Canagliflozin

Antidiabetic Drug

Drug class: Sodium-glucose co-transporter 2 (SGLT2) inhibitor

Canagliflozin (INVOKANA)（中文：卡格列淨）

Common Strengths of Canagliflozin Tablet

Canagliflozin tablets are available in the following strengths:

• 100 mg and 300 mg tablets

Drug Trade Names of Canagliflozin Tablet

Invokana

Drug Usage

• Treatment of type 2 diabetes mellitus.
• Reducing the risk of major adverse cardiovascular events (including myocardial infarction, stroke or death) in adults with type 2 diabetes or who are at risk for cardiovascular disease.
• Reduce the risk of hospitalization for heart failure in adults with type 2 diabetes and established cardiovascular disease.

Mechanism of Action

Canagliflozin inhibits sodium-glucose co-transporter 2 (SGLT2) in the proximal renal tubules, reducing glucose reabsorption and increasing urinary glucose excretion

Route of Administration

Oral

Dosages

• Type 2 diabetes: Starting dose 100 mg once daily, can be increased to 300 mg once daily
• Cardiovascular risk reduction: 100 mg once daily
• Diabetic kidney disease: 100 mg once daily

Renal dose based on eGFR:

• eGFR ≥60 mL/min/1.73 m²: No dose adjustment required
• eGFR 45 to <60 mL/min/1.73 m²: 100 mg once daily
• eGFR 30 to <45 mL/min/1.73 m²: Not recommended for glycemic control, but may be continued for cardiovascular/renal benefits
• eGFR <30 mL/min/1.73 m²: Contraindicated

Side Effects

Frequency	Adverse reactions
Common	Urinary tract infection
	Male and female genital mycotic infections
	Increased urination
	Constipation
	Joint pain
Uncommon	Diabetic ketoacidosis (DKA) - a condition where blood becomes too acidic
	Hypoglycemia (low blood sugar), especially when combined with insulin or sulfonylureas
	Hypotension
	Bone fractures (associated with canagliflozin
	Fournier's gangrene - a rare but serious genital infection
	Lower limb amputations (associated with canagliflozin, though evidence is inconsistent)

Pharmacokinetics

• Absorption
  • Rapidly absorbed, peak plasma concentrations within 1-2 hours
• Metabolism
  • O-glucuronidation
• Elimination
  • Half-life approximately 10.6 hours
• Duration
  • 24 hours (allowing for once-daily dosing)

Drug Precautions

Pregnancy

Not recommended

Breastfeeding

Not recommended

Children and Elderly

Not recommended for children under 18 years. No dose adjustment is required for elderly patients

Renal Impairment

Use with caution, dosage adjustments based on eGFR

Monitoring Requirements

Renal function, volume status, signs of ketoacidosis, foot care

Drug Interaction

May increase the risk of hypoglycemia when used with insulin or insulin secretagogues

FAQ

How Should I Take the Tablet?

Take once daily in the morning, with or without food

What Should I Avoid While Taking?

Avoid excessive alcohol consumption and dehydration

What Happens if I Miss a Dose?

Take it as soon as you remember. If it is close to your next dose, skip the missed dose and continue with your regular schedule. Do not take a double dose