Nesina (Alogliptin) Dosing and Administration
The recommended initial dose of Nesina (alogliptin) is 25 mg once daily, taken orally with or without food, for most adult patients with type 2 diabetes. 1
Standard Initial Dosing
- Start with 25 mg once daily for patients with normal renal function (eGFR ≥60 mL/min/1.73 m²) 1
- Alogliptin can be taken at any time of day, with or without meals, as food does not significantly affect absorption 1, 2
- No titration is required—the 25 mg dose is both the starting and maintenance dose for most patients 1
Dose Adjustments for Renal Impairment
Renal function is the critical determinant for dose modification:
- Mild renal impairment (CrCl ≥60 to <90 mL/min): No dose adjustment needed—use 25 mg once daily 1
- Moderate renal impairment (CrCl ≥30 to <60 mL/min): Reduce to 12.5 mg once daily 1
- Severe renal impairment (CrCl <30 mL/min) or ESRD requiring dialysis: Reduce to 6.25 mg once daily 1
The dose reduction is necessary because alogliptin undergoes primarily renal excretion (76% of the dose), and plasma exposure increases approximately 2-fold in moderate renal impairment 1
Use with Other Diabetes Medications
- Continue metformin unless contraindicated when starting alogliptin, as this remains the foundation of type 2 diabetes therapy 3
- Alogliptin can be used as monotherapy or combined with metformin, pioglitazone, sulfonylureas, voglibose, or insulin 4, 5
- No dose adjustments needed when coadministered with metformin, pioglitazone, glyburide, warfarin, gemfibrozil, ketoconazole, or fluconazole 2
- Consider reducing sulfonylurea doses to minimize hypoglycemia risk when adding alogliptin 3
Mechanism and Expected Efficacy
- Alogliptin inhibits DPP-4 enzyme, prolonging the action of incretin hormones (GLP-1 and GIP), which stimulate glucose-dependent insulin release and suppress glucagon secretion 1, 6
- Peak DPP-4 inhibition exceeds 93% within 2-3 hours of dosing and remains above 80% at 24 hours 1
- Expected HbA1c reduction: 0.4-1.0% over 26 weeks of treatment 2, 4
- Postprandial glucose reductions of approximately 30 mg/dL compared to placebo 1
Special Populations
- Elderly patients (≥65 years): No dose adjustment required based on age alone 1
- Hepatic impairment (Child-Pugh A or B): No dose adjustment needed; use caution in severe hepatic impairment (Child-Pugh C) as this has not been studied 1
- Pregnancy/Lactation: No human data available; use only if clearly needed 1
Common Adverse Effects and Safety
- Most common adverse events: nasopharyngitis, headache, and upper respiratory tract infection 2
- Low risk of hypoglycemia when used as monotherapy or with metformin 4, 5
- Weight neutral—does not cause weight gain or loss 4, 5
- Monitor for signs of pancreatitis during therapy, though this is rare 2
- The EXAMINE trial demonstrated no increased cardiovascular risk in high-risk patients with recent acute coronary syndrome 5
Critical Pitfalls to Avoid
- Never use the 25 mg dose in patients with moderate or severe renal impairment—this results in excessive drug exposure and increased adverse event risk 1
- Do not discontinue metformin when starting alogliptin unless contraindicated 3
- Alogliptin is minimally dialyzable (only 7% removed over 3 hours), so hemodialysis is not useful in overdose situations 1
- Do not mix or dilute alogliptin with other medications 1