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Iimveliso

I-API-Drug Peptide Ziconotide/OMEGA-CGTX MVII A N-uhlobo lwesithinteli sekhalsiyam

Inkcazelo emfutshane:

I-Ziconotide yi-artificial synthesis ye-hydrophilic polypeptide ω-MVIIA kwi-peptide yetyhefu ye-Pacific fish-eating snail-chicken heart snail, kwaye yeyokuqala entsha engeyo-opioid druganalgesic ukuba isetyenziswe ekliniki.I-Ziconotide ingasetyenziselwa njengechiza le-non-opioid analgesic yolawulo lwe-intrathecal.


Iinkcukacha zeMveliso

Iithegi zeMveliso

Malunga nale Nto

Ifanelekile kwi-injection ye-intrathecal kunye nezinye iindlela zonyango (ezifana ne-systemic analgesics, i-adjuvant therapy okanye i-sheath) i-Ziconotide inamandla, ikhethiweyo kunye nokuguqulwa kwe-N-uhlobo lwe-voltage-sensitive calcium blocker blocker, esebenzayo kwiintlungu eziphikisayo, kwaye ayivelisi. ukunganyangeki kweziyobisi emva kokulawulwa kwexesha elide, kwaye ayibangeli ukuxhomekeka ngokomzimba nangokwengqondo, kwaye ayibangeli ukudakumba okusongela ubomi ngenxa yokugqithisa ngokweqile.Idosi yemihla ngemihla ecetyiswayo incinci, inesiphumo esihle sokunyanga, ukhuseleko oluphezulu, ukusabela okungathandekiyo okuncinci, akukho kuxhathisa kumachiza kunye nokuba likhoboka.Le mveliso inethemba elikhulu lemarike njenge-painkiller.

Imveliso Dispaly

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Kutheni Khetha Thina

Ngokwezibalo ezingaphelelanga, iziganeko zentlungu ehlabathini malunga ne-35% ~ 45% okwangoku, kwaye iziganeko zentlungu kubantu abadala ziphezulu kakhulu, malunga ne-75% ~ 90%.Uphando lwaseMelika lubonisa ukuba iziganeko ze-migraine zanda ukusuka kwi-23.6 yezigidi kwi-1989 ukuya kwi-28 yezigidi kwi-2001. Kuphando lweentlungu ezingapheliyo kwiidolophu ezithandathu zaseChina, kufunyenwe ukuba iziganeko zentlungu engapheliyo kubantu abadala yi-40%, kwaye izinga lonyango lwezonyango yi-35%;Iziganeko zentlungu engapheliyo kubantu abadala yi-65% ~ 80%, kwaye izinga lokubona ugqirha ngu-85%.Kwiminyaka yakutshanje, iindleko zonyango zokuthomalalisa iintlungu zinyuka unyaka nonyaka.
Ukususela kwi-2013 ukuya kuJulayi 2015, iZiko loPhando lwentlungu e-United States kunye namaziko amaninzi ezonyango aqhube ixesha elide, i-multi-center kunye ne-observational study kwi-injection ye-intrathecal ye-ziconotide kwi-93 izigulane zabasetyhini abadala abamhlophe abaneentlungu ezinzima ezingapheliyo.Intlungu ye-digital score scale kunye ne-sensory score yezigulane ezine-injection ye-intrathecal ye-ziconotide kwaye ngaphandle kwe-injection ye-ziconotide yafaniswa Phakathi kwabo, izigulane ze-51 zisebenzisa i-injection ye-intrathecal ye-ziconotide, ngelixa izigulane ze-42 azizange.Amanqaku asezantsi entlungu ayeyi-7.4 kunye ne-7.9, ngokulandelanayo.I-dose ephakanyisiweyo ye-injection ye-intrathecal ye-ziconotide yayiyi-0.5-2.4 mcg / ngosuku, eyayihlengahlengiswa ngokwempendulo yentlungu yesigulane kunye nemiphumo emibi.I-dose eyi-avareji yokuqala yayiyi-1.6 mcg / ngosuku, i-3.0 mcg / ngosuku kwiinyanga ze-6 kunye ne-2.5 kwiinyanga ze-9.Kwiinyanga ze-12, bekuyi-1.9 mcg / ngosuku, kwaye emva kweenyanga ze-6, izinga lokunciphisa laliyi-29.4%, izinga lokunyuka kwe-6.4%, kwaye izinga lokuphucula i-sensory score laliyi-69.2% kunye ne-35.7% ngokulandelanayo.Emva kweenyanga ze-12, izinga lokuhla laliyi-34.4% kunye ne-3.4% ngokulandelanayo, kwaye izinga lokuphucula i-sensory score yayingama-85.7% kunye nama-71.4% ngokulandelanayo.Imiphumo emibi kakhulu yayiyi-nausea (19.6% kunye ne-7.1%), i-hallucination (9.8% kunye ne-11.9%) kunye nesiyezi (13.7% kunye ne-7.1%).Iziphumo zolu phononongo ziphinde zaqinisekisa ukusebenza kunye nokhuseleko lwe-ziconotide ecetyiswayo njengenaliti yomgca wokuqala we-intrathecal.

Uphononongo lokuqala kwi-ziconotide lunokulandelwa emva kwe-1980s, xa ukusetyenziswa konyango olunokubakho lwe-peptides eqinile kunye neprotheni kwi-conus venom ihlolwe okokuqala.Ezi zi-conotoxins zi-peptides ezincinci ezizityebi kwiibhondi ze-disulfide, ngokuqhelekileyo i-10-40 i-residus ubude, ukujolisa iziteshi ezahlukeneyo ze-ion, i-GPCR kunye neeprotheni zokuthutha ngokufanelekileyo nangokukhetha.I-Ziconotide yi-25-peptide ephuma kwi-Conus magus, equkethe iibhondi ezintathu ze-disulfide, kunye ne-b-fold yayo emfutshane ihlelwe ngokwendawo ibe yi-spatially ye-dimensional structure, evumela ukuba inqande ngokukhethekileyo iziteshi zeCaV2.2.


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