Lasmiditan
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Lasmiditan
Lasmiditan, sold under the brand name Reyvow, is a medication used for the acute (active but short-term) treatment of migraine with or without aura (a sensory phenomenon or visual disturbance) in adults. It is not useful for prevention. It is taken by mouth. Common side effects include sleepiness, dizziness, tiredness, and numbness. Lasmiditan was approved in the United States in October 2019 and became available in February 2020. It was developed by Eli Lilly. The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication. Pharmacology Mechanism of action Lasmiditan is a serotonin receptor agonist that, like the unsuccessful LY-334,370, selectively binds to the 5-HT1F receptor subtype. A number of triptans have been shown to act on this subtype as well, but only after their affinity for 5-HT1B and 5-HT1D has been made responsible for their anti-migraine activity. The lack of affinity for these receptors might result in fewer side effects rel ...
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Serotonin Receptor Agonist
A serotonin receptor agonist is an agonist of one or more serotonin receptors. They activate serotonin receptors in a manner similar to that of serotonin (5-hydroxytryptamine; 5-HT), a neurotransmitter and hormone and the endogenous ligand of the serotonin receptors. Non-selective agonists Serotonergic psychedelics such as tryptamines (e.g., psilocybin, psilocin, , 5-MeO-DMT, bufotenin), lysergamides (e.g., , ergine ()), phenethylamines (e.g., mescaline, 2C-B, 25I-NBOMe), and amphetamines (e.g., , ) are non-selective agonists of serotonin receptors. Their hallucinogenic effects are specifically mediated by activation of the 5-HT2A receptor. Drugs that increase extracellular serotonin levels such as serotonin reuptake inhibitors (e.g., fluoxetine, venlafaxine), serotonin releasing agents (e.g., fenfluramine, ), and monoamine oxidase inhibitors (e.g., phenelzine, moclobemide) are indirect non-selective serotonin receptor agonists. They are used variously as antidepressants, ...
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First-in-class Medication
A first-in-class medication is a pharmaceutical that uses a "new and unique mechanism of action" to treat a particular medical condition. While the Food and Drug Administration's Center for Drug Evaluation and Research tracks first-in-class medications and reports on them annually, first-in-class is not considered a regulatory category. Although many first-in-class medications qualify as breakthrough therapies, Regenerative Medicine Advanced Therapies and/or orphan drugs, first-in-class status itself has no regulatory effect. Examples Controversy Safety By definition, a first-in-class drug does not have the safety evidence from analogous products that not-first-in-class drugs would have. However, a study investigating recalls and warnings in relation to first-in-class drugs approved between 1997 and 2012 by Health Canada has found that first-in-class drugs actually have a more favourable benefit-to-harm ratio. Economics First-in-class drugs are often seen as commerci ...
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Antimigraine Drugs
Antimigraine drugs are medications intended to reduce the effects or intensity of migraine headache. They include drugs for the treatment of acute migraine symptoms as well as drugs for the prevention of migraine attacks. Treatment of acute symptoms Examples of specific antimigraine drug classes include triptans (first line option), ergot alkaloids, ditans and gepants. Migraines can also be treated with unspecific analgesics such as nonsteroidal anti-inflammatory drugs Non-steroidal anti-inflammatory drugs (NSAID) are members of a therapeutic drug class which reduces pain, decreases inflammation, decreases fever, and prevents blood clots. Side effects depend on the specific drug, its dose and duration of ... (NSAIDs) or acetaminophen. Opioids are not recommended for treatment of migraines. Triptans The triptan drug class includes 1st generation sumatriptan (which has poor bioavailability), and second generation zolmitriptan. Due to their safety, efficacy and selectiv ...
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5-HT1F Receptor
5-hydroxytryptamine (serotonin) receptor 1F, also known as HTR1F is a 5-HT1 receptor protein and also denotes the human gene encoding it. Agonists * 5-''n''-Butyryloxy-DMT: >60-fold selectivity versus 5-HT1E receptor * BRL-54443 - mixed 5-HT1E/1F agonist * Eletriptan - mixed 5-HT1B/1D/1E/1F/2B/7 agonist * LY-334,370 - as well as related benzamides * LY-344,864 (N- 3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl4-fluorobenzamide) * Naratriptan - mixed 5-HT1B/1D/1F agonist * Lasmiditan - selective 5-HT1F agonist, a first-in-class ditan Ditans are a class of abortive medication for the treatment of migraines. The first ditan, Eli Lilly's lasmiditan, was approved by the FDA in 2019. Ditans selectively bind to the 5-HT1F receptor subtype. A number of triptans have been shown to ... molecule Antagonists ''MLS000756415'' See also * 5-HT1 receptor * 5-HT receptor References Further reading * * * * * * * * External links * * Seroto ...
