Gliptins/DPP4-i Flashcards
Gliptins/DPP4-i: MOA
- Potentiate the effects of incretin hormones (which are involved in the physiologic regulation of glucose homeostasis)
- DDP4-i degrades incretins, but with inhibitor it blocks incretin degradation which stimulate insulin secretion
Gliptins/DPP4-i: Site of Action
Incretin effect
- Suppresses glucagon secretion (glucagon secretion)
- Slows gastric emptying (GI)
- Reduces food intake (appetite control)
- Promotes ß-cell proliferation (insulin secretion)
Gliptins/DPP4-i: Drugs
Januvia (sitagliptin)
Tradjenta (linagliptin)
Onglyza (saxagliptin)
Nesina (alogliptin)
Sitagliptin (Januvia): Dosing
- Optimal dose: 100mg daily
- CrCl 30-49 mL/min: 50mg
- CrCl <30 mL/min: 25mg
Linagliptin (Tradjenta): Dosing
- 5 mg daily
(ONLY ONE DOES NOT NEED RENAL DOSE ADJUSTMENT)
Saxagliptin (Onglyza): Dosing
- Optimal dose: 5mg daily
- CrCl <50 mL/min: 2.5mg
Alogliptin (Nesina): Dosing
- Optimal dose: 25mg daily
- CrCl >30 to <60 mL/min: 12.5mg
- CrCL <30 mL/min or on dialysis: 6.25mg
Gliptins/DPP4-i: Side effects
- Nasopharyngitis
- URI
If Pt has Heart failure, does not recommend for Gliptins
Gliptins/DPP4-i: Drug interactions
Onglyza (saxagliptin)
- Conivaptan
Tradjenta (linagliptin)
- Carbamazepine
- Efavirenz
- Phenytoins
- Rifampins
- St. John’s wort
Gliptins/DPP4-i: Contraindications
- Hypersensitivity
- T1DM
- DKA
Gliptins/DPP4-i: Precautions
- Impaired renal function
- History of pancreatitis
- Impaired hepatic function
- Heart failure (saxagliptin/alogliptin)
- Use with GLP-1 RA (vice versa)
Gliptins/DPP4-i: Counseling points
- Take once a day; same time each day
- Can be taken with or without food
- Avoid alcohol
ASK ABOUT: Nasopharyngitis and URI
Gliptins/DPP4-i: Monitoring
- FBG/PPG
Time to peak effect: 6-8 weeks