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Buprenorphine , sold under the brand name Subutex, among others, is an opioid used to treat opioid addiction , moderate acute pain and moderate chronic pain. It is a semisynthetic derivative of thebaine. It is a mixed partial agonist opioid receptor modulator. Buprenorphine was approved for medical use in the United States in Its primary uses in medicine are in the treatment of those addicted to opioids, such as heroin and oxycodone , but it may also be used to treat pain, and sometimes nausea in antiemetic intolerant individuals, most often in transdermal patch form. It has veterinary medical use for treatment of pain in dogs and cats. Both buprenorphine and methadone are medications used for detoxification, short- and long-term opioid replacement therapy. Buprenorphine has the advantage of being only a partial agonist; hence negating the potential for life-threatening respiratory depression in cases of abuse. Rehabilitation programs consist of 'detox' and 'treatment' phases. The treatment phase begins once the person is stabilized and receives medical clearance. This portion of treatment consists of multiple therapy sessions, which include both group and individual counseling with various chemical dependency counselors, psychologists, psychiatrists, social workers, and other professionals. In addition, many treatment centers utilize twelve-step facilitation techniques, embracing the step programs practiced by such organizations as Alcoholics Anonymous and Narcotics Anonymous. Some people on maintenance therapies have veered away from such organizations as Narcotics Anonymous, instead opting to create their own twelve-step fellowships such as Methadone Anonymous or depart entirely from the twelve-step model of recovery, seeking a program which is secular and based on science such as SMART Recovery rather than faith. A transdermal patch is available for the treatment of chronic pain. It is not indicated for use in acute pain, pain that is expected to last only for a short period of time, or post-operative pain, nor is it indicated or recommended for use in the treatment of opioid addiction. 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. Buprenorphine treatment carries the risk of causing psychological or physical dependence. Buprenorphine has a slow onset, has a mild effect, and is very long acting with a half-life of 24 to 60 hours. Once a patient has stabilized on the drug, there are two treatment options: The most severe and serious adverse reaction associated with opioid use, in general, is respiratory depression, the mechanism behind fatal overdose. Buprenorphine behaves differently than other opioids in this respect, as it shows a ceiling effect for respiratory depression. Buprenorphine effects can be antagonised with a continuous infusion of naloxone. Concurrent use of buprenorphine with other CNS depressants such as alcohol or benzodiazepines is contraindicated as it may lead to fatal respiratory depression. Benzodiazepines, in recommended doses, are not contraindicated in individuals tolerant to either opioids or benzodiazepines. People on high-dose buprenorphine therapy may be unaffected by even large doses of opioids such as oxycodone , morphine , or hydromorphone. It is also 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 , \\\\\\\\\\\\\\[26\\\\\\\\\\\\\\] 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. 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 the bile. The elimination half-life of buprenorphine is 20—73 hours mean 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 \\\\\\\\\\\\\\[44\\\\\\\\\\\\\\] 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, remains an issue because it is a long-acting opiate. 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. Buprenorphine has been used in the treatment of the neonatal abstinence syndrome , \\\\\\\\\\\\\\[66\\\\\\\\\\\\\\] 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. Australian Medicines Handbook ed. American Society of Health-System Pharmacists. Retrieved 17 March Retrieved 25 February Veterinary Pharmacology and Therapeutics 9 ed. The Complete Drug Reference. Retrieved 6 April The Cochrane Database of Systematic Reviews 2: McGonagle D October Reducing the stigma of methadone use'. Retrieved 7 July Buprenorphine — The unique opioid analgesic. Archived from the original on 15 December Retrieved 15 December Annals of Internal Medicine. Retrieved 14 August 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'. 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. Journal of Clinical Psychopharmacology. Retrieved 21 September 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: Conotoxins Neosaxitoxin Saxitoxin Tetrodotoxin Others: Buprenorphine Evenamide Menthol mint Safinamide Tricyclic antidepressants. Atracotoxins Robustoxin , Versutoxin Ciguatoxins Poneratoxin. 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. Webarchive template wayback links Template: Views Read Edit View history. In other projects Wikimedia Commons. This page was last edited on 21 October , at By using this site, you agree to the Terms of Use and Privacy Policy. Sublingual , buccal , IM , IV , transdermal , intranasal , rectally , by mouth. 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.

Субутекс википедия

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Бупренорфин

Buprenorphine

Suboxone (Субоxоне)

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Suboxone (Субоxоне)

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Бупренорфин

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Бупренорфин

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Buprenorphine

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