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Atosiban Ukuthintela Ukuzalwa Kwangethuba

ixabiso Reference: USD 50-150

  • Igama lemveliso Atosiban
  • Inombolo yeCAS. 90779-69-4
  • MF I-C43H67N11O12S2
  • MW 994.19
  • EINECS 806-815-5
  • Ukuxinana 1.254±0.06 g/cm3(Kuxelwe kwangaphambili)
  • Indawo yokubilisa 1469.0±65.0 °C(Kuxelwe kwangaphambili)

Inkcazo eneenkcukacha

Ukuzalwa ngaphambi kwexesha kubangela imingcipheko ebalulekileyo kunye nomthwalo kwiintsapho zombini kunye noluntu ngokubanzi. Ngenxa yoko, ukuthintela kunye nokunyangwa kokuzalwa ngaphambi kwexesha kubaluleke kakhulu. I-Tocolytics, efana ne-atosiban, idlala indima ebalulekileyo ekubambezelekeni kokubeleka kwangaphambili kunye nokukhusela umntwana ongekazalwa. I-Atosiban, i-cyclic nonapeptide kunye ne-oxytocin analogue, isebenza njengomchasi okhuphisanayo we-oxytocin receptors kwi-uterus, i-decidua, kunye ne-fetus membranes. Ngokuthintela ukunyanzeliswa kwesibeleko, i-atosiban iye yavela njengesixhobo esibalulekileyo seklinikhi kunyango lokuzalwa kwangaphambi kwexesha.

I-Atosiban, njenge-oxytocin edibeneyo kunye ne-vasopressin i-V1A i-receptor antagonist, inika indlela ekhethekileyo yokuthintela ukunyanzeliswa kwesibeleko. Ukufana kwesakhiwo phakathi kwe-oxytocin receptor kunye ne-vasopressin V1A i-receptor idinga ukuvinjelwa kwangaxeshanye kuzo zombini iindlela ze-receptor ukuze kuthintelwe ngokufanelekileyo ukunyanzeliswa kwesibeleko. Ngokungafaniyo nezinye i-tocolytics ezifana ne-beta-agonists, i-block blockers ye-calcium, kunye ne-prostaglandin synthase inhibitors, i-atosiban's dual receptor antagonism ivumela ukuvinjelwa okusebenzayo kwe-contraction ye-uterine. I-Oxytocin, ngaphezu kokuvuselela i-contraction ye-uterine, iphinda ikhuthaze ukuveliswa kunye nokukhululwa kwe-PGF2α, ebangela ukuba i-uterine iqhube i-muscle contraction. Ubudlelwane obuphezulu be-Atosiban be-oxytocin kunye ne-vasopressin V1A receptors ngokukhuphisanayo zibophelela kula ma-receptors, ngokufanelekileyo ukuthintela iindlela zesenzo se-oxytocin kunye ne-vasopressin. Lo matshini ukhokelela ekunciphiseni ukunyanzeliswa kwesibeleko.


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Enye yeenzuzo ezibalulekileyo ze-atosiban yimiphumo yayo encinci. Ngelixa i-tachycardia ethambileyo, ukuqina kwesifuba, isiyezi, intloko ebuhlungu, isicaphucaphu, kunye ne-dyspnea ziye zaxelwa, ezi ziphumo bezingalindelekanga azifuni nyango lukhethekileyo, kwaye ichiza alifane liyekwe ngenxa yeziphumo ebezingalindelekanga. Ngaphezu koko, i-atosiban inobomi obufutshane be-plasma, ukunciphisa ukuqokelela kwayo kwi-fetus circulation kunye nokunciphisa umngcipheko wemiphumo emibi kwi-fetus.Izilingo zeklinikhi zibonise ukusebenza kwe-atosiban ekwandiseni ukukhulelwa kwabasetyhini abaneeveki ezingaphezu kwe-28 yokukhulelwa. Kwi-multicenter, i-double-blind-blind, ilingo elilawulwa yi-placebo, unyango lwe-atosiban lubangele ukwanda kokukhulelwa ukuya kwiintsuku ze-7. Uvavanyo lweklinikhi oluthelekisayo luye lwabonisa ukuba i-atosiban inesenzo esithelekisekayo se-tocolytic kwi-ritodrine ngelixa inyamezeleka ngcono, ngakumbi malunga neziphumo ebezingalindelekanga zentliziyo kamama. Ezi ziphumo zigxininisa amandla e-atosiban njenge-agent esebenzayo kunye nokunyamezela kakuhle kwi-tocolytic.


Ngaphezu koko, ngaphaya kwendima yayo ekukhuselweni kokuzalwa kwangaphambi kwexesha, i-atosiban ibonise isithembiso ekuphuculeni iziphumo zokukhulelwa kwezigulane ezine-implantation failure (RIF) ezidlulayo kwi-vitro fertilization-embryo transfer (IVF-ET). Uphononongo luchaze ukuphuculwa okubalulekileyo kumazinga okukhulelwa, kunye nokunyuka ukusuka kwi-zero ukuya kwi-43.7% xa i-atosiban isetyenziswe.

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I-Atosiban, njenge-vasopressin/oxytocin receptor antagonist ekhuphisanayo, idlala indima ebalulekileyo ekuthinteleni ukuzalwa kwangaphambi kwexesha. Ikhono layo lokuthintela ukunyanzeliswa kwe-uterine ngokusebenzisa ukuchasana kwe-receptor ezimbini kwenza kube sisixhobo esibalulekileyo sokulibazisa umsebenzi wangaphambi kwexesha. Iziphumo ebezingalindelekanga zincinci, ubomi obufutshane besiqingatha seplasma, kunye nokuqokelelana okulinganiselweyo kumjikelezo wosana kuphucula ngakumbi iprofayile yokhuseleko. Ukongezelela, amandla e-atosiban ekuphuculeni iziphumo zokukhulelwa kwizigulane ezinokusilela okuphindaphindiweyo kokufakelwa kwe-IVF-ET kubonisa ukuguquguquka kwayo kunye nokubanakho kwiyeza lokuzala. Uphando oluqhubekayo kunye nokusetyenziswa kweklinikhi ye-atosiban kunokufaka isandla kakhulu ekunciphiseni umthwalo wokuzalwa kwangaphambi kwexesha kwiintsapho kunye noluntu.

Inkcazo

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