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Acetazolamide

Acetazolamide, it is an carbonic anhydrase inhibitor. More

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Description

Acetazolamide, it is an carbonic anhydrase inhibitor.

Generic Name

Acetazolamide

Chemical names

Acetazolamide, Diamox, Diacarb, Glaupax, Acetazolamid

Brand names

Abzole, Avva, Acetamide, Acetariv, Acetamin, Diamox, Iopar-S, Synomax, Zolamide

IUPAC name

N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide

Pharmacokinetics

  • Absorption: Moderately rapid absorption from the GI tract; peak plasma concentrations after 2 hours (oral).
  • Distribution: Concentrates in the renal cortex and red blood cells
  • Excretion: Urine

Actions

Acetazolamide is a potent carbonic anhydrase inhibitor, effective in the control of fluid secretion, in the treatment of certain convulsive disorders and in the promotion of diuresis in instances of abnormal fluid retention. Acetazolamide is not a mercurial diuretic. Rather, it is a nonbacteriostatic sulfonamide possessing a chemical structure and pharmacological activity distinctly different from the bacteriostatic sulfonamides.

Dosage/Dosage form

The dose ranges from 250 mg to 1 g for 24 hours, usually in divided doses.

  • Dieresis: 250-375 mg/day
  • Epilepsy: 250-1000 mg/day
  • Glaucoma: 250-1000 mg/day

Therapeutic uses

Acetazolamide used as a diuretic, for epileptic seizures, glaucoma, benign intracranial hypertension (pseudotumor cerebri), altitude sickness, cystinuria, and dural ectasia. 

Adverse effects/Side effects

Drowsiness, ataxia, paraesthesia, anorexia, confusion, dizziness, thirst, depression, headache; malaise, GI distress, metabolic acidosis, polyuria, hyperuricaemia, renal calculi, nephrotoxicity, hepatic dysfunction.

Interaction

  • The risk or severity of adverse effects can be increased when Acebutolol is combined with acetazolamide
  • The risk or severity of adverse effects can be increased when Aldesleukin is combined with acetazolamide
  • The risk or severity of adverse effects can be increased when Alfentanil is combined with acetazolamide
  • May cause osteomalacia with anticonvulsants.

Contraindications

Pregnancy and lactation. Hypersensitivity to sulphonamides, hepatic cirrhosis, potassium or sodium depletion, hepatic insufficiency, severe renal impairment, hyperchloraemic acidosis, severe pulmonary obstruction, adrenocortical insufficiency, chronic noncongestive angle-closure glaucoma.

Storage

  • Store at 15-30°C.

Information

Molecular weight

222.245

Molecular formula

C4H6N4O3S2

CAS number

59-66-5

Precautions

  • IM route is not recommended.
  • Caution when driving or operating machinery.