Canagliflozin Hemihydrate

Indications

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

Pharmacology

Canagliflozin is an inhibitor of subtype-2 sodium-glucose co-transport protein (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter reduces the reabsorption of glucose from renal tubules, leading to more excretion of glucose in urine.

Dosage & Administration

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.

Interaction

UGT inducers (e.g. rifampin, phenytoin): Canagliflozin exposure is reduced. Consider increasing dose from 100 mg to 300 mg.
Digoxin: Canagliflozin may slightly increase the concentration of digoxin in the body when both drugs are being taken.

Contraindications

History of serious hypersensitivity reaction to Canagliflozin, severe renal impairment, End Stage Renal Disease (ESRD), or on dialysis patients.

Side Effects

The most common adverse reactions of Canagliflozin are female genital mycotic infections, urinary tract infection and increased urination. Other side effects of Canagliflozin include low blood pressure, increases potassium blood levels (hyperkalemia), low blood glucose and increases Low-Density Lipoprotein (LDL-C).

Pregnancy & Lactation

Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. For nursing mother discontinue drug or nursing.

Precautions & Warnings

Not for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis.

Therapeutic Class

Sodium-glucose Cotransporter-2 (SGLT2) Inhibitors

Storage Conditions

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