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List Of Investigational Analgesics
This is a list of investigational analgesics, or analgesics that are currently under development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses.'' Opioid receptor modulators * Axelopran/oxycodone – combination of a centrally active μ-opioid receptor agonist and a peripherally selective μ-, κ-opioid receptor, κ-, and δ-opioid receptor receptor antagonist, antagonist. * Cebranopadol (GRT-6005) – non-selective μ-opioid receptor, nociceptin receptor, and δ-opioid receptor full agonist and κ-opioid receptor partial agonist * Desmetramadol (''O''-desmethyltramadol; Omnitram) – μ-opioid receptor agonist, norepinephrine reuptake inhibitor (NRI), and 5-HT2C receptor, 5-HT2C receptor antagonist. * Lexanopadol (GRT-6006, GRT13106G) – non-selective opioid receptor agonist * Oxycodone/naltrexone – combination of a μ-opioid receptor agonist and a μ- and κ-opioid ...
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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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Ralfinamide
Ralfinamide (INN) (code names NW-1029, FCE-26742A, PNU-0154339E) is a multimodal drug which is under investigation by Newron Pharmaceuticals for the treatment of neuropathic pain and other pain conditions such as post-operative dental pain. It has a relatively complex pharmacology, acting as a mixed voltage-gated sodium channel blocker (including Nav1.7), N-type calcium channel blocker, noncompetitive NMDA receptor antagonist, and monoamine oxidase B inhibitor. It has thus far progressed as far as phase IIb/ phase III clinical trials. In 2010 it failed a phase II trial for lower back pain. Encouraging Phase II results have been announced for neuropathic pain. See also * List of investigational analgesics * Safinamide, different fluorine position * Evenamide, structurally-related antipsychotic in development * Lacosamide, used for partial-onset seizures and diabetic neuropathic pain * Ziconotide, FDA approved peptide Peptides (, ) are short chains of amino acids ...
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PF-05089771
PF-05089771 is a selective, small-molecule Nav1.7 and Nav1.8 voltage-gated sodium channel blocker under development by Pfizer as a novel analgesic. As of June 2014, it has completed phase II clinical trials for wisdom tooth removal and primary erythromelalgia. See also * List of investigational analgesics This is a list of investigational analgesics, or analgesics that are currently under development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in pare ... References External links PF-05089771 - AdisInsight Analgesics Sodium channel blockers Fluoroarenes Chlorobenzenes Thiadiazoles Pyrazoles Sulfonamides Pfizer brands {{analgesic-stub ...
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Funapide
Funapide (INN) (former developmental code names TV-45070 and XEN402) is a novel analgesic under development by Xenon Pharmaceuticals (formerly in partnership with Teva Pharmaceutical Industries) for the treatment of a variety of chronic pain conditions, including osteoarthritis, neuropathic pain, postherpetic neuralgia, and erythromelalgia, as well as dental pain. It acts as a small-molecule Nav1.7 and Nav1.8 voltage-gated sodium channel blocker. Funapide is being evaluated in humans in both oral and topical formulations, and as of July 2014, has reached phase IIb clinical trials. See also * List of investigational analgesics This is a list of investigational analgesics, or analgesics that are currently under development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in pare ... References External links Funapide - AdisInsight Analgesics Benzodioxoles Furans Local ...
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DSP-2230
DSP-2230 is a selective small-molecule Nav1.7 and Nav1.8 voltage-gated sodium channel blocker which is under development by Dainippon Sumitomo Pharma for the treatment of neuropathic pain. As of June 2014, it is in phase I/ phase II clinical trials. See also * List of investigational analgesics This is a list of investigational analgesics, or analgesics that are currently under development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in pare ... References External links * Amines Analgesics Cyclobutyl compounds Ethers Fluoroarenes Imidazopyridines Sodium channel blockers {{Analgesic-stub ...
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Cenobamate
Cenobamate, sold under the brand names Xcopri (US) and Ontozry (EU), is a medication used for the treatment of partial-onset seizures, a kind of epilepsy, in adults. It is taken by mouth. Cenobamate was approved for medical use in the United States in November 2019 and placed in Schedule V of the Controlled Substances Act in March 2020. Cenobamate was approved for medical use in the European Union in March 2021. Medical uses In the United States, cenobamate is indicated for the treatment of partial-onset seizures in adults. In the European Union, it is indicated for the adjunctive treatment of focal-onset seizures with or without secondary generalization in adults with epilepsy who have not been adequately controlled despite a history of treatment with at least two anti-epileptic medications. Contraindications Cenobamate shortens the QT interval of the heart rhythm. It is therefore contraindicated in people with familial short QT syndrome, a very rare disease of th ...
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Sodium Channel Blocker
Sodium channel blockers are drugs which impair the conduction of sodium ions (Na+) through sodium channels. Extracellular The following naturally-produced substances block sodium channels by binding to and occluding the extracellular pore opening of the channel: * Alkaloids: ** Saxitoxin (STX) ** Neosaxitoxin (NSTX) ** Tetrodotoxin (TTX) Intracellular Drugs which block sodium channels by blocking from the intracellular side of the channel include: * Local anesthetics: ''lidocaine'' * Class I antiarrhythmic agents * Various anticonvulsants: ''phenytoin, oxcarbazepine (derivative of carbamazepine)'' Unknown mechanism * Calcium has been shown to block sodium channels which explains the effects of hypercalcemia and hypocalcemia. * Lamotrigine is known to block sodium channels but it is not known whether it is extracellular or intracellular. * Cannabidiol (CBD) has been shown to cause inhibitory effects on sodium currents. This voltage-dependent inhibition is non-selective in nature ...
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