JANUVIA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for JANUVIA (JANUVIA).
Selective inhibitor of dipeptidyl peptidase-4 (DPP-4), increasing levels of active incretin hormones (GLP-1, GIP), enhancing glucose-dependent insulin secretion and suppressing glucagon release.
| Metabolism | Primarily excreted unchanged in urine; minimal hepatic metabolism via CYP450 isoenzymes (CYP3A4, CYP2C8) to inactive metabolites. |
| Excretion | Renal: approximately 87% (79% unchanged sitagliptin, 16% metabolites). Fecal/biliary: 13% (metabolites and unchanged drug). |
| Half-life | Terminal elimination half-life: 12.4 hours. Clinical context: supports once-daily dosing in patients with normal renal function. |
| Protein binding | 38% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | Vd: approximately 198 L or 2.8 L/kg (based on body weight). Indicates extensive extravascular distribution. |
| Bioavailability | Oral bioavailability: 87%. High and consistent absorption. |
| Onset of Action | Oral: onset of glucose-lowering effect within 1 hour; peak DPP-4 inhibition occurs within 2-4 hours. |
| Duration of Action | Duration: approximately 24 hours, allowing once-daily dosing. Significant DPP-4 inhibition sustained over 24 hours. |
| Action Class | DPP-4 inhibitors |
| Brand Substitutes | Sitabite 100mg Tablet, Sita OD 100mg Tablet, Macsita 100mg Tablet, Sitanorm 100mg Tablet, Sitapride 100 Tablet, Istavel 50mg Tablet, Sitared 50 Tablet, Sita OD 50 Tablet, Suitglip 50 Tablet, Sitapride 50mg Tablet, MSN Sita 25mg Tablet, Suitglip 25 Tablet, Istavel 25mg Tablet, Sitapride 25mg Tablet, Sitanorm 25 Tablet |
100 mg orally once daily
| Dosage form | TABLET |
| Renal impairment | eGFR ≥45 mL/min/1.73 m²: 100 mg once daily. eGFR 30-44 mL/min/1.73 m²: 50 mg once daily. eGFR <30 mL/min/1.73 m² or ESRD on dialysis: 25 mg once daily. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh class A or B). Not recommended for severe hepatic impairment (Child-Pugh class C) due to lack of data. |
| Pediatric use | Not approved for pediatric patients under 18 years. No established dosing guidelines. |
| Geriatric use | No dose adjustment required based on age alone. However, renal function should be assessed prior to initiation and monitored periodically; dose adjust per renal function if eGFR <45 mL/min/1.73 m². |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for JANUVIA (JANUVIA).
| Breastfeeding | Unknown if excreted in human milk. M/P ratio not available. Caution advised; consider risk-benefit. |
| Teratogenic Risk | FDA Pregnancy Category B. No evidence of teratogenicity in animal studies. Limited human data; risk cannot be excluded. Use only if clearly needed. |
| Fetal Monitoring | Monitor blood glucose, HbA1c, and renal function. Fetal surveillance as per standard obstetric care. |
■ FDA Black Box Warning
None
| Serious Effects |
["History of serious hypersensitivity reaction to sitagliptin or any component of the formulation","Type 1 diabetes","Diabetic ketoacidosis"]
| Precautions | ["Pancreatitis (acute, hemorrhagic, necrotizing)","Hypoglycemia when used with sulfonylureas or insulin","Hypersensitivity reactions (anaphylaxis, angioedema, Stevens-Johnson syndrome)","Acute renal failure requiring dialysis","Bullous pemphigoid requiring hospitalization","Severe and disabling arthralgia","Heart failure with other DPP-4 inhibitors, caution in patients with risk factors"] |
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| Fertility Effects | No adverse effects on fertility in animal studies. No human data available. |