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Encyclopedia > Buprenorphine
Buprenorphine
Systematic (IUPAC) name
(2S)-2-[(-)-(5R,6R,7R,14S)-
9α-cyclopropylmethyl-4,5-epoxy-
6,14-ethanomorphinan-7-yl]-3-hydroxy-
6-methoxy-3,3-dimethylbutan-2-ol
Identifiers
CAS number 52485-79-7
ATC code N02AE01 N07BC01
PubChem 40400
DrugBank APRD00670
Chemical data
Formula C29H41NO4 
Mol. mass 467.64 g/mol
Pharmacokinetic data
Bioavailability 31% (sublingual, from ethanolic solution)
~50-60% (sublingual, high-dose tablet)
~50% (transdermal)
Protein binding 96%
Metabolism hepatic
Half life 37 hours
Excretion biliary and renal
Therapeutic considerations
Pregnancy cat.

C (USA) Image File history File links No higher resolution available. ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... A chemical formula is a concise way of expressing information about the atoms that constitute a particular chemical compound. ... For other uses, see Carbon (disambiguation). ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, symbol, number nitrogen, N, 7 Chemical series nonmetals Group, period, block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... General Name, symbol, number oxygen, O, 8 Chemical series nonmetals, chalcogens Group, period, block 16, 2, p Appearance colorless (gas) very pale blue (liquid) Standard atomic weight 15. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... “Grain alcohol” redirects here. ... A drugs efficacy may be affected by the degree to which it binds to the proteins within blood plasma. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... For the bird, see Liver bird. ... It has been suggested that Effective half-life be merged into this article or section. ... The kidneys are important excretory organs in vertebrates. ... Bile (or gall) is a bitter, yellow or green alkaline fluid secreted by hepatocytes from the liver of most vertebrates. ... Kidneys viewed from behind with spine removed The kidneys are bean-shaped excretory organs in vertebrates. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ...

Legal status

Schedule III (USA)
Schedule 8 (Aust)
Schedule III (UK)
Cat. A{Singapore} The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... For other uses, see Australia (disambiguation). ...

Routes sublingual, IM, IV,transdermal

Buprenorphine, is an opioid drug with partial agonist and antagonist actions. Buprenorphine hydrochloride was first marketed in the 1980s by Reckitt & Colman (now Reckitt Benckiser) as an analgesic, available generally as Buprenex in a 0.3 mg/ml injectable formulation in the United States. In October 2002, the FDA additionally approved Suboxone and Subutex, buprenorphine's high-dose sublingual pill preparations for opioid addiction, and as such the drug is now also used for this purpose. It has been a Schedule III drug under the Convention on Psychotropic Substances[1] since it was rescheduled from Schedule V (the schedule with the lowest restrictions and penalties) just before FDA approval of Suboxone and Subutex. In the recent years, buprenorphine has been introduced in most European countries as transdermal formulation ("patch") for the treatment of chronic pain. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body. ... Sublingual, literally under the tongue, from Latin, refers to a pharmacological route of administration in which certain drugs are entered directly into the bloodstream via absorption under the tongue. ... Intramuscular injection is an injection of a substance directly into a muscle. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... A transdermal patch is a medicated adhesive patch that is placed on the skin to deliver a time released dose of medication through the skin and into the bloodstream. ... An opioid is a chemical substance that has a morphine-like action in the body. ... For other meanings, see Drug (disambiguation). ... Agonists An agonist is a substance that binds to a receptor and triggers a response in the cell. ... Antagonists will block the binding of an agonist at a receptor molecule, inhibiting the signal produced by a receptor-agonist coupling. ... In chemistry, hydrochlorides are salts resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base (mostly amines). ... Reckitt Benckiser plc is one of the worlds leading manufacturers of cleaning products and a member of the FTSE 100 Index of the largest companies traded on the London Stock Exchange. ... An analgesic (colloquially known as a painkiller) is any member of the diverse group of drugs used to relieve pain (achieve analgesia). ... The United States Food and Drug Administration is the government agency responsible for regulating food, dietary supplements, drugs, cosmetics, medical devices, biologics and blood products in the United States. ... Sublingual, literally under the tongue, from Latin, refers to a pharmacological route of administration in which certain drugs are entered directly into the bloodstream via absorption under the tongue. ... An opioid is a chemical substance that has a morphine-like action in the body. ... For other uses, see addicted. ... The Controlled Substances Act (CSA) was enacted into law by the Congress of the United States as Title II of the Comprehensive Drug Abuse Prevention and Control Act of 1970. ... Convention on Psychotropic Substances Opened for signature February 21, 1971 in Vienna Entered into force August 16, 1976 Conditions for entry into force 40 ratifications Parties 175 The Convention on Psychotropic Substances is a United Nations treaty designed to control psychoactive drugs such as amphetamines, barbiturates, and psychedelics. ... The Controlled Substances Act (CSA) was enacted into law by the Congress of the United States as Title II of the Comprehensive Drug Abuse Prevention and Control Act of 1970. ...

