I-Sugammadex Sodiumingumphikisi wenoveli wezidakamizwa eziphumuza imisipha ezingakhiqizi (i-myorelaxants), eyabikwa okokuqala kubantu ngo-2005 futhi kusukela lapho yasetshenziswa emtholampilo eYurophu, e-United States naseJapan.Uma kuqhathaniswa nezidakamizwa zendabuko ze-anticholinesterase, ingakwazi ukuphikisa i-nerve block ejulile ngaphandle kokuthinta izinga le-acetylcholine ye-hydrolyzed kuma-synapses e-cholinergic, igwema imiphumela emibi ye-M ne-N receptor excitation, futhi ithuthukise kakhulu izinga lokuvuka kwe-post-anesthesia.Okulandelayo ukubuyekezwa kokusetshenziswa kwakamuva komtholampilo koshukela we-sodium ngesikhathi sokulala.
1. Uhlolojikelele
I-Sugammadex Sodium iwukuphuma kwe-γ-cyclodextrin eguquliwe ehlehlisa ngokuqondile umphumela wokuvinjwa kwe-neuromuscular of steroidal neuromuscular blocking agents, ikakhulukazi i-rocuronium bromide.I-Sugammadex I-Sodium chelates yamahhala ye-neuromuscular blockers ngemva komjovo futhi yenza ama-blocker e-neuromuscular angasebenzi ngokwenza inhlanganisela ezinzile encibilika emanzini ngokusebenzisa isibopho esiqinile esingu-1:1.Ngokubophezela okunjalo, kwakheka i-concentration gradient eyenza kube lula ukubuya kwesivimbeli se-neuromuscular kusuka enhlanganweni ye-neuromuscular kuya ku-plasma, ngaleyo ndlela ihlehlise umphumela wokuvinjwa kwe-neuromuscular ewukhiqizayo, ikhulule ama-receptors afana ne-nicotinic acetylcholine nokubuyisela ukudluliswa kwe-neuromuscular excitatory.
Phakathi kwe-steroidal neuromuscular blockers, i-Sugammadex Sodium inobudlelwane obuqine kakhulu be-pecuronium bromide, ilandelwa yi-rocuronium, bese kuba yi-vecuronium ne-pancuronium.Kubalulekile ukuqaphela ukuthi ukuqinisekisa ukuguqulwa okushesha nangempumelelo kwemiphumela yokuvimba kwe-neuromuscular, inani eliningiI-Sugammadex SodiumKufanele isetshenziswe ngokuhlobene nama-myorelaxants ajikelezayo.Ukwengeza, i-Sugammadex Sodium ingumphikisi othize we-steroidal neuromuscular blocking agents, futhi ayikwazi ukubopha i-benzylisoquinoline non-depolarizing myorelaxants kanye ne-depolarizing myorelaxants, ngakho-ke, ayikwazi ukuguqula imiphumela yokuvimbela neuromuscular yalezi zidakamizwa.
2. Ukusebenza kwe-sugammadex sodium
Ngokuvamile, umthamo wabaphikisi be-muscarinic ngesikhathi sokuvuka kwe-anesthetic uncike ezingeni lokuvinjelwa kwe-neuromuscular.Ngakho-ke, ukusetshenziswa kwemonitha ye-myoson kusiza ukusetshenziswa okunengqondo kwabaphikisi be-neuromuscular blocking.Imonitha ye-myorelaxation ikhipha ukugqugquzelwa kukagesi okulethwe emithanjeni ye-peripheral, okubangela ukusabela kwemoto (ukudikiza) kumsipha ohambisanayo.Amandla emisipha ayancipha noma ayanyamalala ngemva kokusetshenziswa kwe-myorelaxants.Ngenxa yalokho, izinga lokuvinjwa kwe-neuromuscular lingahlelwa njengokuthi: ibhulokhi ejulile [akukho ukunyakaziswa ngemva kwesitimela ezine-sesine (TOF) noma ukuvuselela i-tonic], i-deep block (akukho ukuxubha ngemva kwe-TOF kanye okungenani nokunyakaziswa okukodwa ngemva kwe-tonic. ukuvuselela), kanye nokuvimba okumaphakathi (okungenani okukodwa kokunyakazisa ngemva kwe-TOF).
