Subutex - General Information:A derivative of the opioid alkaloid thebaine that is a more potent and longer lasting analgesic than morphine. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use. [PubChem]
Pharmacology:Subutex is a synthetic opioid analgesic and thebaine derivative, with a longer duration of action than morphine. Subutex 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. Subutex 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. Subutex depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.
Subutex for patients
Your doctor has ordered buprenorphine, a strong analgesic (painkiller), to relieve your pain. The drug will be added to an intravenous fluid that will drip through a needle or catheter placed in your vein. You will probably receive sufentanil continuously for around-the-clock pain relief. Your doctor also may order other pain medications to make you feel more comfortable. This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information. Your health care provider (doctor, nurse, or pharmacist) may measure the effectiveness and side effects of your treatment using laboratory tests and physical examinations. It is important to keep all appointments with your doctor and the laboratory. The length of treatment depends on how you respond to the medication.
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.
SUBOXONE and SUBUTEX should not be administered to patients who have been shown to be hypersensitive to buprenorphine, and SUBOXONE should not be administered to patients who have been shown to be hypersensitive to naloxone.
Additional information about SubutexSubutex Indication: For the treatment of moderate to severe pain, peri-operative analgesia, and opioid dependence.
Mechanism Of Action: Subutex's analgesic effect is due to partial agonist activity at mu-opioid receptors. Subutex 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 Interactions: Not Available
Food Interactions: Not Available
Generic Name: Buprenorphine
Synonyms: Buprenorfina [Inn-Spanish]; Buprenophine; Buprenorphine Hcl; Buprenorphinum [Inn-Latin]
Drug Category: Narcotics; Analgesics, Opioid; Narcotic Antagonists
Drug Type: Small Molecule; Illicit; Approved; Investigational
Other Brand Names containing Buprenorphine: Buprenex; Subutex; Temgesic;
Absorption: 31% bioavailability (sublingual)
Toxicity (Overdose): Manifestations of acute overdose include pinpoint pupils, sedation, hypotension, respiratory depression and death.
Protein Binding: 96%
Biotransformation: Hepatic. Buprenorphine undergoes both N-dealkylation to norbuprenorphine and glucuronidation. The N-dealkylation pathway is mediated by cytochrome P-450 3A4 isozyme. Norbuprenorphine, an active metabolite, can further undergo glucuronidation.
Half Life: 37 hours
Dosage Forms of Subutex: Tablet Sublingual
Chemical IUPAC Name: Not Available
Chemical Formula: C29H41NO4
Buprenorphine on Wikipedia: http://en.wikipedia.org/wiki/Buprenorphine
Organisms Affected: Humans and other mammals
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