Semaglutide

Makhalidwe Oyambira

Kodi Semaglutide ndi chiyani?

Semaglutide ndi glucagon-ngati peptide-1 receptor agonist yomwe imagwiritsidwa ntchito mwa anthu omwe ali ndi matenda a shuga a 2 monga kuwonjezera pa zakudya ndi masewera olimbitsa thupi kuti azitha kuyendetsa bwino glycemic.. Semaglutide ndi mtundu wa GLP-1 wokhala ndi 94% yotsatizana homology kwa GLP-1 yamunthu. Imatha kumangirira ku GLP-1 receptor ndikuyambitsa cholandilira kuti chichepetse shuga m'magazi powonjezera insulin Kupanga ndikuchepetsa katulutsidwe ka glucagon ngati GLP-1 receptor agonist. Kuphatikiza apo, semaglutide imatha kuchitapo kanthu m'mimba mwa kuchedwa kutulutsa m'mimba kuti ipangitse kudzaza; pa ubongo mwa kupondereza chilakolako; ndi pa circulatory dongosolo pokonza intima yowonongeka komanso kukonza endothelial ntchito.

Kodi Semaglutide Imagwira Ntchito Motani?

Semaglutide ufa ndi agonist wa glucagon-ngati peptide-1 receptor. Imawonjezera kupanga kwa insulin, a timadzi zomwe zimachepetsa kuchuluka kwa shuga m'magazi, potengera zotsatira za incretin glucagon-like peptide-1 (GLP-1). Zikuwonekeranso kuti zimalimbikitsa kuchulukana kwa maselo a pancreatic beta, omwe amachititsa kupanga insulini ndikumasulidwa. Kuonjezera apo, AASraw semaglutide imatha kuchepetsa kupanga glucagon, hormone yomwe imayambitsa glycogenolysis (kutulutsidwa kwa ma carbs osungidwa kuchokera ku chiwindi) ndi gluconeogenesis (kupanga kwa shuga watsopano). Amachepetsa kudya mwa kuletsa njala ndikuchepetsa chimbudzi m'mimba, zomwe zimathandizira kuwonda. Zimalepheretsa kulakalaka kudya, kulakalaka chakudya, komanso kusunga mafuta.

Kafukufuku wa Semaglutide

①Mau oyamba

Semaglutide ndi mankhwala omwe adapangidwa kuti azichiza matenda a shuga. Komabe, idadziwika ngati mankhwala ochepetsa thupi atapezeka kuti amathandizira anthu kuchepetsa thupi, kuphatikiza munthu wachiwiri wolemera kwambiri padziko lonse lapansi, Elon Musk. Posachedwapa, phunziroli—-Kamodzi-Weekly Semaglutide mu Achinyamata Omwe Ali ndi Kunenepa Kwambiri-- lofalitsidwa mu New England Journal of Medicine (NEJM) wapeza kuti semaglutide ingathandizenso achinyamata onenepa kwambiri kuchepetsa thupi komanso kulimbikitsa thanzi la mtima.

②Zotsatira zazikulu

• Achinyamata onenepa kwambiri omwe adatenga semaglutide mlungu uliwonse adawona kuwonjezeka kwa 16.1% mu index mass index (BMI) muyeso lachipatala lapadziko lonse la 3a, poyerekeza ndi kuwonjezeka kwa 0.6% pagulu la placebo.
• Semaglutide ndi glucagon-ngati peptide 1 (GLP-1) receptor agonist yomwe imatha kuchepetsa chilakolako, zakudya, ndi kudya kwa kalori, zomwe zimapangitsa kuti zikhale zogwira mtima kuchepetsa thupi.
• Chiyeso chachikulu chachipatala chinasonyeza kuti semaglutide ili ndi zotsatira zodabwitsa monga mankhwala ochepetsa thupi, ndipo gulu lochizira limataya pafupifupi 15.3 kg.
• Mu June 2021, US Food and Drug Administration (FDA) idavomereza malonda a semaglutide (Semaglutide), mankhwala ochepetsa thupi omwe ali ndi dzina lamalonda la Wegovy.
• Kafukufuku waposachedwa adapeza kuti semaglutide idaposa placebo pakuchepetsa thupi komanso kusintha kwazomwe zingayambitse matenda amtima mwa achinyamata onenepa kwambiri.
• Pambuyo potenga semaglutide, zinthu zowopsa za mtima monga chiuno chozungulira, index ya magazi a shuga HbA1c, cholesterol chonse, otsika kwambiri komanso otsika kwambiri a lipoprotein cholesterol, triglycerides, ndi triglycerides bwino.
• Gulu la semaglutide linapambana gulu la placebo pamiyezo yokhudzana ndi kulemera kwa moyo, chifukwa makamaka chifukwa cha zitonthozo zapamwamba za thupi.

