ACETAZOLAMIDE – Drug Information

Generic Name: Acetazolamide

Therapeutic Classification: Diuretics

Description:

Acetazolamide, is a carbonic anhydrase inhibitor, prescribed for glaucoma, edema due to congestive heart failure, epileptic seizure, idiopathic intracranial hypertension, cystinuria, periodic paralysis, central sleep apnea and dural ectasia. It is also used to prevent and reduce the symptoms of altitude or acute mountain sickness and moderate to severe metabolic or respiratory alkalosis. This medication reduces the activity of carbonic anhydrase protein. Acetazolamide is available as a generic drug and is also used as a diuretic.

Mechanism of Action:

Acetazolamide inhibits the carbonic anhydrase enzyme, reducing rate of aqueous humor formation and thus lowering IOP and produces diuretic effect.

Pharmacokinetics:

  • Onset
    • 60-90 minutes (oral); 2 minutes (IV).
  • Duration
    • 8-12 hours (oral); 4-5 hours (IV).
  • Absorption
    • Moderately rapid absorption from the GI tract; peak plasma concentrations after 2 hours (oral).
  • Distribution
    • Concentrates in the red blood cells and renal cortex; enters the breast milk. Protein-binding: High.
  • Excretion
    • Through Urine as unchanged drug; 3-6 hours (elimination half-life).

Contraindications for Acetazolamide:

Acetazolamide contraindicated in patients with adrenal gland problems, low levels of potassium or sodium in blood, kidney problems, liver problems, high levels of chloride in blood, electrolyte problems, hypersensitivity Pregnancy and for Children.

Warnings and Precautions for Acetazolamide:

  • Use with cautions in patients with history of kidney stones, sickle cell anemia, lung diseases, increased eye pressure, respiratory problem, elderly, who are taking other medications, any allergy, during pregnancy and breastfeeding.
  • Do not drive a car or operate machinery while taking this medication because this medication may cause dizziness, drowsiness or vision changes.
  • Should be limit alcoholic beverages.
  • While taking this medication should be Monitor blood sugar, complete blood cell count regularly.
  • This medication should not be used in children less than 12 because it may affect normal growth.
  • Caution is advised for the patients who receiving concomitant high-dose aspirin and acetazolamide, as anorexia, tachypnea, lethargy, coma and death have been reported.

Adverse Reactions / Side Effects of Acetazolamide:

  • Most Common side effects are tingling in the fingers and toes, tiredness, loss of appetite ,dry mouth, headache, nausea, vomiting, stomach pain.
  • Central Nervous System: Drowsiness and confusion, and seizures.
  • ENT: Ringing in the ear, taste alterations (parageusia) especially for carbonated drinks, sore throat, and Some may also experience blurred vision but this usually disappears shortly after discontinuing the medication.
  • Genitourinary: Painful urination, blood in stool/urine, dark urine, and excessive passage of urination.
  • Metabolic: Increases the risk of kidney stones, liver impairment, metabolic acidosis, increased thirst, and electrolyte imbalance.
  • Skin: Unusual bleeding or bruising and photosensitivity.

Dosage for Acetazolamide:

The dose of Acetazolamide ranges from 250 mg to 1 g, for 24 hours, usually in divided doses for amounts over 250 mg.

Adult- PO Diuresis 250-375 mg/day. Glaucoma; Epilepsy 250-1,000 mg/day. Prophylaxis of high altitude sickness 500-1,000 mg/day. Epilepsy 8-30 mg/kg/day in divided doses. IV Chronic open angle glaucoma 250-1000 mg 24 hourly.

Acetazolamide comes as a tablet and capsule form, to take by mouth with food. If you are taking the extended-release form of acetazolamide, do not crush or chew the capsules.

Storage Condition:

Intravenous

Store between 15-30°C (59-86°F).

Reconstituted solution may be stored at for 3 days at 2-8°C (36-46°C) or 12 hours at 15-30°C (59-86°F).

Oral

Store at 15-30°C.

Trade Names / Brand Names of Acetazolamide:

India:

Acetamide |Diamox (250mg) | Iopar-SR (250mg) | Mazetol (100mg/5ml) | Acetamide | Avva SR | Carbadac 200 (200mg) | Acetamide (250mg) | Diamox (250mg) | AC-Mox | Synomax | Mazetol (200mg) | Actazid | Avva | Avva | Tegrital (400mg) | Mazetol (400mg) | Acetamide (250mg) | Tegrital-CR (300mg) | Antilep (300mg) | Tegrital (200mg) | Diamox (250mg) | Tegrital (100mg) | Mezapin (200mg) | Mazetol (300mg) | Zac | Axytex | Tegrital-CR (200mg) | Actamid

International:

Acetamide Tab, Abzole, Acetamin Tab, Acetariv Tab, Avva Tab, Diamox Tab, Iopar-Sr Cap, Synomax Tab, Zolamide Tab

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