Buprenorphine
During the 1980s, Reckitt & Colman began marketing buprenorphine hydrochloride under the name Buprenex. Buprenex is primarily found in 0.324 mg/ml injectable formulations. 0.324 mg buprenorphine hydrochloride is equivalent to 0.3 mg buprenorphine. A prescription medication for people addicted to heroin or other opiates that acts by relieving the symptoms of opiate withdrawal such as agitation, nausea and insomnia.
Abstract
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Street Names
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Brand Names
Suboxone (buprenorphine & naloxone sublingual tablets)
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History
During the 1980s, Reckitt & Colman began marketing buprenorphine hydrochloride under the name Buprenex. Buprenex is primarily found in 0.324 mg/ml injectable formulations. 0.324 mg buprenorphine hydrochloride is equivalent to 0.3 mg buprenorphine.
On October 8, 2009, Roxane Laboratories of Columbus, Ohio, United States won FDA approval for a generic preparation of Subutex and as of October 23, 2009 announced that it is ready for distribution nationwide in 2 mg and 8 mg sublingual dosages. The demand for this generic was so high that Roxane did not produce enough to meet market demand, resulting in pharmacies running out and being unable to order more.
Pharmacology
The chemical formula for buprenorphine is: C29H41NO4
It has a very high binding affinity to the mu-opioid receptor; however, due to the fact that it is only a partial opioid agonist, it does not produce the same "high" or "rush" of full agonists (morphine, oxycodone, heroin). These two properties must be carefully considered in any given situation for two reasons. Most importantly, the long half-life and high binding affinity can complicate situations involving overdosage. For individuals dependent on full-agonist opioids, if there is not sufficient time between the last dose of the full-agonist and the dosing of buprenorphine, it can trigger precipitated withdrawal.
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Uses
It can be used for short detoxification only over several days, and then tapered off over several days.
It can be used for detoxification, then transitional maintenance at a steady state for several weeks or months, followed by tapering off.
It can be used for detoxification, followed by long term maintenance at a steady state for long term opiate replacement therapy.
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Scheduling
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Psychological and physical addiction liability
Common effects associated with the use of buprenorphine are similar to those of other opioids and include: nausea and vomiting, drowsiness, dizziness, headache, memory loss, cognitive and neural inhibition, perspiration, itchiness, dry mouth, miosis, orthostatic hypotension, male ejaculatory difficulty, decreased libido, and urinary retention. Constipation and CNS effects are seen less frequently than with morphine. Hepatic necrosis and hepatitis with jaundice have been reported with the use of buprenorphine, especially after intravenous injection of crushed tablets. The most severe and serious adverse reaction associated with opioid use in general is respiratory depression, the mechanism behind fatal overdose
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Long term effects
The long-term effects of buprenorphine have not been studied extensively due to their short time on the market. However, experts suggest that they may be similar to those of other opioids. Upon cessation, some long-term effects of buprenorphine may persist. Depression, fatigue, and insomnia are the three most commonly reported symptoms. Some people experience nausea, confusion, and physical weakness. Studies are continually conducted to determine the long-term effects of buprenorphine and in time conclusive evidence will be attained.
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Physical Effects
The physical effects of buprenorphine are as below:
Pain relief
Sedation
Nausea
Vomiting
Dizziness
Headache
Constipation
Sweating
Insomnia
Urinary retention
Miosis
Euphoria or dysphoria
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Withdrawal Effect
Buprenorphine withdrawal is generally milder than that which is experienced from full agonist. Buprenorphine must be tapered slowly due to its long half-life, which can cause withdrawal to kick in later than with the traditional fast-acting opiates. Buprenorphine withdrawal symptoms can linger for a few months, which is why a slow, modest taper is preferred to a quicker taper. Below are some possible withdrawal symptoms:
Depression/dysphoric mood
Nausea and vomiting
Muscle aches and cramps
Insomnia
Mild fever
Lacrimation
Rhinorrhea
Profuse sweating
Piloerection
Diarrhea
Frequent yawning
Drug craving
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Medical Treatment options
Buprenorphine is sometimes used only during the detox protocol with the purpose of reducing the patient's use of mood-altering substances. It considerably reduces opioid withdrawal symptoms that are normally experienced by opioid-dependent patients.
Psychological treatment options
Psychological treatment
Related drugs
The drugs that are similar to buprenorphine are:
Methadone
Naloxone
Diamorphine
Dihydrocodeine
Dextropropoxyphene
Dipipanone
Dextromoramide.
Related Synthetics
The related synthetics to buprenorphine are:
Oxycodone
Hydrocodone
Hydromorphone
Fentanyl
Methadone
Naloxone
References
[1] http://www.thatspoppycock.com/opiates/buprenorphine/
[2] http://www.rxlist.com/script/main/art.asp?articlekey=38304
[3] http://www.sobermd.us/drugs_details/buprenorphine
[4] http://www.drugs.com/sfx/buprenorphine-side-effects.html
[5] http://www.justice.gov/dea/concern/buprenorphine.html
Related Resources
http://www.rxlist.com/script/main/art.asp?articlekey=38304 - Click here
http://www.drugs.com/sfx/buprenorphine-side-effects.html - Click here
http://www.justice.gov/dea/concern/buprenorphine.html - Click here
Footnotes
Date Published | 10/03/2012 |
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Posting Date | 10/03/2012 |