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PostPosted: Sun Jun 03, 2012 9:30 am 
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Many of the people on this forum seem to be completely unaware of how this miraculous drug exhibits its unique and life-saving properties. Here's a little information I'll include written for the layperson to extend appreciation and to educate.

I. Pharmacology:

a. Clinical Pharmacology

Buprenorphine is classified as an agonist/antagonist. Buprenorphine (the active ingredient in Suboxone) is a partial agonist at the Mu-Opioid Receptors (MOR). A partial agonist differs from a full-agonist (such as Oxycodone or Heroin) in that it activates the MOR - the main type of opioid receptor necessary to produce the euphoria and dreaminess contentment out of 3 other subtypes [delta, kappa, and NO/FQ]) in a partial manner. This means that it binds to the MOR and partially activates it, which elicits a moderate response but one not as strongly and potent as a full-agonist such as oxycodone, or methadone. Interestingly, buprenorphine has a wide-array of other effects at different receptors. For instance it is a antagonist at the Kappa Receptor (when activated it causes dysphoria) which could explain some of it's therapeutic effects and novel application to attenuating chronic pain. Additionally, it is a partial antagonist at the NO/FQ receptor which mediates pain pathways.

Buprenorphine is an extremely potent analgesic (painkiller) 25-40x as potent at equianalgesic doses to morphine. For instance just 0.3mg of buprenorphine sublingually is approximately equivalent to 30mg of an oral dose of morphine. Buprenorphine also exhibits extremely high binding-affinity to the MOR and acts as a competitive antagonist (fights for) the MOR in presence of another opioid (such as morphine) so that the morphine is displaced by the buprenorphine and is unable to activate the receptors, another reason why it's difficult to get "high" on opioids when on buprenorphine, but this is responsible for this blockade effect - as the naloxone is present in Suboxone to deter illicit intravenous adminstration, though it is poorly absorbed via the sublingual route, therefore, is not the reason why one can't get "high" on other opioids, which is thought to be a common misconception.

b. Etiology:

Buprenorphine was first isolated in the 1950's by a team of pharmacologists led by Kenneth Bentley and is known as a Bentley Compound. It is considered a thevinol or orvinol which means it can be synthesized from either of two of the main alkaloids in the Opium Poppy ("Papaver Somniferum") thebaine, and oripavine.

The Drug Addiction Treatment Act of 2000 (DATA 2000) overruled a series of rulings from the early 1900's changing the government's stance on treating opioid addiction and in 2002 Suboxone & Subutex were rescheduled from CV to CIII (controlled substance[s]) when approved for the detoxification and maintenance of opioid addiction, now mentioned in the DSM-IV-TR (Diagnostics and Statistical Manuel of Mental Disorders) as a brain disease, chemical dependency.

c. Antidepressent Potential:

In the 1990's a clinical trial conducted at the Harvard Medical School found that the majority of the patients whom suffered from refractor depression and were diagnosed with non-psychotic unipolar depression could be treated with success with buprenorphine whereas typical thymoleptic antidepressents were ineffective. This could provide an interesting pathway in the future to help perhaps manage and augment traditional psychiatric medications with buprenorphine for those whom don't respond or respond poorly to neuro/thymoleptics. This application is being further studied.

d. Treatment of Chronic Pain:

A new formulation recently made available to the public to combat chronic pain that requires round-the-clock analgesia is known as Butrans, a transdermal analgesic patch (similar to Fentanyl patches, but of much lower potency than that of the high-dose sublingual Suboxone tablets) and are intended for moderate to chtronic pain and for non-tolerant individuals (to opioids). The dose is much lower, in micrograms (mcg), 5, 10, or 20mcg (per hour) patches that release a constant amount of buprenorphine per hour and last for up to 7 days. Buprenorphine can be used as a novel pain management tool and is worth pursuing in the future for these applications.

Hopefully this knowledge was useful to some people, and remember educate yourselves to empower yourselves.

KeefSom, Pseudopharmacologist

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Fond Du Lac Psychiatry
Dr. Jeffrey Junig, M.D., Ph.D.

  • Board Certified Psychiatrist
  • Asst Clinical Professor, Medical College of Wisconsin

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