FARXIGA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FARXIGA (FARXIGA).
Selective inhibitor of sodium-glucose cotransporter 2 (SGLT2), reducing renal glucose reabsorption and lowering blood glucose.
| Metabolism | Primarily metabolized via UGT1A9 and UGT2B7 glucuronidation; minor CYP metabolism (CYP3A4). |
| Excretion | Renal (33% as parent, 66% as glucuronide conjugates in urine); fecal (1.5% as parent); biliary (minor). |
| Half-life | Terminal elimination half-life 12-13 hours; supports once-daily dosing. Steady-state reached in 5 days. |
| Protein binding | 91%; primarily to serum albumin. |
| Volume of Distribution | ~72 L (not L/kg, absolute Vd ~72 L); extensive distribution into extravascular tissues. |
| Bioavailability | 78% after oral administration (fasted); high fat meal decreases Cmax and AUC by 30-50% but no significant clinical effect. |
| Onset of Action | Oral: 2-4 hours (urinary glucose excretion). |
| Duration of Action | Approximately 24 hours; sustained urinary glucose excretion over 24 hours with once-daily dosing. |
10 mg orally once daily, with or without food.
| Dosage form | TABLET |
| Renal impairment | eGFR >= 45 mL/min/1.73 m²: no adjustment; eGFR 25-44 mL/min/1.73 m²: not recommended for glycemic control, may be used for heart failure and chronic kidney disease; eGFR < 25 mL/min/1.73 m²: contraindicated for glycemic control, not recommended for heart failure or chronic kidney disease. |
| Liver impairment | Mild to moderate hepatic impairment (Child-Pugh A and B): no dose adjustment; severe hepatic impairment (Child-Pugh C): not recommended. |
| Pediatric use | Not indicated for pediatric patients below 18 years of age; safety and efficacy not established. |
| Geriatric use | No dose adjustment required based on age; consider renal function and risk of volume depletion, especially in patients >= 75 years. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FARXIGA (FARXIGA).
| Breastfeeding | Dapagliflozin is excreted in animal milk; unknown in human milk. M/P ratio not established. Discontinue breastfeeding due to potential risk to the infant. |
| Teratogenic Risk | Dapagliflozin is not recommended during the second and third trimesters due to potential fetal renal toxicity. Limited human data in the first trimester; animal studies show fetal toxicity at high doses. Avoid use in pregnant women. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Severe renal impairment (eGFR <30 mL/min/1.73 m2)","End-stage renal disease or dialysis","History of serious allergic reaction to dapagliflozin"]
| Precautions | ["Volume depletion (hypotension, dehydration)","Ketoacidosis (euglycemic or diabetic ketoacidosis)","Acute kidney injury","Urosepsis and pyelonephritis","Lower limb amputation (especially in patients with prior amputation, peripheral vascular disease, neuropathy, diabetic foot ulcers)","Necrotizing fasciitis of the perineum (Fournier gangrene)","Genital mycotic infections","Hypoglycemia with concomitant insulin or sulfonylurea use"] |
Loading safety data…
| Monitor maternal renal function, volume status, and blood glucose. Fetal monitoring includes ultrasound for renal development and amniotic fluid volume if inadvertently exposed. |
| Fertility Effects | No adverse effects on fertility observed in animal studies. Human data lacking. |