Contents

Commercial preparations

British firm Reckitt & Colman (now Reckitt Benckiser) first marketed buprenorphine under the trade names Temgesic (sublingual/parenteral preparations, no active additives) and Buprenex (parenteral, no active additives). Two more recent formulations from Reckitt Benckiser have been approved for opioid addiction treatment in the U.S.: Subutex (bitter sublingual, no active additives; in 2 mg and 8 mg dosages) and Suboxone (Lemon-lime flavored sublingual, one part naloxone for every four parts buprenorphine; hexagon shaped tablet in 2 mg and 8 mg dosages). Suboxone contains opiate agonist as well as the opioid antagonist naloxone to deter illicit intravenous preparation of the tablet. This is intended to attenuate the effects of buprenorphine on opioid-naive users should this formulation be injected - however no human studies have been done demonstrating the efficacy of this approach with buprenorphine and a growing number of street reports indicate that the naloxone is ineffective. Reckitt Benckiser plc is one of the worlds leading manufacturers of cleaning products and a member of the FTSE 100 Index of the largest companies traded on the London Stock Exchange. ... For the magazine, see Marketing (magazine). ... Sublingual, literally under the tongue, from Latin, refers to a pharmacological route of administration in which certain drugs are entered directly into the bloodstream via absorption under the tongue. ... In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... Food additives are substances added to food to preserve flavor or improve its taste and appearance. ... In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... Food additives are substances added to food to preserve flavor or improve its taste and appearance. ... Formulation ... Reckitt Benckiser plc is one of the worlds leading manufacturers of cleaning products and a member of the FTSE 100 Index of the largest companies traded on the London Stock Exchange. ... The United States, the FDA approves drugs. ... An opioid is a chemical substance that has a morphine-like action in the body. ... For other uses, see addicted. ... Motto: (Out Of Many, One) (traditional) In God We Trust (1956 to date) Anthem: The Star-Spangled Banner Capital Washington D.C. Largest city New York City None at federal level (English de facto) Government Federal constitutional republic  - President George Walker Bush (R)  - Vice President Dick Cheney (R) Independence from... Sublingual, literally under the tongue, from Latin, refers to a pharmacological route of administration in which certain drugs are entered directly into the bloodstream via absorption under the tongue. ... Food additives are substances added to food to preserve flavor or improve its taste and appearance. ... “Kg” redirects here. ... “Kg” redirects here. ... “Lymon” redirects here. ... Sublingual, literally under the tongue, from Latin, refers to a pharmacological route of administration in which certain drugs are entered directly into the bloodstream via absorption under the tongue. ... Naloxone is a drug used to counter the effects of opioid overdose, for example heroin and morphine overdose. ... For other uses, see Hexagon (disambiguation). ... This article does not cite any references or sources. ... “Kg” redirects here. ... “Kg” redirects here. ... An opioid is a chemical substance that has a morphine-like action in the body. ... Antagonists will block the binding of an agonist at a receptor molecule, inhibiting the signal produced by a receptor-agonist coupling. ... Naloxone is a drug used to counter the effects of opioid overdose, for example heroin and morphine overdose. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... This article does not cite any references or sources. ... This article is about Physics. ... An opioid is a chemical substance that has a morphine-like action in the body. ... Formulation ... An injection is a method of putting liquid into the body with a hollow needle and a syringe which is pierced through the skin long enough for the material to be forced into the body. ... This article is about modern humans. ... In the scientific method, an experiment (Latin: ex- periri, of (or from) trying) is a set of observations performed in the context of solving a particular problem or question, to support or falsify a hypothesis or research concerning phenomena. ... Efficacy is the ability to produce a desired amount of a desired effect. ... Naloxone is a drug used to counter the effects of opioid overdose, for example heroin and morphine overdose. ...


A solution for injection (usually by the intramuscular route) is marketed for the UK veterinary market by Alstoe Animal Health as Vetergesic, licenced for analgesia and sedation in dogs. Intramuscular injection is an injection of a substance directly into a muscle. ... Veterinary medicine is the application of medical diagnostic and therapeutic principles to companion, domestic, exotic, wildlife, and production animals. ... Sedation is a medical procedure involving administration of sedative drugs, generally to facilitate a medical procedure, such as endoscopy, vasectomy, or minor surgery with local anaesthesia. ... This article is about the domestic dog. ...


Since 2001 buprenorphine is also available transdermally in 35, 52.5 and 70 mcg/hour transdermal patch, that delivers the dose over 96 hours. This application form is marketed as Transtec in most European countries by Gruenenthal [2] (Napp Pharmaceuticals.in the UK [3] Norpharma in Denmark) for the treatment of moderate to severe cancer pain and severe non-cancer pain not responding to non-opioids. Moreover, a new 5, 10 and 20 mcg/hour patch is marketed as Butrans or Norspan, a once weekly patch for severe chronic pain not responding to non-opioids, marketed by Napp Pharmaceuticals Ltd., and Mundipharma and Gruenenthal respectively. “Kg” redirects here. ... A 21mg dose Nicoderm CQ patch applied to the right arm A transdermal patch or skin patch is a medicated adhesive patch that is placed on the skin to deliver a time released dose of medication through the skin and into the bloodstream. ... “Kg” redirects here. ... A 21mg dose Nicoderm CQ patch applied to the right arm A transdermal patch or skin patch is a medicated adhesive patch that is placed on the skin to deliver a time released dose of medication through the skin and into the bloodstream. ... For the magazine, see Marketing (magazine). ...


