| 词条 | Mometasone |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 457636529 | IUPAC_name = (9R,10S,11S,13S,14S,16R,17R)-9-chloro-17-(2-chloroacetyl)-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl furan-2-carboxylate | image = Mometasone furoate.svg | width = 250px | image2 = Mometasone furoate ball-and-stick.png | width2 = 250px | tradename = Nasonex, Asmanex, Elocon, others[1] | Drugs.com = {{drugs.com|monograph|mometasone_furoate}} | pregnancy_US = C | legal_US = Rx-only | routes_of_administration = Topical, inhalation (nasal spray) | class = Corticosteroid; Glucocorticoid | bioavailability = Nasal spray is virtually undetectable in plasma; but systemic availability is comparable to fluticasone[1] | protein_bound = 98% to 99% | metabolism = Liver | elimination_half-life = 5.8 hours | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 105102-22-5 | CAS_supplemental = {{CAS|83919-23-7}} | UNII_Ref = {{fdacite|changed|FDA}} | UNII = 8HR4QJ6DW8 | ATC_prefix = D07 | ATC_suffix = AC13 | ATC_supplemental = {{ATC|R01|AD09}}, {{ATC|R03|BA07}} | PubChem = 441336 | DrugBank_Ref = {{drugbankcite|changed|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 390091 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 47564 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 1161 | synonyms = 9α,21-Dichloro-11β,17α-dihydroxy-16α-methylpregna-1,4-diene-3,20-dione 17α-(2-furoate) | chemical_formula = C22H28Cl2O4 for mometasone C27H30O6Cl2 as furoate | molecular_weight = 427.361 g/mol (mometasone) 521.4 g/mol (furoate) | SMILES = O=C(O[C@]2(C(=O)CCl)[C@H](C)C[C@H]3[C@@H]4CCC\\1=C\\C(=O)\\C=C/[C@]/1(C)[C@@]4(Cl)[C@@H](O)C[C@]23C)c5occc5 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C27H30Cl2O6/c1-15-11-19-18-7-6-16-12-17(30)8-9-24(16,2)26(18,29)21(31)13-25(19,3)27(15,22(32)14-28)35-23(33)20-5-4-10-34-20/h4-5,8-10,12,15,18-19,21,31H,6-7,11,13-14H2,1-3H3/t15-,18+,19+,21+,24+,25+,26+,27+/m1/s1 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = WOFMFGQZHJDGCX-ZULDAHANSA-N }}Mometasone, also known as mometasone furoate, is a steroid medication used to treat certain skin conditions, hay fever, and asthma.[2][3][4] Specifically it is used to prevent rather than treat asthma attacks.[2] It can be applied to the skin, inhaled, or used in the nose.[2][3][4] Common side effects when used for asthma include headache, sore throat, and thrush.[2] Common side effects when used in the nose includes upper respiratory tract infections and nose bleeds.[4] Common side effects when applied on the skin include acne, skin atrophy, and itchiness.[3] It works by decreasing inflammation.[2] Mometasone furoate was patented in 1981 and came into medical use in 1987.[5] It is avaliable as a generic medication.[6] A month supply of the inhaler in the United Kingdom costs the NHS about 30 £ while the nasal spray is less than 2 £ as of 2019.[6] In 2016 it was the 165th most prescribed medication in the United States with more than 3 million prescriptions.[7] {{TOC limit}}Medical usesMometasone furoate is used in the treatment of inflammatory skin disorders (such as eczema and psoriasis) (topical form), allergic rhinitis (such as hay fever) (topical form), asthma (inhalation form)[8][9] for patients unresponsive to less potent corticosteroids, and penile phimosis.[10] In terms of steroid strength, it is more potent than hydrocortisone, and less potent than dexamethasone.[11] Some low-quality evidence suggests the use of mometasone for symptomatic improvement in children with adenoid hypertrophy.[12] Mometasone is used to alleviate inflammation and itchiness in skin conditions that respond to treatment with glucocorticoids such as psoriasis and atopic dermatitis.[13][14] Nasal mometasone is used in adults (including the elderly) and children over two years of age, to diminish the symptoms such as hay fever (seasonal allergic rhinitis) and other allergies (perennial rhinitis), including nasal congestion, discharge, pruritus, and sneezing and to treat nasal polyps.[25] AsthmaMometasone furoate can be used with formoterol for the treatment of asthma, due to its anti-inflammatory properties.[12][15] PharmacologyPharmacodynamicsMometasone furoate reduces inflammation by causing several effects:[16][17][18]
