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Metformin

GLUCOPHAGE

Pronunciation: met-FOR-min

Metformin ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Metformin ballicule
Metformin GLUCOPHAGE mascot mnemonic cartoon
Visual mnemonic: Metformin mascot
“Mr Met formin’ Glucose Fudge”

What it isBiguanide that suppresses hepatic gluconeogenesis and improves insulin sensitivity; first-line for type 2 diabetes.

Why this oneWeight-neutral to weight-losing, causes no hypoglycemia as monotherapy, and carries the longest safety record of any oral agent.

What limits itRenally cleared: avoid below eGFR 30 and hold around iodinated contrast. GI intolerance is the usual reason it fails; long-term use depletes B12.

Metformin molecular structure (skeletal formula)
Molecular structure: Metformin

FDA-approved for

Off-label

FDA label

BOXED WARNING Lactic acidosis: rare but potentially fatal; risk raised by renal/hepatic impairment, iodinated contrast, age ≥65, hypoxic states, excess alcohol. If suspected, discontinue and use prompt hemodialysis.
FDA dosingPopulationStartTargetMax
Type 2 diabetes mellitusAdults500 mg BID or 850 mg QD (with meals)Titrate to glycemic control2550 mg/day divided
Type 2 diabetes mellitusPediatric 10–16 yr500 mg BID (with meals)Titrate to glycemic control2000 mg/day divided BID

Titration Increase by 500 mg weekly or 850 mg every 2 weeks

Renal Contraindicated if eGFR <30; do not initiate if eGFR 30–45; reassess if eGFR falls <45; check eGFR before and ≥annually

Hepatic Avoid use in hepatic impairment (lactic acidosis risk)

Instructions

Available strengths

Contraindications

Cautions

Adverse reactions

Pregnancy Limited data insufficient to establish risk; published studies show no clear association with birth defects or miscarriage

Lactation Present in human milk; insufficient data on effects on infant or milk production

Cost

Metformin (GLUCOPHAGE)
What pharmacies pay · NADAC 9/30/26
Strength#/mogeneric $/moCostPlus
500 mgtab60 BID$0.87offered
625 mgtab60 BID$751.60not offered
750 mgtab60 BID$876.30offered
850 mgtab60 BID$1.44offered
1000 mgtab60 BID$1.39offered

Other forms: Metformin ER (GLUCOPHAGE XR)

Generic entry2002

⚠ BOXED WARNING

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryB

Defining liabilityGI intolerance and vitamin B12 deficiency; severe renal/hypoxic illness can precipitate lactic acidosis.

Open Metformin in the interactive console ↗

Memory aids: interaction avatars

Metformin OCT2/MATE1 substrate avatar mnemonic
OCT2/MATE1 substrate

Open Metformin in the interactive console ↗