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Oxycodone
Oxycodone, sold under various brand names such as Roxicodone and OxyContin (which is the extended release form), is a strong, semi-synthetic opioid used medically for treatment of moderate to severe pain. It is highly addictive and a commonly drug abuse, abused drug. It is usually taken oral administration, by mouth, and is available in immediate release, immediate-release and controlled release, controlled-release formulations. Onset of pain relief typically begins within fifteen minutes and lasts for up to six hours with the immediate-release formulation. In the United Kingdom, it is available by injection. Combination drug, Combination products are also available with oxycodone/paracetamol, paracetamol (acetaminophen), oxycodone/ibuprofen, ibuprofen, oxycodone/naloxone, naloxone, naltrexone, and oxycodone/aspirin, aspirin. Common side effects include euphoria, constipation, nausea, vomiting, Anorexia (symptom), loss of appetite, Somnolence, drowsiness, dizziness, itching, X ...
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Oxycodone/aspirin
Oxycodone/aspirin (trade name Percodan) is a combination drug marketed by Endo Pharmaceuticals. It is a tablet containing a mixture of 325 mg (5 Grain (unit), grains) of aspirin and 4.8355 mg of oxycodone, oxycodone HCl (equivalent to 4.3346 mg of oxycodone as the free base); it is an opioid/non-opioid combination used to treat moderate to moderately severe pain. The safety of the combination during pregnancy has not been established, although aspirin is generally contraindicated during pregnancy, and the drug has been placed in Pregnancy category, pregnancy category D. Inactive ingredients include Quinoline Yellow WS, D&C Yellow 10, FD&C Yellow 6, microcrystalline cellulose, and corn starch. Percodan was first marketed by DuPont Pharmaceuticals and prescribed in the United States in 1950. Once a widely prescribed painkiller, it has largely been replaced by alternative oxycodone compounds containing paracetamol (acetaminophen) instead of aspirin, such as Percocet. ...
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Noroxycodone
Noroxycodone is the major metabolite of the opioid analgesic oxycodone. It is formed from oxycodone in the liver via N-demethylation predominantly by CYP3A4. Noroxycodone binds to and activates the μ-opioid receptor (MOR) similarly to oxycodone, although with one-third of the affinity of oxycodone and 5- to 10-fold lower activational potency. However, although a potent MOR agonist, noroxycodone poorly crosses the blood-brain-barrier into the central nervous system, and for this reason, is only minimally analgesic in comparison. See also * Norbuprenorphine * Norbuprenorphine-3-glucuronide * Norhydrocodone * Normorphine * Noroxymorphone Noroxymorphone is an opioid which is both a metabolite of oxymorphone and oxycodone and is manufactured specifically as an intermediate in the production of narcotic antagonists such as naltrexone and others. It is a potent agonist of the μ-op ... References 4,5-Epoxymorphinans Ketones Opioid metabolites {{analgesic-stub ...
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Oxycodone/naloxone
Oxycodone/naloxone, sold under the trade name Targin and Targinact (in the UK) among others, is a combination pain medication. It is available as modified-release tablets and is taken by mouth. The oxycodone component is an opioid and is responsible for the pain-relieving effects. Naloxone opposes the effects of opioids but is poorly absorbed into the body when given orally, meaning almost all the dose stays within the gastrointestinal tract and reduces the local side effects from the oxycodone, namely constipation as the naloxone binds to the opioid receptors in the gut, preventing the opioid from attaching. This does not affect its analgesic efficacy compared to Oxycontin. Constipation was significantly relieved in a 2008 study. The drug was released in 2006 in Germany and is available in some other European countries since 2009. In the UK, the 10 mg oxycodone / 5 mg naloxone and 20 mg/10 mg strengths were approved in December 2008, and the 40 mg/20&nbs ...
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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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Oxycodone/paracetamol
Oxycodone/paracetamol, sold under the brand name Percocet among others, is a fixed-dose combination of the opioid oxycodone with paracetamol (acetaminophen), used to treat moderate to severe pain. In 2020, it was the 69th most commonly prescribed medication in the United States, with more than 10million prescriptions. History The United States Food and Drug Administration (FDA) first approved Percocet in 1976, under application ANDA 085106. Society and culture Implicated in deaths In June 2009, an FDA advisory panel recommended that Percocet, Vicodin, and every other combination of acetaminophen with narcotic analgesics be limited in their sales because of their contributions to an alleged 400 acetaminophen-related deaths in the U.S. each year, that were attributed to acetaminophen overdose and associated liver damage. In December 2009, the ''Canadian Medical Association Journal'' reported a study finding a fivefold increase in oxycodone-related deaths in Ontario (mostly ...
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Oxymorphone
Oxymorphone (sold under the brand names Numorphan and Opana among others) is a highly potent opioid analgesic indicated for treatment of severe pain. Pain relief after injection begins after about 5–10 minutes, after oral administration it begins after about 30 minutes, and lasts about 3–4 hours for immediate-release tablets and 12 hours for extended-release tablets. The elimination half-life of oxymorphone is much faster intravenously, and as such, the drug is most commonly used orally. Like oxycodone, which metabolizes to oxymorphone, oxymorphone has a high potential to be abused. It was developed in Germany in 1914. It was patented in 1955 and approved for medical use in 1959. In June 2017 the FDA asked Endo Pharmaceuticals to remove its product from the US market. This was in part due to the opioid epidemic in the US, and the fact that a 2012 reformulation failed to stop illicit injection of the drug. Endo responded by voluntarily removing Opana ER from the market a mon ...