③Mapeto

Semaglutide yasonyezedwa kuti ndi mankhwala othandiza kuchepetsa thupi, ndipo kafukufuku waposachedwapa wasonyeza kuti angakhalenso opindulitsa kwa achinyamata onenepa kwambiri. Pamene mankhwala kugwirizana ndi ena m`mimba zotsatira zoyipazi, zapezeka kuti zimapangitsa kuti pakhale chiopsezo cha mtima komanso moyo wabwino.

Source:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9997064/

Ubwino Wogwiritsa Ntchito Semaglutide

Semaglutide ndi mankhwala osinthika omwe amapereka zabwino zambiri kwa anthu omwe ali ndi matenda osiyanasiyana. Zina mwazofala zomwe zingapindule pogwiritsa ntchito AASraw Semaglutide imaphatikizapo Type 2 Diabetes Mellitus, zoopsa za caidiovascular, kunenepa kwambiri, ndi Alzheimer's.

①Kuchepetsa Milingo ya Glucose

Semaglutide ndi GLP-1 receptor agonist yomwe imathandizira kuchepetsa kuchuluka kwa shuga m'magazi mwa anthu omwe ali ndi matenda amtundu wa 2 pogwiritsa ntchito njira zingapo. Zimathandizira katulutsidwe ka insulin, zomwe zimathandiza kusuntha shuga kuchokera m'magazi kupita m'maselo momwe angagwiritsire ntchito mphamvu. Semaglutide imachepetsanso kutulutsa kwa glucagon, komwe kumachepetsa kupanga shuga ndi chiwindi. Kuphatikiza apo, imachepetsa kutulutsa m'mimba, zomwe zimachepetsa kuchuluka kwa shuga m'magazi mukatha kudya.

M'mayesero azachipatala, semaglutide yawonetsedwa kuti imachepetsa kwambiri milingo ya HbA1c, yomwe ndi chizindikiro cha kuwongolera kwanthawi yayitali kwa shuga m'magazi. Mu kuyesa kwa SUSTAIN-1, semaglutide inachepetsa milingo ya HbA1c ndi 1.5% poyerekeza ndi placebo, ndipo muyeso la SUSTAIN-10, idachepetsa kuchuluka kwa HbA1c ndi 1.8% poyerekeza ndi placebo. Semaglutide yasonyezedwanso kuti imathandizira kuchepetsa kusala kudya kwa plasma glucose ndi postprandial glucose excursions.

②Kuchepetsa Chiwopsezo cha Zochitika Zamtima

Semaglutide yasonyezedwa kuti ichepetse chiopsezo cha zochitika zazikulu za mtima (MACE) monga imfa ya mtima, infatal myocardial infarction, ndi sitiroko yosafa kwa akuluakulu omwe ali ndi matenda a shuga a 2 ndi matenda oyambitsa matenda a mtima. Phinduli linawonedwa mu mayesero a SUSTAIN-6 ndi PIONEER-6, omwe adawonetsa kuchepa kwakukulu kwa MACE ndi chithandizo cha semaglutide poyerekeza ndi placebo. Kuphatikiza apo, Semaglutide yawonetsedwa kuti ikuwongolera zinthu zingapo zowopsa zamtima monga kuthamanga kwa magazi, mbiri ya lipid, komanso zizindikiro za kutupa kwa anthu omwe ali ndi matenda a shuga a 2. Mu mayesero a SUSTAIN-6, semaglutide inagwirizanitsidwa ndi kuchepa kwakukulu kwa kuthamanga kwa magazi kwa systolic ndi kusintha kwa mbiri ya lipid, kuphatikizapo kuchepetsa cholesterol chonse, LDL cholesterol, ndi triglycerides.

③Kuchepetsa thupi

Semaglutide ndi yamphamvu kuwonda wothandizira, ngakhale mwa anthu opanda shuga. Semaglutide imagwira ntchito pochepetsa kudya komanso kudya kwa calorie, zomwe zimapangitsa kuchepa kwa thupi. Izi zimatheka chifukwa cha zotsatira zake pakatikati pa mitsempha ya m'mimba ndi m'mimba. Semaglutide imagwira ntchito pa hypothalamus, yomwe imayang'anira njala ndi kukhuta, ndipo imachepetsa chikhumbo chofuna kudya mwa kuwonjezera kukhudzika. Kuonjezera apo, semaglutide imachepetsa kuchepa kwa m'mimba, zomwe zimatalikitsa kumva kukhuta mutatha kudya komanso kuchepetsa chilakolako chofuna kudya.

