Acetazolamide: Drug information

For additional information see "Acetazolamide: Patient drug information" and "Acetazolamide: Pediatric drug information"

For abbreviations, symbols, and age group definitions show table

Pharmacologic Category

Antiseizure Agent, Miscellaneous;
Carbonic Anhydrase Inhibitor;
Diuretic, Carbonic Anhydrase Inhibitor;
Ophthalmic Agent, Antiglaucoma

Dosing: Adult

Acute mountain sickness/high-altitude cerebral edema

Acute mountain sickness/high-altitude cerebral edema:

Prevention, moderate- to high-risk situations:

Note: Use in addition to gradual ascent; start the day before (preferred) or on the day of ascent (Ref).

Oral (immediate release): 125 mg twice daily; may be discontinued after staying at the same elevation for 2 to 4 days or if descent is initiated (Ref).

Treatment:

Acute mountain sickness:

Note: For moderate to severe acute mountain sickness, some experts prefer dexamethasone or use acetazolamide as an adjunct to dexamethasone (Ref).

Oral (immediate release): 250 mg twice daily (Ref). Continue until descent or 24 hours after resolution of symptoms. Note: Some experts suggest 125 mg twice daily may be sufficient (Ref).

High-altitude cerebral edema (adjunct):

Oral (immediate release): 250 mg twice daily in combination with dexamethasone (Ref). Continue until descent or 24 hours after resolution of symptoms (Ref).

Note: Although ER dosage formulations are FDA-approved for acute mountain sickness, the lowest available capsule dose (500 mg) exceeds current dosing recommendations for acute mountain sickness/high-altitude cerebral edema (Ref).

Edema or general volume overload

Edema or general volume overload (adjunctive therapy):

Note : Optimize loop diuretic therapy before using adjunctive diuretic therapies; combination diuretic therapy is typically for short-term use to restore euvolemia in patients already taking a high-dose loop diuretic therapy who are resistant (eg, furosemide total daily dose of 160 to 320 mg/day IV or the oral equivalent). Combination diuretic therapy can cause severe electrolyte depletion (eg, potassium, magnesium, sodium); prior to and during therapy, electrolytes should be monitored and appropriately repleted or managed (Ref).

IV, Oral (immediate release): 250 to 500 mg once daily or every other day; may be administered in combination with or shortly before the scheduled loop diuretic. Assess volume status frequently (eg, daily or at least every 2 to 3 days) to determine effectiveness and to avoid overdiuresis. Continue only until euvolemia is restored (Ref).

Elevated intraocular pressure associated with acute angle-closure glaucoma

Elevated intraocular pressure associated with acute angle-closure glaucoma (adjunct):

Note: To be used when there is a ≥1-hour delay to ophthalmologist evaluation, as an adjunct to topical therapy (Ref).

Oral (immediate release), IV: 500 mg once (Ref).

Idiopathic intracranial hypertension

Idiopathic intracranial hypertension (off-label use):

Oral (immediate release, extended release): Initial: 250 to 500 mg twice daily; increase as tolerated by 250 mg every week to reach desired clinical effect or a maximum of 4 g/day (Ref).

Metabolic alkalosis

Metabolic alkalosis (off-label use):

Note: In general, use after treatment of underlying causes and replacement of isotonic saline or potassium chloride when appropriate, or when additional fluids are contraindicated (Ref).

IV (preferred), oral (immediate release): 500 mg as a single dose; may repeat as needed based upon acid-base status with 250 to 500 mg up to once or twice daily (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.

Note: Kidney function-adjusted dose recommendations are based on usual doses up to 1 g/day. There are no dosage adjustments necessary for any degree of kidney dysfunction for single doses of 500 mg (ie, elevated intraocular pressure or initial treatment of metabolic alkalosis) (Ref). Although the manufacturer’s labeling contraindicates use in severe kidney impairment, use may be considered in select patients after careful assessment of risks versus benefits along with close monitoring for adverse effects.

Altered kidney function (Ref): Oral, IV:

CrCl ≥50 mL/minute: No dosage adjustment necessary.

CrCl 30 to <50 mL/minute:

Immediate release: 125 to 250 mg twice daily.

Extended release: Avoid use.

CrCl 10 to <30 mL/minute:

Immediate release: Avoid use; acetazolamide accumulation may result in CNS toxicity; if no alternatives available, may consider 125 mg twice daily with close monitoring.

Extended release: Avoid use.

CrCl <10 mL/minute:

Immediate release: Avoid use; acetazolamide accumulation may result in CNS toxicity; if no alternatives available, may consider 125 mg once daily with close monitoring.

Extended release: Avoid use.

Hemodialysis, intermittent (thrice weekly): Dialyzable (~30%) (Ref): Oral, IV:

Immediate release: Avoid use; acetazolamide accumulation may result in CNS toxicity; if no alternatives available, may consider 125 mg once daily with close monitoring; when scheduled dose falls on a dialysis day, administer after dialysis (Ref).

Extended release: Avoid use (Ref).

Peritoneal dialysis:

Oral, IV: Not significantly dialyzed (6.8%) (Ref):

Immediate release: Avoid use; acetazolamide accumulation may result in CNS toxicity; if no alternatives available may consider 125 mg once daily with close monitoring (Ref).

Extended release: Avoid use (Ref).

CRRT:

Oral, IV: Single doses of 500 mg for elevated intraocular pressure may be considered, otherwise, avoid use (Ref).

PIRRT (eg, sustained, low-efficiency diafiltration):

Oral, IV: Single doses of 500 mg for elevated intraocular pressure may be considered, otherwise, avoid use (Ref).

Dosing: Liver Impairment: Adult

Use is contraindicated in patients with cirrhosis or marked liver disease or dysfunction.

Dosing: Older Adult

Refer to adult dosing. Oral: Initial doses should begin at the low end of the dosage range.

Dosing: Pediatric

(For additional information see "Acetazolamide: Pediatric drug information")

Dosage guidance:

Dosing: Dosing presented in mg/kg/dose and mg/kg/day depending on indication; use caution.

Altitude illness, acute

Altitude illness (mountain sickness), acute:

Prevention: Limited data available: Infants, Children, and Adolescents: Immediate release: Oral: 1.25 mg/kg/dose every 12 hours started either the day before (preferred) or on the day of ascent; maximum dose: 125 mg/dose. Prophylaxis may be discontinued after staying at the target elevation for 2 days (2 to 4 days for individuals who ascended faster than recommended) or when descent initiated for individuals who ascended to target elevation and immediately descend (Ref). Note: Use of medications for prevention may not be necessary in low-risk situations (Ref).

Treatment: Limited data available: Infants, Children, and Adolescents: Immediate release: Oral: 2.5 mg/kg/dose every 12 hours; maximum dose: 250 mg/dose (Ref). Note: With high altitude cerebral edema, dexamethasone is the primary treatment; however, acetazolamide may be used adjunctively with the same treatment dose (Ref).

Glaucoma

Glaucoma:

Immediate release: Limited data available:

Infants: Oral: 10 to 20 mg/kg/day in 2 to 4 divided doses (Ref). One study reported doses up to 30 mg/kg/day in infants ≥8 months of age (Ref).

Children: Oral: 10 to 30 mg/kg/day in 2 to 4 divided doses; maximum daily dose: 1,000 mg/day (Ref).

Adolescents: Oral: 250 to 1,000 mg/day in 2 to 4 divided doses (Ref).

Extended release (eg, Diamox sequels): Children ≥12 years and Adolescents: Oral: 500 mg twice daily (Ref).

Edema

Edema (diuresis): Limited data available: Infants, Children, and Adolescents: Oral (immediate release), IV: 5 mg/kg/dose once daily or every other day (Ref).

Epilepsy, short-term management

Epilepsy, short-term management: Limited data available: Note: Acetazolamide is not included in current guidelines for the treatment of epilepsy (Ref).

Infants, Children, and Adolescents: Immediate release: Oral: Usual range: 4 to 16 mg/kg/day in 3 to 4 divided doses; may titrate; maximum daily dose: 30 mg/kg/day not to exceed 1,000 mg/day (Ref). Note: Doses >16 mg/kg/day have not shown significant added benefit.

Intracranial hypertension

Intracranial hypertension (pseudotumor cerebri): Limited data available:

Children: Immediate release: Oral: Usual reported initial dose: 15 to 25 mg/kg/day in 2 to 3 divided doses; may increase if needed to a maximum daily dose of 100 mg/kg/day not to exceed 2,000 mg/day. Therapy may be continued for several months until resolution of headache, disc swelling, and visual field abnormalities (Ref).

Adolescents: Immediate release: Oral: Initial: 500 mg twice daily; may increase if needed; maximum daily dose: 4,000 mg/day (Ref).

Metabolic alkalosis

Metabolic alkalosis: Limited data available; dosing regimens variable:

Infants, Children, and Adolescents: IV, Oral (immediate release): Usual reported initial dose: 5 mg/kg/dose every 6 to 8 hours for 24 hours; evaluate response, additional doses may be required (Ref). Dosing regimens described in the literature vary from 5 mg/kg/dose once daily up to 10 mg/kg/dose every 6 to 12 hours (Ref). In adults, the reported dosing is 500 mg as a single dose (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

Immediate release, injection: There are no dosing adjustments provided in the manufacturer's labeling. Based on experience in adult patients, dosage adjustment may be necessary.

Extended-release capsules: Children ≥12 years and Adolescents:

Mild or moderate kidney impairment: There are no dosage adjustments provided in the manufacturer's labeling. Acetazolamide is renally eliminated; use caution and monitor closely. In adults, some experts recommend to avoid use.

Severe kidney impairment: Use is contraindicated.

Dosing: Liver Impairment: Pediatric

Immediate release, injection: There are no dosing adjustments provided in the manufacturer's labeling. Based on experience in adult patients, use in patients with marked liver impairment should be avoided.

Extended-release capsules: Children ≥12 years and Adolescents:

Use is contraindicated in patients with cirrhosis or marked liver disease or dysfunction.

Adverse Reactions (Significant): Considerations

Aplastic anemia

Case reports of aplastic anemia, including fatalities, have been reported with acetazolamide (Ref).

Mechanism: Non–dose-related; idiosyncratic. May be related to acetazolamide sulfonamide group (Ref).

Onset: Varied; has occurred within 7 weeks to a median of 3 months after treatment initiation (Ref).

Growth retardation

Growth retardation (reduced height and/or weight) has been reported in children receiving chronic (>1 year) acetazolamide therapy for adjunctive treatment of seizures in combination with antiseizure medication monotherapy. Growth returned to original level after discontinuation of acetazolamide (Ref).

Mechanism: Related to the pharmacologic action; may result in metabolic acidosis, possibly leading to growth retardation (Ref).

Hypersensitivity reactions (immediate and delayed)

Immediate hypersensitivity reactions, including anaphylaxis and urticaria, have been reported with acetazolamide (Ref). Delayed hypersensitivity reactions range from maculopapular skin rash to rare severe cutaneous adverse reactions, including Stevens-Johnson syndrome, drug reaction with eosinophilia and systemic symptoms, and acute generalized exanthematous pustulosis (Ref).

Mechanism: Immediate hypersensitivity reactions: Non–dose-related; immunologic (ie, IgE-mediated, with specific antibodies formed against a drug allergen following initial exposure) (Ref). Delayed hypersensitivity reactions: Non–dose-related; immunologic (ie, involving a T-cell mediated drug-specific immune response) (Ref).

Onset: Immediate hypersensitivity reactions: Rapid; generally occurs within 1 hour of administration (Ref) but may occur up to 6 hours after exposure (Ref). Delayed hypersensitivity reactions: Varied; typically occur days to 8 weeks after drug exposure (Ref), but may occur more rapidly (usually within 1 to 4 days) upon reexposure (Ref).

Risk factors:

• Cross-reactivity: Limited published information regarding possible cross-reactivity between acetazolamide and other sulfonamides (Ref). Cross-reactivity between acetazolamide, a nonantibiotic sulfonamide, and antibiotic sulfonamides is unlikely to occur (Ref). Cross-reactivity among carbonic anhydrase inhibitors is unknown.

• Ethnicity: Increased risk in patients of Korean, Chinese, and Japanese descent (Ref).

Metabolic acidosis

Acetazolamide use has been associated with metabolic acidosis, which may lead to treatment discontinuation and, in some cases, death (Ref).

Mechanism: Related to pharmacologic action. Prevents bicarbonate reabsorption in the renal tubules, leading to metabolic acidosis (Ref).

Onset: Rapid; typically occurs within 2 to 4 days of therapy initiation (Ref).

Risk factors:

• Diabetes (Ref)

• Kidney impairment (Ref)

• Older adults (Ref)

• Uncompensated or severe COPD (Ref)

Paresthesia

Acetazolamide use has been associated with paresthesia, which may limit tolerability and lead to nonadherence (Ref).

Mechanism: Dose-related; may result in metabolic acidosis, possibly leading to paresthesia (Ref).

Risk factors:

• Higher doses (Ref)

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

Frequency not defined:

Cardiovascular: Flushing

Dermatologic: Allergic skin reaction, skin photosensitivity

Endocrine & metabolic: Electrolyte disorder, hyperglycemia, hypoglycemia, hypokalemia, hyponatremia

Gastrointestinal: Decreased appetite, diarrhea, dysgeusia, melena, nausea, vomiting

Genitourinary: Glycosuria, hematuria, polyuria

Hematologic & oncologic: Immune thrombocytopenia, leukopenia

Hepatic: Abnormal hepatic function tests, cholestatic jaundice, fulminant hepatic necrosis, hepatic insufficiency

Local: Pain at injection site

Nervous system: Ataxia, confusion, depression, dizziness, drowsiness, excitement, fatigue, flaccid paralysis, headache, malaise

Otic: Auditory disturbance, tinnitus

Miscellaneous: Fever

Postmarketing:

Dermatologic: Acute generalized exanthematous pustulosis (Ref), maculopapular rash (Ref), Stevens-Johnson syndrome (Ref), toxic epidermal necrolysis (Ref), urticaria (Ref)

Endocrine & metabolic: Growth suppression (children) (Ref), metabolic acidosis (Ref)

Genitourinary: Crystalluria (Ref)

Hematologic & oncologic: Agranulocytosis (Ref), aplastic anemia (Ref), thrombocytopenia (Ref)

Hypersensitivity: Anaphylaxis (Ref), drug reaction with eosinophilia and systemic symptoms (Ref)

Nervous system: Paresthesia (Ref)

Ophthalmic: Acute angle-closure glaucoma (Ref), choroidal detachment, choroidal effusion (Ref), myopia (Ref)

Renal: Kidney failure (Ref)

Respiratory: Noncardiogenic pulmonary edema (Ref)

Contraindications

Hypersensitivity to acetazolamide, sulfonamides, or any component of the formulation; marked hepatic disease or insufficiency; decreased sodium and/or potassium levels; adrenocortical insufficiency; cirrhosis; hyperchloremic acidosis; severe renal disease or dysfunction; long-term use in noncongestive angle-closure glaucoma

Note: Although the FDA-approved product labeling states this medication is contraindicated in patients with hypersensitivity to sulfonamide-containing drugs, the scientific basis of this cross-sensitivity has been challenged. Additionally, although the manufacturer’s labeling contraindicates use in severe kidney impairment, use may be considered in select patients after careful assessment of risks versus benefits along with close monitoring for adverse effects.

Canadian labeling: Additional contraindications not in US labeling: Hemorrhagic glaucoma; glaucoma due to peripheral anterior synechias; metabolic acidosis.

Warnings/Precautions

Concerns related to adverse effects:

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).

• Sulfonamide (“sulfa”) allergy: The FDA-approved product labeling for many medications containing a sulfonamide chemical group includes a broad contraindication in patients with a prior allergic reaction to sulfonamides. There is a potential for cross-reactivity between members of a specific class (eg, two antibiotic sulfonamides). However, concerns for cross-reactivity have previously extended to all compounds containing the sulfonamide structure (SO₂NH₂). An expanded understanding of allergic mechanisms indicates cross-reactivity between antibiotic sulfonamides and nonantibiotic sulfonamides may not occur or at the very least this potential is extremely low (Brackett 2004; Johnson 2005; Slatore 2004; Tornero 2004). In particular, mechanisms of cross-reaction due to antibody production (anaphylaxis) are unlikely to occur with nonantibiotic sulfonamides. T-cell-mediated (type IV) reactions (eg, maculopapular rash) are not well understood and it is not possible to completely exclude this potential based on current insights. In cases where prior reactions were severe (Stevens-Johnson syndrome/TEN), some clinicians choose to avoid exposure to these classes.

Disease-related concerns:

• Bariatric surgery: Presurgical assessment of the indication for use, symptoms, and goals of therapy should be documented to enable postsurgical assessment. Monitor for continued efficacy after bariatric surgery and consider switching to an alternate medication if condition worsens.

• Diabetes: Use with caution in patients with prediabetes or diabetes mellitus; may see a change in glucose control.

• Hepatic impairment: Use with caution in patients with hepatic dysfunction; in cirrhosis, avoid electrolyte and acid/base imbalances that might lead to hepatic encephalopathy.

• Respiratory acidosis: Use with caution in patients with respiratory acidosis; may worsen acidosis.

Special populations:

• Older adult: Use with caution in the elderly; may be more sensitive to side effects.

Other warnings/precautions:

• Appropriate use: Increasing the dose does not increase diuresis and may increase the incidence of drowsiness and/or paresthesia; often results in a reduction of diuresis.

• IM administration: Painful because of the alkaline pH of the drug; use by this route is not recommended.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule Extended Release 12 Hour, Oral:

Generic: 500 mg

Solution Reconstituted, Injection:

Generic: 500 mg (1 ea)

Solution Reconstituted, Injection [preservative free]:

Generic: 500 mg (1 ea)

Tablet, Oral:

Generic: 125 mg, 250 mg

Generic Equivalent Available: US

Yes

Pricing: US

Capsule, 12-hour (acetaZOLAMIDE ER Oral)

500 mg (per each): $0.82 - $4.29

Solution (reconstituted) (acetaZOLAMIDE Sodium Injection)

500 mg (per each): $27.60 - $52.75

Tablets (acetaZOLAMIDE Oral)

125 mg (per each): $0.24 - $2.18

250 mg (per each): $0.30 - $6.65

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Injection:

Generic: 500 mg (1 ea)

Tablet, Oral:

Generic: 250 mg

Administration: Adult

Oral: May be administered with food.

Bariatric surgery: Acetazolamide is available as an ER formulation and the release characteristics may be significantly altered in an unknown manner in patients who have undergone bariatric surgery; providers should determine if the condition being treated can be safety monitored or if a switch to an alternative formulation is necessary (Ref). Acetazolamide is also available in an IR formulation or parenteral formulation.

IM: IM administration is painful because of the alkaline pH of the drug; use by this route is not recommended.

IV: Direct IV injection is the preferred parenteral route of administration. Specific IV push rates are not provided in the manufacturer's labeling. However, an IV push rate of up to 500 mg over 3 minutes has been reported in a clinical trial (Ref). Additionally, a study to assess cerebrovascular reserve used a rapid IV push of up to 1 g over ≤1 minute (Ref).

Administration: Pediatric

Oral: Administer with food to decrease GI upset.

Capsules, extended release: Do not crush.

Tablets, immediate release:

Administration via feeding tube:

Gastric (eg, NG, G-tube) or post-pyloric (eg, J-tube) tubes (≥8 French): Crush tablet(s) to a fine powder and disperse each tablet in 10 mL purified water; draw up mixture into enteral dosing syringe and administer via feeding tube. Following administration, rinse container used for preparation with purified water; draw up rinse, and administer contents to ensure delivery of entire dose (Ref).

Parenteral:

IV: Direct IV injection is the preferred parenteral route of administration. Specific IV push rates are not provided in the manufacturer's labeling. In an adult trial, IV push rate of 500 mg over 3 minutes was used (Ref); some have recommended a maximum rate of 500 mg/minute (Ref). Additionally, a study in adults to assess cerebrovascular reserve used a rapid IV push of up to 1,000 mg over ≤1 minute (Ref).

IM: Not recommended as the drug's alkaline pH makes it very painful.

Use: Labeled Indications

Acute mountain sickness/high-altitude cerebral edema: Prevention or treatment of symptoms associated with acute mountain sickness (AMS) (IR dosage forms). Note: High-altitude cerebral edema (HACE) is considered a severe form of AMS. Although ER dosage formulations are FDA-approved for AMS, the lowest available capsule dose (500 mg) exceeds current dosing recommendations for AMS/HACE (WMS [Luks 2019]).

Edema or general volume overload: Adjunctive treatment of drug-induced edema or edema due to heart failure.

Elevated intraocular pressure associated with acute angle-closure glaucoma: Treatment of elevated intraocular pressure in patients with acute angle-closure glaucoma prior to surgery or as part of a combination regimen when a patient cannot be seen by an ophthalmologist for ≥1 hour.

Use: Off-Label: Adult

Idiopathic intracranial hypertension; Metabolic alkalosis

Medication Safety Issues

Sound-alike/look-alike issues:

AcetaZOLAMIDE may be confused with acetaminophen

International issues:

Diamox [Canada and multiple international markets] may be confused with Diabinese brand name for chlorpropamide [Multiple international markets]; Dobutrex brand name for dobutamine [Multiple international markets]; Trimox brand name for amoxicillin [Brazil]; Zimox brand name for amoxicillin [Italy] and carbidopa/levodopa [Greece]

Older Adult: High-Risk Medication:

Acetazolamide is identified in the Screening Tool of Older Person's Prescriptions (STOPP) criteria as a potentially inappropriate medication in older adults (≥65 years of age) due to an increased risk of falls (O’Mahony 2023).

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Ajmaline: Sulfonamides may increase adverse/toxic effects of Ajmaline. Specifically, the risk for cholestasis may be increased. Risk C: Monitor

Amantadine: Carbonic Anhydrase Inhibitors may increase serum concentration of Amantadine. Risk C: Monitor

Amphetamines: Carbonic Anhydrase Inhibitors may decrease excretion of Amphetamines. Risk C: Monitor

Carbonic Anhydrase Inhibitors: May increase adverse/toxic effects of Carbonic Anhydrase Inhibitors. The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Management: Avoid concurrent use of different carbonic anhydrase inhibitors if possible. Monitor patients closely for the occurrence of kidney stones and with regards to severity of metabolic acidosis. Risk X: Avoid

CycloSPORINE (Systemic): AcetaZOLAMIDE may increase serum concentration of CycloSPORINE (Systemic). Risk C: Monitor

Desmopressin: Hyponatremia-Associated Agents may increase hyponatremic effects of Desmopressin. Risk C: Monitor

Dexketoprofen: May increase adverse/toxic effects of Sulfonamides. Risk C: Monitor

Diacerein: May increase therapeutic effects of Diuretics. Specifically, the risk for dehydration or hypokalemia may be increased. Risk C: Monitor

EPINEPHrine (Systemic): Diuretics may increase arrhythmogenic effects of EPINEPHrine (Systemic). Diuretics may decrease vasopressor effects of EPINEPHrine (Systemic). Risk C: Monitor

Flecainide: Carbonic Anhydrase Inhibitors may decrease excretion of Flecainide. Risk C: Monitor

Fosphenytoin-Phenytoin: AcetaZOLAMIDE may increase adverse/toxic effects of Fosphenytoin-Phenytoin. Specifically, the risk for osteomalacia or rickets may be increased. Risk C: Monitor

Isocarboxazid: May increase hypotensive effects of Diuretics. Risk X: Avoid

Lithium: Carbonic Anhydrase Inhibitors may decrease serum concentration of Lithium. Risk C: Monitor

Mecamylamine: Sulfonamides may increase adverse/toxic effects of Mecamylamine. Risk X: Avoid

Mefloquine: May decrease therapeutic effects of Antiseizure Agents. Mefloquine may decrease serum concentration of Antiseizure Agents. Management: Mefloquine is contraindicated for malaria prophylaxis in persons with a history of seizures. If antiseizure drugs are being used for another indication, monitor antiseizure drug concentrations and treatment response closely with concurrent use. Risk D: Consider Therapy Modification

Memantine: Carbonic Anhydrase Inhibitors may increase serum concentration of Memantine. Risk C: Monitor

MetFORMIN: Carbonic Anhydrase Inhibitors may increase adverse/toxic effects of MetFORMIN. Specifically, the risk of developing lactic acidosis may be increased. Risk C: Monitor

Methenamine: Carbonic Anhydrase Inhibitors may decrease therapeutic effects of Methenamine. Management: Consider avoiding the concomitant use of medications that alkalinize the urine, such as carbonic anhydrase inhibitors, and methenamine. Monitor for decreased therapeutic effects of methenamine if used concomitant with a carbonic anhydrase inhibitor. Risk D: Consider Therapy Modification

MetyraPONE: Coadministration of Antiseizure Agents and MetyraPONE may alter diagnostic results. Management: Consider alternatives to the use of the metyrapone test in patients taking antiseizure agents. Risk D: Consider Therapy Modification

Mianserin: May decrease therapeutic effects of Antiseizure Agents. Risk C: Monitor

Mivacurium: AcetaZOLAMIDE may increase therapeutic effects of Mivacurium. Risk C: Monitor

Opioid Agonists: May increase adverse/toxic effects of Diuretics. Opioid Agonists may decrease therapeutic effects of Diuretics. Risk C: Monitor

Orlistat: May decrease serum concentration of Antiseizure Agents. Risk C: Monitor

Piperacillin: May increase hypokalemic effects of Diuretics. Risk C: Monitor

Polyethylene Glycol-Electrolyte Solution: Diuretics may increase nephrotoxic effects of Polyethylene Glycol-Electrolyte Solution. Risk C: Monitor

Salicylates: May increase adverse/toxic effects of Carbonic Anhydrase Inhibitors. Salicylate toxicity might be enhanced by this same combination. Management: Avoid these combinations when possible.Dichlorphenamide use with high-dose aspirin as contraindicated. If another combination is used, monitor patients closely for adverse effects. Tachypnea, anorexia, lethargy, and coma have been reported. Risk D: Consider Therapy Modification

Sodium Bicarbonate (Systemic): AcetaZOLAMIDE may increase adverse/toxic effects of Sodium Bicarbonate (Systemic). Specifically, the risk of renal calculus formation may be increased. Risk C: Monitor

Sodium Phosphates: Diuretics may increase nephrotoxic effects of Sodium Phosphates. Specifically, the risk of acute phosphate nephropathy may be enhanced. Risk C: Monitor

Reproductive Considerations

Stable disease or disease remission is recommended prior to conception in patients with idiopathic intracranial hypertension. Use of acetazolamide in patients trying to conceive should be based on a shared decision-making process and use should be discontinued prior to pregnancy, if possible (Thaller 2022).

Pregnancy Considerations

Acetazolamide crosses the placenta and can be detected in the newborn at delivery (Ibrahim 2020; Ozawa 2001).

Outcome data following maternal use of acetazolamide during pregnancy for the treatment of idiopathic intracranial hypertension (Falardeau 2013; Golan 2013) or glaucoma (Razeghinejad 2010) are limited. Data are insufficient to evaluate the risk of specific major congenital malformations or neurodevelopment outcomes following in utero exposure to acetazolamide (Pack 2024).

Acetazolamide may be considered for the treatment of idiopathic intracranial hypertension during pregnancy after 20 0/7 weeks' gestation (ACOG 2022). Use of acetazolamide during pregnancy should be based on a shared decision-making process (Thaller 2022). Frequent monitoring is recommended. Patients with stable disease should be monitored every 2 to 3 months during pregnancy; newly diagnosed patients should be monitored every 2 to 3 weeks or more often based on symptoms (Thaller 2022; Vukovic-Cvetkovic 2024).

Breastfeeding Considerations

Acetazolamide is present in breast milk.

Data related to the presence of acetazolamide in breast milk are available from case reports.

• Acetazolamide was detected in breast milk and infant serum following a maternal dose of acetazolamide 500 mg twice daily. Acetazolamide was initiated postpartum. Sampling occurred on days 4 to 5 of therapy, 10 days after delivery. Acetazolamide concentrations in the breast milk were 1.3 to 2.1 mcg/mL, 1 to 9 hours after the dose (4 samples). Acetazolamide concentrations in the infant serum were 0.2 to 0.6 mcg/mL, 2 to 12 hours after nursing (3 samples). Maternal plasma concentrations were 5.2 to 6.4 mcg/mL, 1 to 7 hours after the dose (3 samples). Adverse events were not observed in the breastfed infant (Söderman 1984).

• Breast milk was sampled following maternal use of acetazolamide 500 mg 3 times daily for idiopathic intracranial hypertension during pregnancy in 2 lactating patients. In the first patient, maternal serum concentrations of acetazolamide at delivery were 30 mcg/mL; breast milk concentrations were 4.2 mcg/mL within 1 to 2 days postpartum. Maternal serum levels of acetazolamide at delivery were 10 mcg/mL in the second patient; breast milk concentrations within 2 to 3 days of delivery were 4.2 mcg/mL (Ibrahim 2020).

Due to the potential for serious adverse reactions in the breastfed infant, the manufacturer recommends a decision be made to discontinue breastfeeding or to discontinue the drug, considering the importance of treatment to the mother.

Dietary Considerations

May be taken with food to decrease GI upset. May have additive effects with other folic acid antagonists. Some products may contain sodium.

Monitoring Parameters

Intraocular pressure (30 to 60 minutes after administration for acute angle-closure glaucoma (Pokhrel 2007; Weizer 2021); serum electrolytes; periodic CBC with differential; monitor growth in pediatric patients.

Mechanism of Action

Reversible inhibition of the enzyme carbonic anhydrase resulting in reduction of hydrogen ion secretion at renal tubule and an increased renal excretion of sodium, potassium, bicarbonate, and water. Decreases production of aqueous humor and inhibits carbonic anhydrase in central nervous system to retard abnormal and excessive discharge from CNS neurons.

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: Capsule (extended release): 2 hours; Tablet (immediate release): 1 to 1.5 hours; IV: 2 to 10 minutes

Peak effect: Capsule (extended release): 8 to 18 hours; IV: 15 minutes; Tablet: 2 to 4 hours

Duration: Inhibition of aqueous humor secretion: Capsule (extended release): 18 to 24 hours; IV: 4 to 5 hours; Tablet: 8 to 12 hours

Absorption: Appears to be dose dependent; erratic with daily doses >10 mg/kg

Distribution: Erythrocytes, kidneys; blood-brain barrier

Protein binding: 95%

Half-life: 2.4 to 5.8 hours

Time to peak, plasma: Capsule (extended release): 3 to 6 hours; Tablet: 1 to 4 hours; IV: 15 minutes

Excretion: Urine (70% to 100% [IV, tablet], 47% [extended release capsule] as unchanged drug within 24 hours)

Brand Names: International

International Brand Names by Country

For country code abbreviations (show table)

(AE) United Arab Emirates: Apo acetazolamide | Diamox;
(AR) Argentina: Aceta | Diabo | Diamox | Hydroftal | Matro;
(AT) Austria: Acetazolamid | Diamox;
(AU) Australia: Diamox;
(BD) Bangladesh: Acemox | Edimox | Remox;
(BE) Belgium: Diamox;
(BG) Bulgaria: Dehydratin;
(BR) Brazil: Diamox | Zolamox;
(CH) Switzerland: Diamox | Glaupax;
(CL) Chile: Acetazolamida | Diamox;
(CO) Colombia: Acetazolamida | Diamox | Glaucomed | Viclear;
(CZ) Czech Republic: Diluran;
(DE) Germany: Acemit | Diamox | Diuramid | Glaupax;
(DO) Dominican Republic: Aceta Diazol | Diamox | Oculten;
(EC) Ecuador: Acetazolamida Kronos | Diamox | Glaucomed | Krozemida | Vascor;
(EE) Estonia: Acemide | Acemit | Diacarb | Diamox | Diuramid;
(EG) Egypt: Acetamox | Cidamex;
(ES) Spain: Edemox;
(FI) Finland: Diamox | Oedemin | Oratrol;
(FR) France: Diamox;
(GB) United Kingdom: Acetazolamide dc | Diamox | Eytazox;
(GR) Greece: Diamox | Edemox;
(HK) Hong Kong: Apo acetazolamide | Diamox;
(HR) Croatia: Acetazolamid Agepha | Diamox;
(HU) Hungary: Huma-zolamide;
(ID) Indonesia: Diamox | Glaucon | Glaupax | Glauseta;
(IE) Ireland: Diamox | Glaupax;
(IL) Israel: Diamox | Uramox;
(IN) India: Aceact | Actamid | Avva | Diamox | Diamox er | Esmide | Glumox | I.p.c | Iopar | Iopar sr | P 20 | Trymox | Zolamide;
(IT) Italy: Diamox;
(JO) Jordan: Admox | Diamox;
(JP) Japan: Acetamox | Ailopan | Betaurel nitten | Betaurel seiko | Diamox | Diamox sanken | Didoc | Ditmune | Sethamid;
(KE) Kenya: Acetamox;
(KR) Korea, Republic of: Acetazol | Diamox;
(KW) Kuwait: Diamox;
(LB) Lebanon: Apo acetazolamide | Diamox;
(LT) Lithuania: Dehydratin | Diacarb | Diamox;
(LU) Luxembourg: Diamox;
(LV) Latvia: Dehydratin | Diacarb;
(MA) Morocco: Diamox;
(MX) Mexico: Aceta Diazol | Acetazolamida | Akezol | Diamox;
(MY) Malaysia: Acetomid | Apo acetazolamide | Diamox;
(NG) Nigeria: Axytex | Dilamox | Klydamox;
(NL) Netherlands: Diamox | Glaupax;
(NO) Norway: Acetazolamide blumont | Diamox | Diamox unimedic | Glaupax | Glaupax unimedic;
(NZ) New Zealand: Diamox;
(PE) Peru: Acetak | Acetazolamida | Apo acetazolamida | Diacetaz | Diamox | Glaucozol;
(PH) Philippines: Diamox | Zolmide;
(PK) Pakistan: Acemit | Acemox | Azm | Diamox | Evamox | Setacar;
(PL) Poland: Diamox | Diuramid;
(PR) Puerto Rico: Acetazolamide | Acetazolamide extended release | Diamox;
(PT) Portugal: Acetazolamida | Carbinib | Lediamox;
(PY) Paraguay: Stazol;
(QA) Qatar: Diamox Sodium | Diazomid;
(RO) Romania: Acetazolamida arena | Ederen;
(RU) Russian Federation: Diacarb;
(SA) Saudi Arabia: Apo acetazolamide | Diamox;
(SE) Sweden: Diamox | Glaupax;
(SG) Singapore: Apo acetazolamide | Diamox;
(SI) Slovenia: Acetazolamid | Diamox | Edemox;
(SK) Slovakia: Diluran;
(SR) Suriname: Apo acetazolamide;
(TH) Thailand: Diamox | Glaupax | Medene;
(TN) Tunisia: Diamox;
(TR) Turkey: Diazomid;
(TW) Taiwan: Acetazolamax | Atenezol | Azol | Diamox;
(UA) Ukraine: Diacarb | Radicarb;
(UG) Uganda: Acetamox;
(UY) Uruguay: Acetak | Diamox | Diural;
(VE) Venezuela, Bolivarian Republic of: Acetazolamida | Diamox;
(ZA) South Africa: Azomid | Diamox;
(ZW) Zimbabwe: Apo acetazolamide

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Acetazolamide: Drug information