Na Cocer Peptides 
hashize iminsi 13
INGINGO ZOSE N'AMAKURU Y’IBICURUZWA BITANZWE KURI URU RUBUGA BISANZWE KUBONA AMAKURU N'INTEGO Z'UBUREZI.
Ibicuruzwa byatanzwe kururu rubuga bigenewe gusa mubushakashatsi bwa vitro. Mu bushakashatsi bwa vitro (Ikilatini: * mu kirahure *, bisobanura mu bikoresho by'ibirahure) bikorwa hanze y'umubiri w'umuntu. Ibicuruzwa ntabwo ari imiti, ntabwo byemejwe n’ikigo cy’Amerika gishinzwe ibiryo n’ibiyobyabwenge (FDA), kandi ntigomba gukoreshwa mu gukumira, kuvura, cyangwa gukiza indwara iyo ari yo yose y’ubuvuzi, indwara, cyangwa indwara. Birabujijwe rwose n'amategeko kwinjiza ibyo bicuruzwa mumubiri wabantu cyangwa inyamaswa muburyo ubwo aribwo bwose.
Incamake ya Semaglutid
Semaglutid ni glucagon nshyashya imeze nka peptide-1 reseptor agonist (GLP-1 RA). Glucagon imeze nka peptide-1 (GLP-1) ni imisemburo isanzwe isohoka mumubiri wumuntu igira uruhare runini mugutunganya glucose yamaraso. Iyo urugero rwa glucose rwamaraso ruzamutse, GLP-1 irekurwa kandi ikagenga glucose yamaraso binyuze muburyo butandukanye. Nyamara, ku barwayi ba diyabete, ururenda rwa GLP-1 akenshi ntiruhagije cyangwa ingaruka zarwo ntizihagije. Semaglutide ihuza reseptor ya GLP-1, yigana ingaruka zifatika za GLP-1, bityo ikagira ingaruka zo kuvura diyabete no gucunga ibiro.
Igicapo 1 Kuvura umubyibuho ukabije n'ingaruka zazo mu kugabanya ibiro
Uruhare rwa Semaglutid mu kuvura Diyabete
Gutezimbere Ibanga rya Insuline
Mugihe cyimiterere yumubiri, iyo glucose yamaraso yiyongereye, selile enteroendocrine mumara isohora GLP-1. GLP-1 ihuza reseptor ya GLP-1 hejuru ya selile pancreatic β selile, ikora urukurikirane rw'inzira zerekana ibimenyetso byongera insuline. Semaglutid irashobora kandi guhuza cyane na reseptor ya GLP-1 hejuru ya selile pancreatic β selile, igatera insuline gusohora muburyo bwa glucose. Ibi bivuze ko iyo glucose yamaraso izamutse, Semaglutid itera neza kurekura insuline kugirango igabanye glucose yamaraso; iyo glucose yamaraso iri murwego rusanzwe, ingaruka zayo mugutezimbere insuline iba idakomeye, bityo bikagabanya ibyago byo kurwara hypoglycemia. Ubushakashatsi bwerekanye ko nyuma yo kuvurwa na Semaglutid, urwego rw’abarwayi ba insuline rwiyongera cyane, kandi glucose yamaraso irashobora kugenzurwa neza.
Igishushanyo 2: Uburyo bwo hejuru bwibiro-buringaniye hamwe nuburyo bwo hasi, glucose-centric, na cardiometabolic. Ubuvuzi bushingiye kuri Incretin bumaze gukora murwego rwo hejuru.
Bitandukanye na insuline gakondo ya insuline, nka sulfonylureas, idahwema gutera insuline ititaye ku gipimo cya glucose yamaraso kandi ishobora kongera ibyago byo kurwara hypoglycemia, Semaglutid ya glucose-concentration iterwa na insuline yo mu bwoko bwa insuline ituma igabanya neza urugero rwa glucose mu maraso mu gihe igabanya cyane indwara ya glucose y’amaraso.
Kubuza gusohora glucagon
Glucagon ni imisemburo isohorwa na pancreatic α selile izamura urugero rwa glucose yamaraso, ikora ibinyuranye na insuline. Ku barwayi ba diyabete, ururenda rwa glucagon akenshi ntirukumirwa nubwo urugero rwa glucose rwamaraso ruri hejuru. Semaglutid ikora kuri reseptor ya GLP-1 kuri selile pancreatic α selile kugirango ibuze gusohora glucagon. Iyo ururenda rwa glucagon rugabanutse, glycogenolysis yumwijima hamwe na gluconeogenezi yumubiri irahagarikwa, bikagabanya umusaruro wa glucose endogenous kandi bikagabanya urugero rwamaraso glucose. Abahanga bemeje ko mu barwayi ba diyabete yo mu bwoko bwa 2 bavuwe na Semaglutid, plasma glucagon igabanuka cyane, bikagabanya umusaruro wa glucose w’umwijima kandi bikagira uruhare runini mu guhagarika urugero rwa glucose mu maraso.
