Alogliptin
Drug class: Dipeptidyl peptidase-4 (DPP-4) inhibitor
Alogliptin (NESINA)（中文：阿格列汀）
Common Strengths of Alogliptin
Alogliptin is available in the following strengths:
- 6.25 mg
- 12.5 mg
- 25 mg
Drug Trade Name of Alogliptin
Alogliptin is marketed under several trade name, including:
- Nesina
- Vipidia
- Kazano (when combined with metformin)
- Oseni (when combined with pioglitazone)
Mechanism of Action
Alogliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor. It works by inhibiting the DPP-4 enzyme, which results in increased levels of incretin hormones. These hormones help regulate blood glucose by increasing insulin release and decreasing glucagon levels in a glucose-dependent manner.
Route of Administration
Alogliptin is administered orally in tablet form.
Dosages
- Normal People
- The usual dose is 25 mg once daily.
- Hypertension
- No specific dosage adjustment is required, but caution is advised due to potential cardiovascular effects.
- Heart Failure
- No specific dosage adjustment is required, but caution is advised due to potential cardiovascular effects.
- Diabetic Kidney Disases
- Mild renal impairment (CrCl ≥ 60 to < 90 mL/min)
- No dose adjustment required.
- Moderate renal impairment (CrCl ≥ 39 to < 60 mL/min)
- 12.5 mg once daily.
- Severe renal impairment (CrCl ≥ 15 to < 30 mL/min) or end-stage renal disease (ESRD) (CrCl < 15 mL/min)
- 6.25 mg once daily.
- Mild renal impairment (CrCl ≥ 60 to < 90 mL/min)
Side Effects
| Frequency | Adverse reactions |
|---|---|
| Very common (≥1/10) | None reported |
| Common (≥1/100 to <1/10) | Headache |
| Nasopharyngitis | |
| Upper respiratory tract infection | |
| Uncommon (≥1/1,000 to <1/100) | Hypoglycemia (when used with other antidiabetic drugs) |
| Pruritus | |
| Rash | |
| Rare (≥1/10,000 to <1/1,000) | Pancreatitis |
| Hepatic dysfunction | |
| Hypersensitivity reaction including anaphylaxis and angioedema | |
| Very Rare (<1/10,000) | Severe cutaneous adverse reactions including Stevens-Johnson syndrome |
Pharmacokinetics
- Absorption
- Rapidly absorbed with peak plasma concentrations occurring 1 - 2 hours after dosing. The absolute bioavailability is approximately 100%.
- Distribution
- Alogliptin is 20 - 30% bound to plasma proteins
- Metabolism
- Alogliptin does not undergo extensive metabolism, 60 - 70% of the dose is excreted as unchanged drug in the urine. Limited metabolism primarily via CYP2D6 and CYP3A4.
- Elimination
- Primarily excreted unchanged in urine. The mean terminal half-life is approximately 21 hours.
Drug Precautions
Safety
Use with caution in patients with liver disease. Monitor liver functions tests regularly. Discontinue if pancreatitis or severe hypersensitivity reactions occur.
Pregnancy
Not recommended due to lack of sufficient data on safety.
Breast Feeding
Not recommended due to lack of sufficient data on safety.
Children and Elderly
Not recommended for children. Elderly patients should be monitored closely due to increased risk of adverse effects.
Renal Impairment
Dose adjustments are required for patients with moderate to severe renal impairment and ESRD.
Monitoring Requirements
Regular monitoring of liver function tests and renal function is recommended.
Drug Interaction
Caution with CYP2D6 and CYP3A4 inhibitors. Monitor for hypoglycemia when used with insulin or insulin secretagogues.
FAQs
How should I take the tablet?
Take alogliptin exactly as prescribed by your doctor, usually once daily, with or without food.
What should I avoid while taking?
Avoid alcohol and other medications that can affect liver function. Avoid useing alogliptin if you have a history of severe hypersensitivity reactions to DPP-4 inhibitors.
What happens if I miss a dose?
Take the missed dose as soon as you remember, unless it is close to the time for your next dose. Do not take two doses at one time.
Reference
[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6834733
[2] https://www.accessdata fda.gov/drugsatfda_docs/label/2015/022426s005lbl.pdf
[3] https://www.drugs.com/pro/alogliptin.html
