Acetazolamide, USP is a white to faintly yellowish white, crystalline odorless powder, sparingly soluble in practically boiling water, slightly soluble in alcohol, very slightly soluble in water. Acetazolamide is not metabolized and 90% of the administered dose is excreted unchanged in the urine within the first 24 h. This process involves both active tubular secretion and passive reabsorption. The acetazolamide treated climbers also had less difficulty in sleeping.Acetazolamide therapy is contraindicated in situations in which sodium and/or potassium blood serum levels are depressed, in cases of marked kidney and liver disease or dysfunction, in suprarenal gland failure, and in hyperchloremic acidosis. The diuretic effect of acetazolamide is due to its action in the kidney on the reversible reaction involving hydration of carbon dioxide and dehydration of carbonic acid. In the eye, this inhibitory action of acetazolamide decreases the secretion of aqueous humor and results in a drop in intraocular pressure, a reaction considered desirable in cases of glaucoma and even in certain non-glaucomatous conditions.
Particular caution is recommended in patients with conditions that are associated with, or predispose a patient to, electrolyte and acid/base imbalances, such as patients with impaired renal function (including elderly patients; Some adverse reactions to acetazolamide, such as drowsiness, fatigue, and myopia, may impair the ability to drive and operate machinery.Acetazolamide modifies phenytoin metabolism with increased serum levels of phenytoin.
Inhibition of carbonic anhydrase in this area appears to retard abnormal, paroxysmal, excessive discharge from central nervous system neurons. If rapid ascent is undertaken and acetazolamide is used, it should be noted that such use does not obviate the need for prompt descent if severe forms of high altitude sickness occur, i.e., high altitude pulmonary edema (HAPE) or high altitude cerebral edema.Caution is advised for patients receiving concomitant high-dose aspirin and acetazolamide, as anorexia, tachypnea, lethargy, metabolic acidosis, coma, and death have been reported (Both increases and decreases in blood glucose have been described in patients treated with acetazolamide.
Very slightly soluble in water; slightly soluble in ethanol (~750 g/l) TS; practically insoluble in ether R. Category.
Gradual ascent is desirable to try to avoid acute mountain sickness. Its elimination half‐life is about 4–8 h.Ellis et al. and you may need to create a new Wiley Online Library account.Enter your email address below and we will send you your usernameIf the address matches an existing account you will receive an email with instructions to retrieve your username
It is also used in the treatment of various forms of epilepsy, to prevent or ameliorate the symptoms of acute high altitude sickness and in the promotion of diuresis in instances of abnormal fluid retention, for example, cardiac edema.Acetazolamide shows dose related side effects, the most common of which are diuresis, gastrointestinal (GI) symptoms including cramping, epigastric burning, nausea, and diarrhea and metabolic acidosis.Acetazolamide is very slightly soluble in water; sparingly soluble in boiling water.The WHO recommended dosage form strength is 250 mg.Acetazolamide has been reported to be rapidly and almost completely absorbed from the GI tract (∼100%),Acetazolamide is 70–90% protein‐bound.