Generic
Canagliflozin
5 brands available in the market
At a glance
Canagliflozin is an SGLT2 inhibitor used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It reduces glucose reabsorption in the kidney, leading to increased urinary glucose excretion.
Description
Canagliflozin is an SGLT2 (sodium-glucose co-transporter type 2) inhibitor, responsible for at least 90% of glucose reabsorption in the kidney. Blocking this transporter reduces glucose reabsorption from renal tubules, leading to more glucose excretion in urine.
Canagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It can be used alone or in combination with other antidiabetic medications.
Indications
- Type 2 diabetes mellitus (as an adjunct to diet and exercise)
Therapeutic class
Sodium-glucose Cotransporter-2 (SGLT2) Inhibitors
Pharmacological class
SGLT2 Inhibitor
Pharmacology
Canagliflozin is an SGLT2 inhibitor that blocks the SGLT2 transporter responsible for glucose reabsorption in the proximal renal tubule. This reduces the renal glucose threshold and increases urinary glucose excretion, lowering blood glucose levels.
Mechanism of action
Canagliflozin inhibits SGLT2 transporters, reducing renal glucose reabsorption, lowering the renal glucose threshold, and increasing urinary glucose excretion, thereby lowering blood glucose levels.
Dosage
Adults (≥18 years): Recommended dose: 100 mg once daily before the first meal of the day. May increase to 300 mg once daily in patients tolerating 100 mg/day with eGFR >60 mL/min/1.73 m² and requiring additional glycemic control.
Elderly (>75 years): Starting dose: 100 mg once daily.
Renal impairment:
eGFR >60 mL/min/1.73 m²: No dose adjustment required.
eGFR 45-<60 mL/min/1.73 m²: Do not exceed 100 mg/day.
eGFR <45 mL/min/1.73 m²: Do not initiate; discontinue if eGFR falls below 45 mL/min/1.73 m².
Hepatic impairment: Mild-moderate: No dose adjustment; severe: Caution required.
Note: Not for treatment of type 1 diabetes or diabetic ketoacidosis.
Administration
Take on an empty stomach (before the first meal of the day). Swallow tablets whole; do not chew, crush, or break. Follow the dose and duration as advised by your physician.
Missed dose
If you miss a dose, take it as soon as you remember. Skip the missed dose if it is almost time for your next dose. Do not double the dose.
Side effects
Common side effects (≥5%): Female genital mycotic infections, urinary tract infection, increased urination, increased thirst, nausea, constipation.
Other: Hypotension (postural hypotension), hyperkalemia, hypoglycemia (with other antidiabetic agents), increased LDL cholesterol, toe amputation (rare).
Serious (rare): Diabetic ketoacidosis, acute kidney injury, Fournier's gangrene (life-threatening genital infection), anaphylaxis, angioedema.
Precautions & warnings
- Dehydration and hypotension: Increased urination may cause fluid loss; ensure adequate hydration. Caution in patients taking diuretics, NSAIDs, or renin-angiotensin system blockers for diabetes or dialysis.
- Genital fungal infections and UTIs: Practice good hygiene; inform your doctor if symptoms of infection occur.
- Hypoglycemia: Increased risk when used with insulin or sulfonylureas; monitor blood glucose regularly.
- Diabetic ketoacidosis (DKA): Risk of DKA before surgery, during acute illness, or significantly reduced food intake; monitor blood ketones.
- Renal impairment: Do not use if eGFR <45 mL/min/1.73 m²; monitor eGFR regularly.
- Toe amputation (rare): Caution in patients with peripheral vascular disease, neuropathy, or foot ulcers; perform regular foot examinations.
Contraindications
- History of serious hypersensitivity reaction to canagliflozin
- Severe renal impairment (eGFR <45 mL/min/1.73 m²)
- End-stage renal disease (ESRD) or dialysis
- Diabetic ketoacidosis
- Type 1 diabetes mellitus
Drug interactions
- UGT inducers (rifampin, phenytoin, phenobarbital): Decrease canagliflozin exposure; consider dose increase from 100 mg to 300 mg.
- Digoxin: Canagliflozin may slightly increase digoxin concentrations.
- Insulin and sulfonylureas: Increased risk of hypoglycemia; dose reduction may be needed.
- Diuretics: Increased risk of fluid depletion and hypotension.
Food interactions
Alcohol consumption is unsafe (increases risk of hypoglycemia). Take on an empty stomach (before the first meal of the day).
Use in pregnancy
May be unsafe during pregnancy (Category C). Limited human studies available; animal studies have shown harmful effects on the developing baby. Use only if potential benefit justifies potential risk to the fetus.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Adequate information on use during lactation is not available; discontinue drug or nursing.
Pediatric use
Safety and efficacy in pediatric patients have not been established (under 18 years).
Geriatric use
Elderly (>75 years): Starting dose 100 mg once daily; monitor renal function.
Renal / hepatic impairment
Hepatic impairment: Mild-moderate: No dose adjustment; severe: Caution required (limited information).
Overdose effects
Overdose symptoms: Hypoglycemia, dehydration, electrolyte imbalance, hypotension. No specific antidote; general supportive measures. Consult your doctor immediately if overdose is suspected.
Storage conditions
Store in a dry place away from light and heat. Keep out of reach of children.
Chemical structure
Canagliflozin (C₂₄H₂₅FO₅S)