Acetazolamide

Indications
 Oral
Diuresis
Adult: 250-375 mg once daily or on alternate days. Intermittent treatment is needed for continued efficacy.
Oral
Preoperative management of angle-closure glaucoma
Adult: 250-1000 mg daily in divided doses.
Child: 1 mth-12 yr: 10-20 mg/kg daily. Max: 750 mg daily, in 2-4 divided doses.
Oral
Adjunct in open-angle glaucoma
Adult: 250-1000 mg daily in divided doses.
Child: 1 mth-12 yr: 10-20 mg/kg daily. Max: 750 mg daily, in 2-4 divided doses.
Oral
Epilepsy
Adult: Either alone or with other antiepileptics: 250-1000 mg daily in divided doses.
Child: Neonates and up to 12 yr: Initially, 2.5 mg/kg bid-tid; maintenance: 5-7 mg/kg bid-tid. Max: 750 mg daily.
Oral
Prophylaxis of high-altitude disorders
Adult: 500-1000 mg daily in divided doses. Prompt descent is still advised if severe symptoms such as cerebral or pulmonary oedema occur.
Intravenous
Chronic open-angle glaucoma
Adult: As an adjunct, 0.25-1 g every 24 hr, usually in divided doses. Adjust dose according to symptomatology and ocular tension.
Intravenous
Acute closed angle glaucoma
Adult: 250-500 mg. may repeat 2-4 hr later if needed. Max: 1 g daily.
Intravenous
Epilepsy
Adult: 8-30 mg/kg daily in divided doses. Optimum dose: 375-1000 mg daily. When used with other anticonvulsants, initiate at 250 mg once daily in addition to existing medications and adjust accordingly.

Reconstitution: Reconstitute with at least 5 ml of sterile water for inj to produce a solution containing ≤100 mg/ml. Further dilute with 5% dextrose solution or normal saline for IV infusion.
Incompatibility: Admixture incompatibility: Multivitamins.
Contraindications
 Hypersensitivity to sulphonamides; sodium or potassium depletion, hepatic insufficiency; hepatic cirrhosis; hyperchloraemic acidosis; severe renal impairment; severe pulmonary obstruction; chronic noncongestive angle-closure glaucoma; adrenocortical insufficiency. Pregnancy, lactation.
Warnings / Precautions
 Potassium supplements may be required. Impaired hepatic or renal function; diabetes. Monitor plasma electrolytes and blood count regularly. IM route is not recommended. Caution when driving or operating machinery. Elderly.
Adverse Reactions
 Drowsiness, paraesthesia, ataxia, dizziness, thirst, anorexia, headache; confusion, malaise, depression; GI distress, metabolic acidosis, polyuria, hyperuricaemia, renal calculi, nephrotoxicity, hepatic dysfunction.
Potentially Fatal: Rarely, skin reactions or blood dyscrasias.
Overdose Reactions
 Symptoms may include electrolyte imbalance, acidotic state and central nervous effects. Monitor serum electrolyte levels (particularly potassium) and blood pH levels. Supportive measures are required to restore electrolyte and pH balance. Acidotic state can usually be corrected by the admin of bicarbonate.
Drug Interactions
 Aids penetration of weakly acidic substances like sulphonamides across blood and CSF barrier. May inhibit renal excretion of basic drugs (e.g. quinidine, ephedrine, amphetamines) and promotes excretion of acidic drugs. May increase salicylate toxicity (acidosis). Hypokalaemia with corticosteroids and potassium-wasting diuretics. May increase excretion of lithium and primidone. May cause osteomalacia with anticonvulsants.
Potentially Fatal: May potentiate effect of folic acid antagonists, oral hypoglycaemic agents, oral anticoagulants and severe reactions to sulphonamides.
See Below for More acetazolamide Drug Interactions
Lab Interactions
 May cause false positive results for urinary protein. Interferes with HPLC theophylline assay and serum uric acid levels.
Mechanism of Actions
 Acetazolamide specifically inhibits the enzyme carbonic anhydrase which catalyses the reversible reaction involving the hydration of CO2 and dehydration of carbonic acid. It increases the excretion of HCO3 ions and as well as Na and K leading to alkaline diuresis. Carbonic anhydrase is also inhibited in the CNS to retard abnormal and excessive discharge from neurons.
Onset: 60-90 minutes (oral); 2 minutes (IV).
Duration: 8-12 hr (oral); 4-5 hr (IV).
Absorption: Moderately rapid absorption from the GI tract; peak plasma concentrations after 2 hr (oral).
Distribution: Concentrates in the red blood cells and renal cortex; enters the breast milk. Protein-binding: High.
Excretion: Urine (as unchanged drug); 3-6 hr (elimination half-life).
Administration
 Should be taken with food.
Storage Conditions
 Intravenous: Store between 15-30°C (59-86°F). Reconstituted solution may be stored at for 3 days at 2-8°C (36-46°C) or 12 hr at 15-30°C (59-86°F). Oral: Store at 15-30°C.
ATC Classification
 S01EC01 - acetazolamide ; Belongs to the class of carbonic anhydrase inhibitors. Used in the treatment of glaucoma.
Storage
 Intravenous: Store between 15-30°C (59-86°F). Reconstituted solution may be stored at for 3 days at 2-8°C (36-46°C) or 12 hr at 15-30°C (59-86°F). Oral: Store at 15-30°C.
Available As
  • Acetazolamide 250 mg

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