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1 Department of Pharmacology and the Division of Neurology of the Department of Medicine, The University of Chicago, Chicago 37, Illinois
Combined radioassay and autoradiographic techniques have shown that acetazolamide enters selected areas of the brain in significant quantities. The drug occurs in brain, cerebrospinal fluid and plasma as unchanged acetazolamide.
Two portals of entry of acetazolamide into the brain are utilized. The early pattern is one of diffusion from the cerebrospinal fluid with those tissues having easy access to the cerebrospinal fluid showing the highest drug content. This early diffusional pattern from the cerebrospinal fluid becomes less distinct in time. The second route of entry is blood-to-brain transport.
The distribution of acetazolamide is not well correlated with the known pattern of vascularity in the brain. It is suggested that the early acetazoamide picture may represent in part a distribution in the interstitial fluid compartment. To this end experiments using the sulfate-S35 ion have been designed to measure the extracellular space.
Hippocampus, hypothalamus and caudate nucleus are areas of high acetazolamide uptake and show a discrete retention over contiguous areas. Whether or not this retention is a function of local chemical binding of the drug is a matter of speculation.
Submitted on August 11, 1958
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