Khoom Keeb Kwm
Liraglutide yog tsim los ntawm Danish multinational kws tshuaj lub tuam txhab Novo Nordisk. Hauv xyoo 1990, cov kws tshawb fawb tau tshawb pom tias thaum tib neeg glucagon -zoo li peptide-1 (GLP-1) tuaj yeem txo cov ntshav qab zib kom zoo, nws tau yooj yim degraded los ntawm enzymes hauv lub cev, nrog ib nrab - lub neej ntawm tsuas yog 2 feeb, ua rau nws nyuaj rau tshuaj. Txhawm rau kov yeej qhov kev sib tw no, Novo Nordisk pab pawg tshawb fawb tau siv sijhawm ntau xyoo ua haujlwm ntawm kev hloov kho cov qauv molecular ntawm ntuj GLP-1 siv cov thev naus laus zis recombination: hloov lysine nrog arginine ntawm txoj hauj lwm 34 thiab txuas C16 fatty acid side chain rau lysine ntawm txoj hauj lwm 26. Qhov no ingenious "acylation recombination album" tso cai rau nws mus txuas ntxiv rau cov ntshav. ib nrab-lub neej mus rau kwv yees li 13 teev. Xyoo 2010, liraglutide (lub npe lag luam: Victoza) tau pom zoo thawj zaug hauv Tebchaws Meskas rau kev kho mob ntshav qab zib hom 2; Hauv xyoo 2014, ntau dua liraglutide (lub npe lag luam: Saxenda) tau pom zoo rau kev tswj qhov hnyav, dhau los ua lub ntiaj teb thawj qhov kev txhaj tshuaj poob.
Ntsiab Parameters
Lub Npe Lub Npe: Liraglutide Txhaj Tshuaj
Hom Tshuaj: Tib neeg glucagon-zoo li peptide-1 (GLP-1) analog (97% homology nrog tib neeg GLP-1)
Cov roj formula: C172H265N43O51
Molecular Luj: Kwv yees li 3751.2 Da
Ib nrab-Lub Neej: Kwv yees li 13 teev (txhawb nqa 24-teev ua haujlwm tas li)
Cov Lus Qhia Tshwj Xeeb: Ua ntej- ntim cov cwj mem, feem ntau 3ml: 18mg
Ntsiab Function
Liraglutide activates GLP-1 receptors nyob rau hauv ntau yam ntaub so ntswg thiab kabmob thoob plaws hauv lub cev, tsim ib tug "smart regulatory network":
Dual Pancreatic Regulation (Smart Glucose Lowering): Hauv cov piam thaj hauv cov ntshav- nyob ntawm seb, nws txhawb nqa cov tshuaj insulin tso tawm los ntawm pancreatic cells thaum cov ntshav qabzib nce siab, thaum tib lub sijhawm inhibiting glucagon secretion los ntawm pancreatic cells; Thaum cov ntshav qabzib rov qab mus rau qhov qub, cov nyhuv cia li tsis muaj zog, yog li kev pheej hmoo ntawm hypoglycemia thaum siv ib leeg yog tsawg heev.
Kev Tswj Xyuas Kev Noj Qab Haus Huv: Ua kom txo qis hauv plab hnyuv, ua rau kom muaj kev txaus siab hauv lub plab zom mov, yog li txo qis ntshav qabzib hloov pauv thiab txo qis qab los noj mov.
Central Appetite Suppression: Ua ncaj qha rau ntawm qhov chaw tswj kev noj qab haus huv hauv hypothalamus, inhibiting kev tshaib kev nqhis neurons, txhawb kev satiety, thiab txo cov calorie kom tsawg ntawm nws qhov chaw.
Kev Tiv Thaiv Kab Mob: Txhim kho vascular endothelial muaj nuj nqi thiab txo qis systolic ntshav siab. Nws tau raug pov thawj los txo qhov kev pheej hmoo ntawm cov hlab plawv tuag, tsis yog -faus myocardial infarction, lossis mob stroke hauv cov neeg mob ntshav qab zib hom 2 thiab kab mob plawv.
Cov txiaj ntsig tseem ceeb: Superior Tag Nrho Cov txiaj ntsig Metabolic: Liraglutide tsis tsuas yog txo qis glycated hemoglobin (HbA1c txo mus txog 0.8% -1.5%), tab sis kuj tseem ua rau poob ceeb thawj (qhov hnyav nruab nrab ntawm 5% -10%) thiab txhim kho cov ntsuas metabolic xws li ntshav siab lipids thiab ntshav.
Clear Long-Cov nyhuv ntev thiab kev nyab xeeb: Nws albumin- khi cov khoom ua tiav los ntawm fatty acid sab chains ua rau nws thawj GLP-1 tshuaj kom ua tiav ib zaug- noj txhua hnub, txhim kho cov neeg mob ua raws. Nws cov qauv tsim immunogenicity tsawg ua kom muaj kev nyab xeeb rau kev siv mus ntev.
Txo cov kev pheej hmoo ntawm cov hlab plawv: Nws yog ib qho ntawm ob peb cov piam thaj - txo cov tshuaj nrog cov pov thawj tseeb ntawm cov txiaj ntsig los ntawm kev sim plawv plawv (CVOT), muab kev tiv thaiv lub neej ntxiv rau cov neeg mob uas muaj kab mob atherosclerotic cardiovascular.
Cov xwm txheej siv tau: Hom 2 mob ntshav qab zib mellitus tswj cov neeg laus: Haum rau cov neeg laus cov neeg laus uas cov ntshav qabzib tseem tswj tsis tau zoo tom qab qhov siab tshaj plaws ntawm koob tshuaj metformin lossis sulfonylureas ib leeg. Nws tuaj yeem siv los ua kev kho mob monotherapy lossis ua ke nrog lwm cov piam thaj - txo cov tshuaj.
Txo kev pheej hmoo ntawm plawv plawv: Tshwj xeeb tsim los txo cov kev pheej hmoo ntawm cov teeb meem mob plawv loj hauv cov neeg laus uas muaj ntshav qab zib hom 2 uas tau kuaj pom tias muaj kab mob plawv.
Kev tswj qhov hnyav hnyav: Raws li kev sib txuas rau kev noj zaub mov tsawg - calorie ntau ntau thiab kev tawm dag zog ntau ntxiv, nws yog qhov tsim nyog rau cov neeg laus uas xav tau kev tswj qhov hnyav hauv lub sijhawm ntev. Cov kev tsim nyog tshwj xeeb yog: thawj lub cev qhov hnyav (BMI) Ntau dua lossis sib npaug li 30 kg / m² (obese); los yog BMI Ntau dua lossis sib npaug li 27 kg / m² (hnyav) nrog tsawg kawg ib qhov hnyav -txog kev sib txuam (xws li kub siab, ntshav qab zib hom 2, lossis dyslipidemia).
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