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Pharmacology · SGLT2 inhibitors (gliflozins)

Canagliflozin !

An SGLT2 inhibitor for type 2 diabetes and diabetic kidney disease, with extra warnings about amputations and fractures.

Updated 2026-11-01

The figure shows canagliflozin bound to human SGLT2 (with MAP17) in the glucose-binding site.

Target in 3D: Sodium-glucose cotransporter 2 (SGLT2). PDB structure 8HDH (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Canagliflozin blocks SGLT2 in the proximal tubule, so filtered glucose and sodium are lost in the urine and blood glucose falls independently of insulin. It is less selective than dapagliflozin or empagliflozin and also weakly inhibits intestinal SGLT1, which slightly delays glucose absorption after meals.

  1. Binds SGLT2 on the luminal side of the proximal tubule
  2. Filtered glucose and sodium are no longer reabsorbed
  3. Glucose, calories and some fluid leave in the urine
  4. Glucose falls; glomerular pressure and heart load drop

Pharmacokinetics

Absorption
Oral, once a day.
Metabolism
Mainly glucuronidation.
Elimination
Feces and urine.

Indications

Adverse effects

Common

  • Genital fungal infections (vulvovaginal candidiasis, balanitis)
  • Urinary tract infections and more frequent urination
  • Thirst, dizziness and low blood pressure from fluid loss
  • A small, usually reversible fall in eGFR at the start

Contraindications

  • Hypersensitivity to the drug
  • Not used to control glucose in type 1 diabetes, because of ketoacidosis risk

Key interactions

Insulin or sulfonylureas
Higher risk of hypoglycemia; the other drug is often reduced.
Diuretics (loop or thiazide)
Add to fluid loss and low blood pressure.
Lithium
Serum lithium can fall; levels are checked.
Urine glucose and 1,5-anhydroglucitol tests
Become unreliable for judging glucose control.

What is monitored

  • Kidney function and volume status
  • Daily foot checks in people at risk
  • HbA1c

Administration and safety

  • Oral tablet, once a day, with or without food.
  • Volume status is checked and corrected before the first dose.
  • Usually paused before planned surgery and during acute illness or fasting, to prevent ketoacidosis.

Nursing care

  • Before: kidney function, blood pressure, hydration, genital and urinary symptoms.
  • During: signs of ketoacidosis even with normal glucose; ketones are measured if the patient feels unwell.
  • Teach genital hygiene and to report pain, redness or swelling of the genital or perineal area with fever.
  • Teach that urine glucose tests will be positive and that fluids matter in hot weather or with vomiting.
  • Inspect the feet for sores, infection or new pain; report them promptly.

Pregnancy and breastfeeding

Not recommended in the second and third trimesters, based on kidney effects seen in animals; insulin is the usual choice in pregnancy.

Test yourself

Think of the answer, then tap the question to see it.

Which two warnings are especially linked to canagliflozin among the gliflozins?

Lower-limb amputation and bone fractures.

Which patients need extra foot care on canagliflozin?

Those with previous amputation, peripheral vascular disease, neuropathy or diabetic foot ulcers.

Which second transporter does canagliflozin weakly block?

SGLT1 in the intestine, which slightly delays glucose absorption after meals.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Canagliflozin: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Structure of human SGLT2-MAP17 complex with Canagliflozin (RCSB Protein Data Bank, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.