Ngokusekelwe ezincazelweni ezingenhla, umthamo ophakanyisiwe weshukela we-sodium ukuze uhlehlise i-block emaphakathi yi-2 mg / kg, futhi isilinganiso se-TOF singafinyelela ku-0.9 ngemva kwemizuzu emi-2;umthamo onconywayo wokuhlehlisa i-block ejulile ngu-4 mg / kg, futhi isilinganiso se-TOF singafinyelela ku-0.9 ngemva kwe-1.6-3.3 min.Ukuze kufakwe ngokushesha i-anesthesia, umthamo ophezulu we-rocuronium bromide (1.2 mg/kg) awunconyelwe ukuguqulwa okujwayelekile kwe-block ejulile kakhulu.Kodwa-ke, esimweni sokubuyela okuphuthumayo ekungeneni komoya wemvelo, ukuguqulwa ngo-16 mg/kg weI-Sugammadex SodiumKunconywa.
3. Ukusetshenziswa kwe-Sugammadex Sodium ezigulini ezikhethekile
3.1.Ezigulini zezingane
Idatha evela ezifundweni zomtholampilo zesigaba II iphakamisa ukuthi i-Sugammadex Sodium iyasebenza futhi iphephile kubantu bezingane (kuhlanganise nezinsana, izinsana, izingane kanye nentsha) njengoba injalo kubantu abadala.Ukuhlaziywa kwe-meta okusekelwe ocwaningweni oluyi-10 (amacala angu-575) kanye nocwaningo lweqembu olusanda kushicilelwa (amacala angu-968) luphinde lwaqinisekisa ukuthi isikhathi (i-median) sokuthola kabusha kwesilinganiso se-4th twitch ye-myoclonic kuya ku-1st myoclonic twitch kuya ku-0.9 ezifundweni inikezwe i-rocuronium bromide 0.6 mg/kg kanye ne-Sugammadex Sodium 2 mg/kg ku-T2 isethulo sasiyi-0.6 min kuphela ezinsaneni (0.6 min) uma kuqhathaniswa nezingane (1.2 min) kanye nabantu abadala (1.2 min).1.2 iminithi nengxenye yalabo abadala (1.2 min).Ngaphezu kwalokho, ucwaningo olulodwa lwathola ukuthi i-Sugammadex Sodium yanciphisa ukwenzeka kwe-bradycardia uma kuqhathaniswa ne-neostigmine ehlanganiswe ne-atropine.Umehluko ezenzakalweni zezinye izenzakalo ezimbi ezifana ne-bronchospasm noma isicanucanu sangemva kokuhlinzwa nokuhlanza kwakungabalulekile ngokwezibalo.Kubuye kuboniswe ukuthi ukusetshenziswa kwe-Sugammadex Sodium kunciphisa izigameko zokuhlukunyezwa kwangemva kokuhlinzwa ezigulini zezingane, ezingasiza ekulawuleni isikhathi sokubuyisela.Ngaphezu kwalokho, uTadokoro et al.kuboniswe ocwaningweni lokulawulwa kwecala ukuthi kwakungekho ukuhlobana phakathi kokusabela okweqile kwe-perioperative ku-anesthesia evamile yezingane kanye nokusetshenziswa kwe-sodium sugammadex.Ngakho-ke, ukusetshenziswa kwe-Sugammadex Sodium kuphephile ezigulini zezingane ngesikhathi sokuvuka kwe-anesthesia.
3.2.Isicelo ezigulini asebekhulile
Ngokuvamile, iziguli ezindala zisengozini kakhulu emiphumeleni yokuvinjelwa kwe-neuromuscular residual kuneziguli ezincane, futhi ukululama ngokuzenzekelayo ekuvinjweni kwe-neuromuscular kuhamba kancane.Esifundweni somtholampilo se-multicenter phase III sokuphepha, ukusebenza kahle, kanye ne-pharmacokinetics ye-Sugammadex Sodium ezigulini esezikhulile, bathola ukuthi i-Sugammadex Sodium iguqule i-rocuronium ukuze ikhiqize ukwanda okuncane ngesikhathi sokuvinjelwa kwe-neuromuscular uma kuqhathaniswa neziguli ezingaphansi kweminyaka engu-65 (izikhathi ezilinganiselwe). yemizuzu engu-2.9 nemizuzu engu-2.3 ngokulandelana).Kodwa-ke, izifundo ezimbalwa ziye zabika ukuthi i-sugammadex ibekezelelwa kahle iziguli esezikhulile nokuthi akukho ukuxutshwa komcibisholo owenziwe kabusha okwenzekayo.Ngakho-ke, kubhekwa ukuthi i-Sugammadex Sodium ingasetshenziswa ngokuphepha ezigulini esezikhulile ngesikhathi sokuvuka kwe-anesthesia.
