Carbonic anhydrase
inhibitors
Carbonic anhydrase inhibitors are diuretics
that block the action of carbonic anhydrase. They include acetazolamide and
methazo-lamide.
Carbonic anhydrase inhibitors are absorbed through
the GI tract. Some systemic absorption also occurs after oph-thalmic
administration. They’re distributed in tissues with high carbonic anhydrase
content, such as erythrocytes, plas-ma, kidneys, eyes, liver, and muscle.
Carbonic anhydrase in-hibitors are excreted by the kidneys in urine.
In the kidneys, carbonic anhydrase inhibitors
decrease the availability of hydrogen ions, which blocks the sodium-hydrogen
exchange mechanisms. As a result, urinary excre-tion of sodium, potassium,
bicarbonate, and water increases.
In the eyes, carbonic anhydrase inhibition reduces
aqueous humor production, which reduces intraocular pressure.
Carbonic anhydrase inhibitors are used for diuresis
and to treat glaucoma. Acetazolamide may also be used to treat epilepsy and
acute mountain sickness.
Carbonic anhydrase inhibitors produce a variety of
drug interac-tions:
§ Salicylates may cause carbonic anhydrase
inhibitor toxicity, in-cluding central nervous system depression and metabolic
acido-sis.
§ Diflunisal may increase intraocular pressure
when given with a carbonic anhydrase inhibitor.
§ Acetazolamide used concurrently with
cyclosporine may in-crease cyclosporine levels and the risk of neurotoxicity.
§ Acetazolamide used concurrently with
primidone may decrease serum and urine levels of primidone. (See Adverse reactions tocarbonic anhydrase
inhibitors.)
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