alogliptin
Brand: Nesina
Prototype: sitagliptin
Drug Class: DPP-4 inhibitor
Drug Family: antidiabetic
Subclass: dipeptidyl peptidase-4 inhibitor
Organ Systems: endocrine
Mechanism of Action
Selective DPP-4 inhibitor that blocks GLP-1 and GIP degradation, extending incretin action to glucose-dependently enhance insulin secretion and suppress glucagon, lowering postprandial and fasting glucose.
DPP-4 enzyme
Indications
- type 2 diabetes mellitus
Contraindications
- type 1 diabetes
- DKA
Adverse Effects
Common
- nasopharyngitis
- upper respiratory infections
- headache
Serious
- pancreatitis (rare)
- liver injury (rare but serious: ALF reported)
- heart failure (signal from EXAMINE trial)
- hypersensitivity
Pharmacokinetics (ADME)
| Absorption | oral bioavailability ~100% |
| Distribution | 20% protein bound |
| Metabolism | minimal CYP3A4 and CYP2D6; mostly excreted unchanged |
| Excretion | renal (76% unchanged) |
| Half-life | 21 hours |
| Onset | rapid |
| Peak | 1–2 hours |
| Duration | 24 hours |
| Protein Binding | 20% |
| Vd | 417 L |
Nursing Considerations
- Dose reduction required in moderate (25 mg every other day) and severe renal impairment (12.5 mg daily).
- Monitor LFTs before initiation; rare cases of hepatic failure have been reported; discontinue if LFTs significantly elevated.
- Like other DPP-4 inhibitors: low hypoglycemia risk as monotherapy, weight-neutral profile.
- Reassess need if patient progresses to conditions requiring more aggressive therapy (e.g., established CVD where GLP-1 agonists or SGLT-2 inhibitors would be preferred).
Clinical Pearls
- Alogliptin is the most renally eliminated DPP-4 inhibitor, requiring significant dose adjustments in CKD — but unlike linagliptin, it cannot be used without renal dose modification.
- The EXAMINE trial showed CV non-inferiority for alogliptin, with a mild signal for heart failure hospitalization similar to saxagliptin.
Safety Profile
Pregnancy insufficient-data
Lactation insufficient-data
Renal Adjustment Required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.