Acetazolamide

Aka: Acetazolamide, Diamox, Systemic Carbonic Anhydrase Inhibitor

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II. Indications

  1. High Altitude Sickness treatment and prevention
  2. Pseudotumor Cerebri
  3. Glaucoma
    1. Intraocular Carbonic Anhydrase Inhibitor
      1. Open Angle Glaucoma
    2. Systemic Acetazolamide (IV or oral) Indications
      1. Acute angle closure Glaucoma before surgery
      2. Acute exacerbation of chronic Open Angle Glaucoma
  4. Other indications
    1. Periodic Paralysis
    2. Marfan Syndrome related dural ectasia
    3. Stable Hypercapnic Respiratory Failure (respiratory stimulant)
    4. Epilepsy
      1. FDA approved for Seizures since 1956
      2. Has been used for Catamenial Epilepsy, Myoclonic, Absence and Generalized Seizures
      3. Reiss (1996) Ann Pharmacother 30(5):514-9 [PubMed]

III. Contraindications

  1. Sulfonamide Allergy or Anaphylaxis (relative, Exercise caution)
    1. Sulfonamides may cross react with Carbonic Anhydrase Inhibitors (structurally similar)
  2. Stevens-Johnson Syndrome or Toxic Epidermal Necrolysis history
  3. Hyponatremia
  4. Hypokalemia
  5. Hyperchloremic Metabolic Acidosis
  6. Adrenal Insufficiency
  7. Cirrhosis or other severe liver disease
  8. Severe renal disease

IV. Mechanism

  1. Diuretic in the Carbonic Anhydrase Inhibitor Class
  2. Decreases secretion of Aqueous Humor (Glaucoma)
  3. Decreases Hydrogen Ion at renal proximal tubule
    1. Prevents renal bicarbonate reuptake resulting in urine alkalization (and blood acidification)
    2. Increased renal excretion of Sodium, Potassium, bicarbonate and water
    3. Results in hypokalemic Metabolic Acidosis and Respiratory Alkalosis (mechanism in High Altitude Illness)
      1. Lower resting PaCO2
      2. Higher resting Minute Ventilation
      3. Increased PaO2

V. Dosing: Adults

  1. High Altitude Sickness
    1. Prevention
      1. Adults: 125 mg orally every 12 hours (FDA approved)
        1. Up to 250 mg twice daily may be used (but 125 mg is typically sufficient)
        2. Doses of 1000 mg/day (with added Dexamethasone) have been used for rapid ascent (e.g. rescue)
      2. Children: 2.5 mg/kg up to 125 mg every 12 hours (off-label)
      3. Start 24 hours before ascent
      4. Continue for 72 hours or until acclimitization to highest sleeping altitude
    2. Insomnia at altitude: 125 mg orally at bedtime
    3. Treatment: Adults
      1. Start: 250 mg orally twice daily
      2. Range: 500 to 1000 mg/day divided every 8 to 12 hours (every 12 to 24 hours if extended release)
      3. Often used in combination with Dexamethasone
  2. Pseudotumor Cerebri
    1. Dose range: 125-250 mg orally daily to three times daily
  3. Open Angle Glaucoma acute exacerbation or Acute Narrow Angle Glaucoma prior to surgery
    1. See Intraocular Carbonic Anhydrase Inhibitor
    2. Dose: 250 mg orally or IV every 4-6 hours (maximum 1 gram/day)
      1. May use an initial loading dose of 500 mg once
      2. May decrease dose to 250 mg orally every 12 hours if effective

VI. Dosing: Children

  1. High Altitude Sickness Prevention
    1. Dose: 2.5 to 5 mg/kg/day in divided doses up to 125 mg orally twice daily

VII. Adverse Effects: Common

  1. Electrolytes and acid base
    1. Hypokalemia
    2. Hyponatremia
    3. Metabolic Acidosis
  2. Neuropsychiatric
    1. Peripheral Paresthesias (common)
    2. Taste Dysfunction (Dysgeusia) with bitter or Metallic Taste
    3. Headache
    4. Drowsiness
    5. Depressed Mood
    6. Decreased Libido
    7. Fatigue
  3. Gastrointestinal
    1. Nausea or Vomiting
    2. Abdominal Cramping
    3. Black Stool
    4. Diarrhea
  4. Renal
    1. Polyuria
    2. Ureteral Stones

VIII. Adverse Effects: Uncommon but Serious

  1. Stevens-Johnson Syndrome
  2. Anaphylaxis
  3. Blood Dyscrasias

IX. Drug Interactions

  1. Cyclosporine
  2. Salicylates

X. Safety

  1. Pregnancy Category C
    1. Not recommended in pregnancy
  2. Safe in Lactation

XI. Resources

  1. Acetazolamide Tablets (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0913db35-3f08-4d82-8394-486bd9a487c4

XII. References

  1. Olson (2020) Clinical Pharmacology, Medmaster, Miami, p. 62-3
  2. Hamilton (2010) Tarason Pocket Pharmacopeia, p. 224
  3. Lovecchio (2017) Crit Dec Emerg Med 31(8): 28
  4. Lovecchio (2022) Crit Dec Emerg Med 36(3): 28

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Cost: Medications

acetazolamide (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
ACETAZOLAMIDE 125 MG TABLET Generic $0.14 each
ACETAZOLAMIDE 250 MG TABLET Generic $0.20 each
ACETAZOLAMIDE ER 500 MG CAP Generic $0.35 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

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