Buprenorphine chemical structure
Find information on thousands of medical conditions and prescription drugs.

Suboxone

Buprenorphine, also colloquially referred to as bupe, is an opioid drug with partial agonist and antagonist actions. Buprenorphine hydrochloride was first marketed in the 1980s by Reckitt & Colman (now Reckitt Benckiser) as an analgesic, yet is now primarily used for the treatment of opioid addiction. It is a Schedule III drug under the Convention on Psychotropic Substances. more...

Home
Diseases
Medicines
A
B
C
D
E
F
G
H
I
J
K
L
M
N
O
P
Q
R
S
Growth hormone
Salbutamol
Salmeterol
Sandimmune
Sandostatin
Sansert
Saquinavir
Sarafem
Satric
Scopolamine
Seasonale
Secobarbital
Secretin
Selegiline
Semprex-D
Sensipar
Sensorcaine
Serax
Serevent
Serine
Seroquel
Serostim
Serrapeptase
Sertindole
Sertraline
Serzone
Sevelamer
Sevoflurane
Sibutramine
Sildenafil
Silibinin
Simvastatin
Sinemet
Sinequan
Singulair
Sirolimus
Skelaxin
Sodium cyclamate
Solage
Soma
Somatostatin
Sotahexal
Sotalol
Sotret
Spiperone
Spiriva
Spironolactone
Sporahexal
Sporanox
SPS
SSD
Stanozolol
Stavudine
Stelazine
Stilbestrol
Stilbetin
Stimate
Stiripentol
Strattera
Streptokinase
Streptomycin
Suboxone
Subutex
Sucralfate
Sucralfate
Sufentanil
Sulbactam
Sulfamethoxazole
Sulfanilamide
Sulfasalazine
Sulforidazine
Sulla
Sulpiride
Sultamicillin
Sumatriptan
Suprefact
Suramin sodium
Sustaire
Sustiva
Suxamethonium chloride
Symmetrel
Synarel
Synercid
Synthroid
Syntocinon
Zaleplon
T
U
V
W
X
Y
Z

Commercial preparations

Britsh firm Reckitt & Colman (now Reckitt Benckiser) first marketed buprenorphine under the trade names Temgesic (sublingual/parenteral preparations, no active additives) and Buprenex (parenteral, no active additives). Two more recent formulations from Reckitt Benckiser have been approved for opioid addiction treatment in the U.S.: Subutex (lemon-lime flavored sublingual, no active additives; in 2mg and 8mg dosages) and Suboxone (orange-tang flavored sublingual, one part naloxone for every four parts buprenorphine; hexagon shaped tablet in 2mg and 8mg dosages). Suboxone contains the opioid antagonist naloxone to deter illicit intravenous preparation of the tablet, this is intended to attenuate the effects of buprenorphine on opioid-naive users should this formulation be injected - however no human studies have been done demonstrating the efficacy of this approach with buprenorphine. It must also be noted that buprenorphine in and of itself will induce a precipitated withdrawal syndrome if ingested by an acutely opioid dependant/intoxicated individual.

Buprenorphine is also delivered transdermally in 25, 50 and 75 mcg/hour. The trade name in the UK is Transtec, and manufactured by Napp. A new 5, 10 and 20 mcg/hour patch marketed as Bu'7rans (Bu-trans), where the 7 indicates its once weekly dosage for pain in osteoarthritis.

Pharmacology and pharmacokinetics

Buprenorphine is a thebaine derivative, and its analgesic effect is due to partial agonist activity at μ-opioid receptors. Buprenorphine is also a κ-opioid receptor antagonist. The partial agonist activity means that opioid receptor antagonists (e.g., an antidote such as naloxone) only partially reverse the effects of buprenorphine.

Buprenorphine hydrochloride is administered by intramuscular injection, intravenous infusion, via a transdermal patch, or as a sublingual tablet. It is not administered orally, due to very high first-pass metabolism. Buprenorphine is metabolised by the liver, via the CYP3A4 isozyme of the cytochrome p450 enzyme system, into norbuprenorphine (by N-dealkylation) and other metabolites. The metabolites are further conjugated with glucuronic acid and eliminated mainly through excretion into the bile. The elimination half-life of buprenorphine is 20.4–72.9 hours (mean 34.6).

