Class: Anticonvulsant, Carbonic anhydrase inhibitor
- Tablets 125 mg
- Tablets 250 mg
- Injection, lyophilized powder for solution 500 mg
- Capsules, ER 500 mg
Inhibits carbonic anhydrase enzyme, reducing rate of aqueous humor formation and thus lowering IOP; produces diuretic effect; retards neuronal conduction in brain.
ER T max is 3 to 6 h. Immediate-release T max is 1 to 4 h.
ER is 18 to 24 h; immediate-release is 8 to 12 h.
Indications and Usage
Prevention or lessening of symptoms associated with acute mountain sickness (oral only); adjunctive treatment of chronic simple (open-angle) glaucoma and secondary glaucoma; preoperative treatment of acute congestive (closed-angle) glaucoma; adjunctive treatment of centrencephalic epilepsies (eg, petit mal, generalized seizures); edema caused by CHF and drug-induced edema (tablet and IV only).
Familial periodic paralysis; malignant glaucoma; prevention of migraine.
Hypersensitivity to any ingredients in the formulations; depressed sodium and/or potassium serum levels; marked kidney and liver disease or dysfunction; suprarenal gland failure; hyperchloremic acidosis; cirrhosis; long-term use in chronic noncongestive angle-closure glaucoma.
Dosage and AdministrationAcute Mountain Sickness
Adults and Children 12 yr of age and older
PO 500 to 1,000 mg per day in divided doses twice daily. In circumstances of rapid ascent, 1,000 mg is recommended. It is preferable to initiate dosing 24 to 48 h before ascent. Continue for 48 h while at high altitude, or longer as necessary to control symptoms.Chronic Simple (Open-Angle) Glaucoma
PO Tablets / IV 250 mg to 1 g per day, usually in divided doses for amounts above 250 mg.Adults and Children 12 yr of age and older
PO ER capsules 500 mg 2 times daily. It may be necessary to adjust the dose, but it has usually been found that a dose in excess of 1 g does not produce an increased effect.Diuresis in CHF
PO Tablets / IV Initially 250 to 375 mg (5 mg/kg) every morning; then give on alternate days or for 2 days alternating with 1 day of rest.Drug-Induced Edema
PO Tablets / IV 250 to 375 mg daily for 1 to 2 days, alternating with a day of rest.Secondary Glaucoma/Acute Congestive Closed-Angle Glaucoma
PO Tablets / IV 250 mg every 4 h or 250 mg twice daily. In some acute cases, initially administer 500 mg, then 125 to 250 mg every 4 h.Adults and Children 12 yr of age and younger
ER capsules 500 mg 2 times daily. It may be necessary to adjust the dose, but it has usually been found that a dose in excess of 1 g does not produce an increased effect.Seizures
PO Tablets / IV 8 to 30 mg/kg per day in divided doses; optimum range is 375 to 1,000 mg/day. When drug is given in combination with other anticonvulsants, initial dosage is 250 mg daily.
- Direct IV administration is preferred. IM administration is not recommended.
- Reconstitute following manufacturer's guidelines using at least 5 mL of sterile water for injection.
- Do not administer if particulate matter, cloudiness, or discoloration is noted.
- Discard any unused solution.
Store ER capsules at 68° to 77°F. Store tablets and powder for injection at 59° to 86°F. Store reconstituted injectable solution at 36° to 46°F for up to 3 days or use within 12 h of reconstitution if stored at 59° to 86°F.
By alkalinizing the urine, the urinary excretion of amphetamines is decreased, enhancing the magnitude and duration of effects. Avoid coadministration, especially in overdose situations.Beta-blockers
Coadministration may cause severe mixed acidosis in patients with respiratory disorders. Use with caution. If acidosis occurs, discontinue one or both drugs.Carbonic anhydrase inhibitors (eg, methazolamide)
Because of additive effects, avoid other carbonic anhydrase inhibitors.Cyclosporine
Cyclosporine concentrations may be elevated, increasing the pharmacologic effect and adverse reactions. Monitor cyclosporine concentrations and adjust the cyclosporine dose as needed.Folic acid antagonists
The pharmacologic effects of folic acid antagonists may be increased. Use with caution.Hydantoins (phenytoin)
Phenytoin serum concentrations may be elevated, increasing the pharmacologic effects and risk of toxicity. Use with caution. Monitor phenytoin concentrations and the patient's response. Adjust the phenytoin dose as needed.Lithium
Lithium serum concentrations may be reduced, decreasing the therapeutic response. Monitor lithium concentrations and the patient's response. If an interaction is suspected, adjust the lithium dose as needed.Methenamine
Acetazolamide may interfere with the antibacterial effect of methenamine. Avoid coadministration. Consider use of a urinary antimicrobial agent not affected by urinary alkalinization.Primidone
Plasma concentrations of primidone and its metabolites may be reduced, decreasing the anticonvulsant effect. Use with caution when starting, stopping, or changing the dose of acetazolamide. If an interaction is suspected, consider use of an alternative anticonvulsant agent.Quinidine
Quinidine serum levels may be increased. Because of urinary alkalinization, urinary excretion of quinidine is decreased, increasing the pharmacologic and toxic effects. Use with caution. Monitor quinidine concentrations and cardiac function when starting or stopping acetazolamide. Adjust the quinidine dose as needed.Salicylates
May cause acetazolamide accumulation and toxicity, including CNS depression, and metabolic acidosis, coma, and death. Monitor salicylate concentrations, acid-base parameters, and CNS status. Adjust the acetazolamide dose as needed.Sodium bicarbonate
Coadministration increases the risk of renal calculus formation. Avoid coadministration.Topiramate
Concomitant use of topiramate with acetazolamide may increase the risk of kidney stone formation. Avoid coadministration.
