OBJECTIVE: To summarize the pharmacology, pharmacokinetics, efficacy,
and safety of acetazolamide and to evaluate its therapeutic role in pa
tients with epilepsy. DATA SOURCES: A computerized search of the MEDLI
NE (OVID) datal,ase (1966-1994) was used to identify publications rega
rding acetazolamide. The MEDLINE search was supplemented by informatio
n from textbooks. STUDY SELECTION: Included were English-language;revi
ew articles, clinical trials, cohort studies, and case reports. Topics
investigated included basic pharmacology, therapeutics, toxicology, a
dverse reactions, dosage, administration, and pharmacokinetics of acet
azolamide. DATA SYNTHESIS: Acetazolamide, a carbonic anhydrase inhibit
or, has been approved for the treatment of epilepsy since 1953. Acetaz
olamide is primarily used in combination therapy with other antiepilep
tic medications in both children and adults although it may be used as
monotherapy. Drug concentration monitoring has not been found to be r
outinely beneficial. Adverse effects include kidney stones, metabolic
acidosis, lethargy, appetite suppression, paresthesias, and rare blood
dyscrasias. Partial tolerance may develop to the antiepileptic activi
ty. CONCLUSIONS: Acetazolamide is a beneficial adjunctive agent in the
pharmacotherapy of epilepsy and should be considered in refractory ep
ilepsy. Although it may be useful in partial, myoclonic, absence, and
primary generalized tonic-clonic seizures uncontrolled by other market
ed agents, acetazolamide has been inadequately studied by current stan
dards and its use has been limited.