Home Drug Guide Sitagliptin Hydrochloride

Drug Guide

Generic Name

Sitagliptin Hydrochloride

Brand Names Brynovin

Classification

Therapeutic: Antidiabetic agent

Pharmacological: Dipeptidyl peptidase-4 (DPP-4) inhibitor

FDA Approved Indications

Type 2 diabetes mellitus (as adjunct to diet and exercise)

Mechanism of Action

Inhibits DPP-4 enzyme, increasing incretin levels (GLP-1 and GIP), which enhances insulin secretion and decreases glucagon levels in a glucose-dependent manner.

Dosage and Administration

Adult: 100 mg once daily, with or without food

Pediatric: Not approved for children

Geriatric: Dose adjustment based on renal function; no initial dose adjustment needed in elderly with normal renal function

Renal Impairment: Adjust dose based on renal function: 50 mg if CrCl 30-50 mL/min, 25 mg if CrCl <30 mL/min

Hepatic Impairment: No specific adjustment recommended

Pharmacokinetics

Absorption: Rapidly absorbed, bioavailability ~87%

Distribution: Low protein binding (~38%)

Metabolism: Minimal hepatic metabolism; primarily excreted unchanged in urine

Excretion: Excreted mainly via kidneys; renal clearance approximates plasma clearance

Half Life: 12.4 hours

Contraindications

Hypersensitivity to sitagliptin or any component

Precautions

Renal impairment—dose adjustment required; risk of pancreas-related adverse events; monitor pancreas enzymes; caution in patients with a history of pancreatitis

Adverse Reactions - Common

Headache (Common)
Nasopharyngitis (Common)
Upper respiratory infection (Common)
Diarrhea (Less common)

Adverse Reactions - Serious

Pancreatitis (Serious, rare)
Hypersensitivity reactions including anaphylaxis (Serious, rare)
Severe cutaneous adverse reactions (Rare)

Drug-Drug Interactions

None specifically identified, but caution with other agents affecting renal function

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor blood glucose regularly; assess for signs and symptoms of pancreatitis; renal function tests at baseline and periodically

Diagnoses:

Risk for unstable blood glucose levels
Risk of pancreatitis

Implementation: Administer once daily, with or without food; reinforce diet and exercise recommendations; monitor renal function periodically

Evaluation: Assess blood glucose control; monitor for adverse effects, including pancreatitis

Patient/Family Teaching

Take medication exactly as prescribed; do not stop abruptly without consulting healthcare provider
Report symptoms of pancreatitis: severe abdominal pain, nausea, vomiting
Maintain recommended diet and exercise regimen
Be aware of signs of hypoglycemia, especially when used with other antidiabetic medications

Special Considerations

Black Box Warnings:

None currently

Genetic Factors: None specified for sitagliptin

Lab Test Interference: None known

Overdose Management

Signs/Symptoms: Potential hypoglycemia; unlikely to cause severe symptoms alone due to glucose-dependent mechanism

Treatment: Supportive care; glucose administration if hypoglycemia occurs; no specific antidote

Storage and Handling

Storage: Store at room temperature, away from moisture and heat

Stability: Stable as per manufacturer specifications