Canagliflozin is used alongside diet and exercise to improve blood glucose control in adults with type 2 diabetes mellitus.

Canagliflozin is a selective inhibitor of the sodium-glucose co-transporter 2 (SGLT2), which is responsible for the majority of glucose reabsorption in the kidneys. By blocking this transporter, it reduces glucose reabsorption in the renal tubules and increases the excretion of glucose through urine.

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 who have CrCl>60 ml/min or who requires additional glycemic control. No dose adjustment is required for mild renal impairment. For moderate renal impairment (CrCl 45–60 ml/min) Canagliflozin 100 mg is recommended.

UGT enzyme inducers such as rifampin and phenytoin may decrease the exposure of canagliflozin; therefore, dose adjustment from 100 mg up to 300 mg may be considered.

Co-administration with digoxin may result in a slight increase in digoxin concentration.

Canagliflozin is contraindicated in patients with a history of serious hypersensitivity to the drug, severe renal impairment, end-stage renal disease (ESRD), or those undergoing dialysis.

Common adverse effects include genital fungal infections (especially in females), urinary tract infections, and increased urination. Other possible effects include hypotension, elevated potassium levels (hyperkalemia), hypoglycemia, and increased levels of low-density lipoprotein (LDL-C).

Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the expected benefit outweighs the potential risk to the fetus. For nursing mothers, either the drug should be discontinued or breastfeeding should be stopped.

This medication is not indicated for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis.

Sodium-glucose Cotransporter-2 (SGLT2) Inhibitors

Store in a dry place away from heat and light. Keep out of the reach of children.