Yes

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

Lowers intraocular pressure to treat glaucoma, also as a diuretic, adjunct treatment of refractory seizures and acute altitude sickness; centrencephalic epilepsies (sustained release not recommended for anticonvulsant)

C

Clinical effects on the fetus: Despite widespread usage, no reports linking the use of acetazolamide with congenital defects have been located

Breast-feeding/lactation: The American Academy of Pediatrics considers acetazolamide to be compatible with breast-feeding

Hypersensitivity to sulfonamides or acetazolamide, patients with hepatic disease or insufficiency; patients with decreased sodium and/or potassium levels; patients with adrenocortical insufficiency, hyperchloremic acidosis, severe renal disease or dysfunction, or severe pulmonary obstruction; long-term use in noncongestive angle-closure glaucoma

Use in impaired hepatic function may result in coma; use with caution in patients with respiratory acidosis and diabetes mellitus; impairment of mental alertness and/or physical coordination may occur

I.M. administration is painful because of the alkaline pH of the drug

Drug may cause substantial increase in blood glucose in some diabetic patients; malaise and complaints of tiredness and myalgia are signs of excessive dosing and acidosis in the elderly

>10%:

Central nervous system: Malaise

Gastrointestinal: Anorexia, diarrhea, metallic taste

Genitourinary: Polyuria

Neuromuscular & skeletal: Muscular weakness

1% to 10%: Central nervous system: Mental depression, drowsiness

<1%: Fever, fatigue, rash, hyperchloremic metabolic acidosis, hypokalemia, hyperglycemia, black stools, GI irritation, dryness of the mouth, dysuria, bone marrow suppression, blood dyscrasias, paresthesia, myopia, renal calculi

Symptoms of overdose include low blood sugar, tingling of lips and tongue, nausea, yawning, confusion, agitation, tachycardia, sweating, convulsions, stupor, and coma

Hypoglycemia should be managed with 50 mL I.V. dextrose 50% followed immediately with a continuous infusion of 10% dextrose in water (administer at a rate sufficient enough to approach a serum glucose level of 100 mg/dL). The use of corticosteroids to treat the hypoglycemia is controversial, however, the addition of 100 mg of hydrocortisone to the dextrose infusion may prove helpful.

Decreased effect: Increased lithium excretion and altered excretion of other drugs by alkalinization of urine (such as amphetamines, quinidine, procainamide, methenamine, phenobarbital, salicylates); primidone serum concentrations may be decreased

Increased toxicity: Cyclosporine trough concentrations may be increased resulting in possible nephrotoxicity and neurotoxicity; salicylate use may result in carbonic anhydrase inhibitor accumulation and toxicity including CNS depression and metabolic acidosis; digitalis toxicity may occur if hypokalemia is untreated

Reconstituted solution may be stored up to 12 hours at room temperature (15°C to 30°C) and for 3 days under refrigeration (2°C to 8°C)

Standard diluent: 500 mg/50 mL D₅W

Minimum volume: 50 mL D₅W

Stability of IVPB solution: 5 days at room temperature (25°C) and 44 days at refrigeration (5°C)

Reconstitute with at least 5 mL sterile water to provide a solution containing not more than 100 mg/mL; further dilution in 50 mL of either D₅W or NS for I.V. infusion administration

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 to decrease production of aqueous humor; also inhibits carbonic anhydrase in central nervous system to retard abnormal and excessive discharge from CNS neurons

Onset of effect: Extended release capsule: 2 hours; peak effect: 3-6 hours; I.V.: 2 minutes; peak effect: 15 minutes; Tablet, peak effect: 1-4 hours

Peak effect: Extended release capsule: 3-6 hours; Tablet: 1-4 hours; I.V.: 15 minutes

Duration: Extended release capsule: 18-24 hours; Tablet: 8-12 hours; I.V.: 4-5 hours

Distribution: Distributes into erythrocytes, kidneys; crosses blood-brain barrier; crosses placenta and distributes into milk to ~30% of plasma concentrations

Protein binding: 95%

Half-life: 2.4-5.8 hours

Elimination: 70% to 100% of I.V. or tablet dose is excreted unchanged in the urine within 24 hours

