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Manufacturer
TARO PHARM USA
SKU
51672402301

acetazolamide 250 mg tablet

Generic
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Uses

Acetazolamide shares the uses of the carbonic anhydrase inhibitors; however, the extended-release capsules are intended for use only for the adjunctive treatment of open-angle (noncongestive, chronic simple) or secondary glaucoma, for short-term preoperative therapy in angle-closure glaucoma (obstructive, narrow-angle) when delay of surgery is desired in order to lower intraocular pressure, and for prevention or amelioration of symptoms associated with acute high-altitude sickness (mountain sickness).

Acetazolamide is used as an adjunct to other anticonvulsants in the management of centrencephalic epilepsies (e.g., petit mal, unlocalized seizures). Tolerance to the anticonvulsant effects of acetazolamide develop quickly, and the drug may be ineffective for prolonged therapy. Although acetazolamide may be useful in partial, myoclonic, absence, and primary generalized tonic-clonic seizures that have not responded adequately to other anticonvulsants, acetazolamide has not been evaluated in controlled clinical studies in specific seizure types.

Acetazolamide is used to increase altitude tolerance in the prevention or amelioration of symptoms (e.g., headache, lassitude, insomnia, nausea, shortness of breath, dizziness) associated with acute mountain sickness in climbers attempting rapid ascent and in those who are very susceptible to the condition despite gradual ascent. Use of acetazolamide does not obviate prompt descent in patients who develop severe forms of acute mountain sickness (e.g., high-altitude pulmonary and/or cerebral edema). The drug does not prevent acute mountain sickness, but rather shortens the time of acclimatization. Acetazolamide also is used in the treatment and prevention of high-altitude sleep disorders.

Dosage and Administration

Reconstitution and Administration

Acetazolamide is administered orally. Acetazolamide sodium is preferably administered by direct IV injection; IM administration is painful because of the alkaline pH of the drug solution and therefore is not recommended.

Acetazolamide sodium sterile powder is reconstituted by adding at least 5 mL of sterile water for injection to a vial containing 500 mg of acetazolamide to provide a solution containing not more than 100 mg/mL.

When an oral liquid preparation of acetazolamide is needed, the appropriate number of commercially available tablets may be crushed and suspended in cherry, chocolate, raspberry, or any other highly flavored carbohydrate syrup. (Elixirs or other vehicles containing alcohol or glycerin will not disguise the bitter taste of the drug.) Up to 500 mg of acetazolamide can be suspended in 5 mL of syrup; however, suspensions containing 250 mg of the drug per 5 mL of syrup are more palatable. Suspensions of acetazolamide in syrup are stable for about 1 week. Alternatively, up to one tablet of acetazolamide may be softened in 2 teaspoonsful of hot water and added to 2 teaspoonsful of honey or syrup, then swallowed all at once. This liquid should be prepared just prior to administration. The drug will not dissolve in fruit juices, nor will the taste be disguised.

Dosage

Dosage of acetazolamide should be adjusted according to the patient's requirements and response. Dosage of acetazolamide sodium is expressed in terms of acetazolamide.

Glaucoma

In the adjunctive treatment of open-angle glaucoma in adults, 250 mg of acetazolamide is usually administered orally 1-4 times daily. Adult dosage of the extended-release capsules is 500 mg twice daily, usually in the morning and evening. Acetazolamide dosage in excess of 1 g daily in adults usually does not produce an increased effect. Patients whose glaucoma is not adequately controlled by twice-daily administration of the extended-release capsules may respond to therapy with the tablet or parenteral preparations of acetazolamide. In adults with secondary glaucoma and preoperatively in adults with acute angle-closure glaucoma, 250 mg of acetazolamide in tablet formulation may be administered orally every 4 hours.Some adults have responded to short-term therapy with 250 mg twice daily. In some acute glaucomas, an initial oral dose of 500 mg followed by 125-250 mg every 4 hours in adults may be preferable.

When IV therapy is used in adults with secondary glaucoma and preoperatively in adults with acute angle-closure glaucoma, the recommended dosage of acetazolamide is 250 mg every 4 hours. Some adults have responded to short-term therapy with 250 mg twice daily. In some acute glaucomas, an initial IV dose of 500 mg followed by 125-250 mg every 4 hours in adults may be preferable.

