(R)-8-(3-Amino-piperidin-1-yl)-7-koma-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3

Linagliptin Linagliptin, lopangidwa ndi Boehringer Ingelheim, lidavomerezedwa ndi FDA pa Meyi 2, 2011. Amagwiritsidwa ntchito kuphatikiza zakudya ndi masewera olimbitsa thupi kuti athe kuwongolera kuchuluka kwa shuga m'magazi mwa anthu omwe ali ndi matenda amtundu wa 2.Linagliptin imathandizira kuwongolera shuga m'magazi mwa odwala poletsa dipeptidyl peptidase-4 (DPP-4).

Incretin (Incretin) imakhala ndi zotsatira zolimbikitsa kutulutsidwa kwa insulin ndi ma cell a pancreatic islet B, makamaka kuphatikiza insulinotropic polypeptide (GIP) yodalira glucose ndi glucagon-like polypeptide-1 (GLP-1).DDP-4 ndi serine protease yomwe ili pamwamba pa maselo.Amamangiriza ku mapuloteni ndipo amapezeka kwambiri mu plasma ndi minyewa yosiyanasiyana m'thupi (monga impso, chiwindi, matumbo ang'onoang'ono a intestinal villi, endothelial cell, etc.).Linagliptin ndi choletsa chosankha cha DPP-4 chomwe chimalepheretsa ntchito ya enzyme pomanganso DPP-4, kuchedwetsa kuwonongeka kwa GLP-1, kumawonjezera ntchito ya GLP-1, komanso kumalimbikitsa kudalira kwa shuga m'njira yodalira insulin. amachepetsa kuchuluka kwa glucagon m'magazi, motero amawongolera kuchuluka kwa shuga m'magazi mwa odwala omwe ali ndi matenda amtundu wa 2.

Poyerekeza ndi zoletsa zina za DPP-4, zabwino zazikulu za Linagliptin ndi: ili ndi chitetezo chabwino kwambiri cha aimpso ndipo imatha kuchepetsa hemoglobin ya glycosylated.Linagliptin imatulutsidwa makamaka mu ndowe mu mawonekedwe a prototype.Pambuyo pakamwa, kutulutsa kwaimpso ndi 5% yokha ya kuchuluka komwe kumayendetsedwa.Ngakhale ataperekedwa kudzera m'mitsempha, 30.8% yokha ndiyomwe imatulutsidwa kudzera mu impso.Choncho, palibe chifukwa cha odwala omwe akulandira chithandizo.Nthawi zonse fufuzani ntchito ya chiwindi ndi impso ndi kusintha kwa mlingo.Odwala onse angathe kukonza mofanana mlingo kuti alembedwe mosavuta.
Zoyipa zodziwika bwino za Linagliptin ndi matenda a kupuma, kupindika kwa mphuno, kupweteka kwa minofu, kupweteka kwa mutu komanso zilonda zapakhosi.