Pharmacology and pharmacokinetics

Buprenorphine is a thebaine derivative, and its analgesic effect is due to partial agonist activity at μ-opioid receptors, i.e., when the molecule binds to a receptor, it is only partially activated in contrast to an full agonist such as morphine. Buprenorphine also has very high binding affinity for the μ receptor such that opioid receptor antagonists (e.g. naloxone) only partially reverse its effects. These two properties must be carefully considered by the practitioner, as an overdose cannot be easily reversed (although overdose is unlikely in addicts or people with tolerance to opioids who use the drug sublingually as meant in the case of Subutex/Suboxone, especially if there are no benzodiazepines involved), and use in persons physically dependent on full-agonist opioids may trigger opioid withdrawal that also cannot be easily reversed and can last over 24 hours, as the drug's mean half-life is 37 hours. A minor constituent of opium, thebaine or paramorphine (C19H21NO3) is chemically similar to both morphine and codeine, but produces stimulatory rather than depressant effects. ... An analgesic (colloquially known as a painkiller) is any member of the diverse group of drugs used to relieve pain (achieve analgesia). ... Agonists An agonist is a substance that binds to a receptor and triggers a response in the cell. ... To meet Wikipedias quality standards, this article may require cleanup. ... 3D (left and center) and 2D (right) representations of the terpenoid molecule atisane. ... In biochemistry, a receptor is a protein on the cell membrane or within the cytoplasm or cell nucleus that binds to a specific molecule (a ligand), such as a neurotransmitter, hormone, or other substance, and initiates the cellular response to the ligand. ... Agonists An agonist is a substance that binds to a receptor and triggers a response in the cell. ... Morphine (INN) (IPA: ) is a highly potent opiate analgesic drug and is the principal active agent in opium and the prototypical opiate. ... Chemical affinity results from electronic properties by which dissimilar substances are capable of forming chemical compounds. ... The μ opioid receptors (MOR) are a class of opioid receptors with high affinity for enkephalins and beta-endorphin but low affinity for dynorphins. ... To meet Wikipedias quality standards, this article may require cleanup. ... Antagonists will block the binding of an agonist at a receptor molecule, inhibiting the signal produced by a receptor-agonist coupling. ... Naloxone is a drug used to counter the effects of opioid overdose, for example heroin and morphine overdose. ... The phrase chemical property is context-dependent, but generally refers to a materials behavior at ambient conditions (i. ... A general practitioner (GP), family physician or family practitioner (FP) is a physician/medical doctor who provides primary care. ... A drug overdose occurs when a chemical substance (i. ... An opioid is any agent that binds to opioid receptors found principally in the central nervous system and gastrointestinal tract. ... Benzodiazepine tablets The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsant, amnestic and muscle relaxant properties. ... For other uses, see addicted. ... Agonists An agonist is a substance that binds to a receptor and triggers a response in the cell. ... An opioid is any agent that binds to opioid receptors found principally in the central nervous system and gastrointestinal tract. ... An opioid is a chemical substance that has a morphine-like action in the body. ... Withdrawal, also known as withdrawal syndrome, refers to the characteristic signs and symptoms that appear when a drug that causes physical dependence is regularly used for a long time and then suddenly discontinued or decreased in dosage. ...


Buprenorphine is also a κ-opioid receptor antagonist, and partial/full agonist at the recombinant human ORL1 nociceptin receptor.[4] κ-Opioid receptors are involved with analgesia, but activation also produces marked nausea and dysphoria. ... An additional opioid receptor has been identified and cloned based on homology with the cDNA. This receptor is known as the nociceptin receptor or ORL 1 receptor. ... Opioid receptors are a group of G-protein coupled receptors with opioids as ligands. ...


Buprenorphine hydrochloride is administered by intramuscular injection, intravenous infusion, via a transdermal patch, or as a sublingual tablet. It is not administered orally, due to very high first-pass metabolism. Buprenorphine is metabolised by the liver, via the CYP3A4 isozyme of the cytochrome P450 enzyme system, into norbuprenorphine (by N-dealkylation) and other metabolites. The metabolites are further conjugated with glucuronic acid and eliminated mainly through excretion into the bile. The elimination half-life of buprenorphine is 20–73 hours (mean 37). Due to the mainly hepatic elimination there is no risk of accumulation in patients with renal impairment and in the elderly. In chemistry, hydrochlorides are salts resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base (mostly amines). ... Intramuscular injection is an injection of a substance directly into a muscle. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... A transdermal patch is a medicated adhesive patch that is placed on the skin to deliver a time released dose of medication through the skin and into the bloodstream. ... The first pass effect (or first pass metabolism) is a phenomenon of drug metabolism. ... For the bird, see Liver bird. ... Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1. ... Cytochrome P450 Oxidase (CYP2E1) Cytochrome P450 oxidase (commonly abbreviated CYP) is a generic term for a large number of related, but distinct, oxidative enzymes (EC 1. ... Buprenorphine, also colloquially referred to as bupe, is an opioid drug with partial agonist and antagonist actions. ... The α-D form of glucuronic acid. ... The elimination half-life of a drug (or any xenobiotic agent) refers to the timecourse necessary for the quantity of the xenobiotic agent in the body (or plasma concentration) to be reduced to half of its original level through various elimination processes. ...


The main active metabolite, norbuprenorphine, is a δ-opioid receptor and ORL1 receptor agonist, μ- and κ-opioid receptor partial agonist, but buprenorphine antagonizes its effects.[4] δ-Opioid receptor activation produces analgesia. ...


