I-Lasmiditan: I-New Migraine Drug kuPayipi

Okunye okunye okumele kube yi-triptans, kodwa imiphumela emibi ingase ibe nemkhawulo

I-Migraines iqhubeka ihlala isifo esiyingozi sezinzwa-ngisho nokufakwa kwama- triptan , okuyimithi ngokuvamile esetshenziselwa ukuhlukumeza ukuhlaselwa kwe-migraine okulinganiselayo kuya kweqile.

Inkinga nge-triptans yukuthi abamane nje basebenzela abantu-amaphesenti angaphezu kuka-35, ngokusho kwedatha yesayensi. Futhi, ngezinye izikhathi abantu bawagwema ngenxa yemiphumela emibi engathandeki, njengobunzima besifuba, ubuhlungu bomphimbo nobunzima, kanye nokugubha nokuzizwa.

Ngakho-ke, ingabe kukhona enye indlela yokuthatha i-triptan ye-migraine? Kungase kube khona eyodwa ekugcineni futhi kuthiwe yi-lasmiditan. Njenganoma imuphi umuthi, i-lasmiditan nayo ingase ibe nezinsizakalo ezithile ezidingeke zihlungwe ngabacwaningi.

Noma kunjalo, ukufunda ngalesi sidakamizwa sokulwa ne-anti-migraine kunesithakazelo sakho kangcono njengoba kungase kubonakale njengendlela enhle kakhulu kuwe esikhathini esizayo. Ukwengeza, uma kusebenza kahle, i-lasmiditan ingase ihlinzeke ngokuqondisisa okwengeziwe kwe-biology ngemuva kokuhlaselwa kwe- migraine . Futhi, ngokuqondile, lizosekela inkolelo ye-neural yemvelaphi ye-migraine ngokuphambene nenkolelo yezinsiza zemvelaphi ye-migraine.

Ingabe i-Lasmiditan iphephile futhi iphumelele?

Kuze kube manje, kunezivivinyo ezimbili zesigaba II zokuhlukumezeka:

Cabanga Ngenye

Ngokwesifundo se-Phase II esilawulwa yi-placebo esingahleliwe, i-lasmiditan ibonakala iyasebenza ekwelapheni ama-migraines ajwayelekile. Kulolu cwaningo, abahlanganyeli babenomsebenzi wokuthola iphilisi ye-placebo noma iphilisi ye-lasmiditan yokulinganisa okulinganayo (50mg, 100mg, 200mg, no-400mg).

Imiphumela yabonisa ukuthi yonke imithi yokuhlukumezeka yenza ngcono ukuphendula kwekhanda (kuchazwa njengokunciphisa ubuhlungu obukhulu noma obunzima be-migraine kuya ebuhlungu noma abuhlungu) emahoreni amabili ngemuva kokuba ikhanda liqale, kuqhathaniswa ne-placebo.

Nakuba ethembise njengendlela yokwelashwa okuphumelelayo, ukwehla kwesidakamizwa kungase kube nemiphumela emibi ehlobene ne-neurological, okuyinto abanye abahlanganyeli abaye babhekana nezinga eliphakeme le-doimalitan dose.

Lemiphumela emibi ifakiwe:

Study Two

Esinye isigaba sesibili sifunda eCephalalgia sibheka ukuphathwa kwe-intravenous (IV) ye-lasmiditan, okusho ukuthi yanikezwa nge-vein. Abahlanganyeli besifundo babenomuthi oyinhloko we-migraine we-modra futhi bathola umthamo we-IV we-lasmiditan noma i-placebo dose esibhedlela.

Imiphumela yabonisa ukuthi ngesikhathi sezinyanga ezingu-20mg, ukukhululeka kwekhanda (okuchazwe futhi njengokunciphisa ubuhlungu obukhulu noma akekho emahoreni amabili) kwakungamaphesenti angu-64 futhi i-placebo yayingamaphesenti angu-45.

Imiphumela emibi njengesizungu, i-paresthesia, nokuzwakala kwesisindo (ngokuvamile isilungu) kwakuvame kakhulu eqenjini lezinkathazo kuneqembu lama-placebo (amaphesenti angu-65 nangu-43%).

Izifundo Zithini Zisho?

Zombili lezi zifundo zisho ukuthi imilamiditan imithi ephumelelayo yokwelapha izidakamizwa ezinzima. Noma kunjalo, izifundo ziveza izinkinga zokubekezelelana mayelana nemiphumela emibi. Ucwaningo lwesigaba se-III luyadingeka ukuze kukhishwe lezi zithinta imiphumela yochungechunge lwezinzwa njengoba lezi zingase zibe yizici zokuvimbela ukusetshenziswa esikhathini esizayo.

Indlela Ukusebenza Kwe-Lasmiditan

Ngokufanayo nezinye izidakamizwa ze-migraine, indlela ecacile yokusebenza komdabu akucaci kahle.

Lokho kusho ukuthi siyazi ukuthi ivuselela izitho ezithile ze-serotonin ebuchosheni-nakubuchopho bama-migraineurs, amazinga we-serotonin atholakale ancipha.

