buprenorphine (thing)

Pharmacologic class

semisynthetic opioid, narcotic analgesic

Buprenex (low-dose injectable solution, 0.3 mg/ml)
Subutex, Subozone (sublingual tablets, 0.4, 2 and 8 mg)
Temgesic (sublingual tablets, 0.2 and 0.4 mg, low-dose injectable solution, 0.3 mg/ml)

opiate addiction with severe withdrawal symptoms
moderate to severe pain

mu opioid partial agonist
kappa opioid antagonist
delta opioid agonist

use of benzodiazepines (possible interactions include breathing difficulties, coma and death)

recommended not to be used with MAO inhibitors
use with caution in respiratory compromise, and impaired liver or renal function

Used with other central nervous system depressants such as anesthetic agents, antihistamines, phenothiazines, barbiturates and tranquilizers, may increase CNS and respiratory depression

CNS: sedation, confusion, lethargy, agitation
CV: bradycardia
respiratory: decreased respiration rate
GI: constipation
GU: urinary retention
skin: itching

Buprenorphine is derived from the morphine alkaloid thebaine. It is most commonly used in the treatment of opiate addiction.
Buprenorphine has a rather significant abuse potential, although it causes significantly less euphoria than heroin or methadone. However, in a recent study it was found that using a combination naloxone-buprenorphine pill significantly reduces the abuse potential, as naloxone prevents euphoria by blocking the opioid receptor sites.
Buprenorphine is currently not approved and consequently not legally available in the US for the treatment of opiate addiction, except when used as an investigational new drug.
Several NIDA-funded studies have found that buprenorphine is a safe and effective treatment for opiate addiction. Particularly, it was found that buprenorphine is more effective than the current standard opiate substitution drug, methadone.
Buprenorphine is currently in schedule V in the US, but DEA is proposing a rescheduling to schedule III.
In Finland, Pentti Karvonen, a doctor who imported Subutex and Temgesic tablets from France and prescribed them to addicts as part of a substitution treatment program was sentenced to jail for five years. During the trial, the leader of the Finnish National Public Health Institute's drug laboratory testified that buprenorphine has an abuse potential comparable to that of heroin. (Note that heroin is Schedule I.)
Methadone treatment is problematic, since methadone is addictive. Buprenorphine, while effectively helping alleviate withdrawal symptoms, has a much lower addiction potential and is therefore much better in treatment that aims to end a person's opiate addiction once and for all.
From 1994 to 1998 in France, buprenorphine was implicated in 1.4 times more deaths than methadone. However, since the number of buprenorphine users was 14 times greater, it was found that buprenorphine is a much safer drug.
Buprenorphine tablets are to be placed under the tongue and allowed to dissolve. Chewing or swallowing them will make them ineffective. Buprenorphine is sometimes injected, particularly when used as a substitute for street heroin. Reports state that some addicts prefer injected buprenorphine to low-quality street heroin. Dosages range from 4 to 32 milligrams per day for heroin dependence.

August 8th, 2002