In addition to the glucocorticoid properties of mometasone furoate, it is a very potent agonist of the progesterone receptor as well as a partial agonist of the mineralocorticoid receptor.[19] Mechanism of actionMometasone, like other corticosteroids, possesses anti-inflammatory, antipruritic, and vasoconstrictive properties. For allergies, corticosteroids reduce the allergic reactions in various types of cells (mastocytes and eosinophils) that are responsible for allergic reactions. Mometasone and other corticosteroids circulate in the blood easily, crossing cellular membranes and binding with cytoplasmic receptors, resulting in the transcription and synthesis of proteins. It also inhibits the actions of the enzyme cytochrome P450 2C8 which participates in the activity of monooxygenase.[20] The inflammation is reduced in decreasing the liberation of hydrolace acids of leukocytes, the prevention of the accumulation macrophages in the sites of inflammation, the interference with adhesion of leukocytes to capillary walls, the reduction of the permeability of the capillary membranes and consequently edema, the reduction of complementary components, inhibition of histamine and kinin liberation, and interference with scar tissue formation.[21] The proliferation of fibroblasts and collagen deposits is also reduced. It is believed that the action of corticosteroid anti-inflammatory agents is bound to inhibitive proteins of phospholipase A2, collectively called lipocortins. The lipocortins, in turn, control the biosynthesis of potent mediators of inflammation as the prostaglandins and leukotrienes, inhibiting the liberation of the molecular precursors of arachidonic acid. Intranasal mometasone alleviates symptoms such as rhinorrhea aquosa, nasal congestion, nasal drip, sneezing, and pharyngeal itching. Topical administration applied to skin reduces the inflammation associated with chronic or acute dermatosis. PharmacokineticsMetabolismExtensive metabolic hepatic metabolism of mometasone furoate to multiple metabolites occurs. No principal metabolites are detectable in plasma. After in vitro incubation, one of the minor metabolites formed is furoate 6β-hydroxymometasone. In human hepatic microsomes, the formation of these metabolites is regulated by CYP3A4.[16] MometasoneMometasone by itself is a synthetic, steroidal glucocorticoid or corticosteroid that was never marketed.[22][23][24] The C17α furoate ester of mometasone, is the marketed medication.[22][23][24] Mometasone furoate acts as a prodrug of mometasone.[25] In addition to its glucocorticoid activity, mometasone also has very potent progestogenic activity and acts as a partial agonist of the mineralocorticoid receptor.[26] Society and cultureBrand namesAs of 2016 mometasone furoate was available worldwide in formulations for nasal, oral inhalation, and topical administration, for human and for veterinary use, and in combinations with other drugs, under many brand names.[27] It was available as of 2016 as the single active agent in the following brands: Alcom, Altosone, Asmanex, Atozon, Aureox, Belloseta, Bioelementa, Biometasona, Bloctimo, Borgasone, Breso, Broner, Codermo, Cortynase, Cutimom, Cutizone, Cutticom, Dance, Demoson, Dergentil, Derimod, Dermacortine, Dermaten, Dermome, Dermosona, Dermotasone, Dermovel, Desdek, Ecelecort, Ecural, Edelan, Elica, Elisone, Elisox, Elitasone, Elna, Elocan, Elocom, Elocon, Elocortin, Elofute, Elomet, Elomox, Eloskin, Eloson, Elosone, Elovent, Elox, Etacid, Eversone, Eztom, F-Din, Fenisona, Flazcort, Flogocort, Fremomet, Frondava, Fu Mei Song, Fulmeta, Furo, Furoato de Mometasona, Furoderm, Gistan-H, Honmet, Iflacort, Intercon, Ivoxel, Kalmente, Konex, Ladexol, Lisoder, Logren, Loksin, Lomeane, M-Furo, Makiren, Mefurosan, Melocort, Mena, Mesone, Metacortil, Metactiv, Metaflam, Metagra, Metasafe, Metason, Metasone, Metaspray, Metatop, Metaz, Metmin, Metsone, Midermin, Mifusin, Minyear, Mofacort, Mofulex, Mofur, Mofuroate, Molison, Momate, Momax, Momecon, Momecort, Momecutan, Momederm, MomeGalen, Momegen, Momekort, Momelab, Momentum, Momeplus, Momerid, Momeson, Momesone, Momester, Momet, Mometa, Mometagen, Mometason, Mometasona, Mometasona Furoato, Mometasone Furoate, Mometasone Furoate Hydrate, Mometasonfuroaat, Mometasonfuroat, Mometasoni furoas, Mometasonum, Mometasyn, Mometasyn, Mometax, Mometazon, Mometazona, Mometazona Fuorat, Mometazonfuroat, Mometix-AQ, Momevate, Momexa, Mommex, Mommox, Momtas, Monaliz, Monez, Monovel, Monovo, Mosone, Motaderm, Motaneal, Movesan, Mtaz, Mundoson, Murozo, Myrey, Narinex, Nasamet, Nasehaler, Nasocure, Nasomet, Nasometin, Nasonex, Nassomet, Nazofix, Nazoster, Netonox, Nexomist, Novasone, Ovison, Ovixan, Oximax, Pharmecort, Pluster, Pronasal, Propel, Prospiril, Pydercon, Rinelon, Rinitek, Rino-Val, Rinobudex, Rinonex, Rinosal, Rinosona, Rinoval, Risonel, Sensicort, Septopic, Silkaren, Soneta, Suavicort, Suqi, Synaller, Tabunex, Topcort, Topison, Uniclar, Uniderm, Vizomet, Yperod, Zalconex, and Zynovate.[27] CombinationsThe following combination drugs were available as of 2016:[27]
