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
Interactions:
DrugBank: Interactions for Buprenorphine
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
Buprenorphine News (When available)
Small businesses garner 18% more in loans in '0505 Jan 2006 Albany Times Union, American Bio launches new drug-testing kit KINDERHOOK -- American Bio Medica Corp. has begun offering a test to detect the presence of buprenorphine in urine. ...
American Bio Medica Offers Test for BuprenorphineJan 3, 2006 Genetic Engineering News, NASDAQ: ABMC) today announced they have begun offering a point of collection drug screen that detects the presence or absence of buprenorphine in a urine ...
Lewistown gives NYC pointers in heroin warJan 1, 2006 Patriot-News, And, thanks to the use of a relatively new medication called buprenorphine, lives shattered by drug abuse were being put back together. ...
Police bust two with 268 kg of hashishJan 3, 2006 Kantipur Online, In yet another incident, police yesterday arrested Yadav Timilsina of Parsa and Jokhu Raut of Birgunj with 831 ampules of Buprenorphine injection from Jhonchhe ...
Delegation: Ease access to addiction medicationDec 10, 2005 MaineToday.com, ...the federal government to exempt the state's doctors from a rule that says each can treat no more than 30 opiate-dependent patients with the drug buprenorphine ...
Heroin returns to Finnish drug scene, several deaths this yearDec 19, 2005 Helsingin Sanomat, There was a gap in the market, and many addicts took to intravenous use of buprenorphine, a drug commonly used in pill form in the weaning of addicts from ...
Addicts Buying Dangerous Drug 'Cocktails' at ClinicsDec 23, 2005 Inter Press Service (subscription), Drug substitutes such as Subutex (buprenorphine) or, more recently in Malaysia, methadone, are legitimately used by doctors to reduce the craving among drug ...
IOM Report Focuses on the "Quality Chasm" in Mental Health and ...Dec 15, 2005 Psychiatric Services (subscription) The TIP also outlines best practices in the use of methadone, buprenorphine, and naltrexone, including appropriate dosages of medication, medically supervised ...
Doctor now focuses on disputed skin diseaseDec 14, 2005 Santa Fe New Mexican, He also helped her get off methadone by providing her with Subatex and Suboxone, which both contain buprenorphine and are used to fight opiate addictions. ...
Pankaj Talukder (Narinjara News)Dec 2, 2005 Narinjara News, The drugs like spasoproxybone, ganja, alcohol, phensedyle, opium, cough syrup, nitrazepam, detroproxythene and buprenorphine are used by the addicts. ...
Drug dependence specialist takes UAMS addiction chairDec 4, 2005 Arkansas Democrat-Gazette (subscription), ...to study the behavioral economics of drug choice, impulsivity in drug dependence and improving combined behavioral treatment with buprenorphine, a new ...
DESPERATE HOUSEWIVES� NOT DESPERATE ENOUGHJan 3, 2006 I-Newswire.com (press release) REAL DESPERATE HOUSEWIVES have our own stash of Xanax, Prozac, Valium, Ativan, Buprenex, Oxycontin, Soma, Hydroxyzine, Ultram, Vicodin, Darvon, Tylenol with ...
Sleeping Through Detox Poses HazardsJan 12, 2006 Psychiatric Times, A randomized trial comparing anesthesia-, buprenorphine- (Subutex) and clonidine- (Catapres) assisted heroin detoxification found similarity in withdrawal ...
Addicts Buying Dangerous Drug 'Cocktails' at ClinicsDec 23, 2005 Inter Press Service (subscription), Drug substitutes such as Subutex (buprenorphine) or, more recently in Malaysia, methadone, are legitimately used by doctors to reduce the craving among drug ...