Canagliflozin Drug Profile

What is Canagliflozin?

Canagliflozin is an oral antidiabetic medication belonging to a class of drugs called SGLT2 (sodium-glucose cotransporter 2) inhibitors. It is primarily prescribed to help control blood sugar levels in adults with type 2 diabetes mellitus. This medication works by preventing the kidneys from reabsorbing glucose, allowing excess sugar to be eliminated through urine.

Uses

Canagliflozin has several approved medical uses:

• Type 2 diabetes management: Used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes
• Cardiovascular risk reduction: Approved to reduce the risk of major adverse cardiovascular events in adults with type 2 diabetes and established cardiovascular disease
• Kidney disease progression: Helps reduce the risk of end-stage kidney disease, doubling of serum creatinine, and cardiovascular death in patients with type 2 diabetes and diabetic nephropathy
• Heart failure management: May be used to reduce hospitalization for heart failure in patients with type 2 diabetes and cardiovascular disease
• Combination therapy: Often prescribed alongside other diabetes medications like metformin when single-drug therapy is insufficient

How it works

Canagliflozin blocks SGLT2 proteins in the kidneys, which are responsible for reabsorbing about 90% of filtered glucose back into the bloodstream. By inhibiting these transporters, the medication causes excess glucose to be eliminated through urine, effectively lowering blood sugar levels. This mechanism also leads to modest weight loss and blood pressure reduction due to the loss of calories and fluid through increased urination.

Side effects

Common side effects include:

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• Increased urination and thirst
• Genital yeast infections (particularly in women)
• Urinary tract infections
• Nausea and constipation
• Fatigue and dizziness
• Low blood pressure (hypotension)
• Increased cholesterol levels
• Dehydration

Serious side effects to watch for:

• Diabetic ketoacidosis (even with normal blood sugar levels)
• Severe kidney problems or kidney failure
• Serious genital infections (necrotizing fasciitis)
• Bone fractures and decreased bone density
• Lower limb amputation (particularly toe and foot)

Warnings and precautions

• Kidney function: Not recommended for patients with severe kidney impairment (eGFR less than 30 mL/min/1.73m²) and should be used cautiously in those with moderate kidney disease
• Pregnancy and breastfeeding: Not recommended during pregnancy, especially in the second and third trimesters, as it may harm fetal kidney development. Safety during breastfeeding is not established
• Amputation risk: Patients with a history of amputation, peripheral vascular disease, or diabetic foot ulcers may have increased risk of lower limb amputation
• Volume depletion: Use caution in elderly patients, those with kidney impairment, or patients taking diuretics due to increased risk of dehydration and low blood pressure
• Type 1 diabetes: Should not be used in patients with type 1 diabetes as it increases the risk of diabetic ketoacidosis

Interactions

• Insulin and insulin secretagogues: May increase risk of hypoglycemia; dosage adjustments may be necessary
• Diuretics: Combined use may increase risk of dehydration and low blood pressure
• Digoxin: Canagliflozin may increase digoxin levels, requiring monitoring of digoxin concentrations
• Rifampin: This antibiotic may decrease canagliflozin effectiveness by increasing its metabolism
• Phenytoin and phenobarbital: These seizure medications may reduce canagliflozin blood levels
• UGT enzyme inducers: Medications that induce UGT enzymes may decrease canagliflozin effectiveness
• Lithium: May affect lithium levels, requiring closer monitoring
• ACE inhibitors and ARBs: Combined use may increase risk of kidney problems, especially in elderly patients

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Dosage

For adults with type 2 diabetes, the typical starting dose is 100 mg once daily, taken before the first meal of the day. The dose may be increased to 300 mg once daily if additional glycemic control is needed and the patient tolerates the medication well. For patients with moderate kidney impairment (eGFR 30-60 mL/min/1.73m²), the maximum recommended dose is 100 mg daily. Dosage should always be individualized and determined by a healthcare provider based on kidney function, tolerability, and treatment goals.

Sources: FDA DailyMed drug labels (public domain), BNF, WHO Essential Medicines List. This article is for informational purposes only and does not constitute medical advice. Always consult your healthcare provider before starting or stopping any medication.

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