Early human studies of a new carbonic anhydrase inhibitor (NSD 3004) with anticonvulsant properties

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Abstract
NSD 3004 is a nondiuretic carbonic anhydrase inhibitor which has shown anticonvulsant properties in animal experiments. The studies reported here with volunteers and patients confirmed the strong binding to carbonic anhydrase in human erythrocytes and an extremely long half‐life in these. The half‐life in plasma from 8 volunteers was 28 ± 4 hours (mean ± standard deviation) and the steady‐state concentration in plasma was 5.7 ± 1.3 µg per milliliter (mean ± standard deviation) on 200 mg. daily. About 10 per cent of the dose was excreted unchanged in the urine and about 20 per cent ay a conjugate. Low values of PCO2 and standard bicarbonate in arterial blood and of total CO2 in venous blood were seen during a two week medication. No other deviations were found in the clinical parameters. Electroencephalography including automatic period analysis revealed no changes related to NSD 3004 medication. Expected effects such as light paresthesias and slight dyspnea on exertion were observed in some volunteers and patients. NSD 3004 seemed to exhibit antiepileptic properties in human subjects; an extensive clinical evaluation is needed.

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