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Oliceridine
Oliceridine, sold under the brand name Olinvyk, is an opioid medication that is used for the treatment of moderate to severe acute pain in adults. It is given by intravenous (IV) injection. The most common side effects include nausea, vomiting, dizziness, headache, constipation, itchy skin and low oxygen levels in blood. It was approved for medical use in the United States in August 2020. Medical uses Oliceridine is indicated for short-term intravenous use in hospitals or other controlled clinical settings, such as during inpatient and outpatient procedures. It is not indicated for at-home use. Adverse effects The safety profile of oliceridine is similar to other opioids. As with other opioids, the most common side effects of oliceridine are nausea, vomiting, dizziness, headache and constipation. Prolonged use of opioid analgesics during pregnancy can result in neonatal opioid withdrawal syndrome. Olinvyk carries a boxed warning about addiction, abuse and misuse; life-t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trevena Inc
Trevena, Inc. is a clinical stage biopharmaceutical company, headquartered in Chesterbrook, Pennsylvania, USA, and is involved in the discovery and development of G-protein coupled receptors (GPCR) biased ligands. Trevena was founded in 2007 with technology licensed from Duke University, which originated in the labs of company founders Robert Lefkowitz winner of the 2012 Nobel Prize in Chemistry and Howard Rockman. Trevena's approach to drug discovery is based on utilizing ligand bias, or functional selectivity, at GPCR targets to produce drugs with improved efficacy and reduced side effect profiles. Trevena was named one of the top 15 US startups of 2008 by Business Week. Trevena's expertise lies in engineering "biased ligands" that activate only the beneficial signaling pathways downstream of a GPCR to unlock new biology and avoid drug adverse effects. Trevena's pipeline currently includes a clinical stage mu-opioid biased ligand for post-operative pain, and discovery-stage prog ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Biased Agonist
Functional selectivity (or agonist trafficking, biased agonism, biased signaling, ligand bias, and differential engagement) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the endogenous hormone or peptide) at the same receptor. Functional selectivity can be present when a receptor has several possible signal transduction pathways. To which degree each pathway is activated thus depends on which ligand binds to the receptor. Functional selectivity, or biased signaling, is most extensively characterized at G protein coupled receptors (GPCRs). A number of biased agonists, such as those at muscarinic M2 receptors tested as analgesics or antiproliferative drugs, or those at opioid receptors that mediate pain, show potential at various receptor families to increase beneficial properties while reducing side effects. For example, pre-clinical studies with G protein biased agonists at the μ-opioid receptor show equivalent ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Intravenous Therapy
Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutrients for those who cannot, or will not—due to reduced mental states or otherwise—consume food or water per os, by mouth. It may also be used to administer pharmaceutical drug, medications or other medical therapy such as blood transfusion, blood products or electrolytes to correct electrolyte imbalances. Attempts at providing intravenous therapy have been recorded as early as the 1400s, but the practice did not become widespread until the 1900s after the development of techniques for safe, effective use. The intravenous route is the fastest way to deliver medications and fluid replacement throughout the body as they are introduced directly into the circulatory system and thus quickly distributed. For this reason, the intravenous route ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Internalization
In biochemistry, in the biological context of organisms' regulation of gene expression and production of gene products, downregulation is the process by which a cell decreases the production and quantities of its cellular components, such as RNA and proteins, in response to an external stimulus. The complementary process that involves increase in quantities of cellular components is called upregulation. An example of downregulation is the cellular decrease in the expression of a specific receptor in response to its increased activation by a molecule, such as a hormone or neurotransmitter, which reduces the cell's sensitivity to the molecule. This is an example of a locally acting (negative feedback) mechanism. An example of upregulation is the response of liver cells exposed to such xenobiotic molecules as dioxin. In this situation, the cells increase their production of cytochrome P450 enzymes, which in turn increases degradation of these dioxin molecules. Downregulation or upr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Biased Ligands
Bias is an inclination toward something, or a predisposition, partiality, prejudice, preference, or predilection. Bias may also refer to: Scientific method and statistics * The bias introduced into an experiment through a confounder * Algorithmic bias, machine learning algorithms that exhibit politically unacceptable behavior * Cultural bias, interpreting and judging phenomena in terms particular to one's own culture * Funding bias, bias relative to the commercial interests of a study's financial sponsor * Reactivity bias, a bias resulting from participants behaving differently when they know they are being observed. In survey research this is sometimes called response bias. ** Hawthorne effect, often relates to improving performance in response to an intervention ** John Henry effect, sometimes relates to a behavioural change due to rivalry between groups, which may have negative outcomes ** Observer-expectancy effect, is when researcher expectations influence participant ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesics
An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. 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, recent research has suggested that classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants may be considered as an alternative. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing to the substantial risks and high chances of overdose, misuse, and addiction in the absence of medical supervision. Etymology The word ''analgesic'' derives ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TRV734
TRV734 is a drug developed by Trevena Inc which acts as a biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment. It is closely related to oliceridine and has a similar pharmacological profile, but unlike oliceridine which has to be injected, TRV734 is suitable to be administered orally. See also * PZM21 * SHR9352 * SR-17018 * Tegileridine Tegileridine is a drug which acts as a μ-opioid receptor agonist. It is closely related to compounds such as oliceridine, TRV734, and SHR9352, and shares a similar profile as a biased agonist selective for activation of the G-protein ... References Mu-opioid receptor agonists Pyridines Fluoroarenes Spiro compounds Oxygen heterocycles Secondary amines {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tegileridine
Tegileridine is a drug which acts as a μ-opioid receptor agonist. It is closely related to compounds such as oliceridine, TRV734, and SHR9352, and shares a similar profile as a biased agonist selective for activation of the G-protein G proteins, also known as guanine nucleotide-binding proteins, are a family of proteins that act as molecular switches inside cells, and are involved in transmitting signals from a variety of stimuli outside a cell to its interior. Their ... signalling pathway over β-arrestin 2 recruitment. In January 2024, tegileridine was approved in China for the treatment of moderate to severe pain after abdominal surgery. See also * PZM21 * SR-17018 References Mu-opioid receptor agonists 2-Pyridyl compounds Spiro compounds Oxygen heterocycles Secondary amines Ethoxy compounds Drugs developed by Jiangsu Hengrui {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SHR9352
SHR9352 is a drug which acts as a potent and selective biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment. It was structurally derived from oliceridine by replacing the benzylic side chain with a cyclised group, although only some compounds in the series retained the desired biased agonist profile, with some derivatives such as compound 12 being potent, unbiased μ-opioid full agonists. ] See also * PZM21 * SR-17018 * Tegileridine * TRV734 TRV734 is a drug developed by Trevena Inc which acts as a biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment. It is closely related to oliceridine and has a simi ... References External links * Mu-opioid receptor agonists 1,3-Dithiolanes 2-Pyridyl compounds Spiro compounds {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hypoventilation
Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By definition it causes an increased concentration of carbon dioxide ( hypercapnia) and respiratory acidosis. Hypoventilation is not synonymous with respiratory arrest, in which breathing ceases entirely and death occurs within minutes due to hypoxia and leads rapidly into complete anoxia, although both are medical emergencies. Hypoventilation can be considered a precursor to hypoxia, and its lethality is attributed to hypoxia with carbon dioxide toxicity. Causes Hypoventilation may be caused by: *A medical condition such as stroke affecting the brainstem *Voluntary breath-holding or underbreathing, for example, hypoventilation training or the Buteyko method. *Medication or drugs, typically when taken in accidental or intentional overdose. Opioids are a well-known cause of drug-induced hypoventilation due to the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
