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Buprenorphine

From Academic Kids

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Buprenorphine.png
Chemical structure of buprenorphine.


Buprenorphine
(2S) - 2 - [ (-) - (5R, 6R, 7R, 14S) - 9a - cyclopropylmethyl - 4,5 - epoxy - 3 - hydroxy - 6 - methoxy - 6,14 - ethanomorphinan - 7 - yl] - 3,3 - dimethylbutan - 2 - ol
Empiric formula C29H41NO4
Molecular weight 467.64
Bioavailability ?
Metabolism Liver
Elimination half life 35 h
Excretion Bile and urine
ATC code N02AE01 / N07BC01
Pregnancy category C (USA)

Buprenorphine is a partial opioid agonist and also an opioid antagonist. It came out as an analgesic in the 1980s, but is nowadays used also for the treatment of opioid addiction. It is sold under trade names such as Temgesic (sublingual tablet of pure Buprenorphine, used mostly outside the US), Buprenex (pure injectable buprenorphine), Subutex(lemon-lime flavored sublingual) Subutex is an oval shaped tablet in 2mg,4mg, and 8mg dosages. Subutex contains pure Buprenorphine, Suboxone(orange-tang flavored sublingual) Suboxone is a 6 sided hexagon shaped tablet, comes in 2mg, 4mg, and 8mg dosages. Suboxone is combined with naloxone). The naloxone is to deter addicts from trying to inject the tablet. Buprenorphine is a Schedule III drug under the Convention on Psychotropic Substances[1] (http://www.incb.org/pdf/e/list/green.pdf).

Contents

Mode of action

Buprenorphine is a thebaine derivative, and its analgesic effect is due to agonism of μ subtype of opioid receptor. Buprenorphine is also a κ- antagonist. Unlike other opioids, naloxone can only partially revert the effects of buprenorphine. Buprenophine has quite a long effect, 48 hours, due to its slow dissociation from the opioid receptors. Patients build tolerance towards buprenorphine fairly quickly.

Pharmacokinetics

Buprenorphine is administered as hydrochloride as either intramuscular or intravenous injection or as sublingual tablets. It is not administered orally, due to very high first-pass metabolism. Burenorphine is metabolised in the liver into an active metabolite, norbuprenorphine by N-dealkylation via CYP-3A4. The metabolites are further conjugated with glucuronic acid and eliminated mainly through excretion into the bile.

See Instant Detox (http://www.wired.com/wired/archive/13.01/detox.html) and The Bitter Pill (http://www.wired.com/wired/archive/13.04/bupe.html) from Wired magazine.

Side effects

Most common side effects are drowsiness, nausea, sweating and dizziness. High doses can also cause respiratory depression, which can be dangerous, for there is no dependable antagonist. Buprenorphine causes addiction, but mainly psychological dependence.

There is debate as to whether Buprenorphine has the potential to cause liver damage in some patients. Due to the potential threat of developing jaundice of the liver, it is recommended that doctors refrain from prescribing this synthetic opiod to any patient suffering from liver or kidney problems.

Treatment

Buprenorphine is starting to have incredable sucess in treating opioid addiction (ex. heroin, oxycodone, hydrocodone, morphine, and hydromorphone) This has much to do with the creation of Suboxone and Subutex. Prior to these new sublingual (when a pill is to be disolved under the tounge, so that the medication can be absorbed into the many tiny veins that reside there) tablets, Buprenorphine could only be administered by injection. Even then, the medication was mostly used in hospitals for adressing pain. Only recently has Buprenorphine been approved for treatment of opiate addiction. Unfortunatly there are strict laws in the US to control the drug. The Government is very worried about diversion of this medicine. So Doctor's are legally allowed only 30 patient's in which they may prescribe the drug for maintenance. Even then, not just any doctor can prescribe this medication, only those who have attained a special certification in opiate treatment. The result is that there are many addicts who want help, and not enough doctors to help them all. So many addicts are forced to wait on long waiting list's.

Buprenorphine vs. Methadone

Buprenorphine and Methadone are both used for short term and long term maintenance. There are diffrences though and Buprenorphine has many benefits over methadone maintenance for opiate dependent people. The first has mostly to do with conveniance. Once an addict has found a doctor who can help, they're usually prescribed a month's worth of the drug in which they can fill in a pharmacy and take home. The only requirment is that the patient must receive some kind of addiction therapy during the time they take the drug. Each Buprenorphine pill's effects last nearly 48 hours. It is common for people to take a dose every 2 days, but many also take a dose every day. With Methadone, most patient's must visit a methadone clinic everyday for a dose that will last 24 hours. Take home pills are only dispensed on weekends, or to people in long term good standing. The second benefit of Buprenorphine has to do with addiction to the treatment drugs themselves. Both Buprenorphine and Methadone are addictive opiate substances. They work by filling the opiate receptors of the brain so that the patient feels no physical need for the opiate they originally had a problem with. (mainly heroin) However, while Buprenorphine is addictive (more mentally then physically) the doctor will always taper the dose for the patient at a very slow rate. Sometimes even down to dosage's as small as 1mg. This completly eliminates any physical discomfort of withdrawl. Addiction therapy continues to help with any psychological dependence. The diffrence with Methadone in this area is that it is far more physically and psychologicaly addictive. Often addicts who start with heroin and go into Methadone treatment end up with a even more nasty addiction. People often end up taking Methadone for the rest of their lives because of this, while most Buprenorphine patients stop the drug within a week to a couple years. This is the case because Methadone stays in the body's system for a long time. So quitting Methadone has even more severe withdrawl symptoms then heroin itself. There are also large numbers of people who go into Buprenorphine treatment to get help detoxing from Methadone. Also of note, Buprenorphine dosn't cause anywhere near the amount of pleasurable opiate effects as Methadone. This causes less diversion of Buprenorphine then Methadone.

Buprenorphine in Inpatient Rehabilitation Hospitals

The practice of using Buprenorphine (Subutex or Suboxone) in a inpatient rehab setting is increasing rapidly. These hospital's usually offer two programs. These are Detox, and Treatment. Detox usually includes medicated detoxing from the drug of dependency as well as therapy. Treatment starts after a person has detox'd and includes lots of therapy. Patient's who go into rehab by there own choice (not forced by law enforcement) can often choose to go only for detox, or for both detox and treatment. Though completing both programs is recommended. Most patient's will stay as long as their insurance will pay for it (many stay from 90 days to 6 months). The Buprenorphine is only used during the Detox portion of the program. Buprenorphine is a godsend for addict's during this time because it completly eliminates all the horrible withdrawl symptoms they would normally experience if quitting a drug like heroin cold turkey. Detox programs usually last for around 6 to 7 days. During this time suboxone or subutex will be administered by a nurse. Generally the patient will receive 2 dose's each day. Most often during day 1-3 each day's dose usually totals around 8-16mg.(of either suboxone or subutex) After that the dosage is slowly tapered each day and the medication is usually stopped 1 day prior to the end of the detox program.


Where to find doctors that can prescribe you Buprenorphine to help you get over your addiction

The following website is a directory of all the doctors in the United States who can prescribe this medication: http://www.suboxone-directory.com/


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