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Sumatriptan torgovi marki Imitrex i Treximet selektivnij agonist 5NT1 receptoriv 1 yakij vikoristovuyut dlya likuvannya migreni ta klasternogo golovnogo bolyu 2 Jogo prijmayut peroralno intranazalno abo pidshkirno 3 Terapevtichnij efekt zazvichaj nastaye vprodovzh troh godin 3 Sumatriptan Sistematichna nazva IUPAC 1 3 2 Dimethylaminoethyl 1H indol 5 yl N methyl methanesulfonamideIdentifikatoriNomer CAS 103628 46 2Kod ATC N02CC01PubChem 5358DrugBank DB00669Himichni daniFormula C14H21N3O2S Mol masa SMILES eMolecules amp PubChemFarmakokinetichni daniBiodostupnist 15 peroralno 96 pidshkirno Zv yazuvannya 14 21 Metabolizm MAOPeriod napivrozpadu 2 5 hoursVidilennya 60 secha 40 fekaliyiTerapevtichni zasterezhennyaKat vagitnosti Leg status CA POM UK only US Prescription onlyShlyahi vvedennya peroralno pidshkirno intranazalno transdermal electrophoresisJogo osnovnij efekt yak agonista serotoninovogo 5 HT1B 1D receptora 4 mozhe sprichiniti poshireni pobichni efekti taki yak tisk u grudnij klitci vtoma blyuvannya pokolyuvannya ta zapamorochennya 3 Serjozni pobichni efekti mozhut vklyuchati serotoninovij sindrom infarkti insulti ta sudomi 3 Pri nadmirnomu vzhivanni mozhut viniknuti golovni boli vid nadmirnogo vzhivannya likiv en 3 Nezrozumilo chi bezpechno vikoristovuvati pid chas vagitnosti abo goduvannya grudmi 5 Mehanizm diyi ne zovsim vivchenij preparat vhodit do grupi triptanu 3 Sumatriptan buv zapatentovanij u 1982 roci ta shvalenij dlya medichnogo vikoristannya v 1991 roci 6 Vin vhodit do pereliku osnovnih likarskih zasobiv VOOZ 7 Vin dostupnij yak zagalnij preparat 2 U 2020 roci ce buv 111 j lik yakij najchastishe priznachayut u Spoluchenih Shtatah iz ponad 5 miljoniv receptiv 8 9 Vin takozh dostupnij yak kombinovanij produkt sumatriptan naproksen Zmist 1 Medichne vikoristannya 2 Pobichni efekti 3 Mehanizm diyi 4 Farmakokinetika 5 Istoriya 6 Suspilstvo i kultura 6 1 Pravovij status 6 2 Dzheneriki 6 3 Superechka 7 Primitki 8 PosilannyaMedichne vikoristannya RedaguvatiSumatriptan efektivnij dlya pripinennya abo polegshennya intensivnosti migreni ta klasternogo golovnogo bolyu 10 Vin najbilsh efektivnij yaksho prijmati jogo nezabarom pislya pochatku bolyu 10 In yekcijnij sumatriptan ye bilsh efektivnim nizh inshi formi 11 Peroralnij sumatriptan takozh mozhna vikoristovuvati dlya likuvannya golovnogo bolyu pislya punkciyi duralnoyi obolonki 12 Pobichni efekti RedaguvatiPeredozuvannya sumatriptanu mozhe sprichiniti sulfgemoglobinemiyu ridkisnij stan pri yakomu kolir krovi zminyuyetsya z chervonogo na zelenij vnaslidok integraciyi sirki v molekulu gemoglobinu 13 Yaksho zupiniti vzhivati sumatriptan stan zminyuyetsya vprodovzh kilkoh tizhniv Serjozni sercevi zahvoryuvannya v tomu chisli letalni vinikali pislya zastosuvannya sumatriptanu v in yekciyah abo tabletkah Povidomlyalosya pro vazospazm koronarnih arterij tranzitornu ishemiyu miokarda infarkt miokarda shlunochkovu tahikardiyu ta fibrilyaciyu shlunochkiv 14 Najposhirenishimi pobichnimi efektami 15 pro yaki povidomlyali shonajmenshe 2 paciyentiv u kontrolovanih doslidzhennyah sumatriptanu pri migreni ye netipovi vidchuttya paresteziyi ta