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Sodium-glucose co-transporter 2 (SGLT2), expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen.

Canagliflozin is an inhibitor of SGLT2. By inhibiting SGLT2, canagliflozin reduces reabsorption of filtered glucose and lowers the renal threshold for glucose (RTG), and thereby increases urinary glucose excretion.


Canagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Canagliflozin is not recommended in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis.

[edit] DOSAGE

  • The recommended starting dose is 100 mg once daily, taken before the first meal of the day
  • Dose can be increased to 300 mg once daily in patients tolerating Canagliflozin 100 mg once daily who have an Estimated Glomerular Filtration Rate of 60 mL/min/1.73 m2or greater and require additional glycemic control
  • Canagliflozin is limited to 100 mg once daily in patients who have an Estimated Glomerular Filtration Rate of 45 to less than 60 mL/min/1.73 m2
  • Assess renal function before initiating Canagliflozin . Do not initiate Canagliflozin if Estimated Glomerular Filtration Rate is below 45 mL/min/1.73 m2
  • Discontinue Canagliflozin if Estimated Glomerular Filtration Rate falls below 45 mL/min/1.73 m2


  • History of serious hypersensitivity reaction to Canagliflozin
  • Severe renal impairment, ESRD, or on dialysis


  • Hypotension: Before initiating Canagliflozin, assess volume status and correct hypovolemia in patients with renal impairment, the elderly, in patients with low systolic blood pressure, or if on diuretics, ACEi, or ARB. Monitor for signs and symptoms during therapy
  • Impairment in Renal Function: Monitor renal function during therapy. More frequent monitoring is recommended in patients with Estimated Glomerular Filtration Rate below 60 mL/min/1.73 m2
  • Hyperkalemia: Monitor potassium levels in patients with impaired renal function and in patients predisposed to hyperkalemia
  • Hypoglycemia: Consider a lower dose of insulin or the insulin secretagogue to reduce the risk of hypoglycemia when used in combination with Canagliflozin
  • Genital mycotic infections: Monitor and treat if indicated
  • Hypersensitivity reactions: Discontinue Canagliflozin and monitor until signs and symptoms resolve
  • Increased LDL-C: Monitor LDL-C and treat per standard of care
  • An FDA clinical trial to assess the effect of canagliflozin on bone mineral density over two years in 714 elderly individuals showed that canagliflozin caused greater loss of bone mineral density at the hip and lower spine than placebo.


  • UGT inducers (e.g., rifampin): Canagliflozin exposure is reduced. Consider increasing dose from 100 mg to 300 mg
  • Digoxin: Monitor digoxin levels


  • Pregnancy Category C (US): No adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Nursing mothers: Discontinue drug or nursing


Most common adverse reactions associated with Canagliflozin (5% or greater incidence): female genital mycotic infections, urinary tract infection, and increased urination.


Understanding Type 2 Diabetes
A simple explanation of what diabetes is

[edit] BIBLIOGRAPHY (Revised: 05/2014)


Diabetes (Antidiabetic drugs)
Insulin Secretagogues (drugs that increase insulin release from pancreas) Sulfonylureas Chlorpropamide (Diabinese)   Glibenclamide or Glyburide (Diabeta, Micronase, Glynase, Daonil, Euglycon)   Gliclazide (Diamicron)   Glimepiride (Amaryl, Solosa)   Glipizide (Glucotrol, Minidiab, Glibenese)   Gliquidone (Glurenorm)
Meglitinides Repaglinide (Prandin, Novonorm)   Nateglinide (Starlix)
Dipeptidyl peptidase-4 inhibitors Linagliptin (Trajenta)   Saxagliptin (Onglyza)   Sitagliptin (Januvia)   Vildagliptin (Galvus)
Incretin mimetics (GLP-1 agonists and analogs) Exenatide (Byetta)   Liraglutide (Victoza)   Lixisenatide (Lyxumia)   Dulaglutide (Trulicity)
Insulin Sensitizers (drugs that decrease insulin resistance)
Biguanides Metformin (Glucophage)
Thiazolidinediones Pioglitazone (Actos)
Drugs that retard the digestion and absorption of carbohydrates in the small intestine
Alpha-glucosidase inhibitors Acarbose (Glucobay, Precose)
Drugs that reduce glucose absorption in the kidney and increase glucose excretion in the urine
Sodium glucose cotransporter 2 (SGLT2) inhibitors Canagliflozin (Invokana)   Dapagliflozin (Farxiga)   Empagliflozin (Jardiance, Glyxambi, Synjardi)
Insulin and insulin analogs
Intermediate acting insulins Insulin lispro protamine (Humalog BASAL)   Isophane human insulin : Human insulin protamine (NPH) (Humulin I, Protaphane)
Long-acting insulins‎ Insulin detemir (Levemir)   Insulin glargine (Lantus)
Fast-acting insulins‎ Regular insulin : Insulin (Human recombinant) (Actrapid, Humulin R)
Ultra-rapid-acting insulins‎‎ Insulin aspart (Novorapid)   Insulin glulisine (Apidra)   Insulin lispro (Humalog)   Insulin human (Inhalation Powder) (Afrezza)
Premixed insulin‎‎‎ (ultra-rapid-acting + intermediate acting Insulin aspart / Insulin aspart protamine (Novomix)   Insulin lispro / Insulin lispro protamine (Humalog Mix)
Inhaled Insulin Insulin human (Inhalation Powder) (Afrezza)
Combination therapy
Sulfonylurea + Metformin Glibenclamide / Metformin (Bieuglicon M, Diaglimet, Glibomet, Gliconorm, Glicorest, Suguan M)
Thiazolidinedione + Metformin Pioglitazone / Metformin (Competact, Glubrava)
Thiazolidinedione + Sulfonylurea Pioglitazone / Glimepiride (Tandemact)
Dipeptidyl peptidase-4 inhibitors + Metformin Linagliptin / Metformin (Jentadueto)   Sitagliptin / Metformin (Efficib, Janumet, Velmetia)   Vildagliptin / Metformin (Eucreas)