Plasma concentrations after application of transdermal buprenorphine increase steadily and the minimum effective therapeutic dose (100 pg/ml) is reached at 11 hours and 21 hours for a single 35 and 70 g/h patch, respectively. Peak plasma concentration (Cmax) is reached in about 60 hours (305 and 624 pg/ml for the 35 and 70 g/h strength patch, respectively), and is markedly longer than with 0.3 mg intravenous buprenorphine (0.41 hours). Transdermal buprenorphine has a half-life of approx. 30 hours, and a bioavailability of approximately 50%, which is comparable to sublingual buprenorphine .


Clinical use

Indications

Pain indications

Depending on the application form, buprenorphine is indicated for the treatment of moderate to severe chronic pain or for peri-operative analgesia. For the treatment of chronic pain, the transdermal formulations are nowadays preferred, which can be used both for chronic cancer pain as well as chronic non-malignant pain e.g. musculosceletal and neuropathic pain. The intravenous formulation is mainly used in postoperative pain (e.g. as PCA- patient controlled analgesia) and the sublingual formulation is e.g. used as breakthrough medication for patients with basic transdermal treatment. Advantages of buprenorphine in the treatment of chronic pain are – from a clinical perspective- its relatively long half-life, the option of sublingual and transdermal application and the excellent safety profile (ceiling effect for respiratory depression, lack of immunosuppressive effect, low pharmacokinetic interaction potential, no accumulation in renal impairment).


Antidepressant features

A clinical trial conducted at Harvard Medical School in the mid-1990s demonstrated that a majority of unipolar non-psychotic patients with major depression refractory to conventional thymoleptic antidepressants could be successfully treated with buprenorphine.[5] See opioids for other (predominantly favorable) experiments with buprenorphine and other opioids for psychological relief. However, psychological distress is currently not an approved indication for the use of any opioid, and legally it falls in a "grey zone" that is technically legal but a doctor could still face charges regardless (but not for off-label scripting in itself, simply being singled out by the DEA, who prosecute doctors often for using controlled substances for approved uses ("too much"). [1][2] The doctor still needs the proper DEA licensing under the Drug Addiction Treatment Act of 2000 to prescribe Subutex or Suboxone for opioid addiction/dependence. Psychosis is a psychiatric classification for a mental state in which the perception of reality is distorted. ... On the Threshold of Eternity. ... A recent form of antidepressant medication - Prozac Serotonin-norepinephrine reuptake inhibitor, Venlafaxine An antidepressant, in the most common usage, is a medication taken to alleviate clinical depression or dysthymia (milder depression). ... An opioid is any agent that binds to opioid receptors found principally in the central nervous system and gastrointestinal tract. ... The DEAs enforcement activities may take agents anywhere from distant countries to suburban U.S. homes. ...


Contraindication

Like other opiates, buprenorphine can cause drowsiness, vomiting and respiratory depression. Taking buprenorphine in conjunction with central nervous system (CNS) depressants such as sedatives, tranquilizers, alcohol, and especially benzodiazepines can be particularly dangerous [6]. Falling asleep while abusing this drug, especially while combining it with other central nervous system depressants, can be extremely dangerous and thus greatly increases the chance of serious complications or death. Somnolence (or drowsiness, or hypersomnia) is a state of near-sleep, a strong desire for sleep, or sleeping unusually long periods. ... Emesis redirects here. ... In medicine, hypoventilation exists when ventilation is inadequate to perform gas exchange. ... A diagram showing the CNS: 1. ... A sedative is a substance that depresses the central nervous system (CNS), resulting in calmness, relaxation, reduction of anxiety, sleepiness, and slowed breathing, as well as slurred speech, staggering gait, poor judgment, and slow, uncertain reflexes. ... A sedative is a substance that depresses the central nervous system (CNS), resulting in calmness, relaxation, reduction of anxiety, sleepiness, and slowed breathing, as well as slurred speech, staggering gait, poor judgment, and slow, uncertain reflexes. ... Alcoholic beverages. ... Benzodiazepine tablets The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsant, amnestic and muscle relaxant properties. ...


Adverse effects

Common adverse drug reactions associated with the use of buprenorphine are similar to those of other opioids and include: nausea and vomiting, drowsiness, dizziness, headache, itch, dry mouth, miosis, orthostatic hypotension, male ejaculatory difficulty, decreased libido, urinary retention. Constipation and CNS effects are seen less frequently than with e.g. morphine [7] Hepatic necrosis and hepatitis with jaundice have been reported with the use of buprenorphine, especially after intravenous injection of crushed tablets. An adverse drug reaction (abbreviated ADR) is a term to describe the unwanted, negative consequences sometimes associated with the use of medications. ... Miosis should not be confused with meiosis, the cellular division process involved in sexual reproduction. ... Orthostatic hypotension (also known as postural hypotension, orthostatic intolerance and, colloquially, as head rush or a dizzy spell) is a sudden fall in blood pressure, typically greater than 20/10 mm Hg, that occurs when a person assumes a standing position, usually after a prolonged period of rest. ... Constipation or irregularity, is a condition of the digestive system where a person (or animal) experiences hard feces that are difficult to egest; it may be extremely painful, and in severe cases (fecal impaction) lead to symptoms of bowel obstruction. ...


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 [7].Moreover, former doubts on the antagonisation of the respiratory effects by Naloxone have been disproved: Buprenorphine effects can be antogonised with a continuous infusion of Naloxone [8]. Of course, concurrent use of buprenorphine and CNS depressants (such as alcohol or benzodiazepines) is contraindicated as it may lead to fatal respiratory depression.