vidchuttya tepla holodu pro yaki povidomili 4 u grupi placebo ta 5 6 u grupah sumatriptanu bil ta inshi vidchuttya stiskannya vklyuchno z vidchuttyam bolyu u grudyah pro yaki povidomlyali 4 u grupi placebo ta 6 8 u grupah sumatriptanu nevrologichni simptomi zapamorochennya pro yaki povidomlyali menshe 1 u grupi placebo ta menshe 1 2 u grupah sumatriptanu Nezduzhannya vtoma sposterigalisya mensh nizh u 1 grupi placebo ta u 2 3 grup sumatriptanu Porushennya snu sposterigalosya mensh nizh u 1 u grupi placebo do 2 u grupi sumatriptanu Mehanizm diyi RedaguvatiSumatriptan molekulyarno podibnij do serotoninu 5 HT i ye agonistom receptora 5 HT tip 5 HT 1D i 5 HT 1B 16 Osnovnij terapevtichnij efekt sumatriptanu pov yazanij z jogo ingibuvannyam vivilnennya peptidu pov yazanogo z genom kalcitoninu CGRP jmovirno cherez jogo diyu 5 HT1D 1B agonista receptora 17 Ce bulo pidtverdzheno efektivnistyu neshodavno rozroblenih preparativ spryamovanih na CGRP ta antitil rozroblenih dlya profilaktiki migreni 18 Yak agonizm receptoriv 5 HT1D 1B prignichuye vivilnennya CGRP do kincya ne zrozumilo vvazhayetsya sho CGRP viklikaye sensibilizaciyu nociceptivnih nejroniv trijchastogo nerva sho spriyaye viniknennyu bolyu pri migreni 19 Pokazano takozh sho sumatriptan znizhuye aktivnist trijchastogo nerva sho jmovirno poyasnyuye efektivnist sumatriptanu pri likuvanni klasternih golovnih boliv Pokazano sho in yekcijna forma preparatu kupiruye klasternij golovnij bil protyagom 30 hvilin u 77 vipadkiv 20 Farmakokinetika RedaguvatiSumatriptan vipuskayetsya v dekilkoh formah tabletki pidshkirni in yekciyi nazalnij sprej Peroralnij prijom u viglyadi sukcinatnoyi soli maye nizku biodostupnist chastkovo cherez presistemnij metabolizm chastina jogo rozsheplyuyetsya v shlunku ta krovi persh nizh dosyagne cilovih arterij Tabletovana forma shvidkogo vivilnennya z takoyu zh biodostupnistyu ale visokoyu koncentraciyeyu mozhe dosyagti terapevtichnih efektiv u serednomu na 10 15 hvilin ranishe nizh inshi preparati dlya peroralnogo zastosuvannya Pri in yekcijnomu vvedenni sumatriptan diye shvidshe zazvichaj protyagom 10 hvilin ale efekt trivaye korotshe Sumatriptan metabolizuyetsya perevazhno monoaminoksidazoyu A do 2 5 metilsulfamoyil metil i ndol 3 il octovoyi kisloti yaka potim kon yuguyetsya z glyukuronovoyu kislotoyu Ci metaboliti vivodyatsya iz secheyu ta zhovchyu Lishe blizko 3 aktivnogo preparatu mozhe buti vidnovleno v nezminnomu viglyadi Ne maye prostogo pryamogo zv yazku mizh koncentraciyeyu sumatriptanu farmakokinetika yak takoyi v krovi ta jogo efektom proti migreni farmakodinamika Cej paradoks pevnoyu miroyu vdalosya virishiti shlyahom porivnyannya shvidkosti vsmoktuvannya riznih kompozicij sumatriptanu a ne absolyutnih kilkostej preparatu yaki voni dostavlyayut 21 22 Istoriya Redaguvati nbsp Sumatriptan u flakonahU 1991 roci Glaxo otrimala dozvil na sumatriptan yakij buv pershim dostupnim triptanom U lipni 2009 roku FDA SShA shvalila odnorazovu formu sumatriptanu dlya struminnih in yekcij Aparat zabezpechuye pidshkirnu in yekciyu sumatriptanu bez vikoristannya golki Ranishe avtoinzhektori z golkami buli dostupni v Yevropi ta Pivnichnij Americi 23 U lipni 2008 roku