Invokana

Invokana

Generic Name

Invokana

Mechanism

  • Inhibits renal SGLT2 in the proximal tubule → ↓ glucose reabsorption (≈90 % of filtered glucose)
  • Glucosuria lowers plasma glucose, reduces HbA1c, and promotes modest weight loss.
  • Lowers post‑prandial glucose without affecting insulin secretion, thus minimal risk of hypoglycemia when used alone.

Pharmacokinetics

  • Absorption: Rapid, peak plasma concentration 2–4 h post‑dose; bioavailability ~70 % with food.
  • Distribution: 60 % protein‑bound; large volume of distribution (~80 L).
  • Metabolism: Primarily glucuronidation (UGT1A3, UGT1A8) → inactive metabolites; minimal CYP450 involvement.
  • Elimination: 80 % excreted unchanged in urine, 20 % fecal.
  • Half‑life: ~13 h (steady‑state ~24 h).
  • Dose adjustment: No adjustment needed in mild‑moderate renal impairment; contraindicated if CrCl < 30 mL/min.

Indications

  • Adjunct to diet and exercise for glycemic control in T2DM.
  • FDA‑approved dose: 100 mg orally once daily; may increase to 300 mg once daily if tolerated and no renal dysfunction.
  • Evidence for cardiovascular risk reduction (CAN SURE study) in high‑risk patients.

Contraindications

  • Contraindicated: Severe renal impairment (CrCl < 30 mL/min), end‑stage renal disease, or dialysis.
  • Warnings:
  • Genitourinary infections (vaginal, urinary tract) → prophylaxis or prompt treatment.
  • Volume depletion → caution in heart failure, dehydration, or diuretic use.
  • Euglycemic diabetic ketoacidosis (DKA) → educate on signs; monitor ketones in high‑risk situations.
  • Hypoglycemia only when combined with insulin or sulfonylureas.
  • Hyperuricemia / gout → monitor uric acid; consider allopurinol if recurrent.
  • Cancer: Possible increased risk of bladder cancer; monitor symptoms, consider discontinuation if suspicious.

Dosing

  • Starting dose: 100 mg once daily, orally, with or without food.
  • Titration: After 4 weeks, if HbA1c ≥ 1 % above target and no renal contraindication, increase to 300 mg once daily.
  • Administration tip: Take in the morning to reduce nocturia.
  • Missed dose: Skip; do not double dose next day.
  • Special populations: No dose adjustment in mild‑moderate hepatic impairment; avoid in severe renal disease.

Adverse Effects

Common (≥ 2 %)Serious (≤ 2 %)
• Genital mycotic infection (vaginal, balanitis) • Euglycemic DKA
• Urinary tract infection • Acute kidney injury (rare)
• Volume depletion (orthostatic hypotension, dizziness) • Acute gout flare
• Mild GI upset (nausea, diarrhea) • Fournier’s gangrene (very rare)
• Hyperuricemia

Monitoring

  • Baseline & every 3 months: HbA1c, serum creatinine, eGFR, uric acid.
  • Renal function: CrCl < 30 mL/min → discontinue.
  • Volume status: Check BP, weight; advise adequate hydration.
  • Ketone monitoring: In patients with reduced oral intake, recent surgery, or high insulin‑to‑canagliflozin ratio.
  • Urinary tract/genital health: Evaluate symptoms, culture if indicated.
  • Pregnancy: Category B; avoid during pregnancy and lactation.

Clinical Pearls

  • “Rule of 300”: When HbA1c remains ≥ 1 % above target after 4 weeks, increase from 100 mg to 300 mg—no renal dose adjustment needed until eGFR < 30 mL/min.
  • Early DKA detection: Even with near‑normal glucose, patients on canagliflozin may develop ketoacidosis—emphasize ketone testing if symptoms arise.
  • Gout caution: Canagliflozin increases uric acid; pre‑emptive allopurinol in patients with prior gout flares reduces risk.
  • Weight loss synergy: Pair with a low‑carb diet for enhanced weight loss; monitor caloric intake to avoid dehydration.
  • Cardiovascular edge: In high‑risk T2DM patients (≥ 2 CV risk factors), consider Invokana for its proven 22 % relative risk reduction in major adverse cardiovascular events (MACE).
  • Avoid in elderly on diuretics: Combined diuretic and SGLT2 inhibitor therapy heightens volume depletion risk—adjust fluid and BP monitoring accordingly.

*Use this drug card as a quick reference for evidence‑based practice and student review.*

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Medical Disclaimer: Medical definitions are provided for educational purposes and should not replace professional medical advice, diagnosis, or treatment.

AI Content Disclaimer: Some definitions may be AI-generated and may contain inaccuracies. Always verify with authoritative medical references.

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