Mayesero achipatala awonetsa ubwino wolemetsa wa semaglutide.Mu pulogalamu ya STEP, yomwe inayesa kugwiritsa ntchito semaglutide pofuna kuchepetsa kulemera kwa anthu opanda matenda a shuga, semaglutide inagwirizanitsidwa ndi kulemera kwakukulu poyerekeza ndi placebo. Ophunzira omwe adalandira semaglutide kamodzi pa sabata adataya pafupifupi 15% ya kulemera kwa thupi lawo pa masabata a 68, pamene omwe adalandira placebo adataya 2.4% yokha.

Kwa anthu omwe ali ndi matenda a shuga a 2, semaglutide imatha kubweretsa zopindulitsa zina zoonda. Mu mayeso a SUSTAIN 7, omwe adayesa mphamvu ndi chitetezo cha semaglutide mwa anthu omwe ali ndi matenda a shuga a 2, semaglutide idalumikizidwa ndi kuchepa kwakukulu kwa kulemera kwa thupi poyerekeza ndi placebo. Omwe adalandira semaglutide adataya pafupifupi 4.6 kg, pomwe omwe adalandira placebo adataya 1.2 kg yokha.

④Kuchiza Matenda a Alzheimer's Symptom

Kafukufuku wambiri wasonyeza kuti semaglutide ili ndi neuroprotective properties motsutsana ndi amyloid-β plaques mu cell line ya neuroblastoma (SH-SY5Y), kutanthauza kuti semaglutide ikhoza kuchepetsa zizindikiro za matenda a Alzheimer's. Zitsanzo za zinyama zasonyezanso kuti semaglutide ili ndi zotsatira za neuroprotective pa zinyama. Malinga ndi kulengeza kwa Novo Nordisk, kuwonetsa mapiritsi a semaglutide a matenda a Alzheimer's (AD) ali pachipatala. Mayesero awiri apadziko lonse a Phase III, EVOKE ndi EVOKE plus, ali mkati, ndipo pafupifupi odzipereka a 3,700 akuyembekezeka kulembedwa. Kafukufukuyu poyerekeza ndi malo a placebo, adayesa kukwera kwa mapiritsi a semaglutide pazidziwitso zachidziwitso mu maphunziro omwe ali ndi vuto lochepa lachidziwitso (MCI) kapena dementia wofatsa chifukwa cha AD.

Chenjezo: Ndikofunikira kugula semaglutide kuchokera kuzinthu zodalirika, apo ayi, simungapeze mphamvu yabwino ya semaglutide.Monga katswiri wopanga semaglutide ndi wogulitsa, AASraw ikufuna kupereka semaglutide yoyera padziko lonse lapansi. Ngati muli ndi zosowa, AASraw's semaglutide ndi yabwino kwa inu.

Zotsatira za Semaglutide?

Semaglutide, monga mankhwala aliwonse, angayambitse zotsatira zoyipazi.

①Wamba zotsatira zoyipazi monga:

• nseru
• kusanza
• kutsekula
• ululu m'mimba
• Kutaya njala
• kudzimbidwa
• mutu
• kutopa
• chizungulire

②Zotsatira zochepa koma zowopsa kwambiri zingaphatikizepo:

• Pancreatitis
• Hypoglycemia (shuga wotsika wamagazi)
• Kuvulala kwakukulu kwa impso
• Matenda a shuga a retinopathy
• Matenda a Gallbladder
• Zosokonezeka
• Matenda a chithokomiro

Zindikirani: Kutalika kwa zotsatira za semaglutide kungasinthe malinga ndi munthu payekha komanso kuopsa kwa zotsatira zake. Nthawi zambiri, zotsatira za semaglutide ndi zosakhalitsa ndipo zidzasintha pamene thupi lanu limasintha mankhwala. Wamba zotsatira zoyipazi monga nseru, kutsekula m'mimba, kusanza, kudzimbidwa, ndi mutu zimatha kutha pakadutsa masiku angapo mpaka sabata. Ngati mukukumana ndi zachilendo kapena zovuta zotsatira zoyipazi mukatenga semaglutide, pitani kwa dokotala mwamsanga. Kuonjezera apo, kugula semaglutide ndi khalidwe lapamwamba kuchokera kwa ogulitsa odalirika, monga AASraw, ndizofunikira.