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5-HT1F Agonists
5-hydroxytryptamine (serotonin) receptor 1F, also known as HTR1F is a 5-HT1 receptor protein and also denotes the human gene encoding it. Agonists * 5-''n''-Butyryloxy-DMT: >60-fold selectivity versus 5-HT1E receptor * BRL-54443 - mixed 5-HT1E/1F agonist * Eletriptan - mixed 5-HT1B/1D/1E/1F/2B/7 agonist * LY-334,370 - as well as related benzamides * LY-344,864 (N- 3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl4-fluorobenzamide) * Naratriptan - mixed 5-HT1B/1D/1F agonist * Lasmiditan - selective 5-HT1F agonist, a first-in-class ditan Ditans are a class of abortive medication for the treatment of migraines. The first ditan, Eli Lilly's lasmiditan, was approved by the FDA in 2019. Ditans selectively bind to the 5-HT1F receptor subtype. A number of triptans have been shown to ... molecule Antagonists ''MLS000756415'' See also * 5-HT1 receptor * 5-HT receptor References Further reading * * * * * * * * External links * * Seroto ...
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LY-334,370
LY-334370 is a selective 5-HT1F receptor agonist which was under development by Eli Lilly and Company for the treatment of migraine headaches. The drug showed efficacy in a phase II clinical trial but further development was halted due to toxicity detected in animals. See also * CP-135807 * Lasmiditan Lasmiditan, sold under the brand name Reyvow, is a medication used for the acute (active but short-term) treatment of migraine with or without aura (a sensory phenomenon or visual disturbance) in adults. It is not useful for prevention. It is ... * SN-22 References External links * 5-HT1F agonists Eli Lilly and Company brands Indoles Piperidines Benzamides Fluoroarenes Abandoned drugs {{nervous-system-drug-stub ...
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Open-label
An open-label trial, or open trial, is a type of clinical trial in which information is not withheld from trial participants. In particular, both the researchers and participants know which treatment is being administered. This contrasts with a double-blinded trial, where information is withheld both from the researchers and the participants to reduce bias. Open-label trials may be appropriate for comparing two similar treatments to determine which is most effective, such as a comparison of different prescription anticoagulants, or possible relief from symptoms of some disorders when a placebo is given. An open-label trial may still be randomized. Open-label trials may also be uncontrolled (without a placebo group Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dieta ...), with all parti ...
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Controlled Substances Act
The Controlled Substances Act (CSA) is the statute establishing federal government of the United States, federal drug policy of the United States, U.S. drug policy under which the manufacture, importation, possession, use, and distribution of certain substances is regulated. It was passed by the 91st United States Congress as Title II of the Comprehensive Drug Abuse Prevention and Control Act of 1970 and signed into law by President Richard Nixon. The Act also served as the national implementing legislation for the Single Convention on Narcotic Drugs. The legislation created five schedules (classifications), with varying qualifications for a substance to be included in each. Two federal agencies, the Drug Enforcement Administration (DEA) and the Food and Drug Administration (FDA), determine which substances are added to or removed from the various schedules, although the statute passed by Congress created the initial listing. Congress has sometimes scheduled other substances th ...
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Committee For Medicinal Products For Human Use
The Committee for Medicinal Products for Human Use (CHMP), formerly known as Committee for Proprietary Medicinal Products (CPMP), is the European Medicines Agency's committee responsible for elaborating the agency's opinions on all issues regarding medicinal products for human use. See also * Committee for Medicinal Products for Veterinary Use The Committee for Medicinal Products for Veterinary Use (CVMP) is the European Medicines Agency's committee responsible for elaborating the agency's opinions on all issues regarding veterinary medicines. Text was copied from this source which is © ... References External links Committee for Medicinal Products for Human Use (CHMP) Health and the European Union {{eu-stub ...
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Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ...
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European Medicines Agency
The European Medicines Agency (EMA) is an agency of the European Union (EU) in charge of the evaluation and supervision of medicinal products. Prior to 2004, it was known as the European Agency for the Evaluation of Medicinal Products or European Medicines Evaluation Agency (EMEA).Set up by EC Regulation No. 2309/93 as the European Agency for the Evaluation of Medicinal Products, and renamed by EC Regulation No. 726/2004 to the European Medicines Agency, it had the acronym EMEA until December 2009. The European Medicines Agency does not call itself EMA either – it has no official acronym but may reconsider if EMA becomes commonly accepted (secommunication on new visual identity an). The EMA was set up in 1995, with funding from the European Union and the pharmaceutical industry, as well as indirect subsidy from member states, its stated intention to harmonise (but not replace) the work of existing national medicine regulatory bodies. The hope was that this plan would not onl ...
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