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Alogliptin

Alogliptin

Nesina Vipidia Kazano (combination with metformin) Oseni (combination with pioglitazone)

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Updated: December 06, 2025

Overview

Alogliptin is an oral antidiabetic medication belonging to the dipeptidyl peptidase-4 (DPP-4) inhibitor class, commonly referred to as 'gliptins.' It is used in the management of type 2 diabetes mellitus to improve glycemic control. By inhibiting the DPP-4 enzyme, alogliptin enhances the activity of incretin hormones, which play a key role in glucose homeostasis. This drug is generally well-tolerated and carries a lower risk of hypoglycemia compared to other antidiabetic agents. It may be used as monotherapy or in combination with other glucose-lowering medications, such as metformin, sulfonylureas, or insulin, depending on the patient's needs.

Drug Class

Antidiabetic agent, Dipeptidyl peptidase-4 (DPP-4) inhibitor

Mechanism of Action

Alogliptin selectively inhibits the DPP-4 enzyme, which degrades incretin hormones like glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). • Prolongs active GLP-1 and GIP levels • Enhances glucose-dependent insulin secretion from pancreatic β-cells • Suppresses glucagon secretion from pancreatic α-cells • Reduces hepatic glucose production

Pharmacokinetics

Absorption: Rapidly absorbed after oral administration with ~100% bioavailability (not affected by food) Distribution: Moderate tissue distribution with ~20% plasma protein binding Metabolism: Minimally metabolized via CYP2D6 and CYP3A4 (~10% of dose) Excretion: Primarily excreted unchanged in urine (60-70%) with some fecal elimination Half-life: Approximately 21 hours (allows once-daily dosing)

Pharmacodynamics

• Lowers fasting and postprandial glucose levels • Reduces HbA1c by ~0.5-1.0% • Weight-neutral effects • Preserves β-cell function in animal models • Minimal risk of hypoglycemia when used as monotherapy

Indications

• Management of type 2 diabetes mellitus as monotherapy when diet and exercise alone are insufficient • Adjunctive therapy to diet and exercise in combination with other antidiabetic agents (e.g., metformin, sulfonylureas, thiazolidinediones, or insulin)

Contraindications

Absolute: • Hypersensitivity to alogliptin or any component of the formulation • History of serious hypersensitivity reactions (e.g., anaphylaxis, angioedema) Relative: • History of pancreatitis • Severe renal impairment (requires dose adjustment)

Dosage & Administration

Type 2 diabetes (normal renal function): 25 mg once daily Type 2 diabetes (renal impairment): • eGFR ≥60 mL/min: 25 mg daily • eGFR 30-59 mL/min: 12.5 mg daily • eGFR <30 mL/min: 6.25 mg daily Combination therapy: Adjust based on concomitant medications

Special Populations

Pediatric: Safety and efficacy not established in patients <18 years Geriatric: No dose adjustment required based on age alone Renal impairment: Requires dose adjustment as above Hepatic impairment: No dose adjustment needed for mild-to-moderate impairment; not studied in severe impairment

Adverse Effects

Common (>10%): • Nasopharyngitis • Headache • Upper respiratory tract infections Serious (<1%): • Acute pancreatitis • Severe hypersensitivity reactions • Hepatic toxicity • Bullous pemphigoid

Drug Interactions

• Strong CYP2D6/CYP3A4 inducers: May reduce alogliptin efficacy • Insulin secretagogues (e.g., sulfonylureas): May increase hypoglycemia risk • ACE inhibitors: Potential additive angioedema risk

Warnings & Precautions

• Monitor for signs/symptoms of pancreatitis • Assess renal function before initiation and periodically thereafter • Discontinue if severe hypersensitivity occurs • Observe for bullous pemphigoid (rare skin reaction) • Use caution in heart failure patients

Pregnancy & Lactation

Pregnancy: Category B - Use only if potential benefit justifies potential risk (limited human data) Lactation: Unknown if excreted in human milk; caution advised when prescribing to nursing women

Monitoring Parameters

• HbA1c (every 3-6 months) • Renal function (baseline and periodically) • Fasting plasma glucose • Signs/symptoms of pancreatitis • Hypoglycemia (when used with insulin or sulfonylureas)

Patient Counseling

• Take once daily with or without food • Report unusual abdominal pain, nausea, or vomiting (pancreatitis signs) • Recognize symptoms of hypoglycemia (shaking, sweating, confusion) • Maintain recommended diet and exercise regimen • Inform providers about all medications being taken

Storage & Stability

• Store at 20-25°C (68-77°F) • Protect from moisture • Keep in original container with desiccant

Clinical Pearls

• Consider in patients needing oral therapy with low hypoglycemia risk • Useful in elderly patients with renal dose adjustment • May be combined with SGLT2 inhibitors for additive effects • Monitor for rare but serious skin reactions • Less effective in patients with advanced β-cell failure

References

• FDA Prescribing Information: Nesina (alogliptin) tablets • DeFronzo RA, et al. Diabetes Care. 2012;35(12):2604-2611 • American Diabetes Association. Standards of Medical Care in Diabetes - 2023 • Scheen AJ. Clin Pharmacokinet. 2010;49(10):625-641