Drug reference

Canagliflozin

SGLT2 Inhibitor · Antidiabetic

SGLT2 InhibitorAntidiabetic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

1 major

SEVERE in our sources

PREGNANCY

Avoid.

FDA category + note

Top interactions

GatifloxacinSevereDatabaseDDInter

Mechanism

Canagliflozin reversibly inhibits sodium-glucose cotransporter 2 (SGLT2) in the renal proximal convoluted tubule. This action reduces glucose reabsorption and consequently increases urinary glucose excretion, leading to a reduction in blood glucose levels.

Indications

Type 2 diabetes mellitus as monotherapy (if metformin inappropriate)Type 2 diabetes mellitus in combination with insulin or other antidiabetic drugs (if existing treatment fails to achieve adequate glycaemic control)Type 2 diabetesmanagement of diabetes mellitus (type 2)treatment of type 2 diabetes (combined with metformin as preferred regimen)heart failure with reduced ejection fraction (reduce cardiovascular death and hospitalization)type 2 diabetes (reduce cardiovascular mortality, nonfatal stroke, nonfatal myocardial infarction, hospitalization for heart failure, total mortality)protect against declining renal function in type 2 diabetesprotect against end-stage kidney disease in type 2 diabetesprotect against death due to kidney disease in type 2 diabetesprotect against acute kidney injury in type 2 diabetestype 2 diabetes mellitusTreatment of type 2 diabetes (in combination with other oral agents and insulin)Decrease progression of renal disease in diabetic nephropathyDecrease hospitalization for heart failure in type 2 diabetes with diabetic nephropathy

Dosing

Adult: 100 mg once daily; increased if tolerated to 300 mg once daily if required, dose to be taken preferably before breakfast. Dose of concomitant insulin or drugs that stimulate insulin secretion may need to be reduced. Manufacturer advises increase dose if tolerated to 300 mg once daily with concurrent use of rifampicin.
Renal adjustment: Use with caution. Dose recommended not to exceed 100 mg/d with an estimated GFR of 45–59.
Hepatic adjustment: Avoid in severe impairment (risk of increased exposure).
Max dose: 300 mg once daily

Pharmacokinetics

Peak effect

1-2 h

Half-life

11–17

Bioavailability

Rapidly absorbed by the gastrointestinal (GI) tract.

Protein binding

highly protein bound (>85%)

Metabolism

hepatic metabolism

Excretion

excretion of metabolites in the urine and feces

Contraindications

Ketoacidosis
Debilitated patients
Elderly patients (no information available)
Malnourished patients
Severe hepatic impairment
severe renal impairment
end-stage renal disease

Side effects

Common

Abdominal paindiarrhoeahypoglycaemiareproductive tract infectionsurinary tract infectionshypoglycemiapolyuriadehydrationhyperphosphatemiahypermagnesemiahyperkalemiahypovolemiahypotensionLower urinary tract infectionsGenital mycotic infectionsTransient worsening of renal function

Serious

Cardiovascular disease
constipation
hepatic function abnormal
vasculitis
vision disorders
vomiting
Acute coronary syndrome
hypoglycaemic coma
nausea
skin reactions
ketoacidosis (rare)
reduced bone density
bone fractures
lower limb amputation (controversial)
tumorgenicity (controversial)
necrotizing fasciitis of perineum
Diabetic ketoacidosis (euglycemic DKA)
Lower extremity amputation (warning previously issued, but removed based on further studies)