Acetazolamide has been used as an inhibitor of carbonic anhydrase for over 60 years. The drug has various applications and is used in today's medicine, especially in the context of a treatment of the green cat and various neurological diseases and as a preventive against altitude sickness.

What is acetazolamide?

Acetazolamide is a carbonic anhydrase inhibitor. It is used, for example, to achieve a preventive effect against altitude sickness in mountaineers.

Acetazolamide is a carbonic anhydrase inhibitor. It is mainly used in medicine to reduce the pressure inside the eye, to reduce water retention in the body and to achieve a preventive effect against altitude sickness in mountaineers.

As a rule, the drug is administered orally, injection solutions are the exception. The effect of acetazolamide based solely on an inhibition of the enzyme carbonic anhydrase. The two aforementioned direct effects of the substance are based on an increased excretion of sodium and potassium in the kidney and the reduction of the formation of aqueous humor.

Pharmacological action

Acetazolamide acts on the kidney, among other things, where a slightly increased water excretion can take place through the body's own urine. At the same time the urine production in the body is increased, whereby the water excretion is also favored.

In the inner eye acetazolamide reduces the pressure, which is why the drug is also used as part of glaucoma therapy. Positive in view of possible altitude sickness is the impact on the lungs, which are better aerated by acetazolamide. Cerebral edema, a side effect of altitude sickness, is also reduced by the administration of acetazolamide.

However, the drug loses its effect as soon as the patient has become accustomed to the external circumstances through acclimatization. After the administration of acetazolamide, the body absorbs the drug in the maximum dose of 250 milligrams usually within two hours. In the case of mothers, the drug also enters the breast milk, but without demonstrable, negative effects on breast milk or on the child.

Medical application & use

First and foremost, acetazolamide is used to treat chronic wide-angle glaucoma, which is also popularly known as the green star. By lowering the intraocular pressure, the course of the disease and the subsequent treatment are positively influenced.

Edema of any kind, including cerebral edema, may be alleviated but not completely cured. Anticonvulsant effects have also been demonstrated in patients with epilepsy without, however, being able to establish a reason for this effect of acetazolamide. Another application is inflammation in the area of ​​the pancreas and the fight against pancreatic fistulas.

Acetazolamide is an important element in the prevention of altitude sickness: up to 20% of inexperienced mountaineers suffer from altitude sickness from an altitude of 3, 000 meters; from 4, 000 meters on, this proportion rises to 80%. With adequate administration of acetazolamide, the risk of disease decreases by 45% to 55% (the exact value depends on the dosage).

Acetazolamide has a hitherto poorly understood but proven effect on migraineurs whose cause of disease is mutated calcium channels. However, the drug is not (yet) used in active migraine therapy.

Risks & Side Effects

Undesirable effects of acetazolamide in relative frequency mainly affect fatigue and dizziness or sudden headache. If administered as a prevention of altitude sickness, taste disorders, nausea and even diarrhea are among the more common side effects.

Anorexia, vomiting or a permanent feeling of heat may also be the result of the administration of acetazolamide. Furthermore, acetazolamide should under no circumstances be used during pregnancy as it could lead to malformations of the unborn child.

An overdose does not seem to have any strong negative effects, but in this context only animal experiments are available as a reference point. The potential for interaction with other drugs has so far been little researched, but the use of drugs containing sulfonamides has been shown to cause skin reactions and changes in the blood count. Basic care should be taken when conditions of acidosis are present. Tags: 

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