I-Triptans , imithi yendabuko esetshenziselwa ukuphatha ama-migraines ajwayelekile, futhi ibophezela ku-serotonin receptors. Ngakho-ke, i-lasmiditan ihlukile kanjani kusuka ku-triptans? Ochwepheshe baqaphele ukuthi ama-lasmiditan ayakhethisa kakhulu kunama-triptan-awahlanganisi kuma-receptors ase-serotonin ukuthi, uma esebenze, aholela ekutheni i-blood constriction ye-blood (okuyinto i-triptans eyenzayo).

Eqinisweni, lesi sici esibi (esibizwa ngokuthi i-vasoconstriction) sinqabile kakhulu kuma-triptans futhi yingakho ziphikisana nabantu abanomlando we:

Ngaphezu kwalokho, ezifundweni zesilwane, ukutholakala kwezidakamizwa kutholakala ukuvimbela amanothi axhumene nokuvuselelwa kagesi kwe-ganglion trigeminal. Lokhu kufanelana nemibono emisha mayelana nokuthi "kungani" ngemuva kwekhanda le-migraine, okungukuthi ubuhlungu akusona umphumela oyinhloko wesitsha segazi okhulisa ukuzungeza ubuchopho, kodwa kunalokho ukuvuselelwa kwezintambo ze-trigeminal nerve.

Ngakho-ke, izidakamizwa zenza imbangela eyengeziwe yemisipha ye-migraine ubuhlungu ngokuphambene nesisulu (isitsha segazi). Lokhu kungase kuchaze ukuthi kungani ama-triptans engasebenzi kwabanye abafudukayo.

Ezinye izindlela zokwelapha ezingenakulungiswa

Kusengaphambili kakhulu ukusho ukuthi ama-lasmiditan azohambela kanjani, kodwa okungenani kunezinketho ezintsha ezishayayo, futhi ziyashintsha indlela esiqonda ngayo ukuthi i-migraines iyakhula kanjani. Isibonelo, uma uhlelo lwe-trigeminal luvuliwe ngesikhathi se-migraine, izinto ezifana ne-calcitonin ehlobene ne-peptide ehlobene nefu (CGRP) zikhishwa. Lezi ziphinde zandise izitsha zegazi ezungeze ubuchopho. Imithi evimba amaprotheni i-CGRP noma ngokuyibophezela ngokuqondile noma ebophezela ekutholeni i-receptor yayo ithuthukiswa, futhi izifundo zokuqala zithembisayo.

Ngaphezu kwalokho, futhi okuthakazelisayo nakakhulu amadivaysi (hhayi imithi) evuselela izinzwa ezithile, njenge-vagus nerve noma i-nerve supraorbital. Lezi zingase zibe izinqumo ezinhle kubantu abangakwazi ukuthatha noma ukubekezelela izidakamizwa zamanje ezisemlomo. Kodwa-ke, kungaba yindleko ephezulu nezomshwalense kungaba yinkinga.

Izwi elivela

Ngokuvamile, isithombe esikhulu lapha ukuthi lesi sigameko sibonakala siphumelele kwizifundo ezimbili zesigaba II ukuze kuphumuze ubuhlungu be-migraine. Kodwa, kubalulekile ukukhumbula ukuthi izifundo eziningi zidinga ( izigaba zesigaba III ) ukuze kukhishwe imiphumela emibi yesimiso sezinzwa njengoba lezi zingase zibe izici ezithile ezikhungethwe abanye abantu. Izindaba ezinhle ukuthi kukhona ukubhalisa noma ukuqhubekela phambili izifundo zesigaba III ngalesi sikhathi.

> Imithombo:

> Aggarwal M, Puri V, Puri S. Serotonin noCGRP ku-Migraine. Ann Neurosci . 2012 Apr; 19 (2): 88-94.

> Capi M et al. Lasmiditan yokwelashwa kwe-migraine. Izazi zezokwelapha ze-Opin Investig . 2017 Feb; 26 (2): 227-34.

> Farkkila M et al. Ukusebenza nokubekezela kwe-lasmiditan, i-agonist ye-receptor ye-5-HT (1F) yomlomo, yokwelapha okuphawulekayo kwe-migraine: isigaba sesi-2 esilawulwa yilabo bantu abalawulwa yi-placebo, i-parallel-group, isifundo esisodwa. I-Lancet Neurol. 2012 Meyi; 11 (5): 405-13.

> Ferrari MD et al. Ukwelashwa okunamandla kwe-migraine ne-5-HT1F receptor agonist lasmiditan ekhethiwe - isilingo esicatshangelwayo sokuhlolwa kwesimo. I-Cephalalgia . 2010 Oct; 30 (10): 1170-8.

> Uhlobo lwe-Tfelt-Hansen, u-Olesen J. I-agonist lasmiditan engu-5-HT1F ye-receptor lasmiditan njengokwelashwa kokuhlaselwa kwe-migraine: ukubuyekezwa kokuhlolwa kwe-phase 2 elawulwa yi-placebo. I-J Headache Pain . 2012 Jun; 13 (4): 271-75.