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Buprenorphine , sold under the brand name Subutex, among others, is an opioid used to treat opioid addiction , acute pain , and chronic pain. Side effects may include respiratory depression decreased breathing , sleepiness, adrenal insufficiency , QT prolongation , low blood pressure , allergic reactions , and opioid addiction. Buprenorphine was approved for medical use in the United States in Its primary use is for the initial treatment of those with opioid addiction. Both buprenorphine and methadone are medications used for detoxification, short- and long-term opioid replacement therapy. Effectiveness of buprenorphine and methadone appear similar, with similar side effects. A transdermal patch is available for the treatment of chronic pain. Common adverse drug reactions associated with the use of buprenorphine are similar to those of other opioids and include: Constipation and CNS effects are seen less frequently than with morphine. The most severe side effect associated with buprenorphine is respiratory depression insufficient breathing. Buprenorphine treatment carries the risk of causing psychological or physical dependence. Buprenorphine has a slow onset and a long half-life of 24 to 60 hours. Once a person has stabilized on the medication, there are three options: It is difficult to achieve acute opioid analgesia in persons using buprenorphine for opioid replacement therapy. Buprenorphine has been reported to possess the following pharmacological activity: In simplified terms, buprenorphine can essentially be thought of as a non-selective, mixed agonist—antagonist opioid receptor modulator , \\\\\\\\\\\\\\\\\[28\\\\\\\\\\\\\\\\\] acting as a weak partial agonist of the MOR, an antagonist of the KOR, an antagonist of the DOR, and a relatively low-affinity, very weak partial agonist of the ORL Although buprenorphine is a partial agonist of the MOR, human studies have found that it acts like a full agonist with respect to analgesia in non-opioid-tolerant individuals. The active metabolites of buprenorphine are not thought to be clinically important in its central nervous system effects. Unlike some other opioids and opioid antagonists, buprenorphine binds only weakly to and possesses little if any activity at the sigma receptor. Buprenorphine also blocks voltage-gated sodium channels via the local anesthetic binding site, and this underlies its potent local anesthetic properties. Similarly to various other opioids, buprenorphine has also been found to act as an agonist of the toll-like receptor 4 , albeit with very low affinity. These glucuronides are then eliminated mainly through excretion into bile. The elimination half-life of buprenorphine is 20 to 73 hours mean 37 hours. Due to the mainly hepatic elimination, there is no risk of accumulation in people with renal impairment. The glucuronides of buprenorphine and norbuprenorphine are also biologically active , and represent major active metabolites of buprenorphine. It has a small antinociceptive effect and no effect on respiration. It has a sedative effect but no effect on respiration. Buprenorphine is a semi-synthetic analogue of thebaine \\\\\\\\\\\\\\\\\[46\\\\\\\\\\\\\\\\\] and is fairly soluble in water, as its hydrochloride salt. Buprenorphine and norbuprenorphine may be quantitated in blood or urine to monitor use or abuse, confirm a diagnosis of poisoning, or assist in a medicolegal investigation. There is a significant overlap of drug concentrations in body fluids within the possible spectrum of physiological reactions ranging from asymptomatic to comatose. Therefore, it is critical to have knowledge of both the route of administration of the drug and the level of tolerance to opioids of the individual when results are interpreted. Physical dependence and withdrawal from buprenorphine itself remain important issues since buprenorphine is a long-acting opioid. RX was named buprenorphine and began trials on humans in In the United States, buprenorphine Subutex and buprenorphine with naloxone Suboxone were approved for opioid addiction by the United States Food and Drug Administration in October Prior to the passage of this law, such treatment was not permitted in outpatient settings except for clinics designed specifically for drug addiction. The waiver, which can be granted after the completion of an eight-hour course, is required for outpatient treatment of opioid addiction with Subutex and Suboxone. Initially, the number of patients each approved physician could treat was limited to ten. This was eventually modified to allow