Incretin Lecture Flashcards
DPP-4 inhibitors
The gliptins, all have slightly different metabolism.
Linagliptin is not metabolised but excreted in its parent form via the bile, however, it is also the least potent - may be useful for patients with compromised renal function/liver functions
Other gliptins are more efficacious with vildagliptin causing the largest decrease in HbA1c.
GLP-1 agonists
Exenatide - short acting (2-4 hours)
Lixisenatide - short acting (2-4 hours) and appears to cause slightly milder side effects
Liragulatide - once daily, longer half life due to fatty acid chain allowing serum albumin association.
Exenatide LAR - once weekly exentatide, due to encapsulation in microspheres which are slowly degraded in the body and exenatide diffuses out gradually.
Albiglutide - covalently binding ligand of GLP-1R and is DPP-4 resistant, weekly dosing, however just been withdrawn due for economic reasons
Dulaglutide - 2 GLP-1 analogues linked by IgG Fc fragment, weekly dosing.
Semaglutide - similar to liraglutide, but with large linker molecule and extended fatty acid chain, longest half life, weekly dosing, in clinical trials and has CV benefit and it is hoped can be converted to oral version.