endogenous opioids) that naturally occur in their systems at insufficient levels.
When taking these patients into account, a better term than the word "addict" or DDP (drug dependent person) would be opiate receptor deficient (ORD)
Buprenorphine's superior efficacy when dealing with these disorders is due to the aforementioned unique pharmacological profile as a PARTIAL MU RECEPTOR AGONIST combined with a FULL KAPPA RECEPTOR ANTAGONIST.
FACT: Buprenorphine is the strongest kappa receptor antagonist currently legal to use anywhere throughout the world. There is a large body of evidence that implicates mu agonists in anxiety and depressive disorders
Fink et al 1970, Kline et al 1977, Angst et al 1979, Pickar et al 1981
Pfeifer et al 1986, Schmauss and Heimrich et al 1988, Frecksa et al 1989,
Matussk and Hoehe et al 1989.)
The kappa antagonism of Buprenorphine also offers a new approach in the treatment of depressive disorders. Clinical studies have shown that the overproduction or under-removal of the endogenous kappa agonist dynorphin can have a direct causal relationship with various depressive disorders.
Therefore, a kappa antagonist would be of great clinical value in this treatment paradigm.
Buprenorphine is the strongest kappa antagonist currently available for clinical use.
Buprenorphine's unique pharmacological profile referenced earlier make it the only medication that offers this concurrent treatment alternative.
Additionally, clinical studies suggest that Buprenorphine increases the levels of the neurotransmitter dopamine in the brain pathways that control pleasure indicating a third method of effect. Conventional antidepressants and antipsychotics work gradually over a period of weeks or months, whereas maximal benefit is
apparent with Buprenorphine in a matter of days and in some cases hours.
After undergoing treatment with Buprenorphine, patients report an almost immediate improvement in function, an elevation of mood, and a general feeling of contentment. The fact that a rapid alteration in mental state can be produced by a pharmacological agent suggest an alternate theory to that of treatment with conventional antidepressants and the slow adaptive changes that are associated with simultaneous psychotherapeutic treatment."Perhaps 'Kappa Antagonism' is more than just an "Absence of effect" at the Kappa receptors....
More Opiate Antagonism News:
Buprenorphine is a
mixed µ-agonist/k-antagonist compound (Leander 1987; Sadée et al. 1982) that has been used to treat various forms of addiction in humans (Bracken and Holford 1993; Kosten et al. 1989).
In preliminary studies (Johnson et al. 1989), buprenorphine administered 30 minutes after fluid percussion-induced traumatic brain injury in rats significantly improved neurological outcome at 4
weeks as compared to saline-treated controls Opiate antagonists have been shown to be of benefit in spinal cord injury (Bracken and Holford 1993) and possibly cerebral ischemia
(Adams et al. 1986; Estanol et al. 1985) in humans. Given these preliminary experimental data and the established safety of buprenorphine treatment in humans, buprenorphine appears to be a
potentially attractive therapy for acute brain or spinal cord injury in humans.I find this line of inquiry interesting, as Bup appears to be a very complex Med. Hope U enjoy it 2!
Cisco
poster:cisco
thread:101178
URL: http://www.dr-bob.org/babble/20020327/msgs/101178.html