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Dipyanone
Dipyanone is an opioid analgesic which has been sold as a designer drug, first identified in Germany in 2021. It is closely related to medically used drugs such as methadone, dipipanone and phenadoxone, but is slightly less potent. See also * Desmethylmoramide * IC-26 * Nufenoxole * Pyrrolidinylthiambutene Pyrrolidinylthiambutene is an opioid analgesic drug from the thiambutene family with around 3/4 of the potency of morphine Morphine is a strong opiate that is found naturally in opium, a dark brown resin in poppies ('' Papaver somniferu ... References Opioids Pyrrolidines Mu-opioid receptor agonists Ketones {{analgesic-stub ...
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Nufenoxole
Nufenoxole (SC-27166) is an antidiarrhoeal drug which acts as a peripherally selective opioid agonist, in a similar manner to loperamide and diphenoxylate. While it is able to activate μ-opioid receptors, it fails to cross the blood–brain barrier and so has a selective action against diarrhoea without producing analgesic effects. See also * Dipipanone * Dipyanone Dipyanone is an opioid analgesic which has been sold as a designer drug, first identified in Germany in 2021. It is closely related to medically used drugs such as methadone, dipipanone and phenadoxone, but is slightly less potent. See also ... * Desmethylmoramide References Antidiarrhoeals Mu-opioid receptor agonists Oxadiazoles Peripherally selective drugs {{pharm-stub ...
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Desmethylmoramide
Desmethylmoramide (INN) is an opioid analgesic related to dextromoramide (the active (+)-isomer of moramide) that was synthesized and characterized in the late 1950s but was never marketed. Synthesis The starting diphenylacetylpyrrolidine 0678-46-8can be made in ~84% yield by the reaction of methyldiphenylacetate with pyrrolidine. Or ~62% from amidation of the free acid (by Schotten-Baumann reaction). See also * Dipyanone * Nufenoxole * Phenadoxone Phenadoxone (trade names Heptalgin, Morphidone, and Heptazone) is an opioid analgesic of the open chain class (methadone and relatives) invented in Germany by Hoechst in 1947. It is one of a handful of useful synthetic analgesics which were used ... References Further reading * 4-Morpholinyl compunds Opioids {{analgesic-stub ...
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Opioid
Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, reversing opioid overdose, and suppressing cough. Extremely potent opioids such as carfentanil are approved only for veterinary use. Opioids are also frequently used non-medically for their euphoric effects or to prevent withdrawal. Opioids can cause death and have been used for executions in the United States. Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms. The euphoria attracts recreational use, and frequent, escalating recreational use of ...
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Analgesic
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing ...
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Designer Drug
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances that have been designated by the European Union as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects, and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human trials, the use of some of these drugs may result i ...
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Methadone
Methadone, sold under the brand names Dolophine and Methadose among others, is a synthetic opioid agonist used for chronic pain and also for opioid dependence. It is used to treat chronic pain, and it is also used to treat addiction to heroin or other opioids. Prescribed for daily use, the medicine relieves cravings and removes withdrawal symptoms. Detoxification using methadone can be accomplished in less than a month, or it may be done gradually over as long as six months. While a single dose has a rapid effect, maximum effect can take up to five days of use. The pain-relieving effects last about six hours after a single dose. After long-term use, in people with normal liver function, effects last 8 to 36 hours. Methadone is usually taken by mouth and rarely by injection into a muscle or vein. Side effects are similar to those of other opioids. These frequently include dizziness, sleepiness, vomiting, and sweating. Serious risks include opioid abuse and respiratory depre ...
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Dipipanone
Dipipanone (Pipadone) is a strong opioid analgesic drug, used for acute pain by mouth (PO) for adults - initially 10 mg every 6 hours, then increased if necessary up to 30 mg every 6 hours, with the dose to be increased gradually. It is often used in instances where morphine is indicated but cannot be used due to the patient being allergic to morphine. In analgesic potency 25 mg dipipanone is approximately equivalent to 10 mg morphine. Dosage forms The main preparation of the drug commercially available is mixed with cyclizine (Diconal, Wellconal) which has the advantage of reducing nausea, vomiting and histamine release associated with strong opioid therapy. Dipipanone was also available as an oral mixture 10 mg/5ml without the cyclizine during the 1970s–1980s in the United Kingdom. This form was rare and used normally only in drug trials and in specialist Diconal addiction clinics. Dipipanone is now the only alternative opioid left to use in the UK that is of equal s ...
