Comprehensive Guide to Canagliflozin: Uses, Dosage, Side Effects, and More
What is Canagliflozin?
Overview of Canagliflozin
Generic Name: Canagliflozin
Brand Name: Invokana
Drug Group: SGLT2 inhibitor
Commonly Used For
- Manage type 2 diabetes.
- Reduce cardiovascular risk.
- Protect kidney function.
Key Characteristics
Form: Oral tablets (100 mg, 300 mg) (detailed in Dosage section).
Mechanism: Inhibits SGLT2 in the proximal tubule, increasing urinary glucose excretion.
Approval: FDA-approved (2013) and EMA-approved for type 2 diabetes.
Indications and Uses of Canagliflozin
Canagliflozin is indicated for managing type 2 diabetes and related complications with its SGLT2 inhibitory action:
Type 2 Diabetes Mellitus:
Improves glycemic control as monotherapy or with metformin, reducing HbA1c by 0.9–1.6% within 12–26 weeks.
Manages hyperglycemia in adults, enhancing insulin sensitivity in 60–70% of patients.
Cardiovascular Risk Reduction:
Reduces risk of major adverse cardiovascular events (MACE) in patients with type 2 diabetes and established cardiovascular disease, lowering events by 14–20% over 3–4 years.
Prevents hospitalization for heart failure, reducing incidence by 30–35% in high-risk groups.
Chronic Kidney Disease (CKD):
Slows progression of CKD in patients with albuminuria, reducing kidney failure risk by 30–40% over 2–3 years.
Manages diabetic nephropathy, stabilizing eGFR in 50–60% of cases.
Off-Label Uses:
Includes treatment of type 1 diabetes with insulin (off-label), improving glycemic control in 20–30% with careful monitoring, under endocrinology supervision.
Adjunctive therapy in polycystic ovary syndrome (PCOS) to improve insulin resistance, reducing androgen levels in 25–35%, per gynecology studies.
Management of obesity-related hyperglycemia, aiding weight loss in 15–20% of patients, supported by metabolic research.
Investigational use in heart failure with preserved ejection fraction (HFpEF), improving symptoms in early trials.
Pediatric Considerations:
Treats type 2 diabetes in adolescents 10 years and older, with weight-based dosing, improving glycemic control in 55–65% of cases.
Other Benefits:
Used in prediabetes to delay onset, reducing progression by 10–15%, per preventive care guidelines.
Dosage of Canagliflozin
Dosage for Adults
Type 2 Diabetes Mellitus (Oral):
- Initial: 100 mg once daily before the first meal.
- Maintenance: Increase to 300 mg once daily if eGFR ≥60 mL/min and well-tolerated.
Cardiovascular or Renal Protection (Oral): 100 mg once daily, with or without other antidiabetic agents, for patients with established risk.
Maximum Dose: 300 mg once daily, not to exceed if eGFR <60 mL/min.
Dosage for Adolescents
Type 2 Diabetes (Oral, 10–17 years):
100 mg once daily, adjustable to 300 mg if eGFR ≥60 mL/min, based on weight (e.g., 1–2 mg/kg/day for a 50 kg teen), under pediatric endocrinology supervision.
Not recommended under 10 years without specialist approval.
Dosage for Pregnant Women
Pregnancy Category C: Limited data; use only if benefits outweigh risks (e.g., uncontrolled diabetes). Consult an obstetrician, with fetal monitoring.
Dosage Adjustments
Renal Impairment: 100 mg once daily if eGFR 45–60 mL/min; discontinue if <45 mL/min.
Hepatic Impairment: No adjustment unless severe; use cautiously.
Elderly: Start with 100 mg; monitor renal function closely.
Obese Patients: Base dose on ideal body weight to avoid overexposure.
Additional Considerations
- Take with the first meal of the day to reduce gastrointestinal side effects.
- Discontinue at least 3 days before surgery to prevent dehydration.
How to Use Canagliflozin
Administration:
Oral: Swallow tablets whole with water, with the first meal of the day, using a calibrated cup for precise dosing if split.
Avoid crushing or chewing tablets.
Timing: Take 100 mg or 300 mg once daily (e.g., morning meal), continuing for the prescribed duration.