In people on medium- to long-term maintenance with Suboxone or Subutex do not have a major risk of overdose, as long as the drug is used properly (as prescribed), and benzodiazepines are not prescribed to individuals without a tolerance to opioids. An opioid is any agent that binds to opioid receptors found principally in the central nervous system and gastrointestinal tract. ...


As with other Opioids, dependence and tolerance are rarely a problem when used safely. There is little evidence that buprenorphine is less likely to cause such problems. Maintenance dosages can remain at the same moderate level indefinitely, and in many cases even lowered, without discomfort. Due to buprenorphine's pharmacological actions, raising the dosage will not result in a stronger analgesic effect after a certain point (around 16–32 mg), beyond which the drug will actually have a reduced analgesic effect. An opioid is any agent that binds to opioid receptors found principally in the central nervous system and gastrointestinal tract. ...


The partial agonist activity of buprenorphine combined with its high affinity for μ-opioid receptor means that it may act clinically as an antagonist and thus precipitate opioid withdrawal symptoms when an opioid-dependent patient is commenced on the drug soon after the use of another opioid drug. Patients are advised to wait between 24 and 36 hours after their last use of short-acting opioids (such as heroin or oxycodone) before beginning treatment with buprenorphine. Those using long-acting opioids, such as methadone, should only commence treatment once withdrawal symptoms are present. Beginning any earlier may result in extreme cases of opioid withdrawal. Additionally, it is recommended that the patient be on no more than 30 mg of methadone per day when switching to buprenorphine. To meet Wikipedias quality standards, this article may require cleanup. ... For other uses, see Heroin (disambiguation). ... Not to be confused with oxytocin. ... Methadone is a synthetic opioid, used medically as an analgesic and in the treatment of narcotic addiction. ... Methadone is a synthetic opioid, used medically as an analgesic and in the treatment of narcotic addiction. ...


Dependence treatment

Buprenorphine sublingual preparations are often used in the management of opioid dependence (that is, dependence on heroin, oxycodone, hydrocodone, morphine, oxymorphone, fentanyl or other opioids). The Suboxone and Subutex preparations were approved for this indication by the United States FDA in October 2002. This was only possible due to the Drug Addiction Treatment Act of 2000 that for the first time since 1914-1920 (conflicting Supreme Court rulings - rulings that would not stand to today's Supreme Court as they ruled that maintenance or detox treatment is not medical treatment, and likely was not what was intended by Congress) made it legal for doctors to prescribe opioids themselves to manage addiction ("maintenance") or for short-term detox (special doctors in registered clinics are excluded from these blanket restrictions). This law is limited to Schedules III through V only - thus excluding methadone and stronger opioids. A chemical dependency is such a strong dependency on a substance that it becomes necessary to have this substance just to function properly; The need of a substance developed from abusing the substance, requiring the substance for survival, like the need for food, or water See also: addiction drug tolerance... For other uses, see Heroin (disambiguation). ... Not to be confused with oxytocin. ... Hydrocodone or dihydrocodeinone (marketed as Vicodin, Anexsia, Dicodid, Hycodan (or generically Hydromet), Hycomine, Lorcet, Lortab, Norco, Novahistex, Hydroco, Tussionex, Vicoprofen, Xodol) is a semi-synthetic opioid derived from two of the naturally occurring opiates, codeine and thebaine. ... Morphine (INN) (IPA: ) is a highly potent opiate analgesic drug and is the principal active agent in opium and the prototypical opiate. ... Oxymorphone (Opana, Numorphan) or 14-Hydroxydihydromorphinone is a powerful semi-synthetic opioid analgesic that is derived from thebaine, and is approximately 6-8 times more potent than morphine. ... Fentanyl is an opioid analgesic, first synthesized by Janssen Pharmaceutica (Belgium) in the late 1950s, with a potency many times that of morphine. ... “FDA” redirects here. ...


The use of opioid-replacement therapy in the management of opioid dependence is highly regulated, owing to the sometimes controversial nature of this aspect of harm reduction policy. In the United States, a special federal waiver is required to prescribe Subutex and Suboxone for opioid addiction treatment on an outpatient basis. However, if the doctor meets none of the other clarifications, an 8-hour course is all that is required). Each approved prescriber is allowed to manage only 30 patients on buprenorphine for opioid addiction as outpatients;[9] the U.S. Senate has passed a bill relaxing this restriction for group practices only as of May 25, 2006 [citation needed]. Legislation was passed by Congress in the last few hours prior to Holiday recess in December, 2006 allowing physicians with one year of clinical experience to request an additional exemption within DATA 2000 allowing 100 patient limit efective January 5, 2007. Similar restrictions are placed on prescribers in many other jurisdictions. Buprenorphine is heavily regulated in Australia relatively, and while the number of patients isn't limited generally daily visits for supervised dosing at a pharmacy is required, such as methadone, and methadone where used is used in lower relative doses. [citation needed] On September 21, 2006, actor and comedian Artie Lange revealed on The Howard Stern Show that he had overcome heroin addiction the previous year. He said buprenorphine was essential to countering the effects of opioid withdrawal and described it as a 'miracle pill'. However, others have found that once they begin the treatment, they become addicted to the Buprenorphine, this is because Buprenorphine is still an opiate. The withdrawals from Buprenorphine is quite similar to that of other opiates, but like methadone, it has a long half life, causing a longer, but milder withdrawal. Harm reduction is a philosophy of public health, intended to be a progressive alternative to the prohibition of certain potentially dangerous lifestyle choices. ... Arthur Steven Lange, Jr. ... This article is about the radio show hosted by Howard Stern. ... For other uses, see Heroin (disambiguation). ...


