, sold under the trade name Diamox
, is a carbonic anhydrase
inhibitor that is used to treat glaucoma
, epileptic seizures
, benign intracranial hypertension
(pseudotumor cerebri), altitude sickness
, and dural ectasia
. Acetazolamide is available as a generic drug
and is also used as a diuretic
Mechanism of Action
This drug will block the formation of H+ and H2CO3 from CO2 and H2O. The end result is that bicarbonate
is excreted in the urine. Indirectly, it will block the Na/H exchanger
in the renal proximal tubule by decreasing the conversion of intracellular CO2 and H2O into bicarbonate and a hydrogen
ion that is needed for the Na/H exchanger to reabsorb sodium (and water) back from the tubule lumen. Therefore, there is a natriuretic/diuretic action in addition to the "washing away" of bicarbonate in the urine. The excess luminal water and sodium leads to an increased flow rate that can further disrupt other transporters in the tubule from functioning properly.
Acetazolamide is often used in the treatment of various diseases. For glaucoma sufferers, the drug decreases fluid formation in the eye
resulting in lower intraocular pressure. In epilepsy, its main use is in absence seizures
, with some benefit in other seizure syndromes. It is also used to decrease generation of cerebrospinal fluid
in benign intracranial hypertension
and has shown efficacy in autosomal dominant hyperkalemic periodic paralysis. It's been demonstrated in drug trials to relieve symptoms associated with dural ectasia in indivduals with Marfan Syndrome
. Off-label uses include Acetazolamide as a conjunction drug to merely assist patients with sleep apnea
by lowering blood pH and encourage respiration.
Acute mountain sickness
Acetazolamide is sometimes taken prophylactically
, anywhere between 125 milligrams (mg) to 500 mg per day, starting a few days before going to the higher altitude. Such use is recommended for those ascending from sea level to 3000 meters (9800 feet) in one day, or for those ascending more than 600 meters (2000 feet) per day once above an altitude of 2500 meters (8200 feet). Also, prophylactic use is recommended for those with a significant history of acute mountain sickness.
The drug forces the kidneys to excrete bicarbonate, the conjugate base of carbonic acid. By increasing the amount of bicarbonate excreted in the urine, the blood becomes more acidic. Acidifying the blood stimulates ventilation, which is beneficial during acclimatization.
Note that acetazolamide is not an immediate fix for acute mountain sickness; it speeds up acclimatization which in turn helps to relieve symptoms. This may take up to a day or two, and requires waiting without any further rapid ascent. It is often advisable to descend if even mild acute mountain sickness is experienced. If serious sickness is encountered, descent is considered mandatory unless other circumstances present greater danger.
Common side effects
of using this drug include numbness and tingling
in the fingers and toes, and taste
), especially for carbonated drinks; both are usually due to mild hypokalemia
levels). Some may also experience blurred vision
but this usually disappears shortly after stopping the medication. Acetazolamide also increases the risk of developing calcium oxalate and calcium phosphate kidney stones. Everyone will experience more frequent urination
as a result of using acetazolamide. One should drink more fluids than usual to prevent dehydration
. Acetazolamide prolongs the effects of amphetamines
and related drugs.
Acetazolamide should not be taken by individuals if:
- Ferrer S, Borras J, Martin-Gil J, Martín-Gil FJ.(1989). "Thermal studies on sulfonamide derivative complexes .1. Thermal-behavior of Acetazolamide – Copper complexes". Thermochim Acta, 147(2):321-330.