Diabetes agents · Endocrine
Metformin
Glucophage® · Glumetza®(brand names vary by market)
First among diabetes drugs: effective, weight-neutral, and it does not cause hypoglycemia by itself.
Also: modified release
Mechanism
Reduces hepatic gluconeogenesis (AMPK-linked) and improves peripheral insulin sensitivity; no insulin release, hence no intrinsic hypoglycemia.
Indications
- Type 2 diabetes, first line
- Prediabetes (selected)
- Polycystic ovary syndrome (off-label, jurisdiction-dependent)
Formulations
Dosing concepts
GI tolerance
Start low, go slow, take with food; extended-release rescues many intolerant patients.
Renal function
Dose reduced then stopped as eGFR falls (commonly reduce <45, avoid <30); held during acute illness with dehydration ('sick day' drug).
Concepts, not prescribing instructions. Practice numbers live in current references and local protocols.
Pharmacokinetics
- Bioavailability
- ~50-60%
- Half-life
- ~5-6 h
- Elimination
- renal: Excreted unchanged; accumulates exactly when kidneys fail
Adverse effects
- GI upset: nausea, diarrhea, metallic tastecommon
- Vitamin B12 deficiency with long usecommon
- Lactic acidosisseriousRare, almost always with renal failure, hypoxia, or contrast mishaps.
Contraindications & precautions
Contraindications
- eGFR below the jurisdictional cutoff (commonly 30)
- Acute metabolic acidosis
Precautions
- Iodinated contrast (hold per local protocol)
- Acute illness with dehydration
- Heavy alcohol use
Interactions
Monitoring
HbA1c
Effectiveness · Every 3-6 months
eGFR
The dose and the safety gate · At least annually, more often near cutoffs
B12 periodically with long-term use
Deficiency is insidious and treatable
Counselling points
- Take with meals; stomach upset usually fades over weeks.
- Pause it when seriously unwell with vomiting, diarrhea, or dehydration, and restart when eating and drinking normally.
- It does not cause low sugar on its own.
Clinical pearls
- 'Sick day medication list': metformin, RAAS blockers, diuretics, SGLT2 inhibitors. The ones to pause in dehydration.
References & review
- Metformin product monograph (consult the current version for your market) (monograph)
- Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed. (reference-work)
Last reviewed 2026-08-15 · jurisdiction: global · drug information changes; verify against current references before practice use.