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Norhydrocodone
Norhydrocodone is the major metabolite of the opioid analgesic hydrocodone. It is formed from hydrocodone in the liver via ''N''-demethylation predominantly by CYP3A4. Unlike hydromorphone, a minor metabolite of hydrocodone, norhydrocodone is described as inactive. However, norhydrocodone is actually an agonist of the μ-opioid receptor with similar potency to hydrocodone, but has been found to produce only minimal analgesia when administered peripherally to animals. This is likely due to poor blood-brain-barrier and thus central nervous system penetration. See also * Norbuprenorphine * Norbuprenorphine-3-glucuronide * 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 {{ana ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydrocodone
Hydrocodone, also known as dihydrocodeinone, is a semi-synthetic opioid used to treat pain and as a cough suppressant. It is taken by mouth. Typically, it is dispensed as the combination acetaminophen/hydrocodone or ibuprofen/hydrocodone for pain severe enough to require an opioid and in combination with homatropine methylbromide to relieve cough. It is also available by itself in a long-acting form sold under the brand name Zohydro ER, among others, to treat severe pain of a prolonged duration. Hydrocodone is a controlled drug: in the United States, it is classified as a Schedule II Controlled Substance. Common side effects include dizziness, sleepiness, nausea, and constipation. Serious side effects may include low blood pressure, seizures, QT prolongation, respiratory depression, and serotonin syndrome. Rapidly decreasing the dose may result in opioid withdrawal. Use during pregnancy or breastfeeding is generally not recommended. Hydrocodone is believed to work ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabolite
In biochemistry, a metabolite is an intermediate or end product of metabolism. The term is usually used for small molecules. Metabolites have various functions, including fuel, structure, signaling, stimulatory and inhibitory effects on enzymes, catalytic activity of their own (usually as a cofactor to an enzyme), defense, and interactions with other organisms (e.g. pigments, odorants, and pheromones). A primary metabolite is directly involved in normal "growth", development, and reproduction. Ethylene exemplifies a primary metabolite produced large-scale by industrial microbiology. A secondary metabolite is not directly involved in those processes, but usually has an important ecological function. Examples include antibiotics and pigments such as resins and terpenes etc. Some antibiotics use primary metabolites as precursors, such as actinomycin, which is created from the primary metabolite tryptophan. Some sugars are metabolites, such as fructose or glucose, which ar ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesia
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. Relieving pain (analgesia) is typically an acute process, while managing chronic pain involves additional complexities and ideally a multidisciplinary approach. A typical multidisciplinary pain management team may include: medical practitioners, pharmacists, clinical psychologists, physiotherapists, occupational therapists, recreationa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 Oxycodone, sold under the brand name Roxicodone and OxyContin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Normorphine
Normorphine is an opiate analogue, the N-demethylated derivative of morphine, that was first described in the 1950s when a large group of N-substituted morphine analogues were characterized for activity. The compound has relatively little opioid activity in its own right, but is a useful intermediate which can be used to produce both opioid antagonists such as nalorphine, and also potent opioid agonists such as N-phenethylnormorphine. with its formation from morphine catalyzed by the liver enzymes CYP3A4 and CYP2C8 Cytochrome P4502C8 (CYP2C8) is a member of the cytochrome P450 mixed-function oxidase system involved in the metabolism of xenobiotics in the body. Cytochrome P4502C8 also possesses epoxygenase activity, i.e. it metabolizes long-chain polyunsat .... Normorphine is a controlled substance listed under the Single Convention On Narcotic Drugs 1961 and the laws in various states implementing it; for example, in the United States it is a Schedule I Narcotic controlled ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norbuprenorphine-3-glucuronide
Norbuprenorphine-3-glucuronide (N3G) is a major active metabolite of the opioid modulator buprenorphine. It has affinity for the κ-opioid receptor (Ki = 300 nM) and the nociceptin receptor (Ki = 18 μM), but not for the μ- or δ-opioid receptors. Whether N3G acts as an agonist or antagonist of each of the former two respective sites has yet to be determined. In animals, N3G has been found to produce sedation, decreased locomotion, and a small amount of antinociception, properties which are consistent with the effects of κ-opioid receptor agonists. In addition, N3G has been found to reduce tidal volume but not respiratory rate. Unlike norbuprenorphine, but similarly to buprenorphine and buprenorphine-3-glucuronide, N3G is not a substrate for P-glycoprotein. However, due to its highly hydrophilic nature, N3G nonetheless passes the blood-brain-barrier in only very small amounts. See also * Morphine-3-glucuronide Morphine-3-glucuronide is a metabolite of morphine produce ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norbuprenorphine
Norbuprenorphine is a major active metabolite of the opioid modulator buprenorphine. It is a μ-opioid, δ-opioid, and nociceptin receptor full agonist, and a κ-opioid receptor partial agonist. In rats, unlike buprenorphine, norbuprenorphine produces marked respiratory depression but with very little antinociceptive effect. In explanation of these properties, norbuprenorphine has been found to be a high affinity P-glycoprotein substrate, and in accordance, shows very limited blood-brain-barrier penetration. See also * Norbuprenorphine-3-glucuronide * Buprenorphine-3-glucuronide * Loperamide * 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 Hydroxyarenes Tertiary alcohols Ethers Kappa-opioid receptor agonists Mu-o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Central Nervous System
The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain, spinal cord and retina. The CNS is so named because the brain integrates the received information and coordinates and influences the activity of all parts of the bodies of bilateria, bilaterally symmetric and triploblastic animals—that is, all multicellular animals except sponges and Coelenterata, diploblasts. It is a structure composed of nervous tissue positioned along the Anatomical_terms_of_location#Rostral,_cranial,_and_caudal, rostral (nose end) to caudal (tail end) axis of the body and may have an enlarged section at the rostral end which is a brain. Only arthropods, cephalopods and vertebrates have a true brain, though precursor structures exist in onychophorans, gastropods and lancelets. The rest of this article exclusively discusses the vertebrate central nervous system, which is radically distinct from all other animals. Overview In vertebrates, the brain and spinal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Potency (pharmacology)
In pharmacology, potency or biological potency is a measure of a drug's biological activity expressed in terms of the dose required to produce a pharmacological effect of given intensity. A highly potent drug (e.g., fentanyl, clonazepam, risperidone, benperidol, bumetanide) evokes a given response at low concentrations, while a drug of lower potency (e.g. morphine, alprazolam, ziprasidone, haloperidol, furosemide) evokes the same response only at higher concentrations. Higher potency does not necessarily mean greater effectiveness nor more side effects nor less side effects. Types of potency The International Union of Basic and Clinical Pharmacology (IUPHAR) has stated that "potency is an imprecise term that should always be further defined", and lists of types of potency as follows: Miscellaneous Lysergic acid diethylamide (LSD) is one of the most potent psychoactive drug A psychoactive drug, psychopharmaceutical, mind-altering drug, consciousness-altering drug, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Opioid
Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, including analgesic, pain relief. The terms "opioid" and "opiate" are sometimes used interchangeably, but the term "opioid" is used to designate all substances, both natural and synthetic, that bind to opioid receptors in the brain. Opiates are alkaloid compounds naturally found in the opium poppy plant ''Papaver somniferum''. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, and Cold medicine, suppressing cough. The opioid receptor antagonist naloxone is used to reverse opioid overdose. Extremely potent opioids such as carfentanil are approved only for Veterinary medicine, veterinary use. Opioids are also frequently use ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