Buprenorphine vs Methadone

Buprenorphine and methadone are both used for short-term and long-term opioid maintenance therapy. Each agent has its relative advantages and disadvantages. Methadone is a synthetic opioid, used medically as an analgesic and in the treatment of narcotic addiction. ...


In terms of efficacy (i.e. treatment retention, negative urine samples), high-dose buprenorphine (such as that commonly found with Subutex/Suboxone treatment; 8-16 mg typically) has been found to be superior to 20-40 mg of methadone/day (low dose) and equatable anywhere between 50 mg-70 mg (moderate dose)[10] to up to 100 mg (high dose)[11] methadone/day. (Methadone, however, can continue to increase in effectiveness over 100 mg, although it is a debatable topic, but this would consistute "very high dose" in this measurement commonly used by studies, including those quoted). In all cases, high-dose buprenorphine has been found to be far superior to placebo and an effective treatment for opioid addiction, with retention rates of 50% as a minimum.[10][11][12][13]


Buprenorphine sublingual tablets (Suboxone and Subutex for opioid addiction) have a long duration of action which may allow for dosing every two or three days, as tolerated by the patient, compared with the daily dosing required to prevent withdrawals with methadone. In the United States, following initial management, a patient is typically prescribed up to a one month supply for self-administration. It is often misunderstood that the patient has to receive other therapy in this situation, but the law simply states that the prescribing physician needs to be capable of referring the patient to other addiction treatment (i.e. psychotherapy or support groups,) and many (but not all) physicians are aware of this and simply recommend therapy, or as they deem fit have therapy required.


Buprenorphine relative to methadone is advantageous in that patients can be given the 30 day take home dose, hence making them more compliant relative to those who need to visit a methadone dispensing facility daily to receive their methadone. The facilities, which are federally regulated, only allow patients to take home weekend doses and after months of compliance without missing a day, they are given a week or more worth of methadone to take home.


Buprenorphine may and is generally viewed to have a lower dependence-liability than methadone. Buprenorphine treatment can last anywhere from several days (for detoxification purposes) to several months (sometimes for only a few weeks or up to two or three years) or in more rare cases longer. While not the general goal, and often not intentional with buprenorphine, it can sometimes but rarely be used in an indefinite, often life-long regimen just as methadone can be. The choice of buprenorphine vs. methadone in the mentioned situation (by the patient) is usually due to the benefits of the less-restrictive outpatient treatment; prescriptions for take-home doses for up to a month vs. the heavy restrictions for take-home methadone doses and frequent visits to the clinic, as well as the stigma of going to a methadone clinic.


The usually less-severe withdrawal effects make it usually much easier to discontinue use as opposed to methadone, but no evidence thus far exists that sustaining abstinence post-buprenorphine maintenance is any more likely than post-methadone maintenance, or post-heroin withdrawal. On the other side, going from heroin/other potent opioids to buprenorphine is generally harder than going from the same to methadone. In the eyes of addicts this is an important consideration. Buprenorphine, as a partial μ-opioid receptor agonist, has been claimed and is generally viewed to have a less euphoric effect compared to the full agonist methadone, and was therefore predicted less likely to be diverted to the black market (as reflected by its CIII status vs. methadone's more restrictive CII status), as well as that buprenorphine is generally accepted as unable to be abused (for euphoria) by those with a heroin or other potent opioid habit (however neither drug is supposed to have a euphoric effect when used long-term). Thus far in the United States it is far less often found on the black market vs. methadone, but most street heroin addicts don't even know it exists, and its (legitimate) usage is far less than methadone (and according to many newspapers "underused"). In France where it is used more often than methadone there is more black market availability, although this and the apparent attraction is possibly due to a heroin dry-spell, possible evidence indicated by how it is often combined with benzodiazepines for more of an effect. Benzodiazepine tablets The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsant, amnestic and muscle relaxant properties. ...


Blockade effect

The Suboxone preparation contains the μ-opioid receptor antagonist naloxone which is intended only to prevent abuse of the buprenorphine, not, as is commonly misunderstood, to block the effects of other opiates. Buprenorphine itself binds more strongly to receptors in the brain than do other opioids, making it more difficult to become intoxicated due to other opioids when buprenorphine is in the system, regardless of the presence of the naloxone. (Measurable amounts of naloxone can be absorbed and detected via the sublingual route, and while this is insignificant and has no subjective effect, there are anecdotal reports of hypersensitivity to naloxone in (if proven) rare cases.) If enough buprenorphine is in the system, however, it has the same effect as naloxone in completely or nearly completely blocking or reversing opiate effects from another opioid. 0.3 mg of buprenorphine parenterally is equivalent in antagonistic effect to between 0.4 and 2.0 mg of naloxone parenterally with a much longer half-life. Methadone too blocks the effects of other opioids, and generally just as well, but it is more due to the fact that so much is often used and the tolerance to opiates that comes with it. However, it is still possible to abuse other opioids on either treatment regime. Naloxone is a drug used to counter the effects of opioid overdose, for example heroin and morphine overdose. ... Naloxone is a drug used to counter the effects of opioid overdose, for example heroin and morphine overdose. ...