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Pract. |volume=63 |issue=5 |pages=806–19 |date=May 2009 |pmid=19392928 |doi=10.1111/j.1742-1241.2009.02003.x |url=http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=1368-5031&date=2009&volume=63&issue=5&spage=806|archive-url=https://archive.today/20130105083339/http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=1368-5031&date=2009&volume=63&issue=5&spage=806|dead-url=yes|archive-date=2013-01-05}} 10. ^{{cite journal |author=Khope S |title=Topical mometasone furoate for phimosis |journal=Indian Pediatr |volume=47 |issue=3 |pages=282 |date=March 2010 |pmid=20371899 |pmc= |doi= |url=}} 11. ^{{cite journal|last1=Williams|first1=DM|title=What does potency actually mean for inhaled corticosteroids?|journal=The Journal of Asthma|date=2005|volume=42|issue=6|pages=409–17|pmid=16293535|doi=10.1081/jas-57878}} 12. ^1 {{cite journal|last1=Passali|first1=D|last2=Spinosi|first2=MC|last3=Crisanti|first3=A|last4=Bellussi|first4=LM|title=Mometasone furoate nasal spray: a systematic review.|journal=Multidisciplinary respiratory medicine|date=2 May 2016|volume=11|pages=18|pmid=27141307|pmc=4852427|doi=10.1186/s40248-016-0054-3}} 13. ^{{cite journal|last1=Green|first1=C|last2=Colquitt|first2=JL|last3=Kirby|first3=J|last4=Davidson|first4=P|last5=Payne|first5=E|title=Clinical and cost-effectiveness of once-daily versus more frequent use of same potency topical corticosteroids for atopic eczema: a systematic review and economic evaluation.|journal=Health technology assessment (Winchester, England)|date=November 2004|volume=8|issue=47|pages=iii, iv, 1–120|pmid=15527669|url=https://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0015083/|doi=10.3310/hta8470}} 14. ^{{cite journal|last1=Prakash|first1=A|last2=Benfield|first2=P|title=Topical mometasone. 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L.|author2=Gaman EA |author3=Obach RS. |title=Examination of 209 drugs for inhibition of cytochrome P450 2C8.|publisher=J Clin Pharmacol.| date=Jan 2005 |volume=45|number=1|pages=68–78|pmid=15601807|edition=Pfizer Global Research and Development|location=USA.|section=Pharmacokientics, Pharmacodynamics, and Drug Metabolism}} 21. ^{{cite journal|last1=Blaiss|first1=MS|title=Safety update regarding intranasal corticosteroids for the treatment of allergic rhinitis.|journal=Allergy and Asthma Proceedings|date=2011|volume=32|issue=6|pages=413–8|pmid=22221434|doi=10.2500/aap.2011.32.3473}} 22. ^1 {{cite book|author=J. Elks|title=The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies|url=https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA834|date=14 November 2014|publisher=Springer|isbn=978-1-4757-2085-3|pages=834–}} 23. ^1 {{cite book|title=Index Nominum 2000: International Drug Directory|url=https://books.google.com/books?id=5GpcTQD_L2oC&pg=PA701|date=January 2000|publisher=Taylor & Francis|isbn=978-3-88763-075-1|pages=701–}} 24. ^1 {{cite book|author1=I.K. Morton|author2=Judith M. Hall|title=Concise Dictionary of Pharmacological Agents: Properties and Synonyms|url=https://books.google.com/books?id=mqaOMOtk61IC&pg=PA185|date=31 October 1999|publisher=Springer Science & Business Media|isbn=978-0-7514-0499-9|pages=185–}} 25. ^{{cite book|author1=Ruben Vardanyan|author2=Victor Hruby|title=Synthesis of Best-Seller Drugs|url=https://books.google.com/books?id=A8oHBgAAQBAJ&pg=PA463|date=7 January 2016|publisher=Elsevier Science|isbn=978-0-12-411524-8|pages=463–}} 26. ^{{vcite2 journal | vauthors = Austin RJ, Maschera B, Walker A, Fairbairn L, Meldrum E, Farrow SN, Uings IJ | title = Mometasone furoate is a less specific glucocorticoid than fluticasone propionate | journal = Eur. Respir. J. | volume = 20 | issue = 6 | pages = 1386–92 | year = 2002 | pmid = 12503693 | doi = 10.1183/09031936.02.02472001| url = }} 27. ^1 2 3 {{cite web|title=International brands for Mometasone|url=https://www.drugs.com/international/mometasone.html|publisher=Drugs.com|accessdate=17 November 2016}} External links
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