|
Telcagepant
Telcagepant (INN) (code name MK-0974) is a calcitonin gene-related peptide receptor antagonist which was an investigational drug for the acute treatment and prevention of migraine, developed by Merck & Co. In the acute treatment of migraine, it was found to have equal potency to rizatriptan and zolmitriptan. A Phase IIa clinical trial studying telcagepant for the prophylaxis of episodic migraine was stopped on March 26, 2009, after the "identification of two patients with significant elevations in serum transaminases". A memo to study locations stated that telcagepant had preliminarily been reported to increase the hepatic liver enzyme alanine transaminase Alanine transaminase (ALT) is a transaminase enzyme (). It is also called alanine aminotransferase (ALT or ALAT) and was formerly called serum glutamate-pyruvate transaminase or serum glutamic-pyruvic transaminase (SGPT) and was first characte ... (ALT) levels in "11 out of 660 randomized (double-blinded) study part ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Olcegepant
Olcegepant (INN Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ..., code name BIBN-4096BS) is a calcitonin gene-related peptide receptor antagonist being studied as a potential treatment for migraines. A 2013 meta-analysis found olcegepant and telcagepant were effective and safe compared to placebo. See also * Telcagepant References Amines Antimigraine drugs Carboxamides Organobromides Piperazines Piperidines 4-Pyridyl compounds Quinazolines Calcitonin gene-related peptide receptor antagonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Calcitonin Gene-related Peptide Receptor Antagonist
Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of drugs that act as receptor antagonist, antagonists of the calcitonin gene-related peptide receptor (CGRPR). Several Monoclonal antibody therapy, monoclonal antibodies which binds to the CGRP receptor or peptide have been approved for prevention of migraine. Three small molecule CGRPR antagonists are approved in the U.S. as antimigraine agents. Drugs of this class have also been investigated for use in osteoarthritis. Examples Non-peptide small molecules * Ubrogepant is approved for acute treatment of migraines *Rimegepant (BMS-927711) is approved for acute and preventative treatment of migraines *Atogepant (AGN-241689) is approved for preventative treatment of migraines *Telcagepant (MK-0974), reached phase III clinical trials; development discontinued in 2011. *Olcegepant (BIBN-4096BS) is a drug candidate *BI 44370 TA (BI 44370) * MK-3207 * SB-268262 Monoclonal antibodies targeting the CGRP receptor * Er ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Calcitonin Gene-related Peptide Receptor Antagonists
Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of drugs that act as antagonists of the calcitonin gene-related peptide receptor (CGRPR). Several monoclonal antibodies which binds to the CGRP receptor or peptide have been approved for prevention of migraine. Three small molecule CGRPR antagonists are approved in the U.S. as antimigraine agents. Drugs of this class have also been investigated for use in osteoarthritis. Examples Non-peptide small molecules * Ubrogepant is approved for acute treatment of migraines *Rimegepant (BMS-927711) is approved for acute and preventative treatment of migraines * Atogepant (AGN-241689) is approved for preventative treatment of migraines * Telcagepant (MK-0974), reached phase III clinical trials; development discontinued in 2011. * Olcegepant (BIBN-4096BS) is a drug candidate * BI 44370 TA (BI 44370) * MK-3207 * SB-268262 Monoclonal antibodies targeting the CGRP receptor * Erenumab (AMG-334) is approved for preventi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Imidazopyridines
An imidazopyridine is a nitrogen containing heterocycle that is also a class of drugs that contain this same chemical substructure. In general, they are GABAA receptor agonists, however recently proton pump inhibitors, aromatase inhibitors, NSAIDs and other classes of drugs in this class have been developed as well. Despite usually being similar to them in effect, they are not chemically related to benzodiazepines. As such, GABAA-agonizing imidazopyridines, pyrazolopyrimidines, and cyclopyrrones are sometimes grouped together and referred to as "nonbenzodiazepines." Imidazopyridines include: Sedatives Anxiolytics, sedatives and hypnotics ( GABAA receptor positive allosteric modulators): * Imidazo,2-ayridines: ** Alpidem (original brand name Ananxyl)—an anxiolytic that was withdrawn from the market worldwide in 1995 due to hepatotoxicity. ** DS-1—a GABAA receptor positive allosteric modulator selective for the α4 β3 δ subtype, which is not targeted by other GABAergics ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Piperidines
Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). It is a colorless liquid with an odor described as objectionable, and typical of amines. The name comes from the genus name '' Piper'', which is the Latin word for pepper. Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids, such as natural-occurring solenopsins. Production Piperidine was first reported in 1850 by the Scottish chemist Thomas Anderson and again, independently, in 1852 by the French chemist Auguste Cahours, who named it. Both of them obtained piperidine by reacting piperine with nitric acid. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst: : C5H5N + 3 H2 → C5H10NH Pyridine can also be redu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lactams
A lactam is a cyclic amide, formally derived from an amino alkanoic acid. The term is a portmanteau of the words '' lactone'' + ''amide''. Nomenclature Greek prefixes in alphabetical order indicate ring size: * α-Lactam (3-atom rings) * β-Lactam (4-atom rings) * γ-Lactam (5-atom rings) * δ-Lactam (6-atom rings) * ε-Lactam (7-atom rings) This ring-size nomenclature stems from the fact that a hydrolyzed α-Lactam leads to an α-amino acid and a β-Lactam to a β-amino acid, ''etc''. Synthesis General synthetic methods exist for the organic synthesis of lactams. Beckmann rearrangement Lactams form by the acid-catalyzed rearrangement of oximes in the Beckmann rearrangement. Schmidt reaction Lactams form from cyclic ketones and hydrazoic acid in the Schmidt reaction. Cyclization of amino acids Lactams can be formed from cyclisation of amino acids via the coupling between an amine and a carboxylic acid within the same molecule. Lactamization is most efficient in this ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 select ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abandoned Drugs
Abandon, abandoned, or abandonment may refer to: Common uses * Abandonment (emotional), a subjective emotional state in which people feel undesired, left behind, insecure, or discarded * Abandonment (legal), a legal term regarding property ** Child abandonment, the extralegal abandonment of children ** Lost, mislaid, and abandoned property, legal status of property after abandonment and rediscovery * Abandonment (mysticism) Art, entertainment, and media Film * ''Abandon'' (film), a 2002 film starring Katie Holmes * ''Abandoned'' (1949 film), starring Dennis O'Keefe * ''Abandoned'' (1955 film), the English language title of the Italian war film ''Gli Sbandati'' * ''Abandoned'' (2001 film), a Hungarian film * ''Abandoned'' (2010 film), starring Brittany Murphy * ''Abandoned'' (2015 film), a television movie about the shipwreck of the ''Rose-Noëlle'' in 1989 * ''Abandoned'' (2022 film), starring Emma Roberts * ''The Abandoned'' (1945 film), a 1945 Mexican film * ''The A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alanine Transaminase
Alanine transaminase (ALT) is a transaminase enzyme (). It is also called alanine aminotransferase (ALT or ALAT) and was formerly called serum glutamate-pyruvate transaminase or serum glutamic-pyruvic transaminase (SGPT) and was first characterized in the mid-1950s by Arthur Karmen and colleagues. ALT is found in plasma and in various body tissues but is most common in the liver. It catalyzes the two parts of the alanine cycle. Serum ALT level, serum AST ( aspartate transaminase) level, and their ratio ( AST/ALT ratio) are commonly measured clinically as biomarkers for liver health. The tests are part of blood panels. The half-life of ALT in the circulation approximates 47 hours. Aminotransferase is cleared by sinusoidal cells in the liver. Function ALT catalyzes the transfer of an amino group from L-alanine to α-ketoglutarate, the products of this reversible transamination reaction being pyruvate and L-glutamate. : L-alanine + α-ketoglutarate ⇌ pyruvate + L-g ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
