Pharmacology and clinical considerations for the incretin agents
| CONSIDERATIONS | GLP1 RECEPTOR AGONISTS | DPP4 INHIBITORS | ||
|---|---|---|---|---|
| EXENATIDE20,22,24–31 | LIRAGLUTIDE18,23,32–34 | VILDAGLIPTIN35,36 | SITAGLIPTIN35,37 | |
| Administration | SC injection | Oral tablet | ||
| Half-life, h | 2.4 | 11–15 | 2.5 | 12–14 |
| Dose | 5 or 10 μg, twice daily | 0.6, 1.2, or 1.8 mg, once daily | 50 mg, twice daily | 100 mg, once daily |
| Origin of active incretins following treatment | Exogenous and endogenous | Endogenous | ||
| Effect on insulin level | Large increase | Moderate increase | ||
| Effect on glucagon level | Moderate decrease | |||
| Mean decrease in HbA1c vs placebo, % | Approximately 0.8 | 0.8–1.6 | Approximately 0.7 | 0.6–1.0 |
| Postprandial hyperglycemia | Moderate decrease | Small decrease | ||
| Gastric emptying | Inhibited | No clinically significant effect | ||
| Body weight | Moderate decrease | Neutral | ||
| Tolerability issues* | Nausea | Upper respiratory tract infection | ||
| Incidence of hypoglycemia | Low rate of hypoglycemia when administered as monotherapy in patients with T2DM; risk might increase when used in combination with sulfonylureas | |||
DPP4—dipeptidyl peptidase 4, GLP1—glucagonlike peptide 1, HbA1c—glycated hemoglobin A1c, SC—subcutaneous, T2DM—type 2 diabetes.
↵* For more complete listings of adverse events, consult the respective product monographs.