Note: I.M. administration is not recommended because of pain secondary to the alkaline pH

Children:

Glaucoma:

Oral: 8-30 mg/kg/day or 300-900 mg/m²/day divided every 8 hours

I.M., I.V.: 20-40 mg/kg/24 hours divided every 6 hours, not to exceed 1 g/day

Edema: Oral, I.M., I.V.: 5 mg/kg or 150 mg/m² once every day

Epilepsy: Oral: 8-30 mg/kg/day in 1-4 divided doses, not to exceed 1 g/day; sustained release capsule is not recommended for treatment of epilepsy

Adults:

Glaucoma:

Chronic simple (open-angle): Oral: 250 mg 1-4 times/day or 500 mg sustained release capsule twice daily

Secondary, acute (closed-angle): I.M., I.V.: 250-500 mg, may repeat in 2-4 hours to a maximum of 1 g/day

Edema: Oral, I.M., I.V.: 250-375 mg once daily

Epilepsy: Oral: 8-30 mg/kg/day in 1-4 divided doses; sustained release capsule is not recommended for treatment of epilepsy

Altitude sickness: Oral: 250 mg every 8-12 hours (or 500 mg extended release capsules every 12-24 hours)

Therapy should begin 24-48 hours before and continue during ascent and for at least 48 hours after arrival at the high altitude

Urine alkalinization: Oral: 5 mg/kg/dose repeated 2-3 times over 24 hours

Elderly: Oral: Initial: 250 mg twice daily; use lowest effective dose

Dosing adjustment in renal impairment:

Cl_cr 10-50 mL/minute: Administer every 12 hours

Cl_cr <10 mL/minute: Avoid use ineffective

Hemodialysis: Moderately dialyzable (20% to 50%)

Peritoneal dialysis: Supplemental dose is not necessary

May be administered with food to decrease GI upset

Intraocular pressure, potassium, serum bicarbonate; serum electrolytes, periodic CBC with differential

May cause false-positive results for urinary protein with Albustix®, Labstix®, Albutest®, Bumintest®

Drowsiness is common, may produce depression less commonly

Can rarely cause bone marrow suppression use cautiously with clozapine and carbamazepine; may increase the excretion of lithium

No information available to require special precautions

Metallic taste in >10% of patients; disappears upon drug withdrawal

Take as directed; do not chew or crush long-acting capsule (contents may be sprinkled on soft food). You will need periodic ophthalmic examinations while taking this medication. You may experience drowsiness, dizziness, or weakness (use caution when driving or engaging in tasks that require alertness until response to drug is known); nausea, loss of appetite, or altered taste (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). Monitor serum glucose closely (may cause altered blood glucose in some diabetic patients, or unusual response to some forms of glucose testing); increased sensitivity to sunlight (use sunblock, protective clothing, and avoid exposure to direct sunlight). Report unusual and persistent tiredness; numbness, burning, or tingling of extremities or around mouth, lips, or anus; muscle weakness; black stool; or excessive depression. Pregnancy precautions: Inform prescriber if you are or intend to be pregnant.

Oral: Tablet may be crushed and suspended in cherry or chocolate syrup to disguise the bitter taste of the drug

Parenteral: Reconstitute with at least 5 mL sterile water to provide an I.V. solution containing not more than 100 mg/mL; maximum concentration: 100 mg/mL; maximum rate of I.V. infusion: 500 mg/minute

Capsule, sustained release: 500 mg

Injection: 500 mg

Tablet: 125 mg, 250 mg

Tablets may be crushed and suspended in cherry, chocolate, raspberry, or other highly flavored carbohydrate syrup in concentrations of 25-100 mg/mL; simple suspensions are stable for 7 days. For solutions with longer stability, see references Parastampuria and Alexander.

McEvoy G, ed, AHFS Drug Information 96, Bethesda, MD: American Society of Health System Pharmacists, 1996.

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"American Academy of Pediatrics Committee on Drugs: The Transfer of drugs and Other Chemicals Into Human Milk," Pediatrics, 1994, 93(1):137-150.

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Weiss IS, "Hirsutism After Chronic Administration of Acetazolamide," Am J Ophthalmol, 1974, 78(2):327-8.