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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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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-, and δ-opioid receptor 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 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 receptor antagonist. Sodium channel blockers * BII ...
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Monoamine Oxidase Inhibitor
Monoamine oxidase inhibitors (MAOIs) are a class of drugs that inhibit the activity of one or both monoamine oxidase enzymes: monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). They are best known as effective antidepressants, especially for treatment-resistant depression and atypical depression. They are also used to treat panic disorder, social anxiety disorder, Parkinson's disease, and several other disorders. Reversible inhibitors of monoamine oxidase A (RIMAs) are a subclass of MAOIs that selectively and reversibly inhibit the MAO-A enzyme. RIMAs are used clinically in the treatment of depression and dysthymia. Due to their reversibility, they are safer in single-drug overdose than the older, irreversible MAOIs, and weaker in increasing the monoamines important in depressive disorder. RIMAs have not gained widespread market share in the United States. Medical uses MAOIs have been found to be effective in the treatment of panic disorder with ago ...
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Monoamine Oxidase Inhibitors
Monoamine oxidase inhibitors (MAOIs) are a class of drugs that inhibit the activity of one or both monoamine oxidase enzymes: monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). They are best known as effective antidepressants, especially for treatment-resistant depression and atypical depression. They are also used to treat panic disorder, social anxiety disorder, Parkinson's disease, and several other disorders. Reversible inhibitors of monoamine oxidase A (RIMAs) are a subclass of MAOIs that selectively and reversibly inhibit the MAO-A enzyme. RIMAs are used clinically in the treatment of depression and dysthymia. Due to their reversibility, they are safer in single-drug overdose than the older, irreversible MAOIs, and weaker in increasing the monoamines important in depressive disorder. RIMAs have not gained widespread market share in the United States. Medical uses MAOIs have been found to be effective in the treatment of panic disorder with agoraphobia ...
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Calcium Channel Blockers
Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists are a group of medications that disrupt the movement of calcium () through calcium channels. Calcium channel blockers are used as antihypertensive drugs, i.e., as medications to decrease blood pressure in patients with hypertension. CCBs are particularly effective against large vessel stiffness, one of the common causes of elevated systolic blood pressure in elderly patients. Calcium channel blockers are also frequently used to alter heart rate (especially from atrial fibrillation), to prevent peripheral and cerebral vasospasm, and to reduce chest pain caused by angina pectoris. N-type, L-type, and T-type voltage-dependent calcium channels are present in the zona glomerulosa of the human adrenal gland, and CCBs can directly influence the biosynthesis of aldosterone in adrenocortical cells, with consequent impact on the clinical treatment of hypertension with these agents. CCBs have be ...
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Analgesics
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 t ...
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Peptide
Peptides (, ) are short chains of amino acids linked by peptide bonds. Long chains of amino acids are called proteins. Chains of fewer than twenty amino acids are called oligopeptides, and include dipeptides, tripeptides, and tetrapeptides. A polypeptide is a longer, continuous, unbranched peptide chain. Hence, peptides fall under the broad chemical classes of biological polymers and oligomers, alongside nucleic acids, oligosaccharides, polysaccharides, and others. A polypeptide that contains more than approximately 50 amino acids is known as a protein. Proteins consist of one or more polypeptides arranged in a biologically functional way, often bound to ligands such as coenzymes and cofactors, or to another protein or other macromolecule such as DNA or RNA, or to complex macromolecular assemblies. Amino acids that have been incorporated into peptides are termed residues. A water molecule is released during formation of each amide bond.. All peptides except cyc ...
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Ziconotide
Ziconotide (SNX–111; Prialt), also called intrathecal ziconotide (ITZ) because of its administration route, is an atypical analgesic agent for the amelioration of severe and chronic pain. Derived from ''Conus magus'', a cone snail, it is the synthetic form of an ω-conotoxin peptide. It is 1,000 times as powerful as morphine. In December 2004 the Food and Drug Administration approved ziconotide when delivered as an infusion into the cerebrospinal fluid using an intrathecal pump system. Discovery Ziconotide is derived from the toxin of the cone snail species ''Conus magus''. Scientists have been intrigued by the effects of the thousands of chemicals in marine snail toxins since the initial investigations in the late 1960s by Baldomero Olivera. Olivera, now a professor of biology in the University of Utah, was inspired by accounts of the deadly effects of these toxins from his childhood in the Philippines. Ziconotide was discovered in the early 1980s by University of U ...
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Lacosamide
Lacosamide, sold under the brand name Vimpat among others, is a medication used for the treatment of partial-onset seizures and primary generalized tonic-clonic seizures. It is used by mouth or intravenously. It is available as a generic medication. Medical uses Lacosamide is indicated for the treatment of partial-onset seizures and adjunctive therapy in the treatment of primary generalized tonic-clonic seizures. Off-label use As with other anti-epileptic drugs (AEDs), lacosamide may have a variety of off-label uses, including for pain management and treatment of mental health disorders. Lacosamide and other AEDs have been used off-label in the management of bipolar disorder, cocaine addiction, dementia, depression, diabetic peripheral neuropathy, fibromyalgia, headache, hiccups, Huntington's disease, mania, migraine, obsessive-compulsive disorder, panic disorder, restless leg syndrome, and tinnitus. Combinations of AEDs are often employed for seizure reduction. Studies ar ...
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Evenamide
Evenamide () (developmental code names NW-3509, NW-3509A) is a selective voltage-gated sodium channel blocker, including (and not limited to) subtypes Nav1.3, Nav1.7, and Nav1.8, which is described as an antipsychotic and is under development by Newron Pharmaceuticals as an add-on therapy for the treatment of schizophrenia. The drug has shown efficacy in animal models of psychosis, mania, depression, and aggression. It has completed phase I clinical trials, and phase II clinical trials will be commenced in the third quarter of 2015. See also * List of investigational antipsychotics This is a list of investigational antipsychotics, or antipsychotics 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 ... References External links NW-3509 - Newron PharmaceuticalsNW-3509 - AdisInsight Antipsychotics Carboxamides Experimental drugs ...
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Safinamide
Safinamide (INN; brand name Xadago) is a drug used as an add-on treatment for Parkinson's disease with "off" episodes; it has multiple modes of action, including the inhibition of monoamine oxidase B. SeFDA index page for NDA 207145for updates. It was approved in the European Union in February 2015, in the United States in March 2017, and in Canada in January 2019. Medical uses Safinamide is used to treat idiopathic Parkinson's disease as add-on for people taking a stable dose of levodopa (L-dopa) alone or in combination with other Parkinson drugs, to help with "off" episodes when levodopa stops working. Contraindications Safinamide is contraindicated in people with severe liver impairment, with albinism, retinitis pigmentosa, severe diabetic neuropathy, uveitis and other disorders of the retina. Combination with other monoamine oxidase (MAO) inhibitors and pethidine is also contraindicated. It is not safe for women to take during pregnancy. It is excreted in breast milk ...
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