Nesina

— THERAPEUTIC CATEGORIES —
  • Diabetes

Nesina Generic Name & Formulations

General Description

Alogliptin 6.25mg, 12.5mg, 25mg; tabs.

Pharmacological Class

Dipeptidyl peptidase-4 (DPP-4) inhibitor.

How Supplied

Tabs 6.25mg—30, 90; 12.5mg, 25mg—30, 90, 500

Generic Availability

NO

Mechanism of Action

Alogliptin is a DPP-4 inhibitor that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus. Alogliptin selectively binds to and inhibits DPP-4 but not DPP-8 or DPP-9 activity in vitro at concentrations approximating therapeutic exposures.

Nesina Indications

Indications

Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Limitations of Use

Not for treatment of type 1 diabetes.

Nesina Dosage and Administration

Adult

25mg once daily. Renal impairment: moderate (CrCl ≥30–<60mL/min): 12.5mg once daily; severe (CrCl ≥15–<30mL/min) or ESRD (CrCl <15mL/min or need hemodialysis): 6.25mg once daily.

Children

Not established.

Nesina Contraindications

Not Applicable

Nesina Boxed Warnings

Not Applicable

Nesina Warnings/Precautions

Warnings/Precautions

Assess renal function prior to therapy and periodically thereafter. Monitor for signs/symptoms of pancreatitis, serious hypersensitivity reactions, severe joint pain, or bullous pemphigoid; discontinue if suspected or occurs. Consider risks/benefits in patients with known risk factors for heart failure; monitor for signs/symptoms; evaluate and consider discontinuing if develops. History of angioedema to other DPP-4 inhibitors. Hepatic impairment. Obtain LFTs before starting therapy; interrupt and evaluate if liver enzymes elevated or abnormal tests persist; do not restart if liver injury is confirmed and no other etiology can be found. Pregnancy. Nursing mothers.

Nesina Pharmacokinetics

Absorption

Peak plasma alogliptin concentration (median Tmax) occurred 1 to 2 hours after dosing. Absolute bioavailability: ~100%.

Distribution

Volume of distribution during the terminal phase: 417 L. Plasma protein bound: 20%.

Metabolism

Alogliptin does not undergo extensive metabolism and 60% to 71% of the dose is excreted as unchanged drug in the urine.

Elimination

Renal (76%), fecal (13%). Half-life: ~21 hours.

Nesina Interactions

Interactions

May need lower dose of concomitant sulfonylurea or insulin to reduce risk of hypoglycemia.

Nesina Adverse Reactions

Adverse Reactions

Nasopharyngitis, headache, upper respiratory tract infection; pancreatitis, heart failure, hypersensitivity reactions (eg, anaphylaxis, angioedema, Stevens-Johnson syndrome), hepatic failure (may be fatal), severe and disabling arthralgia.

Nesina Clinical Trials

See Literature

Nesina Note

Not Applicable

Nesina Patient Counseling

See Literature

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