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Phenadoxone
Phenadoxone (trade names Heptalgin, Morphidone, and Heptazone) is an opioid analgesic of the open chain class (methadone and relatives) invented in Germany by Hoechst in 1947. It is one of a handful of useful synthetic analgesics which were used in the United States for various lengths of time in the 20 or so years after the end of the Second World War but which were withdrawn from the market for various or no known reason and which now are mostly in Schedule I of the United States' Controlled Substances Act of 1970, or (like phenazocine and bezitramide) in Schedule II but not produced or marketed in the US. Others on this list are ketobemidone (Ketogin), dextromoramide (Dimorlin, Palfium and others), phenazocine (Narphen and Prinadol), dipipanone (Diconal, Pipadone and Wellconal), piminodine (Alvodine), propiram (Algeril), anileridine (Leritine) and alphaprodine (Nisentil). Phenadoxone has a US DEA ACSCN of 9637 and recently has had a zero annual manufacturing quota under the Con ...
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IC-26
IC-26 (WIN 1161-3, Methiodone) is an analogue of the opioid analgesic methadone, where the carbonyl group has been replaced by the bioisosteric sulfone group. Human and animal studies suggest that IC-26 is around the same potency as methadone, although other studies have found its activity to be inconsistent between different patients, with consistent opioid activity only being seen at a dose several times that of methadone. IC-26 was assessed for its abuse potential, but despite being found to have similar potential to methadone for development of dependence it was never placed under international control as an illegal drug. See also * Dextromoramide * Dipipanone * MT-45 * Phenadoxone Phenadoxone (trade names Heptalgin, Morphidone, and Heptazone) is an opioid analgesic of the open chain class (methadone and relatives) invented in Germany by Hoechst in 1947. It is one of a handful of useful synthetic analgesics which were used i ... References Synthetic opioids Sulfon ...
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Pyrrolidinylthiambutene
Pyrrolidinylthiambutene is an opioid analgesic drug from the thiambutene family with around 3/4 of the potency of morphine Morphine is a strong opiate that is found naturally in opium, a dark brown resin in poppies (''Papaver somniferum''). It is mainly used as a analgesic, pain medication, and is also commonly used recreational drug, recreationally, or to make .... It would be considered an illegal controlled substance analogue in some countries such as the US, Australia and New Zealand, but is legal in countries not possessing a controlled-substances-analog-act equivalent. References Opioids Thiophenes Pyrrolidines Mu-opioid receptor agonists {{analgesic-stub ...
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Opioids
Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, reversing opioid overdose, and suppressing cough. Extremely potent opioids such as carfentanil are approved only for veterinary use. Opioids are also frequently used non-medically for their euphoric effects or to prevent withdrawal. Opioids can cause death and have been used for executions in the United States. Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms. The euphoria attracts recreational use, and frequent, escalating recreational use of o ...
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Pyrrolidines
Pyrrolidine, also known as tetrahydropyrrole, is an organic compound with the molecular formula (CH2)4NH. It is a cyclic secondary amine, also classified as a saturated heterocycle. It is a colourless liquid that is miscible with water and most organic solvents. It has a characteristic odor that has been described as "ammoniacal, fishy, shellfish-like". In addition to pyrrolidine itself, many substituted pyrrolidines are known. Production and synthesis Industrial production Pyrrolidine is prepared industrially by the reaction of 1,4-butanediol and ammonia at a temperature of 165–200 °C and a pressure of 17–21 MPa in the presence of a cobalt- and nickel oxide catalyst, which is supported on alumina. : The reaction is carried out in the liquid phase in a continuous tube- or tube bundle reactor, which is operated in the cycle gas method. The catalyst is arranged as a fixed-bed and the conversion is carried out in the downflow mode. The product is obtained after mu ...
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