3.3.Sebenzisa kwabesifazane abakhulelwe
Kunesiqondiso esincane somtholampilo mayelana nokusetshenziswa kwe-Sugammadex Sodium kwabesifazane abakhulelwe, abavundile nabancelisayo.Kodwa-ke, izifundo zezilwane azitholanga nomthelela emazingeni e-progesterone ngesikhathi sokukhulelwa futhi akukho ukubeletha noma ukukhipha isisu kuwo wonke amagundane, okungaqondisa ukusetshenziswa komtholampilo kwe-Sugammadex Sodium ngesikhathi sokukhulelwa, ikakhulukazi ku-trimester yokuqala.Kubuye kube nenani lezigameko zokusetshenziswa komama koshukela we-sodium ngaphansi kwe-anesthesia ejwayelekile yezingxenye zokuhlinzwa, futhi azikho izinkinga zomama noma ze-fetus ezibikiwe.Nakuba ezinye izifundo zibike ukudluliswa okuncane kwe-transplacental koshukela we-sodium, kusenokuntuleka kwedatha ethembekile.Ngokuphawulekayo, abesifazane abakhulelwe abane-hypertension yokukhulelwa bavame ukuphathwa nge-magnesium sulfate.Ukuvinjelwa kokukhululwa kwe-acetylcholine ngama-ion e-magnesium kuphazamisa ukudluliswa kolwazi lwe-neuromuscular junction, kuphumuza imisipha yamathambo, futhi kukhulule imisipha yemisipha.Ngakho-ke, i-magnesium sulfate ingathuthukisa umphumela wokuvinjwa kwe-neuromuscular we-myorelaxants.
3.4.Isicelo ezigulini ezinokwehluleka kwezinso
I-Sugammadex Sodium kanye ne-sucralose-rocuronium bromide complexes ikhishwa yizinso njenge-prototypes, ukuze i-metabolism ye-Sugammadex Sodium eboshiwe kanye ne-unbound ye-Sugammadex Sodium inwetshwe ezigulini ezinokwehluleka kwezinso.Nokho, idatha yomtholampilo iphakamisa lokhoI-Sugammadex Sodiumingasetshenziswa ngokuphepha ezigulini ezine-renal yesigaba sokuphela, futhi ayikho imibiko yokuvinjelwa kwe-neuromuscular blockade ngemuva kwe-Sugammadex Sodium ezigulini ezinjalo, kodwa le datha inqunyelwe ku-48h ngemuva kokuphathwa kwe-Sugammadex Sodium.Ngaphezu kwalokho, i-sodium sugammadex-rocuronium bromide complex ingaqedwa nge-hemodialysis ene-high-flux filtration membranes.Kubalulekile ukuqaphela ukuthi isikhathi sokuguqulwa kwe-rocuronium nge-sodium sugammadex singase sinwetshwe ezigulini ezinesifo sezinso.Ngakho-ke ukusetshenziswa kokuqapha kwe-neuromuscular kubalulekile.
4. Isiphetho
I-Sugammadex Sodium ihlehlisa ngokushesha ukuvinjelwa kwe-neuromuscular okubangelwa ama-myorelaxants e-aminosteroid amaphakathi futhi ajulile, futhi kunciphisa kakhulu isigameko sokuvinjelwa kwe-neuromuscular residual uma kuqhathaniswa ne-acetylcholinesterase inhibitors evamile.I-sodium sugammadex iphinde isheshise ngokuphawulekayo isikhathi sokukhishwa ngesikhathi sokuvuka, inciphisa inani lezinsuku zokulaliswa esibhedlela, isheshisa ukutholakala kweziguli, inciphise izindleko zokulaliswa esibhedlela, futhi igcine izinsiza zezokwelapha.Kodwa-ke, ukungezwani komzimba kanye ne-arrhythmias yenhliziyo kuye kwabikwa ngezikhathi ezithile ngesikhathi sokusetshenziswa kwe-Sugammadex Sodium, ngakho-ke kusadingeka ukuthi uqaphe ngesikhathi sokusebenzisa i-Sugammadex Sodium futhi ubheke izinguquko zezimpawu ezibalulekile zeziguli, izimo zesikhumba kanye ne-ECG.Kunconywa ukuqapha ukufinyela kwemisipha yamathambo nge-monitor yokuphumula kwemisipha ukuze kunqunywe ngokunembile ukujula kwe-neuromuscular blockade futhi usebenzise umthamo ozwakalayo.i-sodium sugammadexukuthuthukisa ikhwalithi yenkathi yokuvuka.
Isikhathi sokuthumela: Sep-27-2021