Gutinda gusiba gastric
Semaglutid ikora kuri reseptor ya GLP-1 mu nzira ya gastrointestinal kugirango igabanye ubusa gastric. Gusiba byihuse gastrica itera ibiryo kwinjira mumara mato vuba, bigatuma umuvuduko wamaraso wiyongera vuba. Mugutinda gusiba gastrica, ibiryo biguma mu gifu igihe kirekire kandi byinjira mu mara mato gahoro gahoro, bikaviramo kwinjiza glucose buhoro buhoro kandi bikarinda kwiyongera gukabije nyuma ya glucose yamaraso. Izi ngaruka zifasha kugumana urugero rwa glucose rwamaraso nyuma yo kugabanuka no kugabanya ihindagurika ryamaraso glucose. Mu bigeragezo bimwe na bimwe by’amavuriro, abarwayi bavuwe na Semaglutid bagize igabanuka rikabije ry’amaraso ya glucose nyuma y’inyuma y’imihindagurikire y’imihindagurikire y’amaraso ndetse n’imihindagurikire mito mito y’amaraso, bikazamura ubwiza bw’amaraso muri rusange. Byongeye kandi, gutinda kwa gastrici gutinda birashobora gutuma umuntu yumva yuzuye, agafasha kugabanya gufata ibiryo bityo bigafasha mukurinda glucose yamaraso no gucunga ibiro kurundi ruhande.
Igishushanyo 3: Mechanism ya Semaglutid yo gucunga umubyibuho ukabije
Gutezimbere β-Akagari Imikorere
Indwara ya hyperglycemia idakira irashobora kwangiza selile pancreatic β selile, biganisha kumikorere gahoro gahoro. Semaglutid ntago igabanya isukari yamaraso gusa iteza imbere gusohora insuline ahubwo inarinda kandi ikanasana pancreatic β selile, bityo igatezimbere imikorere ya selile. Ubushakashatsi bwa siyansi bwerekanye ko semaglutide ishobora gukora inzira zimwe na zimwe zerekana ibimenyetso byerekana inzira yo gukwirakwiza β-selile, ikabuza β-selile apoptose, bityo ikongera umubare n'imikorere ya β-selile. Mu bushakashatsi bw’inyamaswa ndetse n’ubushakashatsi bumwe na bumwe bw’ubuvuzi, byagaragaye ko nyuma yo gukoresha Semaglutid, ubushobozi bwo gusohora insuline β selile bwongerewe imbaraga, kandi kurwanya insuline byongerewe imbaraga. Ibi bifite akamaro kanini mubuvuzi bwigihe kirekire bwo kuvura diyabete yo mu bwoko bwa 2, kuko bufasha kugabanya umuvuduko windwara no kugabanya ibyago byo kurwara diyabete.
Gushyira mu bikorwa Semaglutid mu kuvura Diyabete
Semaglutid ifite uburyo butandukanye bwo gukoresha mukuvura diyabete. Ku barwayi ba diyabete yo mu bwoko bwa 2 basuzumwe, niba glucose yamaraso itazamutse cyane kandi nta ngorane zikomeye zigaragara cyangwa izindi ngaruka zikomeye, hashobora gutekerezwa monotherapy hamwe na Semaglutid. Ubushakashatsi ku mavuriro bwerekana ko abarwayi bamwe basuzumwe vuba bagabanutse cyane ku gipimo cya hemoglobine A1c (HbA1c) no kugabanuka nyuma y’igihe cyo kwivuza. Kurugero, murukurikirane rwa PIONEER yubushakashatsi, abarwayi bavuwe na Semaglutid monotherapy yo mu kanwa bagabanutse cyane kurwego rwa HbA1c ugereranije nitsinda rya placebo, bafite umutekano mwiza no kwihanganira. Ibyiza byo kwivuza ni uko birinda ingaruka ziterwa n’imiti ijyanye no kuvura hamwe, kandi ubuyobozi bwayo bworoshye bufasha kunoza uburyo bwo kuvura abarwayi.
