NESINA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for NESINA (NESINA).
Inhibitor of dipeptidyl peptidase-4 (DPP-4), preventing inactivation of incretin hormones (GLP-1, GIP), thereby increasing insulin secretion and decreasing glucagon release in a glucose-dependent manner.
| Metabolism | Extensively metabolized via hydrolysis by amidases; minor metabolism by CYP3A4 and CYP2C8. |
| Excretion | Renal: 87% (75% as unchanged drug, 12% as inactive metabolites); Fecal: <1% |
| Half-life | Terminal elimination half-life: 12.4–26.1 hours (mean ~21 hours); supports once-daily dosing |
| Protein binding | ~68% bound to plasma proteins (albumin and α1-acid glycoprotein) |
| Volume of Distribution | ~0.5 L/kg (mean ~51 L); indicates distribution into total body water |
| Bioavailability | Oral: ~100% (absolute bioavailability with minor first-pass effect) |
| Onset of Action | Oral: Peak plasma concentration at 1–4 hours post-dose; inhibition of DPP-4 occurs within 30 minutes |
| Duration of Action | Once-daily dosing; DPP-4 inhibition >80% at 24 hours post-dose; sustained glycemic control over 24 hours |
25 mg orally once daily.
| Dosage form | TABLET |
| Renal impairment | eGFR >= 45 mL/min/1.73 m2: no adjustment. eGFR 30-44: 12.5 mg once daily. eGFR < 30: not recommended. ESRD or dialysis: contraindicated. |
| Liver impairment | No adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe (Child-Pugh C); use not recommended. |
| Pediatric use | Not approved for pediatric use. Safety and efficacy not established. |
| Geriatric use | No dose adjustment based on age alone. Renal function should be assessed; follow renal adjustment guidelines. Caution due to potential age-related renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for NESINA (NESINA).
| Breastfeeding | Excreted in animal milk; unknown in humans. M/P ratio not determined. Not recommended during breastfeeding due to potential for hypoglycemia in the infant. |
| Teratogenic Risk | Pregnancy Category B. No evidence of teratogenicity in animal studies at exposures up to 200 times the human dose. Limited human data; however, based on animal data, risk cannot be excluded. Avoid use in second and third trimesters due to potential for hypoglycemia in the neonate. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Type 1 diabetes mellitus","Diabetic ketoacidosis","History of serious hypersensitivity reaction to alogliptin or any product excipient"]
| Precautions | ["Acute pancreatitis: monitor for symptoms (persistent severe abdominal pain) and discontinue if suspected.","Hypoglycemia: risk increases when used with sulfonylureas or insulin.","Hypersensitivity reactions: angioedema, anaphylaxis, Stevens-Johnson syndrome; discontinue if suspected.","Severe and disabling arthralgia: consider as a cause of joint pain.","Heart failure: consider risks in patients with known cardiovascular disease.","Bullous pemphigoid: monitor for blisters or erosions."] |
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| Monitor maternal blood glucose levels and fetal growth via ultrasound. Assess for signs of hypoglycemia in the neonate post-delivery. |
| Fertility Effects | No significant effects on fertility observed in animal studies. Human data not available. |