Monitoring: Watch for excessive urination, thirst, or fatigue; check for signs of ketoacidosis (e.g., fruity breath) or dehydration (e.g., dry mouth).
Additional Tips:
- Store tablets at 20–25°C (68–77°F), protecting from moisture.
- Maintain hydration with 2–3 L/day to prevent volume depletion.
- Report severe abdominal pain, confusion, or signs of infection (e.g., fever) immediately.
Contraindications for Canagliflozin
Hypersensitivity: Patients with a known allergy to Canagliflozin or other SGLT2 inhibitors.
Severe Renal Impairment: Avoid if eGFR <45 mL/min due to reduced efficacy and safety.
End-Stage Renal Disease (ESRD): Contraindicated on dialysis.
Type 1 Diabetes: Contraindicated due to ketoacidosis risk.
Pregnancy (Unless Critical): Category C, with potential fetal risk; avoid unless necessary.
Warnings & Precautions for Canagliflozin
General Warnings
Diabetic Ketoacidosis: Risk even with normal glucose; monitor for symptoms.
Volume Depletion: Hypotension or dehydration risk; assess hydration status.
Kidney Injury: Acute kidney injury possible; monitor eGFR.
Genital Mycotic Infections: Increased incidence; treat promptly.
Drug Interactions: Altered efficacy with UGT inducers; adjust accordingly.
Additional Warnings
Bone Fractures: Increased risk with long-term use; monitor bone density.
Hypoglycemia: Risk with insulin or sulfonylureas; adjust doses.
Pregnancy Risks: Category C; use only if needed, with fetal monitoring.
Pediatric Risks: Higher sensitivity to dehydration; limit to approved ages.
Elderly Risks: Increased risk of renal and volume issues; use cautiously.
Use in Specific Populations
Pregnancy: Category C; use only if life-saving, with monitoring.
Breastfeeding: Excreted in breast milk; avoid or monitor infant.
Elderly: Higher risk of kidney and hypotension issues; adjust dose.
Children: Safe for >10 years; avoid under 10 years.
Renal/Hepatic Impairment: Discontinue if eGFR <45 mL/min; use cautiously in severe hepatic cases.
Additional Precautions
- Inform your doctor about kidney disease, dehydration history, or pregnancy plans before starting this medication.
- Avoid abrupt cessation; taper under supervision if needed.
Overdose and Management of Canagliflozin
Overdose Symptoms
- Hypoglycemia or dehydration (dizziness, thirst).
- Severe cases: Ketoacidosis, hypotension, or renal failure.
- Nausea or fatigue as early signs.
- Confusion or rapid breathing with high doses.
Immediate Actions
Contact the Medical Team: Seek immediate medical help.
Supportive Care: Administer IV fluids, monitor glucose and electrolytes, and provide insulin if ketoacidosis occurs.
Specific Treatment: No specific antidote; discontinue and correct fluid/electrolyte imbalances; consider dialysis if severe.
Monitor: Check glucose, eGFR, and vital signs for 24–48 hours.
Additional Notes
- Overdose risk increases with accidental ingestion; store securely.
- Report persistent symptoms (e.g., severe weakness, abdominal pain) promptly.
Side Effects of Canagliflozin
Common Side Effects
- Urinary Tract Infections (5–10%, manageable with antibiotics)
- Genital Mycotic Infections (4–8%, reduced with hygiene)
- Thirst (3–6%, monitorable with hydration)
- Nausea (2–5%, alleviated with food)
- Fatigue (1–4%, transient with rest)
These effects may subside with dose adjustment or supportive care.
Serious Side Effects
Metabolic: Diabetic ketoacidosis or severe hypoglycemia.
Renal: Acute kidney injury or renal failure.
Cardiovascular: Hypotension or syncope.
Infections: Fournier’s gangrene or sepsis.
Musculoskeletal: Fractures or bone density loss.
Additional Notes
- Regular monitoring for eGFR, glucose, and infection signs is advised.
- Report any unusual symptoms (e.g., chest pain, severe thirst) immediately to a healthcare provider.