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Oxycodone/ibuprofen
Oxycodone/ibuprofen (INNs, trade name Combunox) is an oral combination drug formulation of the opioid analgesic oxycodone and the nonsteroidal anti-inflammatory drug (NSAID) ibuprofen that is used in the treatment of chronic and acute pain. This particular drug is supplied in a fixed dose combination tablet which contains Oxycodone Hydrochloride, USP 5 mg with Ibuprofen, USP 400 mg. Adverse effects See also * Oxycodone/paracetamol * Oxycodone/aspirin * Hydrocodone/ibuprofen Hydrocodone/ibuprofen (INNs), sold under the brand name Vicoprofen, is a fixed-dose combination analgesic medication used in short-term therapy to relieve severe pain. Vicoprofen combines the analgesic and antitussive properties of hydrocodone ... References External links * Combination analgesics {{analgesic-stub ...
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CYP2D6
Cytochrome P450 2D6 (CYP2D6) is an enzyme that in humans is encoded by the ''CYP2D6'' gene. ''CYP2D6'' is primarily expressed in the liver. It is also highly expressed in areas of the central nervous system, including the substantia nigra. CYP2D6, a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body. In particular, CYP2D6 is responsible for the metabolism and elimination of approximately 25% of clinically used drugs, via the addition or removal of certain functional groups – specifically, hydroxylation, demethylation, and dealkylation. CYP2D6 also activates some prodrugs. This enzyme also metabolizes several endogenous substances, such as hydroxytryptamines, neurosteroids, and both ''m''-tyramine and ''p''-tyramine which CYP2D6 metabolizes into dopamine in the brain and liver. Considerable variation exists in the efficiency and amount of CYP2D6 enzyme produced betwee ...
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Noroxymorphone
Noroxymorphone is an opioid which is both a metabolite of oxymorphone and oxycodone and is manufactured specifically as an intermediate in the production of narcotic antagonists such as naltrexone and others. It is a potent agonist of the μ-opioid receptor, but is poorly able to cross the blood-brain-barrier into the central nervous system, and for this reason, has only minimal analgesic activity. In the United States, noroxymorphone is controlled as a Schedule II Narcotic controlled substance with an ACSCN of 9637 and in 2014 the DEA set annual aggregate manufacturing quotas of 17 500 kilogrammes for conversion and 1262.5 kg for sale. In other countries, it may be similarly controlled, controlled at a lower level, or regulated in another way. See also * Oxymorphone hydrazone * Oxymorphol - a metabolite of oxymorphone and an intermediate in the creation of hydromorphone * Hydromorphone * Oxycodone * Norbuprenorphine Norbuprenorphine is a major active metabolite of ...
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Euphoria
Euphoria ( ) is the experience (or affect) of pleasure or excitement and intense feelings of well-being and happiness. Certain natural rewards and social activities, such as aerobic exercise, laughter, listening to or making music and dancing, can induce a state of euphoria. Euphoria is also a symptom of certain neurological or neuropsychiatric disorders, such as mania. Romantic love and components of the human sexual response cycle are also associated with the induction of euphoria. Certain drugs, many of which are addictive, can cause euphoria, which at least partially motivates their recreational use. Hedonic hotspots – i.e., the pleasure centers of the brain – are functionally linked. Activation of one hotspot results in the recruitment of the others. Inhibition of one hotspot results in the blunting of the effects of activating another hotspot. Therefore, the simultaneous activation of every hedonic hotspot within the reward system is believed to be ...
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Pain Relief
Pain management is an aspect of medicine and health care involving relief of pain (pain relief, analgesia, pain control) in various dimensions, from acute and simple to chronic and challenging. Most physicians and other health professionals provide some pain control in the normal course of their practice, and for the more complex instances of pain, they also call on additional help from a specific medical specialty devoted to pain, which is called pain medicine. Pain management often uses a multidisciplinary approach for easing the suffering and improving the quality of life of anyone experiencing pain, whether acute pain or chronic pain. Relief of pain in general (analgesia) is often an acute affair, whereas managing chronic pain requires additional dimensions. The typical pain management team includes medical practitioners, pharmacists, clinical psychologists, physiotherapists, occupational therapists, recreational therapists, physician assistants, nurses, and dentists. The ...
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Controlled Release
Modified-release dosage is a mechanism that (in contrast to immediate-release dosage) delivers a drug with a delay after its administration (delayed-release dosage) or for a prolonged period of time (extended-release R, XR, XLdosage) or to a specific target in the body (targeted-release dosage).Pharmaceutics: Drug Delivery and Targeting
p. 7-13
Sustained-release dosage forms are s designed to release (liberate) a drug at a predetermined rate in order to maintain a constant drug concentratio ...
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