TRIAPRIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TRIAPRIN (TRIAPRIN).
TRIAPRIN is an inhibitor of sodium-glucose cotransporter 2 (SGLT2), reducing renal glucose reabsorption and lowering blood glucose levels.
| Metabolism | Metabolized primarily via glucuronidation by UGT1A9 and UGT2B7; minor metabolism by CYP3A4. |
| Excretion | Renal excretion of unchanged drug accounts for 60% of elimination; hepatic metabolism (CYP3A4) accounts for 30% with biliary/fecal excretion of metabolites; 10% excreted unchanged in feces. |
| Half-life | Terminal elimination half-life is 12 hours (range 10–14 h) in patients with normal renal function; extends to 24–30 h in moderate renal impairment (CrCl 30–50 mL/min) requiring dose adjustment. |
| Protein binding | 95% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.3 L/kg (approximately 21 L in 70 kg adult), indicating distribution primarily in extracellular fluid. |
| Bioavailability | Oral: 75% (range 65–85%) with high-fat meal increasing AUC by 20%. |
| Onset of Action | Oral: 1–2 hours; Intravenous: 5–10 minutes. |
| Duration of Action | Oral: 8–12 hours; Intravenous: 4–6 hours. Clinical effect correlates with plasma concentrations above 2 µg/mL. |
5 mg orally once daily, titrated to 10 mg once daily as tolerated.
| Dosage form | CAPSULE |
| Renal impairment | For GFR 30-59 mL/min: 2.5 mg once daily; for GFR <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh class A and B: 2.5 mg once daily; Child-Pugh class C: do not use. |
| Pediatric use | Not approved for use in pediatric patients under 18 years of age. |
| Geriatric use | Initiate at 2.5 mg once daily due to increased sensitivity; titrate with caution. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TRIAPRIN (TRIAPRIN).
| Breastfeeding | Excretion into breast milk is unknown; M/P ratio not established. Due to potential for serious adverse reactions in nursing infants, including renal impairment and cardiovascular effects, breastfeeding is not recommended during therapy and for 2 weeks after last dose. |
| Teratogenic Risk | TRIAPRIN is contraindicated in pregnancy; first trimester exposure carries risk of cardiovascular defects and neural tube defects (increased relative risk 2.5-3.0). Second and third trimester exposure is associated with oligohydramnios, renal dysfunction, and premature closure of the ductus arteriosus. Use is discouraged in women of childbearing potential without contraception. |
■ FDA Black Box Warning
There is no black box warning for TRIAPRIN.
| Serious Effects |
["History of serious hypersensitivity reaction to TRIAPRIN","Severe renal impairment (eGFR < 30 mL/min/1.73 m²), end-stage renal disease, or on dialysis","Concomitant use with insulin or insulin secretagogues may increase risk of hypoglycemia"]
| Precautions | ["Risk of volume depletion, hypotension, and electrolyte disturbances","Ketoacidosis in patients with type 1 diabetes and other conditions","Acute kidney injury and impairment in renal function","Urosepsis and pyelonephritis","Risk of lower limb amputation","Necrotizing fasciitis of the perineum (Fournier gangrene)"] |
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| Fetal Monitoring | Monitor fetal ultrasound for amniotic fluid volume and renal function weekly if inadvertent exposure in second or third trimester. Monitor maternal blood pressure, renal function, and liver function tests monthly. Assess fetal growth and ductus arteriosus patency via echocardiography after 20 weeks. |
| Fertility Effects | TRIAPRIN may impair female fertility by causing luteal phase defects and reduced implantation rates based on animal studies. In males, reversible oligospermia and decreased sperm motility have been reported. For both sexes, fertility effects are typically reversible upon discontinuation. |