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Ibicuruzwa

API-Ibiyobyabwenge Peptide Ziconotide / OMEGA-CGTX MVII A N ubwoko bwa calcium ya calcium

Ibisobanuro bigufi:

Ziconotide ni synthèse artificiel ya hydrophilique polypeptide ω-MVIIA muri peptide yubumara ya pasifike yo kurya amafi yo mu nyanja ya pasifika-kurya umutima-inkoko umutima, kandi niwo muti wa mbere mushya utari opioid ukoreshwa mu ivuriro.Ziconotide irashobora gukoreshwa nkumuti utari opioid analgesic kubuyobozi bwimikorere.


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Ibyerekeye Iki kintu

Irakwiriye gutera inshinge nubundi buryo bwo kuvura (nka analgesique sisitemu, imiti ivura cyangwa sheath) Ziconotide numuyoboro ukomeye, uhitamo kandi uhindagurika N-ubwoko bwa N-voltage yumvikanisha calcium ya calcium, ifasha ububabare bubi, kandi ntibitanga umusaruro kurwanya ibiyobyabwenge nyuma yubuyobozi bwigihe kirekire, kandi ntibitera kwishingikiriza kumubiri no mubitekerezo, ntanubwo bitera ihungabana ryubuhumekero byangiza ubuzima kubera kurenza urugero.Igipimo cya buri munsi gisabwa ni gito, hamwe ningaruka nziza zo gukiza, umutekano muke, kutagira ingaruka mbi, nta kurwanya ibiyobyabwenge no kwizizirwa.Iki gicuruzwa gifite isoko ryinshi nkisoko yo kubabaza.

Ibicuruzwa bidahwitse

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Kuki Duhitamo

Dukurikije imibare ituzuye, muri iki gihe umubare w’ububabare ku isi ni 35% ~ 45%, kandi n’ububabare ku bageze mu zabukuru ni bwinshi, hafi 75% ~ 90%.Ubushakashatsi bwakozwe n'Abanyamerika bugaragaza ko indwara ya migraine yiyongereye kuva kuri miliyoni 23,6 mu 1989 igera kuri miliyoni 28 mu 2001. Mu iperereza ry’ububabare budakira mu mijyi itandatu yo mu Bushinwa, byagaragaye ko indwara z’ububabare budakira ku bantu bakuru ari 40%, naho igipimo cyo kwivuza ni 35%;Indwara y'ububabare budakira ku bageze mu zabukuru ni 65% ~ 80%, naho igipimo cyo kubonana na muganga ni 85%.Mu myaka yashize, amafaranga yo kwivuza yo kugabanya ububabare ariyongera uko umwaka utashye.
Kuva mu 2013 kugeza muri Nyakanga 2015, Ikigo cy’ubushakashatsi bw’ububabare muri Amerika ndetse n’ibigo byinshi by’ubuvuzi bakoze ubushakashatsi bwigihe kirekire, hagati y’ibigo byinshi ndetse n’ubushakashatsi ku bijyanye no gutera inshinge za ziconotide mu barwayi 93 b’abakobwa b’abazungu bakuze bafite ububabare bukabije.Ububabare bw'amanota ya digitale hamwe n amanota rusange yunvikana yabarwayi bafite inshinge zatewe na ziconotide kandi nta gutera ziconotide bagereranijwe Muri bo, abarwayi 51 bakoresheje inshinge za ziconotide, mugihe abarwayi 42 batabikoze.Amanota yububabare bwibanze yari 7.4 na 7.9.Igipimo cyasabwe cyo gutera inshinge za ziconotide ni 0.5-2.4 mcg / kumunsi, cyahinduwe ukurikije uko umurwayi yababajwe ningaruka zabyo.Ikigereranyo cyambere cyambere cyari 1,6 mcg / kumunsi, 3.0 mcg / kumunsi mumezi 6 na 2.5 mumezi 9.Ku mezi 12, yari 1,9 mcg / ku munsi, kandi nyuma y'amezi 6, igabanuka ryabaye 29.4%, igipimo cyo kwiyongera kinyuranyo cyari 6.4%, naho igipimo cyo kuzamura amanota muri rusange cyari 69.2% na 35.7%.Nyuma y'amezi 12, igipimo cyo kugabanuka cyari 34.4% na 3.4%, naho iterambere ryamanota rusange ni 85.7% na 71.4%.Ingaruka zo hejuru cyane ni isesemi (19,6% na 7.1%), salusiyo (9.8% na 11.9%) no kuzunguruka (13.7% na 7.1%).Ibyavuye muri ubu bushakashatsi byongeye kwemeza imikorere n'umutekano bya ziconotide isabwa nk'umurongo wa mbere utera inshinge.

Ubushakashatsi bwibanze kuri ziconotide burashobora guhera mu myaka ya za 1980, mugihe ubushakashatsi bwakorewe uburyo bwo kuvura uburyo bukomeye bwo kuvura imiti ikoreshwa na peptide isa na peptide mu burozi bwa conus bwa mbere.Iyi conotoxine ni peptide ntoya ikungahaye kuri disulfide, mubisanzwe ibisigara 10-40 muburebure, kugirango igere kumiyoboro itandukanye ya ion, GPCR hamwe na poroteyine zitwara neza kandi neza.Ziconotide ni 25-peptide ikomoka kuri Conus magus, irimo imigozi itatu ya disulfide, kandi igufi β -gutondekanya mu buryo butandukanye mu buryo budasanzwe, butuma ihitamo guhitamo imiyoboro ya CaV2.2.


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