Semaglutid irashobora kandi gukoreshwa ifatanije nindi miti. Iyo uhujwe na metformin, akaba ariwo muti wambere wumurongo wa diyabete yo mu bwoko bwa 2, utezimbere insuline kandi ugabanya glucose glucose. Iyi miti yombi ifite uburyo bwuzuzanya bwibikorwa, bigafasha kugenzura neza glucose yamaraso. Ubushakashatsi bwerekanye ko uku guhuza gahunda kurushaho kugabanya urwego rwa HbA1c kandi bikavamo kugabanuka cyane. Kurugero, mubigeragezo bimwe na bimwe byamavuriro, abarwayi bavuwe na metformin wongeyeho Semaglutid bagabanutse cyane murwego rwa HbA1c ugereranije nabakomeje kwivuza metformin, hamwe no gutakaza ibiro, nta kwiyongera gukabije kwa hypoglycemia. Ubu buryo bukwiriye abarwayi bafite glucose yamaraso itagenzuwe bihagije hamwe na metformin monotherapy.
Ku barwayi barwaye diyabete yo mu bwoko bwa 2 bafite glucose yuzuye mu maraso kandi bakeneye ubuvuzi bwa insuline, kongera Semaglutid mu buvuzi bwa insuline birashobora kugabanya urugero rwa insuline. Mu kuvura insuline, abarwayi bakunze guhura nibibazo nko kongera ibiro ndetse no kongera ibyago byo kurwara hypoglycemia. Iyo ikoreshejwe hamwe, ingaruka za Semaglutid zo guteza imbere gusohora insuline no guhagarika imisemburo ya glucagon zirashobora guhindura imikoreshereze ya insuline, kugabanya urugero, bityo bikagabanya ingaruka zo kongera ibiro na hypoglycemia. Kurugero, mubushakashatsi bumwe na bumwe bw’ubuvuzi, abarwayi bongeyeho Semaglutid mu buvuzi bwabo bwa insuline bagabanutse ku kigereranyo cya dosiye ya insuline, hamwe no kugabanuka kurwego rwa HbA1c, kugabanuka ibiro, no kugabanuka kwinshuro za hypoglycemia.
Semaglutid irashobora kandi gukoreshwa hamwe nindi miti igabanya ubukana nka SGLT2 inhibitor. SGLT2 ibuza glucose kumaraso muguteza glucose gusohora mu nkari. Guhuza byombi birashobora kurushaho kunoza igenzura ryamaraso glucose binyuze muburyo butandukanye kandi birashobora no kugira ingaruka zifatika mugucunga ibiro.
Uruhare rwa Semaglutid mugucunga ibiro
Kuribwa no kurya
Semaglutid ikora kuri reseptor ya GLP-1 muri sisitemu yo hagati yo hagati, cyane cyane muri hypothalamus. Hypothalamus n'akarere k'ingenzi mu mubiri kugenga ubushake bwo kurya no kuringaniza ingufu. Nyuma yo guhambira reseptor ya GLP-1 muri hypothalamus, semaglutide irashobora kugenga irekurwa rya neuropeptide, nko kugabanya ururenda rwa neuropeptide Y (NPY), nikintu gikomeye gikurura ubushake bwo kurya. Byongeye kandi, Semaglutid irashobora kongera ibikorwa bya neuron ya proopiomelanocortin (POMC), ibikorwa byayo bitanga ibimenyetso byo guhaga. Binyuze muri ubwo buryo, Semaglutid irwanya neza ubushake bwo kurya, bigatuma abarwayi bagabanya ibiryo byabo. Mu bigeragezo by’amavuriro, abarwayi bafite umubyibuho ukabije cyangwa bafite ibiro byinshi bakoresheje Semaglutid bavuze ko ubushake bwo kurya bwaragabanutse no gufata ibiryo, ibyo bikaba ari byo shingiro ryo kugabanya ibiro.
Kongera ingufu zikoreshwa
Usibye guhagarika ubushake bwo kurya, Semaglutid irashobora no guhindura imbaraga za metabolism, bikongera ingufu zikoreshwa. Ubushakashatsi bwerekana ko Semaglutid ishobora kongera ingufu mu kugenzura ibikorwa bya tissue adipose. Umubiri wa adipose wijimye ni ubwoko bwihariye bwamavuta yibikorwa byibanze ni ugukoresha ingufu binyuze muri thermogenez. Semaglutid irashobora gukora inzira zimwe zerekana ibimenyetso mubice byijimye bya adipose, bigatera okiside ya aside irike hamwe na thermogenez. Byongeye kandi, Semaglutid irashobora guhindura imbaraga za metabolism mumyanya nkimitsi, kongera ingufu zikoreshwa ndetse no kuruhuka. Kurugero, mubushakashatsi bwinyamanswa, nyuma yubuyobozi bwa Semaglutid, igipimo cy’ingufu z’inyamaswa cyiyongereye, kandi ibiro by’umubiri byagabanutse nubwo gufata ibiryo byakomeje kuba bimwe, byerekana ko Semaglutid igira uruhare runini mu gucunga ibiro byongera ingufu zikoreshwa.