Mlingo ndi Ulamuliro wa Semaglutide for Reference

Mlingo ndi kayendetsedwe ka semaglutide zimatha kusiyanasiyana malinga ndi zomwe zikugwiritsidwa ntchito. Nawa malangizo ena onse:

① Chizindikiro: Type 2 Diabetes Mellitus

· Subcutaneous jakisoni

Mlungu 1-4: 0.25 mg / sabata

Mlungu wa 5 ndi kupitirira: 0.5 mg / sabata

√ Ngati kuli kofunikira, pakatha masabata osachepera 4 pa mlingo wa 0.5-mg, onjezerani 1 mg subcutaneously kamodzi pa sabata.

√ Ngati kuli kofunikira, patatha masabata osachepera a 4 pa mlingo wa 1-mg, yonjezerani ku 2 mg subcutaneously kamodzi pa sabata; musapitirire 2 mg / sabata.

· Oral Tablet

Tsiku 1-30: 3 mg / tsiku

Tsiku 31 ndi mtsogolo: 7 mg / tsiku

√ Ngati pakufunika, patatha masiku osachepera 30 pa mlingo wa 7-mg, onjezerani 14 mg pamlomo kamodzi patsiku.

√ Zindikirani: Musatenge mapiritsi awiri a 7-mg kuti mukwaniritse mlingo wa 14-mg

②Chizindikiro: Kuwongolera Kulemera Kwambiri

· Subcutaneous jakisoni

Mlungu 1-4: 0.25 mg / sabata

Mlungu 5-8: 0.5 mg / sabata

Mlungu 9-12: 1 mg / sabata

Mlungu 13-16: 1.7 mg / sabata

Mlungu wa 17 ndi mtsogolo: 2.4 mg / sabata (mlingo wokonza)

√ Yambani ndi mlingo wochepa ndipo pang'onopang'ono onjezerani mlingo wokonza kuti muchepetse vuto la m'mimba.

√ Ngati simungathe kulekerera mlingo panthawi yowonjezereka, ganizirani kuchedwetsa kukwera kwa mlingo kwa masabata anai.

√ Ngati sangathe kulekerera yokonza mlingo wa 2.4 mg kamodzi pa sabata, mwina kuchepa kwa 1.7 mg kamodzi pa sabata kwa munthu pazipita 4 milungu; pambuyo pa masabata a 4, onjezerani kukonzanso 2.4 mg kamodzi pa sabata; kusiya ngati sikuloledwa pambuyo kuyesera kachiwiri.

√ Zindikirani: Mlingo ndi kayendetsedwe ka semaglutide zingasiyane malinga ndi zomwe zikugwiritsidwa ntchito. Tsatirani malangizo operekedwa ndi dokotala wanu kapena monga momwe zasonyezedwera pa chizindikiro cha mankhwala. Komanso, yesani zomwe mungathe kuti mugule semaglutide yoyera kuti mukwaniritse bwino.

Kodi mungagule kuti Semaglutide?

Semaglutide, mankhwala omwe amafunidwa kwambiri pochiza matenda a shuga a 2, atchuka kwambiri pakati pa odwala omwe akufunafuna. mayankho ogwira mtima kuwongolera chikhalidwe chawo. Zotsatira zake, misika yapaintaneti yatuluka ngati nsanja yabwino kuti anthu agule semaglutide pa intaneti. Mapulatifomu a digitowa amapatsa makasitomala mwayi wofananiza mitengo, kuwerenga ndemanga, ndikupeza zosankha zingapo kuti zigwirizane ndi zosowa zawo. Komabe, ndikofunikira kuti makasitomala azikhala osamala pogula semaglutide pa intaneti, chifukwa zinthu zabodza kapena zotsika mtengo zitha kusokoneza thanzi lawo. Pochita kafukufuku wokwanira ndikusankha wogulitsa wodalirika komanso wovomerezeka, anthu akhoza kugula molimba mtima semaglutide pa intaneti ndikuwongolera bwino matenda awo a shuga mosavuta.

AASraw cholinga chopanga ndi kupereka mankhwala ophatikizika ndi mankhwala opangira mankhwala (APIs), ndi wothandizira wodalirika wa semaglutide wapamwamba kwambiri ndi zina zokhudzana nazo. Kudzipereka kwawo pakuwongolera bwino kwambiri komanso kutsatira miyezo yamakampani kumawonetsetsa kuti makasitomala amalandira zinthu zabwino zokha za thanzi lawo komanso thanzi lawo. Pogula pa AASraw, anthu omwe akufuna semaglutide akhoza kukhala ndi mwayi wogula, wotetezeka, komanso wodalirika, pamene akupindula ndi chidziwitso chawo chokwanira komanso luso lawo pamunda.

