Acetazolamide

Dosage ; 0.25 - 1.0g daily orally or 1.V.

Acetazolamide Brands

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Acetazolamide More Info

Mode Of Action

Enzyme inhibitor that acts specifically on carbonic anhydrase (the enzyme that catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid). In the eye, its inhibitory action decreases the secretion of aqueous humor and results in a drop in intraocular pressure. In the kidney inhibition of carbonic anhydrase results in renal loss of HCO3 ion, which carries out sodium, water, and potassium. Inhibition of carbonic anhydrase in CNS appears to retard abnormal, paroxysmal, excessive discharge neurons hence its use in CNS conditions like epilepsy.

Drug Indication Chronic simple (open-angle) glaucoma, secondary glaucoma, acute glaucoma when delay of surgery is desired, lowers intraocular pressure, CCF, drug induced oedema, epilepsy.
Precautions Blood monitor (as with other sulphonamides), severe cirrhosis, increasing the dose above the set dose does not increase diuresis, avoiding extravasation as it can cause necrosis, cross-sensitivity with other sulphonamides, not recommended for long time use, elderly.
Contra-Indications Hypersensitivity to sulphonamides, severe renal impairment, hepatic impairment, adrenocortical insufficiency, long-term use in chronic non-congestive angle-closure glaucoma. Severe pulmonary obstruction, low sodium and potassium serum levels
Side Effects Drowsiness, rashes, crystalluria, bone marrow depression, loss of appetite, flaccid paralysis, glycosuria, hepatic impairment, fever, allergic reaction, impotence.
Dosage 0.25 - 1.0g daily orally or 1.V.
Pregnancy Category Category B3
Pregnancy Category Description Drugs which have been taken by only a small number of pregnant women and women of child-bearing age with no any established rise in the frequency of malformations or other direct or indirect detrimental effects on the foetus having been noted. Studies in animals show evidence of an increased occurrence of foetal damage, the significance of which is uncertain in human
Drug Category DRUGS ACTI NG ON THE CARDIO-VASCULAR SYSTEM
Drug Sub-Category Carbonic anhydrase inhibitors

Dosing: Adult

Note: I.M. administration is not recommended.

Glaucoma:

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

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

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

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

Metabolic alkalosis (unlabeled use): I.V. 250 mg every 6 hours for 4 doses or 500 mg single dose; reassess need based upon acid-base status

Mountain sickness: Oral: Manufacturer's labeling: 500-1000 mg daily, in divided doses every 8-12 hours (immediate release tablets) or divided every 12-24 hours (extended release capsules ). Alternative recommendations suggest use of lower doses to reduce side effects: 125-250 mg twice daily for prevention or treatment of mild sickness, and 250 mg twice daily for treatment of moderate sickness (Hackett, 2001). Therapy should begin 24-48 hours before and continue during ascent and for at least 48 hours after arrival at the high altitude.

Note: In situations of rapid ascent (such as rescue or military operations), 1000 mg/day is recommended (manufacturer's labeling).

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

Respiratory stimulant in COPD (unlabeled use): Oral, I.V.: 250 mg twice daily

Dosing: Pediatric

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

Note: I.M. administration is not recommended.

Glaucoma:

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

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

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

Epilepsy: Oral: Refer to adult dosing.

Dosing: Geriatric

Oral: Initial: 250 mg once or twice daily; use lowest effective dose possible.

Dosing: Renal Impairment

Clcr 10-50 mL/minute: Administer every 12 hours.

Clcr <10 mL/minute: Avoid use (ineffective).

Moderately dialyzable (20% to 50%)