In children with glaucoma, the oral dosage of acetazolamide is 8-30 mg/kg or 300-900 mg/m daily, in 3 divided doses. In acute glaucoma in children, 5-10 mg/kg may be administered IV every 6 hours.

Seizure Disorders

As an adjunct to other anticonvulsants in the prophylactic management of seizure disorders, the usual oral or IV dosage of acetazolamide for adults and children is 8-30 mg/kg daily, in divided doses. When acetazolamide is given concurrently with other anticonvulsants, the usual initial dosage is 250 mg daily. The optimum dosage appears to be 375 mg to 1 g daily, although some patients may respond to lower dosage. Some clinicians suggest that dosage in excess of 1 g daily does not result in increased effectiveness. In the prophylactic management of seizure disorders, the addition, withdrawal, or replacement of one anticonvulsant drug with another should be accomplished gradually.

Edema

In edema secondary to congestive heart failure or drug therapy, the usual initial adult oral or IV dosage of acetazolamide is 250-375 mg daily (5 mg/kg) in the morning. Although some patients have received very large doses of acetazolamide in conjunction with other diuretics in order to achieve diuresis, increasing the dose may not increase diuresis and may increase the incidence of adverse effects such as drowsiness or paresthesia. Failures in diuretic therapy with acetazolamide may result from overdoses or too frequent dosage. If the patient fails to continue to lose edema fluid after an initial response, acetazolamide should be withheld for one day to allow for kidney recovery. To avoid loss of diuretic effect, the drug should be given intermittently (on alternate days or for 2 consecutive days followed by a drug-free day).

As a diuretic in children, an acetazolamide dosage of 5 mg/kg or 150 mg/m may be administered orally or IV once daily in the morning.

Acute Mountain Sickness

For the prevention or amelioration of symptoms associated with acute mountain sickness in adult expeditioners or tourist-trekkers, the usual oral dosage of acetazolamide is 0.5-1 g daily in divided doses as appropriate using conventional tablets or extended-release capsules, beginning 24-48 hours before and continued during ascent and for at least 48 hours after arrival at the high altitude; therapy with the drug may be continued at high altitude as necessary to control symptoms. Some clinicians state that acetazolamide 125-250 mg (as conventional tablets) twice daily beginning 24 hours before ascent has been effective in preventing acute mountain sickness; acetazolamide 500 mg (as extended-release capsules) given once every 24 hours also has been effective. For the management of high-altitude sleep disorders, acetazolamide 125 mg at bedtime has been used. For the treatment of acute mountain sickness, some experts recommend an acetazolamide dose of 250 mg given within 24 hours of the onset of symptoms and a second 250-mg dose given 8 hours later.

Other Uses

In the treatment of periodic paralysis, 250 mg of acetazolamide has usually been administered orally 2 to 3 times daily; however, a few patients have responded to 250-375 mg daily, and a few patients have required up to 1.5 g daily.

For further information on chemistry, pharmacology, pharmacokinetics, uses, cautions, drug interactions, laboratory test interferences, and dosage and administration of acetazolamide,

Cautions

Acetazolamide shares the pharmacologic actions and toxic potentials of the carbonic anhydrase inhibitors, and the usual precautions of carbonic anhydrase inhibitor therapy should be observed.

Pharmacokinetics

Absorption

Acetazolamide is well absorbed from the GI tract. Following oral administration of 500 mg of acetazolamide as tablets, peak plasma concentrations of about 12-27 mcg/mL are achieved within 1-3 hours. Low concentrations of acetazolamide are present in plasma 24 hours after the drug is given.

Distribution

Acetazolamide is distributed throughout body tissues; it concentrates principally in erythrocytes, plasma, and kidneys and, to a lesser extent, in liver, muscles, eyes, and CNS. Acetazolamide does not accumulate in tissues. The drug crosses the placenta in unknown quantities. It is not known whether acetazolamide distributes into human milk, but the drug has been detected in the milk of lactating dogs.

Elimination

Acetazolamide is excreted unchanged by the kidneys via tubular secretion and passive reabsorption. After administration of the oral tablets or after IV injection, 70-100% (average 90%) of the dose is excreted in urine within 24 hours; 47% of the dose is excreted within 24 hours following administration of the extended-release capsules.

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