Summary
The disposition of fluvoxamine maleate, a serotonin uptake inhibitor with antidepressant properties, was investigated in healthy volunteers.
Five healthy men each ingested 5 mg of thel4C-labelled drug, and excretion of radioactive substances in the urine was measured over 72 hours.
Ten other healthy volunteers each received orally 100 mg of the non-radioactive drug and their plasma fluvoxamine level was measured over 24 hours.
On average 94 % (range: 87–105 %) of an oral dose was excreted in the urine. The excretion rate was biphasic with half-lives of 2.1 hours (1.7 – 3.2 hours) and 14.5 hours (13 – 16 hours).
The fluvoxamine plasma levels reached their maximum between 2 and 8 hours after administration, the peak levels ranging from 31 to 87 ng/ml after 100 mg dose. The plasma level decreased according to first-order kinetics with a half-life of 14.9 hours (range: 12.7 \2- 19.0 hours).
It is concluded that orally administered fluvoxamine is completely absorbed.
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De Bree, H., Van Der Schoot, J.B. & Post, L.C. Fluvoxamine maleate; Disposition in man. European Journal of Drug Metabolism and Pharmacokinetics 8, 175–179 (1983). https://doi.org/10.1007/BF03188743
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DOI: https://doi.org/10.1007/BF03188743