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!]


FDA approvals - Avodart, Subutex, Suboxone
From American Family Physician, 11/15/02 by Carrie Morantz

* Dutasteride. The U.S. Food and Drug Administration (FDA) approved dutasteride (Avodart) for the treatment of symptomatic benign prostatic hyperplasia (BPH) in men with an enlarged prostate to improve urinary symptoms, reduce risk of acute urinary retention, and reduce the need for BPH-related surgery.

According to the manufacturer, dutasteride inhibits type 1 and type 2 enzymes responsible for the conversion of testosterone to dihydrotestosterone, the primary cause of prostate growth. Side effects may include impotence, decreased libido, breast tenderness, gynecomastia, and ejaculation disorders.

Women and children should not use dutasteride. Women who are pregnant or may become pregnant should not handle dutasteride because of the risk of absorbing dutasteride and the subsequent potential risk to a male fetus. Men treated with dutasteride should not donate blood until at least six months after their final dose to prevent giving the drug to a pregnant woman through a blood transfusion. Dutasteride is contraindicated in men with an allergic reaction to the drug or its ingredients.

* Buprenorphine. Buprenorphine hydrochloride (Subutex) and the combination buprenorphine hydrochloride and naloxone hydrochloride (Suboxone) have been approved for the treatment of opiate dependence. The agents treat opiate addiction by preventing symptoms of withdrawal from heroin and other opiates.

Buprenorphine only is intended for use at the beginning of treatment for drug abuse. Buprenorphine combined with the opiate antagonist naloxone is intended to be the formulation used in maintenance treatment of opiate addiction. Naloxone is added to buprenorphine to guard against intravenous abuse of buprenorphine by persons physically dependent on opiates.

The U.S. Drug Enforcement Administration (DEA) placed buprenorphine in Schedule III under the Controlled Substances Act. Buprenorphine is considered to have less risk for causing psychologic and physical dependence than the drugs in Schedule II (such as morphine, oxycodone, fentanyl, or methadone).

Buprenorphine can be prescribed in an office setting under the Drug Addiction Treatment Act (DATA) of 2000. Until recently, opiate dependence treatments in Schedule II, like methadone, could be dispensed in a very limited number of clinics that specialized in addiction treatment. As a consequence, there have not been enough addiction treatment centers to accommodate all patients desiring therapy. Under this new law, medications for the treatment of opiate dependence that are subject to less restrictive controls than those of Schedule II can be prescribed in a physician's office by specially trained physicians. This change is expected to provide patients greater access to needed treatment.

Side effects most commonly seen with the use of both drugs include cold or influenza-like symptoms, headaches, sweating, sleeping difficulties, nausea, and mood swings. Clinical data indicate that the risk of serious diminished breathing may be less with buprenorphine than other opioids when used in high doses or in overdose situations.

Buprenorphine has been associated with deaths related to diminished breathing, especially when used in combination with alcohol or other central nervous system depressant drugs, according to reports from France, where it has been available for several years.

A risk-management program has been designed to deter abuse and diversion from legitimate use by training physicians regarding proper use of these drugs, close monitoring of drug distribution channels, and child-resistant packaging.

DATA provisions include limits on the number of patients individual physicians are allowed to treat and special DEA registration for the use of this drug, thus providing additional safeguards as buprenorphine enters the office-based treatment setting.

The risk-management program also provides for active and passive surveillance to identify if and when the drugs are being abused. The surveillance will include interviews with substance abusers, monitoring local drug markets, data collection, and the monitoring of adverse event reports. Reports of the results of these surveillance efforts will enable the FDA to identify untoward effects from the availability of buprenorphine and, if indicated, to take appropriate actions to protect the public health.

COPYRIGHT 2002 American Academy of Family Physicians
COPYRIGHT 2002 Gale Group

Return to Suboxone
Home Contact Resources Exchange Links ebay