rozpochalisya doslidzhennya III fazi ionoforetichnogo transdermalnogo plastiru Zelrix Zecuity 24 Cej plastir vikoristovuye nizku naprugu kontrolovanu poperedno zaprogramovanim mikrochipom dlya dostavlyannya odnorazovoyi dozi sumatriptanu cherez shkiru vprodovzh 30 hvilin 25 26 Zecuity buv shvalenij FDA SShA v sichni 2013 roku 27 Prodazhi Zecuity buli pripineni cherez povidomlennya pro opiki ta podraznennya shkiri 28 Suspilstvo i kultura RedaguvatiPravovij status Redaguvati U Spoluchenih Shtatah vin dostupnij lishe za medichnim receptom Vin dostupnij bez recepta v bagatoh shtatah Avstraliyi Produkt vimagaye markuvannya farmacevtom i dostupnij lishe v upakovkah po dva bez recepta likarya 29 Odnak jogo mozhna pridbati bez recepta u Velikobritaniyi 30 ta Shveciyi 31 Dzheneriki Redaguvati Termin diyi patentiv Glaxo na sumatriptan zakinchivsya v lyutomu 2009 roku U toj chas Imitrex prodavavsya priblizno za 25 dolariv za tabletku 32 Potim Par Pharmaceutical predstavila zagalni versiyi sumatriptanu dlya in yekcij sumatriptanu sukcinatu dlya in yekcij 4 i 6 mg startovi nabori ta 4 i 6 mg zapovneni shprici kartridzhi a takozh 6 mg flakoni 33 Mylan Laboratories Inc Ranbaxy Laboratories Sandoz dochirnya kompaniya Novartis Dr Reddy s Laboratories ta inshi kompaniyi viroblyayut generichni versiyi tabletok sumatriptanu v dozah 25 50 i 100 mg Zagalni formi preparatu dostupni na rinkah SShA ta Yevropi pislya zakinchennya terminu diyi patentnogo zahistu Glaxo u vidpovidnih krayinah Forma nazalnogo spreyu sumatriptanu vidoma yak AVP 825 bula rozroblena Avanir i ye zagalnodostupnoyu v deyakih krayinah 34 Superechka Redaguvati Za danimi Amerikanskogo tovaristva golovnogo bolyu paciyenti chasto stverdzhuyut sho yim vazhko otrimati priznacheni yim triptani 35 U SShA triptani koshtuyut vid 12 do 120 dolariv za shtuku i ponad 80 planiv medichnogo strahuvannya SShA vstanovlyuyut obmezhennya na kilkist tabletok dostupnih paciyentu na misyac sho bulo nazvano dovilnim i nespravedlivim 36 Primitki Redaguvati SUMATRIPTAN SUMATRIPTANUM Opis aktivnoyi rechovini a b British national formulary BNF 76 vid 76 Pharmaceutical Press 2018 s 474 ISBN 9780857113382 a b v g d e Sumatriptan Monograph for Professionals Drugs com American Society of Health System Pharmacists Procitovano 3 bereznya 2019 Syed YY January 2016 Sumatriptan Naproxen Sodium A Review in Migraine Drugs 76 1 111 121 PMID 26628293 doi 10 1007 s40265 015 0521 8 Sumatriptan Use During Pregnancy Drugs com Procitovano 3 bereznya 2019 Analogue based Drug Discovery John Wiley amp Sons 2006 s 531 ISBN 9783527607495 World Health Organization model list of essential medicines 22nd list 2021 Geneva World Health Organization 2021 s 40 WHO MHP HPS EML 2021 02 The Top 300 of 2020 ClinCalc Procitovano 7 zhovtnya 2022 Sumatriptan Drug Usage Statistics ClinCalc Procitovano 7 zhovtnya 2022 a b Derry CJ Derry S Moore RA May 2014 Sumatriptan all routes of administration for acute migraine attacks in adults overview of Cochrane reviews The Cochrane Database of Systematic Reviews 2014 5 CD009108 PMC 6469574 PMID 24865446 doi 10 1002 14651858 CD009108 pub2 Dahlof CG 2001 Sumatriptan pharmacological basis and clinical results Current