Inokodzera jekiseni re intrathecal uye dzimwe nzira dzokurapa (zvakadai se systemic analgesics, adjuvant therapy kana sheath) Ziconotide ine simba, inosarudza uye inogadziriswa N-mhando yevoltage-sensitive calcium channel blocker, iyo inoshanda pamarwadzo ekudzivirira, uye haibereki. kusagadzikana kwezvinodhaka mushure mekutonga kwenguva refu, uye hazvikonzeri kutsamira mumuviri nepfungwa, uye hazvikonzerese hupenyu hunotyisa hwekufemerwa nekuda kwekuwedzeredza.Chiyero chezuva nezuva chinokurudzirwa chishoma, chine kurapa kwakanaka, kuchengetedzeka kwakanyanya, kusaita kwakashata, hapana kuramba zvinodhaka uye kupindwa muropa.Ichi chigadzirwa chine tarisiro yakakura yemusika sepainkiller.
Maererano nehuwandu husina kukwana, chiitiko chekutambudzika munyika chinenge 35% ~ 45% panguva ino, uye chiitiko chekutambudzika kune vakwegura chakanyanya kukwirira, inenge 75% ~ 90%.Ongororo yeAmerica inoratidza kuti chiitiko chemigraine chakawedzera kubva pamamiriyoni 23.6 muna 1989 kusvika kumamiriyoni 28 muna 2001. Mukuongorora kwekurwadziwa kusingaperi mumaguta matanhatu muChina, zvinowanikwa kuti chiitiko chekurwadziwa kusingaperi muvanhu vakuru ndeye 40%, uye chiyero chekurapa kurapwa ndeye 35%;Chiitiko chekurwadziwa kusingaperi kune vakwegura ndeye 65% ~ 80%, uye chiyero chekuona chiremba ndeye 85%.Mumakore achangopfuura, mari yekurapa yekunyaradza marwadzo iri kuwedzera gore negore.
Kubva ku2013 kusvika munaJuly 2015, Pain Research Center muUnited States uye masangano akawanda ezvokurapa akaita nguva yakareba, yakawanda-yepakati uye yekucherechedza yekuongorora intrathecal jekiseni ye ziconotide mu 93 vanhu vakuru vechikadzi vachena vane kurwadziwa kwakanyanya kusingaperi.Marwadzo e digital score scale uye huwandu hwekunzwa kwevarwere vane intrathecal injection ye ziconotide uye pasina jekiseni ye ziconotide yakafananidzwa Pakati pavo, varwere ve51 vakashandisa intrathecal injection ye ziconotide, asi varwere ve42 havana.Marwadzo ekutanga emarwadzo aive 7.4 uye 7.9, zvichiteerana.Nhamba yakakurudzirwa yejojo ye intrathecal ye ziconotide yaiva 0.5-2.4 mcg / zuva, iyo yakagadziriswa maererano nemhinduro yekurwadziwa kwemurwere nemigumisiro.Avhareji yekutanga dose yaive 1.6 mcg / zuva, 3.0 mcg / zuva pamwedzi mitanhatu uye 2.5 mumwedzi 9.Pamwedzi ye12, yakanga iri 1.9 mcg / zuva, uye mushure memwedzi ye6, kuderera kwehuwandu hwaive 29.4%, chiyero chekuwedzera chakasiyana chakanga chiri 6.4%, uye chiyero chekuvandudza kwehuwandu hwekunzwa kwepamusoro kwaiva 69.2% uye 35.7% maererano.Mushure memwedzi ye12, chiyero chekudzikira chaive 34.4% uye 3.4% zvakateerana, uye chiyero chekuvandudza chesero chekunzwa mamakisi yaive 85.7% uye 71.4% zvichiteerana.Mhedzisiro yepamusoro yaive yekusvotwa (19.6% uye 7.1%), kuona zvinhu (9.8% uye 11.9%) uye dzungu (13.7% uye 7.1%).Migumisiro yechidzidzo ichi zvakare yakasimbisa kushanda uye kuchengeteka kwe ziconotide inokurudzirwa semutsara wekutanga intrathecal injection.
Chidzidzo chekutanga che ziconotide chinogona kuteverwa kumashure ku1980s, apo mukana wekurapa wekushandiswa kweakaomarara uye mapuroteni-akafanana peptide muhuturu hwe conus akaongororwa kekutanga.Aya maconotoxins madiki peptides akapfuma mu disulfide bond, kazhinji 10-40 masara pakureba, kunongedza akasiyana ion nzira, GPCR uye transporter mapuroteni zvine hunyanzvi uye zvakasarudzwa.Ziconotide inonzi 25-peptide yakabva kuConus magus, iyo ine zvisungo zvitatu zve disulfide, uye pfupi β-fold yayo inorongwa munzvimbo yakasiyana-siyana yetatu-dimensional structure, iyo inobvumira kuti isarudze nzira dzeCaV2.2.
