Canagliflozin Hemihydrate

Prescribing Information (Research Brand)

Indications

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

Therapeutic Class

Sodium-glucose Cotransporter-2 (SGLT2) Inhibitors

Pharmacology

Canagliflozin is a Sodium-glucose co-transporter 2 (SGLT2) inhibitor. 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. By inhibiting SGLT2, Canagliflozin reduces reabsorption of filtered glucose and lowers the renal threshold for glucose (RTG), and thereby increases urinary glucose excretion.

Dosage & Administration

The recommended starting dose of Canagliflozin 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 eGFR of 60 ml/min/1.73 m2 or greater and require additional glycemic control. If the eGFR of Patients is 45 to 60 ml/min/1.73 m2,the dose of Canagliflozin should be 100 mg once daily.

Interaction

UGT enzyme inducers: The efficacy of Canagliflozin may be reduced when Co-administered with UGT enzyme inducers (e.g., with rifampin, phenytoin,phenobarbital, ritonavir).There was an increase in the area AUC and mean peak drug concentration (Cmax) of digoxin (20% and 36%, respectively) when co-administered with Canagliflozin.

Contraindications

History of a serious hypersensitivity reaction to Canagliflozin, Severe renal impairment (eGFR less than 30 mL/min/1.73 m2), end stage renal disease or patients on dialysis.

Side Effects

Dehydration, Vaginal yeast infection, Yeast infection of the penis (balanitis or balanoposthitis)

Pregnancy & Lactation

Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Canagliflozin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known if Canagliflozin passes into breast milk. Discontinue drug or nursing

Precautions

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 eGFR below 60 mL/min/1.73 m2. Do not initiate Canagliflozin if eGFR is below 45 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.

Use in Special Population

Pediatric Uses: Safety and effectiveness of Canagliflozin in pediatric patients under 18 years of age have not been established.

Geriatric Uses: Patients 65 years and older had a higher incidence of adverse reactions related to reduced intravascular volume with Canagliflozin (such as hypotension, postural dizziness, orthostatic hypotension, syncope, and dehydration).

Storage Conditions

Protect from light and moisture. Store below 30°C. Keep medicine out of the reach of children.