Metformin
Metformin
Glucophage, Glucophage XR, Fortamet, Glumetza, Riomet
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Summary
Classes
Common uses
Type 2 diabetes mellitus0, Prediabetes0, Polycystic ovary syndrome0
Pharmacy
Starting dose
500 mg PO once or twice daily with meals; titrate weekly to limit GI effects
Preparations
500 mg, 850 mg, 1000 mg IR tablets; 500 mg, 750 mg, 1000 mg ER tablets; 500 mg/5 mL oral solution
US FDA Max
2550 mg/d (IR); 2000 mg/d (ER)
Pharmacology
Routes
Oral
Onset
Glucose lowering within days; HbA1c effect at 8-12 weeks
Duration
~12 hours (IR); 24 hours (ER)
Half-life
6.2 hours (plasma); ~17 hours in erythrocytes[1]
Bioavailability
50-60% (oral; decreased with food, but food given anyway for GI tolerance)[1]
Pregnancy
Generally considered safe; widely used in PCOS and gestational diabetes; placental transfer occurs.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Metformin activates AMPK and suppresses hepatic gluconeogenesis, with secondary effects on intestinal glucose absorption and the gut microbiome.0 Does not stimulate insulin secretion; minimal hypoglycemia risk as monotherapy. Cleared renally unchanged; dose-adjust by eGFR[1]. Rare lactic acidosis primarily in renal failure or acute illness.
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Glucophage (metformin HCl), Bristol-Myers Squibb, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020357s037s039,021202s021s023lbl.pdf