====== Acetazolamide (Diamox®) ======| | {{ :cardio:diuretics:acetazolamide_structure.svg |}} |^ Acetazolamide || Brand Names | Diamox® || Drug Class | [[cardio:diuretics:carbonic_anhydrase:start|Carbonic Anhydrase Inhibitor]] || Primary Indications | Glaucoma; Altitude sickness; Metabolic alkalosis; Idiopathic intracranial hypertension || Blood Pressure Effect | Mild ↓ BP || Mortality Benefit | No || Elimination | Renal || Black Box Warning | No || FDA Approval | 1954 |===== Overview =====Acetazolamide is a carbonic anhydrase inhibitor that reduces proximal bicarbonate reabsorption, producing a mild diuresis and metabolic acidosis. It is used for glaucoma, altitude sickness, metabolic alkalosis, and to reduce CSF/aqueous production.----===== Mechanism of Action =====**Primary Molecular Target** * Carbonic anhydrase (proximal tubule)**Segment Effects** * ↓ HCO3− reabsorption in proximal tubule * ↑ NaHCO3 and water excretion * Mild natriuresis**Net Physiologic Outcomes** * Mild diuresis * Metabolic acidosis * ↓ Aqueous humor and CSF production----===== Indications ===== * Glaucoma (↓ aqueous humor) * Altitude sickness prophylaxis/treatment * Metabolic alkalosis * Idiopathic intracranial hypertension * Periodic paralysis (selected cases)----===== Black Box Warning =====No black box warning.----===== Contraindications =====Absolute: * Sulfonamide allergy (severe) * Severe hepatic disease (risk of encephalopathy)Relative / Caution: * Hyponatremia * Hypokalemia * Renal impairment * COPD (risk of acidosis)----===== Dosing =====Typical dosing varies by indication: * Glaucoma: 250–1000 mg/day divided * Altitude sickness: 125–250 mg BID * IIH: 500–1000 mg/day (titrate)Renal adjustment: * Required in reduced eGFR----===== Pharmacokinetics =====Absorption: * OralBioavailability: * ~90%Metabolism: * MinimalHalf-life: * ~10–15 hoursElimination: * Renal (unchanged)----===== Adverse Effects =====Common: * Paresthesias * Polyuria * Metallic taste * FatigueSerious: * Metabolic acidosis * Nephrolithiasis * Hypokalemia * Sulfa reactions----===== Drug Interactions =====Increased risk: * Other diuretics (electrolyte loss) * Salicylates (toxicity risk)Avoid combination: * High-dose aspirin in severe renal/hepatic disease----===== Monitoring =====Labs: * Bicarbonate * Electrolytes (K+, Na+) * CreatinineVitals: * Blood pressureClinical: * Symptoms of acidosis * Paresthesias----===== Clinical Pearls ===== * Weak diuretic but powerful for glaucoma/altitude * Causes a non–anion gap metabolic acidosis * Can cause kidney stones (alkaline urine)----===== Comparison Within Class =====Compared to other [[cardio:diuretics:carbonic_anhydrase:start|carbonic anhydrase inhibitors]]: * Shorter BP effect than thiazides/loops * Unique use in altitude sickness/IIH * Most commonly used CAI diuretic----===== Related ===== * [[cardio:diuretics:carbonic_anhydrase:start|Carbonic Anhydrase Inhibitors]] * [[cardio:diuretics:start|Diuretics]] * [[cardio:intro:start|Cardiovascular Pharmacology]]