Clinical use

Buprenorphine is indicated for the treatment of moderate to severe pain, peri-operative analgesia, and opioid dependence. It has a longer duration of action than morphine, and sublingual tablets offer an analgesic effect for 6 to 8 hours. (Joint Formulary Committee, 2004) Australian guidelines recommend against the use of buprenorphine as an analgesic because: its effect is not reversed by naloxone, it may precipitate withdrawal symptoms in people dependent on other opioids, and it may cause dependence itself and has potential for misuse. (Rossi, 2005) When used for opioid dependence, buprenorphine remains effective in the body for up to 48 hours, curbing withdrawal symptoms and counteracting other opioids that may be administered to the patient (licitly or illicitly).

Read more at Wikipedia.org


[List your site here Free!]


Office based therapy for opiate addiction successful
From Nevada RNformation, 11/1/03

"Option Can Increase Number of Patients Seeking Treatment"

The recent U.S. Food and Drug Administration approval of buprenorphine and of a combination product containing buprenorphine and naloxone, developed through more than a decade of research supported by the National Institute on Drug Abuse, National Institutes of Health, has opened the door to mainstream medical treatment for people addicted to opiates, such as heroin and morphine. Now, results of a 2-part, multicenter, clinical trial published in the September 4 issue of the New England Journal of Medicine, provides additional insight into the utility of this treatment outside the traditional addiction treatment clinic setting.

"Buprenorphine represents a major step forward in the treatment of opiate addiction," says Dr. Nora D. Volkow, NIDA Director. "It allows physicians to treat patients for this disease in the same manner that other people are treated for such other chronic illnesses as diabetes or high blood pressure. Office-based buprenorphine increases the availability of therapy by offering patients greater flexibility in treatment scheduling and integration with the mainstream public for their health services."

"Other agonist therapy for opiate addiction is given in a highly regulated setting, which may dissuade many addicted people from seeking help," say lead authors Dr. Paul J. Fudala and T. Peter Bridge.

Dr. Fudala, of the VA Medical Center and University of Pennsylvania School of Medicine, Philadelphia, and Dr. Bridge, then with NIDA/NIH, were the national co-principal investigators of this 2-part trial. In the 4-week component, participants who received office-based treatment with buprenorphine in combination with naloxone (SUBOXONE) fared significantly better than opiate addicts given a placebo. In the other phase of the study, which lasted up to 1 year, buprenorphine and naloxone were administered together in an office-based setting and observations were made about the practicality of this treatment.

Trial participants received treatment at sites in Boston; Cincinnati; Chicago (Hines), Illinois; Los Angeles; New York City; Philadelphia; San Francisco; West Haven, Connecticut; Baltimore; Miami; New Orleans; and San Juan, Puerto Rico.

Buprenorphine is pharmacologically related to morphine. Although the subjective effects of buprenorphine closely resemble those of other opioids, these effects are less dose-dependent than those drugs and a "ceiling effect" has been demonstrated for many of the actions of buprenorphine. Buprenorphine also appears to have somewhat lower abuse potential than drugs such as morphine, heroin, and similar agents.

"Office-based treatment with buprenorphine is a powerful tool in the repertoire of drug-abuse treatment advances that have resulted from NIDA-supported research," says Dr. Volkow. "It does not replace medications now used to treat opiate addiction, but it will help fill the gap in treatment for the more than 1 million Americans addicted to these drugs."

Health Care Providers wishing to provide buprenorphine to their patients must take 8 hours of training and be certified by the U.S. Department of Health and Human Services' Substance Abuse and Mental Health Services Administration.

The National Institute on Drug Abuse is a component of the National Institutes of Health, U.S. Department of Health and Human Services. NIDA supports more than 85 percent of the world's research on the health aspects of drug abuse and addiction. The Institute carries out a large variety of programs to ensure the rapid dissemination of research information and its implementation in policy and practice. Fact sheets on the health effects of drugs of abuse and information on NIDA research and other activities can be found on the NIDA home page at .

Copyright Nevada Nurses Association Nov 2003
Provided by ProQuest Information and Learning Company. All rights Reserved

Return to Suboxone
Home Contact Resources Exchange Links ebay