Buprenex

This page contains recent news articles, when available, and an overview of Buprenex but does not offer medical advice. You should contact your physician with regard to any health issues or concerns.


Overview:

Buprenex
(when available)

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

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.

News Articles on Buprenorphine

Anti-heroin drug buprenorphine is best for helping addicts: study  -  Jun 26, 2008
Buprenorphine, which is marketed as Temgesic or Buprenex, was twice as effective as naltrexone (branded as Revia, Depade or Vivitrol) and the placebo in AFP

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Osteogenic Effects of Traumatic Brain Injury on Experimental ...  Apr 3, 2006
The animals were weighed on a digital scale and received an intramedullary injection of 0.2 mL of cefazolin and 0.1 mL of Buprenex (buprenorphine) into the ... - Journal of Bone and Joint Surgery

Brand Names/Synonyms:
Buprenex is also known by the following brand names and/or synonymsBuprenex; Buprenophine; Buprenorfina [Inn-Spanish]; Buprenorphine; Buprenorphine Hcl; BuprenorphineÊ; Buprenorphinum [Inn-Latin]; RX 6029M; Subutex; Temgesic

Drug Category:
Buprenex is categorized under the following by the FDA: Narcotics; Analgesics, Opioid; Narcotic Antagonists; ATC:N02AE01; ATC:N07BC01

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

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