Medical Research and Opinion 17 Suppl 1 s35 s45 PMID 12463276 doi 10 1185 0300799039117010 Arhiv originalu za 17 lyutogo 2017 Procitovano 16 lipnya 2016 Shaat AM Abdalgaleil MM 1 sichnya 2021 Is theophylline more effective than sumatriptan in the treatment of post dural puncture headache A randomized clinical trial Egyptian Journal of Anaesthesia angl 37 1 310 316 ISSN 1110 1849 doi 10 1080 11101849 2021 1949195 Patient bleeds dark green 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Linn L Farr SJ 2009 Needle free subcutaneous sumatriptan Sumavel DosePro bioequivalence and ease of use Headache 49 10 1435 1444 PMID 19849720 doi 10 1111 j 1526 4610 2009 01530 x Nomer klinichnogo doslidzhennya NCT00724815 dlya The Efficacy and Tolerability of NP101 Patch in the Treatment of Acute Migraine NP101 007 na vebsajti ClinicalTrials gov SmartRelief electronically assisted drug delivery iontophoresis nupathe com Arhiv originalu za 7 January 2016 Procitovano 19 lyutogo 2018 Pierce M Marbury T O Neill C Siegel S Du W Sebree T June 2009 Zelrix a novel transdermal formulation of sumatriptan Headache 49 6 817 825 PMID 19438727 doi 10 1111 j 1526 4610 2009 01437 x Zecuity Approved by the FDA for the Acute Treatment of Migraine nupathe com Arhiv originalu za 7 January 2016 Procitovano 19 lyutogo 2018 Teva pulls migraine patch Zecuity on reports of burning scarring FiercePharma www fiercepharma com angl 13 chervnya 2016 Arhiv originalu za 21 bereznya 2017 Procitovano 10 kvitnya 2017 Poisons Standard June 2017 18 travnya 2017 Arhiv originalu za 31 lipnya 2017 Procitovano 22 lipnya 2017 Press release First Over The Counter OTC migraine pill made available Medicines and Healthcare Products Regulatory Agency Arhiv originalu za 5 December 2014 Procitovano 28 sichnya 2015 European Medicines Agency 23 listopada 2011 Assessment Report Sumatriptan Galpharm 50 mg Tablets European Medicines Agency s 20 Arhiv originalu za 7 January 2016 Procitovano 28 sichnya 2015 GlaxoSmithKline sets out to dupe migraine sufferers with Treximet smoke and mirrors Community Catalyst 24 kvitnya 2008 Procitovano 22 bereznya 2019 Par Pharmaceutical begins shipment of sumatriptan injection Par Pharmaceutical 6 listopada 2008 Arhiv originalu za 10 grudnya 2008 Procitovano 25 listopada 2008 If You Want To Make A Good Drug Great Cost Must Be Factored In Forbes 2 bereznya 2015 Arhiv originalu za 14 lyutogo 2017 Procitovano 13 lyutogo 2017 Variation in Prescription Drug Coverage for Triptans Analysis of Insurance Formularies Headache The Journal of Head and Face Pain Wiley 57 8 2017 1243 1251 PMID 28691382 doi 10 1111 head 13134 Eve Bender 7 veresnya 2017 Practice Matters Wide Variation in Triptan Coverage Across Commercial and Government Health Plans Neurology Today American Academy of Neurology 17 17 7 doi 10 1097 01 NT 0000524839 20893 03 Procitovano 26 chervnya 2022 Posilannya RedaguvatiSUMATRIPTAN SUMATRIPTAN UTIS Sumatriptan Drug Information Portal U S National Library of Medicine nbsp Cya stattya ye zagotovkoyu Vi mozhete dopomogti proyektu dorobivshi yiyi Ce povidomlennya varto zaminiti tochnishim Otrimano z https uk wikipedia org w index php title Sumatriptan amp oldid 40642156