Kugena ibinure bya metabolism
Semaglutid nayo igira ingaruka zoguhindura ibinure. Irashobora guteza imbere igabanuka ryibinure, kugabanya ibinure, no kubuza ibinure. Mu mwijima, Semaglutid irashobora guhagarika ibikorwa bya enzymes nka synthase ya fatty acide, bityo bikagabanya synthesis ya fatty. Byongeye kandi, muri tipusi ya adipose, Semaglutid irashobora gutuma ibinure bigabanuka, bikongera irekurwa rya aside irike yubusa, kandi bikaborohereza kwinjira muri mitochondriya kugirango bigabanye okiside, bityo bigabanye kubika amavuta. Ubushakashatsi ku mavuriro bwerekanye ko nyuma yigihe cyo kuvura hamwe na Semaglutid, ibinure by’umubiri by’abarwayi, cyane cyane ibinure by’imitsi, bigabanuka. Ibi ntabwo bifasha gusa kugabanya ibiro ahubwo binagira ingaruka zikomeye mugutezimbere syndrome de metabolike no kugabanya ibyago byindwara zifata umutima.
Gushyira mu bikorwa Semaglutid mu gucunga ibiro
Ku barwayi bafite umubyibuho ukabije cyangwa umubyibuho ukabije uherekejwe n'indwara zifitanye isano
Semaglutid ifite intego igaragara yabaturage yo gucunga ibiro. Ku barwayi bafite umubyibuho ukabije ufite BMI kg30 kg / m² cyangwa abarwayi bafite ibiro byinshi bafite BMI kg27 kg / m² kandi byibura imiterere imwe ijyanye nuburemere (nka hypertension, diyabete yo mu bwoko bwa 2, cyangwa hypercholesterolemia), ni imiti ifata neza ibiro. INTAMBWE ZIKURIKIRA Ibizamini byamavuriro byagaragaje kugabanuka gukabije kubarwayi bavuwe. Mu bushakashatsi bwa STEP 1, abarwayi bavuwe bageze ku kigereranyo cyo kugabanya ibiro hafi 15% mu byumweru 68, mugihe itsinda rya placebo ryatakaje hafi 2,4%. Ibisubizo byerekana ko bishobora gufasha abarwayi bafite umubyibuho ukabije cyangwa umubyibuho ukabije ufite ibibazo bifitanye isano no kugabanya ibiro bikomeye kandi birambye, kuzamura umusaruro w’ubuzima, no kugabanya ibyago by’indwara ziterwa n'umubyibuho ukabije.
Ufatanije nubuzima bwimibereho
Mu gucunga ibiro, Semaglutid isanzwe ikoreshwa ifatanije nubuzima bwimibereho, harimo kugabanya intungamubiri za calorie no kongera imyitozo ngororamubiri. Niba kugabanya ibiro bishingiye gusa kumiti idahinduye ingeso zubuzima zitari nziza, ingaruka ntizihoraho. Guhuza ubwo buryo bwombi bigira ingaruka zifatika: imiti igabanya ubushake bwo kurya no kongera ingufu zikoreshwa, mugihe kugenzura imirire bigabanya gufata kalori no kongera imyitozo ngororamubiri byongera ingufu zikoreshwa, bigatuma umuntu agabanuka cyane. Kurugero, mubikorwa bimwe na bimwe byubuvuzi, abarwayi bakurikiza gahunda yimirire ya calorie nkeya yateguwe ninzobere mu mirire kandi bakongera igihe cyimyitozo ngororamubiri ya aerobic buri cyumweru mugihe barimo kwivuza bagera ku musaruro mwiza ugabanuka kuruta abishingikiriza gusa kumiti cyangwa kwivanga mubuzima. Ubu buryo bukomatanyije bushimangira akamaro ko gucunga neza mu gucunga ibiro, gufasha abarwayi gushyiraho ubuzima bwiza no kugera ku kugenzura igihe kirekire.
Umwanzuro
Semaglutid yerekana ubushobozi bukomeye haba kuvura diyabete no gucunga ibiro. Mu kuvura diyabete, igenzura neza glucose yamaraso ikoresheje uburyo bwinshi, itezimbere imikorere ya selile, kandi irashobora gukoreshwa nka monotherapy cyangwa ifatanije nindi miti igabanya ubukana. Mu gucunga ibiro, irwanya ubushake bwo kurya, ikongera ingufu zikoreshwa, kandi ikagenga metabolisme y’ibinure, bigatuma ibereye abarwayi bafite umubyibuho ukabije cyangwa ufite ibiro byinshi bafite ibibazo bifitanye isano. Iyo uhujwe nubuzima bwimibereho, bitanga ibisubizo byiza kurushaho.
Inkomoko
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Ibicuruzwa biboneka mubushakashatsi bukoreshwa gusa:
