Acetazolamide (extended-release capsule)
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Gerald Chi
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Overview
Acetazolamide (extended-release capsule) is a carbonic anhydrase inhibitor that is FDA approved for the {{{indicationType}}} of chronic primary open-angle glaucoma and secondary glaucoma. Acetazolamide is also indicated for the prevention or amelioration of symptoms associated with acute mountain sickness despite gradual ascent. Common adverse reactions include dizziness and lightheadedness.
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Glaucoma
- Dosing Information
- The recommended dosage is 1 capsule (500 mg) two times a day. Usually 1 capsule is administered in the morning and 1 capsule in the evening. It may be necessary to adjust the dose, but it has usually been found that dosage in excess of 2 capsules (1 g) does not produce an increased effect. The dosage should be adjusted with careful individual attention both to symptomatology and intraocular tension. In all cases, continuous supervision by a physician is advisable.
In those unusual instances where adequate control is not obtained by the twice-a-day administration of DIAMOX SEQUELS, the desired control may be established by means of DIAMOX (tablets or parenteral). Use tablets or parenteral in accordance with the more frequent dosage schedules recommended for these dosage forms, such as 250 mg every four hours, or an initial dose of 500 mg followed by 250 mg or 125 mg every four hours, depending on the case in question.
Acute Mountain Sickness
- Dosing Information
- Dosage is 500 mg to 1000 mg daily, in divided doses using tablets or extended-release capsules as appropriate. In circumstances of rapid ascent, such as in rescue or military operations, the higher dose level of 1000 mg is recommended. It is preferable to initiate dosing 24 to 48 hours before ascent and to continue for 48 hours while at high altitude, or longer as necessary to control symptoms.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Acetazolamide in adult patients.
Non–Guideline-Supported Use
Glaucoma following surgery; Prophylaxis
- Dosing Information
- 500 mg PO 1 hour postoperatively
Macular retinal edema
- Dosing Information
- 500 mg PO qd for 4 weeks
Periodic ataxia
- Dosing Information
- Doses of 250 to 1000 mg/day have eliminated or decreased the frequency and severity of symptoms such as nausea and vomiting, diplopia, and nystagmus.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
There is limited information regarding Acetazolamide (extended-release capsule) FDA-Labeled Indications and Dosage (Pediatric) in the drug label.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Acetazolamide in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Acetazolamide in pediatric patients.
Contraindications
- Hypersensitivity to acetazolamide or any excipients in the formulation. Since acetazolamide is a sulfonamide derivative, cross sensitivity between acetazolamide, sulfonamides and other sulfonamide derivatives is possible.
- Acetazolamide therapy is contraindicated in situations in which sodium and/or potassium blood serum levels are depressed, in cases of marked kidney and liver disease or dysfunction, in suprarenal gland failure, and in hyperchloremic acidosis. It is contraindicated in patients with cirrhosis because of the risk of development of hepatic encephalopathy.
- Long-term administration of DIAMOX is contraindicated in patients with chronic non-congestive angle-closure glaucoma since it may permit organic closure of the angle to occur while the worsening glaucoma is masked by lowered intraocular pressure.
Warnings
Fatalities have occurred, although rarely, due to severe reactions to sulfonamides including Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, anaphylaxis, agranulocytosis, aplastic anemia, and other blood dyscrasias. Sensitizations may recur when a sulfonamide is readministered irrespective of the route of administration. If signs of hypersensitivity or other serious reactions occur, discontinue use of this drug. Caution is advised for patients receiving concomitant high-dose aspirin and DIAMOX, as anorexia, tachypnea, lethargy, metabolic acidosis, coma, and death have been reported.
Increasing the dose does not increase the diuresis and may increase the incidence of drowsiness and/or paresthesia. Increasing the dose often results in a decrease in diuresis. Under certain circumstances, however, very large doses have been given in conjunction with other diuretics in order to secure diuresis in complete refractory failure.
To monitor for hematologic reactions common to all sulfonamides, it is recommended that a baseline CBC and platelet count be obtained on patients prior to initiating DIAMOX therapy and at regular intervals during therapy. If significant changes occur, early discontinuance and institution of appropriate therapy are important. Periodic monitoring of serum electrolytes is recommended.
Adverse Reactions
Clinical Trials Experience
There is limited information regarding Clinical Trial Experience of acetazolamide in the drug label.
Postmarketing Experience
Body as a whole
Headache, malaise, fatigue, fever, pain at injection site, flushing, growth retardation in children, flaccid paralysis, anaphylaxis.
Digestive
Gastrointestinal disturbances such as nausea, vomiting, diarrhea.
Hematological/Lymphatic
Blood dyscrasias such as aplastic anemia, agranulocytosis, leukopenia, thrombocytopenic purpura, melena.
Hepato-biliary disorders
Abnormal liver function, cholestatic jaundice, hepatic insufficiency, fulminant hepatic necrosis.
Metabolic/Nutritional
Metabolic acidosis, electrolyte imbalance, including hypokalemia, hyponatremia, osteomalacia with long-term phenytoin therapy, loss of appetite, taste alteration, hyper/hypoglycemia.
Nervous
Drowsiness, paresthesia (including numbness and tingling of extremities and face), depression, excitement, ataxia, confusion, convulsions, dizziness.
Skin
Allergic skin reactions including urticaria, photosensitivity, Stevens- Johnson syndrome, toxic epidermal necrolysis.
Special senses
Hearing disturbances, tinnitus, transient myopia.
Drug Interactions
- Aspirin
- DIAMOX modifies phenytoin metabolism with increased serum levels of phenytoin. This may increase or enhance the occurrence of osteomalacia in some patients receiving chronic phenytoin therapy. Caution is advised in patients receiving chronic concomitant therapy. By decreasing the gastrointestinal absorption of primidone, DIAMOX may decrease serum concentrations of primidone and its metabolites, with a consequent possible decrease in anticonvulsant effect. Caution is advised when beginning, discontinuing, or changing the dose of DIAMOX in patients receiving primidone.
Because of possible additive effects with other carbonic anhydrase inhibitors, concomitant use is not advisable. Acetazolamide may increase the effects of other folic acid antagonists. Acetazolamide decreases urinary excretion of amphetamine and may enhance the magnitude and duration of their effect. Acetazolamide reduces urinary excretion of quinidine and may enhance its effect. Acetazolamide may prevent the urinary antiseptic effect of methenamine. Acetazolamide increases lithium excretion and the lithium may be decreased. Acetazolamide and sodium bicarbonate used concurrently increase the risk of renal calculus formation. Acetazolamide may elevate cyclosporine levels.
- Drug/laboratory test interactions
- Sulfonamides may give false negative or decreased values for urinary phenolsulfonphthalein and phenol red elimination values for urinary protein, serum non-protein, and serum uric acid. Acetazolamide may produce an increased level of crystals in the urine.
Acetazolamide interferes with the HPLC method of assay for theophylline. Interference with the theophylline assay by acetazolamide depends on the solvent used in the extraction; acetazolamide may not interfere with other assay methods for theophylline.
Use in Specific Populations
Pregnancy
Teratogenic effects: Pregnancy Category C
Acetazolamide, administered orally or parenterally, has been shown to be teratogenic (defects of the limbs) in mice, rats, hamsters, and rabbits. There are no adequate and well-controlled studies in pregnant women. Acetazolamide should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Acetazolamide (extended-release capsule) in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Acetazolamide (extended-release capsule) during labor and delivery.
Nursing Mothers
Because of the potential for serious adverse reactions in nursing infants from DIAMOX, a decision should be made whether to discontinue nursing or to discontinue the drug taking into account the importance of the drug to the mother. Acetazolamide should only be used by nursing women if the potential benefit justifies the potential risk to the child.
Pediatric Use
The safety and effectiveness of DIAMOX SEQUELS in pediatric patients below the age of 12 years have not been established. Growth retardation has been reported in children receiving long-term therapy, believed secondary to chronic acidosis.
Geriatic Use
Metabolic acidosis, which can be severe, may occur in the elderly with reduced renal function. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant disease or other drug therapy.
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Administration and Monitoring
Administration
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Monitoring
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IV Compatibility
Solution
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Y-Site
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Variable
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Admixture
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Syringe
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TPN/TNA
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Overdosage
Acute Overdose
Management
No specific antidote is known. Treatment should be symptomatic and supportive. Electrolyte imbalance, development of an acidotic state, and central nervous system effects might be expected to occur. Serum electrolyte levels (particularly potassium) and blood pH levels should be monitored. Supportive measures are required to restore electrolyte and pH balance. The acidotic state can usually be corrected by the administration of bicarbonate.
Despite its high intraerythrocytic distribution and plasma protein binding properties, DIAMOX may be dialyzable. This may be particularly important in the management of DIAMOX overdosage when complicated by the presence of renal failure.
Pharmacology
| Template:Px | |
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Acetazolamide (extended-release capsule)
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| Systematic (IUPAC) name | |
| N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide | |
| Identifiers | |
| CAS number | |
| ATC code | S01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox |
| Mol. mass | 222.245 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | None |
| Half life | 2-4 hours |
| Excretion | Urine (90%) |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status |
Prescription Only (S4)(AU) ?(CA) POM(UK) [[Prescription drug|Template:Unicode-only]](US) |
| Routes | oral or intravenous |
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Clinical Studies
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Storage
There is limited information regarding Acetazolamide (extended-release capsule) Storage in the drug label.
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Drug Images
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Patient Counseling Information
Adverse reactions common to all sulfonamide derivatives may occur: anaphylaxis, fever, rash (including erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis), crystalluria, renal calculus, bone marrow depression, thrombocytopenic purpura, hemolytic anemia, leukopenia, pancytopenia, and agranulocytosis. Caution is advised for early detection of such reactions and the drug should be discontinued and appropriate therapy instituted. In patients with pulmonary obstruction or emphysema where alveolar ventilation may be impaired, DIAMOX which may precipitate or aggravate acidosis should be used with caution. Gradual ascent is desirable to try to avoid acute mountain sickness. If rapid ascent is undertaken and DIAMOX is used, it should be noted that such use does not obviate the need for prompt descent if severe forms of high altitude sickness occur, i.e., high altitude pulmonary edema (HAPE) or high altitude cerebral edema. Caution is advised for patients receiving concomitant high-dose aspirin and DIAMOX, as anorexia, tachypnea, lethargy, metabolic acidosis, coma, and death have been reported (see WARNINGS). Both increases and decreases in blood glucose have been described in patients treated with acetazolamide. This should be taken into consideration in patients with impaired glucose tolerance or diabetes mellitus. Acetazolamide treatment may cause electrolyte imbalances, including hyponatremia and hypokalemia, as well as metabolic acidosis. Therefore, periodic monitoring of serum electrolytes is recommended. Particular caution is recommended in patients with conditions that are associated with, or predispose a patient to, electrolyte and acid/base imbalances, such as patients with impaired renal function (including elderly patients; see PRECAUTIONS, Geriatric Use), patients with diabetes mellitus, and patients with impaired alveolar ventilation. Some adverse reactions to acetazolamide, such as drowsiness, fatigue, and myopia, may impair the ability to drive and operate machinery.
Precautions with Alcohol
Alcohol-Acetazolamide interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
Diamox Sequels
Look-Alike Drug Names
- (Paired Confused Name 1a) — (Paired Confused Name 1b)
- (Paired Confused Name 2a) — (Paired Confused Name 2b)
- (Paired Confused Name 3a) — (Paired Confused Name 3b)
Drug Shortage Status
Drug Shortage
Price
References
The contents of this FDA label are provided by the National Library of Medicine.