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

I-Linagliptin Linagliptin, ephuhliswe ngu-Boehringer Ingelheim, yavunywa yi-FDA ngoMeyi 2, 2011. Isetyenziselwa ukudibanisa ukutya kunye nokuzivocavoca ukuphucula ukulawulwa kwamanqanaba e-glucose yegazi kubantu abanesifo sikashukela sohlobo lwe-2.ILinagliptin iphucula ulawulo lweswekile yegazi kwizigulana ngokunqanda i-dipeptidyl peptidase-4 (DPP-4).

I-Incretin (i-Incretin) inefuthe lokukhuthaza ukukhutshwa kwe-insulin ngamaseli e-pancreatic islet B, ngokukodwa kubandakanywa ne-glucose-exhomekeke kwi-insulinotropic polypeptide (GIP) kunye ne-glucagon-like polypeptide-1 (GLP-1).I-DDP-4 yi-serine protease ebekwe kumphezulu weeseli.Ibophelela kwiiprotheni kwaye ikhona ngokubanzi kwi-plasma kunye nezicubu ezahlukeneyo emzimbeni (ezifana nezintso, isibindi, i-intestinal villi encinci, iiseli ze-endothelial, njl.).I-Linagliptin sisithinteli esikhethiweyo se-DPP-4 esithintela umsebenzi we-enzyme ngokubophelela umva kwi-DPP-4, ilibazise ukuthotywa kwe-GLP-1, iphucula umsebenzi we-GLP-1, kwaye ivuselela ngendlela exhomekeke kwi-glucose exhomekeke kwi-insulin kwaye inciphisa inqanaba leglucagon kumjikelezo, ngaloo ndlela ilawula inqanaba le-glucose yegazi kwizigulane ezinesifo seswekile esi-2.

Xa kuthelekiswa nezinye i-DPP-4 inhibitors, ezona nzuzo ziphambili zeLinagliptin zezi: inokhuseleko olubalaseleyo lwezintso kwaye inokunciphisa ngempumelelo i-glycosylated hemoglobin.ILinagliptin ikhutshwa ikakhulu kwilindle ngendlela yomfuziselo.Emva kokulawulwa komlomo, i-renal excretion yi-5% kuphela yemali elawulwayo.Nokuba ifakwe emithanjeni, yi-30.8% kuphela ekhutshwa ngeentso.Ngoko ke, akukho mfuneko yezigulana eziphantsi konyango.Jonga rhoqo umsebenzi wesibindi kunye nezintso kunye nohlengahlengiso lwedosi.Zonke izigulane zinokulungisa ngokulinganayo ithamo ukuze kubhalwe lula.
Iziphumo eziqhelekileyo ezingalunganga zeLinagliptin lusulelo lokuphefumla, ukuxinana kweempumlo, iintlungu zesihlunu, intloko ebuhlungu kunye nomqala obuhlungu.