|
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidiarrhoeal
An anti-diarrhoeal drug (or anti-diarrheal drug in American English) is any medication which provides symptomatic relief for diarrhoea. Types * Electrolyte solutions, while not true antidiarrhoeals, are used to replace lost fluids and salts in acute cases. * Bulking agents like methylcellulose, guar gum or plant fibre (bran, sterculia, isabgol, etc.) are used for diarrhoea in functional bowel disease and to control ileostomy output. * Absorbents absorb toxic substances that cause infective diarrhoea, methylcellulose is an absorbent. * Anti-inflammatory compounds such as bismuth subsalicylate. * Anticholinergics reduce intestinal movement and are effective against both diarrhoea and accompanying cramping. * Opioids' classical use besides pain relief is as an anti-diarrhoeal drug. Opioids have agonist actions on the intestinal opioid receptors, which when activated cause constipation. Drugs such as morphine or codeine can be used to relieve diarrhoea this way. A notable opioid fo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Loperamide
Loperamide, sold under the brand name Imodium, among others,Drugs.co Page accessed September 4, 2015 is a medication used to decrease the frequency of diarrhea. It is often used for this purpose in inflammatory bowel disease and short bowel syndrome. It is not recommended for those with blood in the stool, mucus in the stool, or fevers. The medication is taken by mouth. Common side effects include abdominal pain, constipation, sleepiness, vomiting, and a dry mouth. It may increase the risk of toxic megacolon. Loperamide's safety in pregnancy is unclear, but no evidence of harm has been found. It appears to be safe in breastfeeding. It is an opioid with no significant absorption from the gut and does not cross the blood–brain barrier when used at normal doses. It works by slowing the contractions of the intestines. Loperamide was first made in 1969 and used medically in 1976. It is on the World Health Organization's List of Essential Medicines. Loperamide is available as a ge ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diphenoxylate
Diphenoxylate is a centrally active opioid drug of the phenylpiperidine series that is used as a combination drug with atropine for the treatment of diarrhea. Diphenoxylate is an opioid and acts by slowing intestinal contractions; the atropine is present to prevent drug abuse and overdose. It should not be given to children due to the risk that they will stop breathing and should not be used in people with ''Clostridium difficile'' infection. Medical use Diphenoxylate is used to treat diarrhea in adults; it is only available as a combination drug with a subtherapeutic dose of atropine to prevent abuse. It should not be used in children due to the risk of respiratory depression. It does not appear harmful to a fetus but the risks have not been fully explored. It should not be taken with other central depressants like alcohol, as they can increase its risks. It should not be used for people with diarrhea caused by an infection, for example with ''Clostridium difficile'' infec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
μ-opioid Receptor
The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical μ-opioid receptor agonist is morphine, the primary psychoactive alkaloid in opium. It is an inhibitory G-protein coupled receptor that activates the Gi alpha subunit, inhibiting adenylate cyclase activity, lowering cAMP levels. Structure The structure of the μ-opioid receptor has been determined with the antagonist β-FNA, the agonist BU72, and in a complex with DAMGO and Gi protein. Splice variants Three variants of the μ-opioid receptor are well characterized, though RT-PCR has identified up to 10 total splice variants in humans. Location They can exist either presynaptically or postsynaptically depending upon cell types. The μ-opioid receptors exist mostly presynaptically in the periaqueductal gray region, and in the superfi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Blood–brain Barrier
The blood–brain barrier (BBB) is a highly selective semipermeable membrane, semipermeable border of endothelium, endothelial cells that prevents solutes in the circulating blood from ''non-selectively'' crossing into the extracellular fluid of the central nervous system where neurons reside. The blood–brain barrier is formed by endothelial cells of the Capillary, capillary wall, astrocyte end-feet ensheathing the capillary, and pericytes embedded in the capillary basement membrane. This system allows the passage of some small molecules by passive transport, passive diffusion, as well as the selective and active transport of various nutrients, ions, organic anions, and macromolecules such as glucose and amino acids that are crucial to neural function. The blood–brain barrier restricts the passage of pathogens, the diffusion of solutes in the blood, and Molecular mass, large or Hydrophile, hydrophilic molecules into the cerebrospinal fluid, while allowing the diffusion of Hydr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidiarrhoeals
An anti-diarrhoeal drug (or anti-diarrheal drug in American English) is any medication which provides symptomatic relief for diarrhoea. Types * Electrolyte solutions, while not true antidiarrhoeals, are used to replace lost fluids and salts in acute cases. * Bulking agents like methylcellulose, guar gum or plant fibre (bran, sterculia, isabgol, etc.) are used for diarrhoea in functional bowel disease and to control ileostomy output. * Absorbents absorb toxic substances that cause infective diarrhoea, methylcellulose is an absorbent. * Anti-inflammatory compounds such as bismuth subsalicylate. * Anticholinergics reduce intestinal movement and are effective against both diarrhoea and accompanying cramping. * Opioids' classical use besides pain relief is as an anti-diarrhoeal drug. Opioids have agonist actions on the intestinal opioid receptors, which when activated cause constipation. Drugs such as morphine or codeine can be used to relieve diarrhoea this way. A notable opioid fo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
