Posted by ed_uk on June 21, 2006, at 14:23:45
In reply to Re: 0.12 mg did not work, posted by Declan on June 21, 2006, at 8:50:49
Hi Dec
Buprenorphine is unusual. It is an extremely potent opioid ie. it is effective at very small doses compared with other opioids such as morphine. Buprenorphine is also unusual in that it acts as a partial agonist at opioid receptors ie. when it binds to an opioid receptor it stimulates it but not to the same degree as other opioids.
Buprenorphine binds very tightly to opioid receptors and has a long duration of action, much longer than most opioids (apart from methadone).
ShawnT at neurotransmitter.net provides some interesting information about buprenorphine....
'Buprenorphine is a partial agonist at mu opioid receptors and nociceptin/orphanin FQ (ORL1) receptors. It exhibits antagonist activity at kappa opioid receptors and delta opioid receptors, with less potent effects at the latter. The drug may also act as an antagonist at epsilon opioid receptors. Buprenorphine is an oripavine analgesic used to treat opioid addiction. Its active metabolite norbuprenorphine is a partial agonist at mu and kappa receptors and a full agonist at delta and ORL1 receptors.'
Buprenorphine appears to act mainly at mu opioid receptors. The relevance of its effect at kappa receptors is unclear: it appears to act as a partial agonist.
When injected, buprenorphine may resemble morphine and heroin in its effects. Sublingual and (particularly) transdermal administration would be expected to be less euphoric, possibly resembling oral morphine or codeine - except that bupe has a much longer duration of action.
Some people find opioids remarkably euphoric, whereas other people do not find them euphoric at all. In fact, some people become acutely (psychologically) distressed following the administration of an opioid.
Tolerance to opioids seems to be determined by genetic factors - some people develop rapid tolerance to opioid analgesia whereas other people do not appear to develop tolerance at all. A genetic test to determine the likelihood of tolerance would be extremely useful!
Ed
poster:ed_uk
thread:657263
URL: http://www.dr-bob.org/babble/20060617/msgs/659760.html