Yaiwisi Semaglutide Lipoti Loyesa Ufa-Mtengo wa HNMR

Kodi HNMR ndi chiyani ndipo mawonekedwe a HNMR amakuuzani chiyani? H Nuclear Magnetic Resonance (INMR) spectroscopy ndi njira yowunikira yomwe imagwiritsidwa ntchito poyang'anira khalidwe ndi kufufuza kuti mudziwe zomwe zili ndi kuyera kwa chitsanzo komanso momwe maselo ake amapangidwira. Mwachitsanzo, NMR imatha kusanthula mochulukira zosakaniza zomwe zili ndi mankhwala odziwika. Pazinthu zosadziwika, NMR ingathe (mwina kugwiritsidwa ntchito kufananiza ndi malaibulale owoneka bwino kapena kutengera kapangidwe kake mwachindunji. Kapangidwe koyambira kadziwika, NMR itha kugwiritsidwa ntchito kudziwa momwe ma molekyulu amathandizira komanso kuphunzira zakuthupi pamlingo wa mamolekyulu. monga kusinthana kwa conformational, kusintha kwa gawo, kusungunuka, ndi kufalikira.

Semaglutide- COA

Semaglutide (910463-68-2) -COA

Kodi mungagule bwanji Semaglutide kuchokera ku AASraw?

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❺Katundu wolandilidwa ndi kupereka ndemanga.

Wolemba nkhaniyi:
Dr. Monique Hong adamaliza maphunziro awo ku UK Imperial College London Faculty of Medicine

Scientific Journal paper Wolemba:
1. Aihua Li
Dipatimenti ya Pharmacy, Zhujiang Hospital, Southern Medical University, Guangzhou 510282, Guangdong, China
2. Tae Suk Lee
School of Pharmacy, Sungkyunkwan University, Suwon, Gyeonggi 16419, Republic of Korea
3. Saullo Queiroz Silveira MD
Dipatimenti ya Anesthesiology, Vila Nova Star Hospital / Rede D'Or - CMA Anesthesia gulu, São Paulo, SP, Brazil
4. Fabian Ferreira Martins
Laboratory of Morphometry, Metabolism, and Cardiovascular Diseases, Biomedical Center, Institute of Biology, University of the State of Rio de Janeiro, Rio de Janeiro, Brazil
Dokotala/wasayansiyu savomereza kapena kulimbikitsa kugula, kugulitsa, kapena kugwiritsa ntchito mankhwalawa pazifukwa zilizonse. Aasraw alibe chiyanjano kapena ubale, wonenedwa kapena ayi, ndi dokotala uyu. Cholinga chotchula dokotalayu ndikuvomereza ndikuyamikira ntchito yofufuza ndi chitukuko yomwe asayansi akugwira ntchitoyi.

Tsamba:

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[2] Wilding JPH,Batterham RL,Davies M,Van Gaal LF,Kandler K,Konakli K,Lingvay I,McGowan BM,Oral TK,Rosenstock J,Wadden TA,Wharton S,Yokote K,Kushner RF; CHOCHITA 1 Gulu Lophunzira.Kulemera kwa thupi ndi zotsatira za cardiometabolic pambuyo pochotsa semaglutide: The STEP 1 yowonjezera mayesero.Diabetes Obes Metab.2022 Aug;24(8):1553-1564.

[3] Garvey WT,Batterham RL,Bhatta M,Buscemi S,Christensen LN,Frias JP,Jódar E,Kandler K,Rigas G,Wadden TA,Wharton S; CHOCHITA 5 Gulu Lophunzira. Zotsatira za zaka ziwiri za semaglutide kwa akuluakulu omwe ali ndi kunenepa kwambiri kapena kunenepa kwambiri: mayesero a STEP 5. Nat Med.2022 Oct; 28 (10): 2083-2091.

[4] Knudsen LB, Lau J.Kupeza ndi Kukula kwa Liraglutide ndi Semaglutide.Front Endocrinol (Lausanne).2019 Apr 12; 10:155.

[5] Mahapatra MK,Karuppasamy M,Sahoo BM.Therapeutic Potential of Semaglutide,a Newer GLP-1 Receptor Agonist, mu Kuchepetsa Kunenepa Kwambiri,Non-Alcoholic Steatohepatitis ndi Neurodegenerative Disease: A Narrative Review.Pharm Res.2022 Jun;39(6) ): 1233-1248.

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