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Providing straightforward information pertaining to drugs, drug use & drug policy. The Grey Pages promotes drug-related literacy and advocates a system of viable and tolerant drug policies. This is my personal collection of commentaries, essays, tid-bits, and other such writings on everything ranging from drug use, drug policy and drug-myths, to drug-science, addiction, human behavior, and the workings of the human brain. I started this blog with a particular focus on opioids, and over the past year have found my interest gravitate toward the intriguing, ever-changing world of designer intoxicants (i.e. "research chemicals" or "designer drugs").

Wednesday, May 23, 2012

Up to Date Information on Buprenorphine

I've neglected to see much of the recent literature on buprenorphine in humans, published in very recent years (post 2005). I'll highlight a few relevant points, some of which contradict earlier assumptions about this drug and its action. 

1) In the past, buprenorphine was believed to be of limited value in treating severe pain, especially in opioid tolerant individuals. It was believed that bupe was limited by a ceiling on analgesia at low dose levels, just as is the case for its respiratory depressant action. This is not true - while the peak respiratory depressant effect of buprenorphine is believed to level off at a few milligrams (~4mg roughly), the analgesic efficacy does not level off at this point. It continues increasing linearly with dose. Buprenorphine shows no ceiling on analgesia in transdermal doses up to 7mg per day, while other sources have even cited the absence of a ceiling with doses as high as 8-32mg daily. Bupe may very well be limited by a ceiling on analgesia, but this has not been observed in the dose ranges tested. 

2) Meanwhile, the morphine-like subjective effects of buprenorphine are known to increase linearly with dose, until leveling off anywhere between 8 and 32 mg daily (though typically in the 8-16mg range).

3) Buprenorphine exhibits potent antihyperalgesic properties (possibly associated with its kappaminergic as well as its nociceptoid action). In other words, it prevents long term neuroplastic excitation (i.e. central sensitization) in cases of chronic pain. For this reason, bupe is useful for complicated cases of treatment-resistant pain (including neuropathic pain). 

It seems that buprenorphine is making its way into the mainstream pain market. With all the research being done on this compound, we can expect to continue learning more about the actions of buprenorphine and to put much of the junkie-speculation to rest.


Off Site Sources:

Transdermal Buprenorphine as an Analgesic 
Buprenorphine as an Analgesic 
Buprenorphine and Respiratory Depression
Current Clinical Knowledge of Buprenorphine Pharmacology 

1 comment:

  1. Hi. I take buprenorphine in the form of Suboxone 2mg strips prescribed by my doctor. I have never been able to get pain relief from them, but then again I've been on the minimum tolerable dose. I was hooked on stronger opioids and switched to this to be on the right side of the law. I really wish it DID work on the pain, since my pain is bad. I currently take just 4mg a day (1 strip in the morning, 1 at night). I had been on much higher doses such as 16mg a few years ago. Am I understanding that there is no reason to believe bupe IS an effective pain medication? My pain is from 3 sources: a botched surgery, chronic and constant arthritis, and possibly diabetic neuropathy. My doc has suggested we increase dose from time to time to see if effective pain relief but I keep reporting back no significant. I realize I will always be on pain meds and bupe seems to have the lowest side effects but also lowest pain relief.

    If I wanted to give bupe a chance again as a pain relief, what dose should I try? Is there documentation I can point my doctor to? I think he'd rather see me get the pain relief from bupe than trade for a stronger opiate/opioid.

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