Laboratory Test Interactions
Acetazolamide may give false positive 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 high-performance liquid chromatography method of assay for theophylline. Because interference with the theophylline assay by acetazolamide depends on the solvent used in extraction, acetazolamide may not interfere with other theophylline assay methods.
Ataxia, confusion, convulsions, depression, dizziness, drowsiness, excitement, headache, malaise, paresthesia.
Hearing disturbances, tinnitus, transient myopia.
Diarrhea, loss of appetite, melena, nausea, taste alterations, vomiting.
Crystalluria, glycosuria, hematuria, nephrolithiasis with long-term therapy, polyuria, renal failure.
Agranulocytosis, aplastic anemia, leukopenia, thrombocytopenic purpura.
Abnormal liver function, cholestatic jaundice, fulminant hepatic necrosis, hepatic insufficiency.
Allergic skin reactions, including urticaria, Stevens-Johnson syndrome, TEN, photosensitivity; anaphylaxis.
Metabolic acidosis, electrolyte imbalance (hypokalemia, hyponatremia), hyperglycemia, hypoglycemia.
Fever, flaccid paralysis, flushing, growth retardation in children, injection-site pain.
Fatalities have occurred, although rarely, because of severe reactions to sulfonamides, including agranulocytosis, aplastic anemia, fulminant hepatic necrosis, Stevens-Johnson syndrome, TEN, 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 acetazolamide because anorexia, tachypnea, lethargy, coma, and death have been reported.
Obtain a baseline CBC and platelet count prior to initiating acetazolamide 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.
Category C .
Safety and efficacy not established (tablets/IV); safety and efficacy not established in children younger than 12 yr of age (ER capsules).
Metabolic acidosis, which can be severe, may occur in elderly patients with reduced renal function.
Cross-sensitivity between acetazolamide, sulfonamides, and other sulfonamide derivatives is possible.
Use with caution.
Some adverse reactions, such as drowsiness, fatigue, and myopia, may impair the ability to drive and operate machinery.
Both increases and decreases in blood glucose have occurred.
Increasing dose does not augment diuresis, but may increase drowsiness and paresthesias.
Hyponatremia, hypokalemia, and metabolic acidosis may occur.
Use in pulmonary obstruction and emphysema may aggravate or precipitate acidosis.
Acidosis, CNS effects, electrolyte imbalance.
- Advise patient with glaucoma to continue to use other glaucoma medications prescribed by health care provider unless advised otherwise.
- Advise patient with epilepsy to continue to use other antiepileptic drugs prescribed by health care provider unless advised otherwise.
- Advise patient that urine production may increase following the first few doses of the medication and that this is normal and of no concern. Advise patient to inform health care provider if excessive urine production occurs.
- Advise patient using medication for preventing symptoms of high altitude sickness that if rapid ascent produces symptoms of high altitude sickness, rapid descent is necessary.
- Advise patient to discontinue therapy and contact health care provider immediately if any of the following occur: blood in urine, flank or loin pain, hives, itching, pallor, purple spots under the skin, rash, ringing in ears or hearing changes, sore throat, tingling or tremors in hands or feet, unexplained fever, unusual bleeding or bruising.
- Advise patient to avoid unnecessary exposure to sunlight or tanning lamps and to use sunscreen and wear protective clothing to avoid photosensitivity reactions.
- Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
- Advise patients with diabetes that hyperglycemia or hypoglycemia may occur.
Copyright © 2009 Wolters Kluwer Health.
More about acetazolamide
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