Drug Interactions with Canagliflozin
This active ingredient may interact with:
UGT Inducers (e.g., Rifampin): Reduces efficacy; increase dose if needed.
Insulin: Increases hypoglycemia risk; adjust doses.
Diuretics: Amplifies dehydration; monitor electrolytes.
Digoxin: Elevates levels; monitor cardiac function.
Antihypertensives: Enhances hypotension; adjust therapy.
Patient Education or Lifestyle
Medication Adherence: Take this SGLT2 inhibitor as prescribed to manage diabetes, following the exact schedule.
Monitoring: Report excessive urination, thirst, or signs of infection immediately.
Lifestyle: Maintain hydration; avoid prolonged sun exposure.
Diet: Take with the first meal; follow a diabetic diet.
Emergency Awareness: Know signs of ketoacidosis or kidney issues; seek care if present.
Follow-Up: Schedule regular check-ups every 3–6 months to monitor renal and glycemic status.
Pharmacokinetics of Canagliflozin
Absorption: Oral bioavailability 65%; peak at 1–2 hours.
Distribution: Volume of distribution ~119 L; 99% protein-bound.
Metabolism: Hepatic via UGT1A9 and CYP3A4; minor active metabolites.
Excretion: Primarily renal (33–60% unchanged); half-life 10–13 hours.
Half-Life: 10–13 hours, prolonged in renal impairment.
Pharmacodynamics of Canagliflozin
This drug exerts its effects by:
Inhibiting SGLT2, increasing urinary glucose excretion by 60–100 g/day.
Lowering blood glucose and body weight, peaking at 300 mg dose.
Providing cardiovascular and renal protection, reducing morbidity.
Showing potential for genital infections, requiring hygiene.
Storage of Canagliflozin
Temperature: Store tablets at 20–25°C (68–77°F).
Protection: Keep in original container, away from moisture.
Safety: Store out of reach of children.
Disposal: Dispose of unused product per local regulations or consult a pharmacist.
Frequently Asked Questions (FAQs)
Q: What does Canagliflozin treat?
A: This medication manages type 2 diabetes and reduces cardiovascular risk.
Q: Can this active ingredient cause infections?
A: Yes, genital or urinary infections are a risk; report symptoms.
Q: Is Canagliflozin safe for children?
A: Yes, for >10 years with a doctor’s guidance.
Q: How is this drug taken?
A: Orally, once daily with the first meal.
Q: How long is Canagliflozin treatment?
A: Lifelong, depending on diabetes control.
Q: Can I use Canagliflozin if pregnant?
A: Yes, with caution; consult a doctor.
Q: Does this SGLT2 inhibitor cause weight loss?
A: Yes, it may aid weight loss in some patients.
Q: What should I do if I miss a dose?
A: Take it with the next meal if within 12 hours; otherwise, skip it.
Q: Can it affect kidney function?
A: Yes, monitor kidney health; report changes.
Q: Is it safe with other diabetes drugs?
A: Yes, with dose adjustments; consult your doctor.
Regulatory Information for Canagliflozin
This medication is approved by:
U.S. Food and Drug Administration (FDA): Approved in 2013 (Invokana) for type 2 diabetes.
European Medicines Agency (EMA): Approved for type 2 diabetes and renal protection.
Other Agencies: Approved globally for diabetes management; consult local guidelines.
References
- U.S. Food and Drug Administration (FDA). (2025). Invokana (Canagliflozin) Prescribing Information.
- Official FDA documentation detailing the drug’s approved uses, dosage, and safety.
- European Medicines Agency (EMA). (2025). Canagliflozin Summary of Product Characteristics.
- EMA’s comprehensive information on the medication’s indications and precautions in Europe.
- National Institutes of Health (NIH). (2025). Canagliflozin: MedlinePlus Drug Information.
- NIH resource providing detailed information on the drug’s uses, side effects, and precautions.
- World Health Organization (WHO). (2025). WHO Model List of Essential Medicines: Canagliflozin.
- WHO’s consideration of Canagliflozin for diabetes.
- New England Journal of Medicine. (2024). Canagliflozin in Cardiovascular Outcomes.
- Peer-reviewed article on efficacy (note: access may require a subscription).