approved physicians to treat up to a hundred patients with buprenorphine for opioid addiction in an outpatient setting. Buprenorphine is available under the trade names Cizdol, Suboxone, Subutex typically used for opioid addiction , Temgesic sublingual tablets for moderate to severe pain , Buprenex solutions for injection often used for acute pain in primary-care settings , Norspan and Butrans transdermal preparations used for chronic pain. Buprenorphine has been introduced in most European countries as a transdermal formulation marketed as Transtec for the treatment of chronic pain not responding to non-opioids. It has veterinary medical use for treatment of pain in dogs and cats. Some evidence supports the use of buprenorphine for depression. Buprenorphine has been used in the treatment of the neonatal abstinence syndrome , \\\\\\\\\\\\\\\\\[65\\\\\\\\\\\\\\\\\] a condition in which newborns exposed to opioids during pregnancy demonstrate signs of withdrawal. In one study, buprenorphine was found to be effective in a subset of individuals with treatment-refractory obsessive—compulsive disorder. From Wikipedia, the free encyclopedia. C Risk not ruled out. Journal of Clinical Pharmacology. American Society of Health-System Pharmacists. Retrieved 17 March Retrieved 12 December Retrieved 3 December Centers for Medicare and Medicaid Services. Retrieved 5 December The Cochrane Database of Systematic Reviews. Retrieved 7 July Buprenorphine — The unique opioid analgesic. British Journal of Anaesthesia. Annals of Internal Medicine. Retrieved 14 August A Unique Drug with Complex Pharmacology. Current Neuropharmacology, 2 4 , — Essentials of Pain Medicine E-Book. Br J Clin Pharmacol. Buprenorphine analgesia requires exon associated mu opioid receptor splice variants. Doweiko 14 March Concepts of Chemical Dependency. United States Pharmacopeial Convention. Drug Metabolism and Disposition. The Journal of Pharmacology and Experimental Therapeutics. Norbuprenorphine is a potent opioid agonist'. The Complete Drug Reference. Retrieved 6 April Disposition of Toxic Drugs and Chemicals in Man 8th ed. Annals of the New York Academy of Sciences. Problems of Drug Dependence, Food and Drug Administration October 8, Dying to be Free. Retrieved 25 February Veterinary Pharmacology and Therapeutics 9 ed. Asian journal of psychiatry. Pediatric Clinics of North America. The journal of pediatric pharmacology and therapeutics. Therapeutic Advances in Psychopharmacology. Analgesics N02A , N02B. Meclofenamic acid Mefenamic acid. Cannabidiol Cannabis Nabilone Nabiximols Tetrahydrocannabinol dronabinol. Gabapentin Gabapentin enacarbil Pregabalin Ziconotide. Carbamazepine Lacosamide Local anesthetics e. Treatment of drug dependence N07B. Tricyclic and tetracyclic antidepressants. Amoxapine Maprotiline Mianserin Mirtazapine Setiptiline. Atypical antipsychotics aripiprazole , brexpiprazole , lurasidone , olanzapine , quetiapine , risperidone Buspirone Lithium lithium carbonate , lithium citrate Thyroid hormones triiodothyronine T 3 , levothyroxine T 4. Agonists abridged; see here for a full list: KCNQ K v 7 -specific: Ranolazine Antiarrhythmics class I: Buprenorphine Evenamide Menthol mint Safinamide Tricyclic antidepressants. Retrieved from ' https: Alcohols Cat medications Dog medications Delta-opioid antagonists Drug rehabilitation Ethers Euphoriants Kappa antagonists Morphinans Mu-opioid agonists Nociceptin receptor agonists Nociceptin receptor antagonists Oripavines Phenols Semisynthetic opioids Sodium channel blockers. Views Read Edit View history. In other projects Wikimedia Commons. This page was last edited on 12 September , at By using this site, you agree to the Terms of Use and Privacy Policy. Under the tongue , through the cheek , IM , transdermal , intranasal , rectally , by mouth. Within 30 min \\\\\\\\\\\\\\\\\[3\\\\\\\\\\\\\\\\\]. Up to 24 hrs \\\\\\\\\\\\\\\\\[3\\\\\\\\\\\\\\\\\]. Values are K i nM , unless otherwise noted. The smaller the value, the more strongly the drug binds to the site. Calcium blockers Gabapentin Gabapentin enacarbil Pregabalin Ziconotide. Monoamine oxidase inhibitors Non-selective Irreversible: Adjunctive therapies Atypical antipsychotics aripiprazole , brexpiprazole , lurasidone , olanzapine , quetiapine , risperidone Buspirone Lithium lithium carbonate , lithium citrate Thyroid hormones triiodothyronine T 3 , levothyroxine T 4. Blockers K ATP -specific: Blockers BK Ca -specific: Blockers Amiloride Benzamil Triamterene. Blockers Glibenclamide Lonidamine Piretanide. TRPs See here instead.

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