In the case of preganancy, buprenorphine causes less neo-natal withdrawals than methadone.[14] (and is one of the few cases where Subutex is likely to be used over Suboxone in the United States.) Thus, buprenorphine is preferable during pregnancy.


Switching to buprenorphine from methadone is very difficult and withdrawals lasting several days or more are often encountered mostly when the dose is any higher than 30 mg/day (the suggested and usual dose for switching to buprenorphine), a very low (sub-therapeutic)[citation needed] methadone dose that many methadone maintenance patients have difficulty reaching. Switching to buprenorphine at a higher dose may cause a long-term withdrawal syndrome. Unfortunately, due to this effect, buprenorphine being used during pregnancy over methadone might be a moot point unless the difference is taken into account beforehand by women that possibly will become pregnant. On the other side, switching from buprenorphine to methadone is relatively easy.


Inpatient rehabilitation

The practice of using buprenorphine (Subutex or Suboxone) in an inpatient rehabilitation setting is increasing rapidly [citation needed], whereas methadone-based detox is the standard. It is also being used in social model treatment settings. These rehabilitation programs consist of "detox" and "treatment" phases. The detoxification ("detox") phase consists of medically-supervised withdrawal from the drug of dependency on to buprenorphine, sometimes aided by the use of medications such as benzodiazepines like oxazepam or diazepam (modern milder tranquilizers that assist with anxiety, sleep, and muscle relaxation), clonidine (a blood-pressure medication that may reduce some opioid withdrawal symptoms), and anti-inflammatory/pain relief drugs such as ibuprofen. Switching to buprenorphine from a short-acting drug including Heroin, morphine, fentanyl, hydromorphone and hydrocodone (Vicodin), or oxycodone (Oxycontin and Percocet) is not too difficult for most people, and as long as the patient waited until they were in full withdrawals or longer before starting the buprenorphine medication, little further acute symptoms are an issue; The patient needs to be stabilized on a proper dose and monitored regardless. Switching from methadone is much more difficult, and with all cases if the patient takes buprenorphine prematurely (before full withdrawal symptoms) it can precipitate worse withdrawals than would have been had if the person had waited properly, and they can be long-lasting. The treatment phase begins once the patient is stabilized and receives medical clearance. This portion of treatment is comprised of multiple therapy sessions, which include both group and individual counseling with various chemical dependency counselors, psychologists, psychiatrists, social workers, and other professionals. Additionally, many treatment centers strongly base their treatment models on 12-step principles, such as those practiced by Alcoholics Anonymous and Narcotics Anonymous. Narcotics Anonymous and other 12-step programs do not have any organizational position on the use of any medically prescribed medications, it is each individual members personal decision to determine if their use of prescribed medications has compromised their sobriety or recovery. There are systems similar to or modeled after 12-step programs that accept its use and even acknowledge its power as a tool. Benzodiazepine tablets The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsant, amnestic and muscle relaxant properties. ... Oxazepam (marketed under brand names Alepam, Murelax, Oxascand, Serax, Serepax, Seresta, Sobril) is a drug which is a benzodiazepine derivative. ... Diazepam (IPA: ), first marketed as Valium by Hoffmann-La Roche, is a drug which is a benzodiazepine derivative. ... Clonidine is a direct-acting adrenergic agonist prescribed historically as an anti-hypertensive agent. ... Non-steroidal anti-inflammatory drugs, usually abbreviated to NSAIDs, are drugs with analgesic, antipyretic and anti-inflammatory effects - they reduce pain, fever and inflammation. ... Ibuprofen (INN) (IPA: ) (from the earlier nomenclature iso-butyl-propanoic-phenolic acid) is a non-steroidal anti-inflammatory drug (NSAID) originally marketed as Nurofen and since under various trademarks including Act-3, Advil, Brufen, Dorival, Herron Blue, Panafen, Motrin, Nuprin and Ipren or Ibumetin (Sweden), Ibuprom (Poland), IbuHEXAL, Moment (Italy... For other uses, see Heroin (disambiguation). ... Morphine (INN) (IPA: ) is a highly potent opiate analgesic drug and is the principal active agent in opium and the prototypical opiate. ... Fentanyl is an opioid analgesic, first synthesized by Janssen Pharmaceutica (Belgium) in the late 1950s, with a potency many times that of morphine. ... Hydromorphone is a drug developed in Germany in the 1920s and introduced to the mass market beginning in 1926. ... Hydrocodone or dihydrocodeinone (marketed as Vicodin, Anexsia, Dicodid, Hycodan (or generically Hydromet), Hycomine, Lorcet, Lortab, Norco, Novahistex, Hydroco, Tussionex, Vicoprofen, Xodol) is a semi-synthetic opioid derived from two of the naturally occurring opiates, codeine and thebaine. ... Not to be confused with oxytocin. ... Alcoholics Anonymous (AA) is an informal society for recovering alcoholics. ... This article is about the 12-step program of Narcotics Anonymous (NA). ... This article is about the 12-step program of Narcotics Anonymous (NA). ...


