Buprenex: profile and news

Meditoxofpalmbeach Offers A New Approach to Opiate Dependency May 28, 2005
Buprenorphine, a derivative of thebaine, is an opioid that has been marketed in the United States as the Schedule V parenteral analgesic Buprenex. ... - PR Web (press release),

Area police probe burglaries, assaults Mar 31, 2005
Officer Riley Day made the initial report, which said that stolen were medications including Ketamine, Valium, Buprenex, Hodromorphone, Demorol, Torbugesic ... - Sherman Denison Herald Democrat,

Buprenex Opiate Assisted Protocol Provides Better Drug ... Feb 11, 2005
New Buprenex Opiate Assisted Withdrawal protocol to help addicts with pain free detox is offered by Support Systems Homes, Inc. ... - RxPG NEWS,

Other information

Indication
For the treatment of moderate to severe pain, peri-operative analgesia, and opioid dependence.

Pharmacology
Buprenorphine is a synthetic opioid analgesic and thebaine derivative, with a longer duration of action than morphine. Buprenorphine interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, spinal cord, and other tissues. In clinical settings, buprenorphine exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Buprenorphine may increase the patient's tolerance for pain and decrease the perception of suffering, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Buprenorphine depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.

Mechanism Of Action
Buprenorphine's analgesic effect is due to partial agonist activity at mu-opioid receptors. Buprenorphine is also a kappa-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. The binding to the mu and kappa receptors results in hyperpolarization and reduced neuronal excitability.

Drug Category
Narcotics; Analgesics, Opioid; Narcotic Antagonists; ATC:N02AE01; ATC:N07BC01

Brand Names/Synonyms
Buprenex; Buprenophine; Buprenorfina [Inn-Spanish]; Buprenorphine; Buprenorphine Hcl; BuprenorphineÊ; Buprenorphinum [Inn-Latin]; RX 6029M; Subutex; Temgesic

Dosage Forms
TABLET (SUBLINGUAL)

Absorption
31% bioavailability (sublingual)

Interactions
Interactions for Buprenorphine:

Buprenorphine is metabolized to norbuprenorphine by cytochrome CYP 3A4. Because CYP 3A4 inhibitors may increase plasma concentrations of buprenorphine, patients already on CYP 3A4 inhibitors such as azole antifungals (e.g. ketoconazole), macrolide antibiotics (e.g. erythromycin), and HIV protease inhibitors (e.g. ritonavir, indi-navir and saquinavir) should have their dose of SUBUTEX or SUBOXONE adjusted.

Based on anecdotal reports, there may be an interaction between buprenorphine and benzodiazepines. There have been a number of reports in the post-marketing experience of coma and death associated with the concomitant intravenous misuse of buprenorphine and benzodiazepines by addicts. In many of these cases, buprenorphine was misused by self-injection of crushed SUBUTEX tablets. SUBUTEX and SUBOXONE should be prescribed with caution to patients on benzodiazepines or other drugs that act on the central nervous system, regardless of whether these drugs are taken on the advice of a physician or are taken as drugs of abuse. Patients should be warned of the potential danger of the intravenous self-administration of benzodiazepines while under treatment with SUBOXONE or SUBUTEX.

Chemical IUPAC Name
Not Available

Chemical Formula
C29H41NO4

Half Life
37 hours

Drug Type
Approved Drug

# Accession No
APRD00670

CAS Registry Number
52485-79-7