Dapagliflozin
Unchecked
Dapagliflozin
Farxiga (US), Forxiga (international)
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Summary
Common uses
Type 2 diabetes mellitus0, Heart failure with reduced ejection fraction0, Heart failure with preserved ejection fraction0, Chronic kidney disease0
Pharmacy
Starting dose
10 mg PO once daily in the morning; 5 mg starting in heart failure
Preparations
5 mg, 10 mg tablets
US FDA Max
10 mg/d
Pharmacology
Routes
Oral
Onset
Glycosuria within hours; HbA1c effect at 12 weeks; CV/renal benefits over months
Duration
24 hours
Half-life
~12.9 hours[1]
Bioavailability
~78% (oral; high-fat meal modestly reduces but is not clinically significant)[1]
Pregnancy
Avoid in second and third trimesters; fetal SGLT2 inhibition disrupts kidney development.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Dapagliflozin selectively inhibits sodium-glucose co-transporter 2 (SGLT2) in the renal proximal tubule, blocking ~50-60% of filtered glucose reabsorption and producing dose-dependent glycosuria, natriuresis, and mild osmotic diuresis independent of insulin action.0 Cardiovascular and renal benefits (DAPA-HF, DAPA-CKD, DELIVER) substantially exceed what HbA1c lowering predicts and are attributed to combined effects on preload, blood pressure, intraglomerular pressure via tubuloglomerular feedback, and likely metabolic/inflammatory mechanisms[1]. Genital mycotic infections, euglycemic DKA (especially with insulin reduction or fasting), and rare Fournier's gangrene are the characteristic class adverse effects.
References
[edit | edit source]- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Farxiga (dapagliflozin), AstraZeneca, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/202293s029lbl.pdf