Patients who enter rehabilitation voluntarily (as opposed to those who are court-ordered) can often choose a facility with the option of only staying for detox. Alternatively they can enter treatment facilities that provide the option to complete both detox and longer-term treatment. Completing both increases the probability of success.[citation needed]. Abstinence alone has a very low efficacy in rehabilitating patients. In contrast, buprenorphine maintenance has a high efficacy [15] [10]. Most rehabilitation programs do not have or do not allow scientific studies to be conducted to contrast to abstinence alone and buprenorphine or methadone maintenance, including Narcotics Anonymous. NA's 12 traditions and overriding principle of anonymity would make such research potentially contentious and internally problematic [citation needed]. Whilst the maintenance / abstinence debate is a hot topic and strong arguments in support of both Narcotics Anonymous and buprenorphine maintenance have been made, individuals tend to gravitate the alternative that works best for them. Furthermore, the two approaches need not necessarily be mutually exclusive. Rehabilitation programs typically average about 30 days for primary care, but some may extend anywhere from 90 days to 6 months in an extended care unit. It is considered essential by the programs that administer them that patients in abstinence-based treatment form networks with other recovering addicts and engage in mutual-help groups, aftercare and other related activities after treatment in order to improve their chances of achieving long-term abstinence from opioids. Statistically, long-term abstinence is not widely prevalent. Methadone is a synthetic opioid, used medically as an analgesic and in the treatment of narcotic addiction. ... This article is about the 12-step program of Narcotics Anonymous (NA). ... This article is about the 12-step program of Narcotics Anonymous (NA). ...


Buprenorphine is sometimes used only during the detox protocol with the purpose of reducing the patient's use of mood-altering substances. It considerably reduces acute opioid withdrawal symptoms that are normally experienced by opioid-dependent patients on cessation of those opioids, including diarrhea, vomiting, fever, chills, cold sweats, muscle and bone aches, muscle cramps and spasms, restless legs, agitation, gooseflesh, insomnia, nausea, watery eyes, runny nose and post-nasal drip, nightmares, etc. The buprenorphine detox protocol usually lasts about 7-10 days, provided that the patient does not need to be detoxed from any additional addictive substances, as previously mentioned.


During this time, Suboxone or Subutex will be administered or the patient will be monitored taking the medication. Generally, the patient takes a single dose each day (a single dose may keep the patient comfortable for up to 48-72 hours, but medical professionals in many treatment facilities prescribe one or more than one dose every 24 hours to ensure that a consistent, active level of the medication remains in the patient's central nervous system, a key element of maintenance; also the level of dosage is usually around the previously described plateau, after which there is no noticeable increase in the effects of the drug. Typically, the first day dosage is no more than 8 mg or it may precipitate withdrawals as antagonistic effects overwhelm agonistic effects, after which initial daily dose totals around 8-16 mg (of either Suboxone or Subutex). The dosage is slowly tapered each day and the medication is usually stopped 36-48 hours prior to the end of the detox program, with the patient's vitals monitored up until discharge from the detox program.


During the detox period of any situation, despite the evidence that suggests that the naloxone in Suboxone has no clinically significant effect (except for anecdotal reports of hypersensitivity in (if proven) rare cases), Subutex is urged over Suboxone by the manufacturer and you are likely to receive it during the first few days.


References

  1. ^ List of psychotropic Substances under international control
  2. ^ Transtec Summary of Product Characteristics
  3. ^ Napp Pharmaceuticals
  4. ^ a b Huang P. et al. (2001): "Comparison of pharmacological activities of buprenorphine and norbuprenorphine: norbuprenorphine is a potent opioid agonist", J. Pharmacol. Exp. Ther. 297(2):688-95. PMID 11303059
  5. ^ Bodkin JA. et al. (1995): "Buprenorphine treatment of refractory depression", Journal of Clinical Psychopharmacology 15:49-57. PMID 7714228
  6. ^ Suboxone FAQ
  7. ^ a b Budd K, Raffa RB. (edts.) Buprenorphine- The unique opioid analgesic. Thieme 2005 (ISBN 3-13-1342211-0)
  8. ^ Van Dorp E. et al. (2006) Naloxone reversal of buprenorphine- induced respiratory depression. Anesthesiology 105 (1): 51-57
  9. ^ naabt.org
  10. ^ a b c R. S. Schottenfeld et. al (1997) Department of Psychiatry, Yale University School of Medicine
  11. ^ a b Rolley Johnson et al., NEJM, 343(18):1290-1297, 2000
  12. ^ Strain et al. (1998)
  13. ^ Ling et al. (1998)
  14. ^ G Fischer, P Etzersdorfer, H Eder, R Jagsch, M Langer, M Weninger (1998). Buprenorphine Maintenance in Pregnant Opioid Addicts. European Addiction Research;4 (suppl 1):32-36
  15. ^ Cite error 8; No text given.

External links


  Results from FactBites:
 
Buprenorphine - Wikipedia, the free encyclopedia (1871 words)
Buprenorphine is a thebaine derivative, and its analgesic effect is due to partial agonist activity at μ-opioid receptors, i.e., when the molecule binds to a receptor, it is only partially activated in contrast to a full agonist such as morphine.
Buprenorphine is indicated for the treatment of moderate to severe pain, peri-operative analgesia, and opioid dependence.
Buprenorphine sublingual preparations are often used in the management of opioid dependence (that is, dependence on heroin, oxycodone, hydrocodone, morphine, or other opioids).
Buprenorphine - definition of Buprenorphine - Labor Law Talk Dictionary (260 words)
Buprenorphine is a partial opioid agonist and also an opioid antagonist.
Buprenorphine is a thebaine derivative, and its analgesic effect is due to agonism of μ subtype of opioid receptor.
Buprenorphine is administered as hydrochloride as either intramuscular or intravenous injection or as sublingual tablets.
  More results at FactBites »

 
 

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