Sitagliptin

# Sitagliptin ## Overview - **Classification**: Dipeptidyl Peptidase-4 (DPP-4) Inhibitor - **Mechanism**: Increases active incretin hormones (GLP-1, GIP) by inhibiting DPP-4. This enhances glucose-dependent insulin release and suppresses glucagon secretion. ## Primary Indications 1. **Type 2 Diabetes Mellitus** - As monotherapy or add-on to improve glycemic control. 2. **Type 2 Diabetes Mellitus** - In combination with other antihyperglycemic agents (e.g., metformin, sulfonylureas, insulin, SGLT2 inhibitors). ## Adult Dosing ### Standard Dosing **Type 2 Diabetes Mellitus** - **Dose**: **100 mg** - **Frequency**: Once daily - **Route**: Oral - **Special Considerations**: Can be taken with or without food. ### Dose Adjustments - **Renal Impairment**: - **CrCl ≥ 45 mL/min**: No dose adjustment needed. - **CrCl ≥ 30 to < 45 mL/min**: **50 mg** once daily. - **CrCl < 30 mL/min or ESRD on dialysis**: **25 mg** once daily. - **Hepatic Impairment**: No dose adjustment for mild-to-moderate impairment. Not studied in severe. - **Elderly Patients**: No specific adjustment needed; adjust based on renal function. ## Pediatric Dosing *Sitagliptin is **not indicated** for use in pediatric patients.* ### Neonates (0-28 days) - **Dose**: Not applicable - **Frequency**: Not applicable - **Maximum**: Not applicable - **Special Notes**: Safety and efficacy not established; use is not recommended. ### Infants (1-12 months) - **Dose**: Not applicable - **Frequency**: Not applicable - **Maximum**: Not applicable - **Special Notes**: Safety and efficacy not established; use is not recommended. ### Children (1-12 years) - **Dose**: Not applicable - **Frequency**: Not applicable - **Maximum**: Not applicable - **Special Notes**: Safety and efficacy not established; use is not recommended. ### Adolescents (13-18 years) - **Dose**: Not applicable - **Frequency**: Not applicable - **Maximum**: Not applicable - **Special Notes**: Safety and efficacy not established; use is not recommended. ## Safety Information ### Contraindications - **Absolute**: History of serious hypersensitivity reaction to sitagliptin (e.g., anaphylaxis, angioedema, SJS). - **Absolute**: Type 1 Diabetes Mellitus. - **Absolute**: Diabetic ketoacidosis. ### Common Adverse Effects - **Common (1-10%)**: Nasopharyngitis, headache, upper respiratory tract infection. - **Common (1-10%)**: Diarrhea, nausea, abdominal pain. - **Serious but Rare**: Acute pancreatitis, severe hypersensitivity reactions (anaphylaxis, angioedema), bullous pemphigoid, renal failure (worsening). ### Key Drug Interactions - **Digoxin**: Sitagliptin can slightly increase digoxin levels. - **Digoxin**: Monitor digoxin levels if co-administered, though usually not clinically significant. - **Cyclosporine**: No clinically significant interaction observed. - **Warfarin**: No clinically significant effect on PT/INR. ## Monitoring & Follow-up - **Before Treatment**: Baseline renal function (CrCl). - **During Treatment**: Periodically monitor HbA1c to assess glycemic control. - **During Treatment**: Monitor renal function as clinically indicated, especially with dose adjustments. - **Clinical Signs**: Monitor for severe, persistent abdominal pain (possible pancreatitis). - **Clinical Signs**: Monitor for signs of hypersensitivity (rash, urticaria, swelling). - **Clinical Signs**: Monitor for blistering or erosions of the skin (bullous pemphigoid). ## Clinical Pearls - 💡 **Tip 1**: Take **once daily** with or without food for convenience. - 💡 **Tip 2**: Always adjust dose based on **renal function** to avoid accumulation. - 💡 **Tip 3**: Educate patients on symptoms of **pancreatitis** and to seek immediate medical help if they occur. - 💡 **Tip 4**: Not effective and not indicated for Type 1 Diabetes or diabetic ketoacidosis. > **⚠️ Important**: This information is for educational purposes only. Always consult current prescribing information, local guidelines, and clinical judgment before prescribing.