Review of the animal pharmacology and pharmacokinetics of fluvoxamine.

Abstract

1 Fluvoxamine maleate is a compound from the series of 2‐ aminoethyloximethers of aralkylketones which possesses marked inhibition effects on 5‐hydroxytryptamine (5‐HT) uptake by blood platelets and brain synaptosomes. In contrast, it has no effect on noradrenaline uptake processes. 2 Fluvoxamine is completely absorbed in rats and dogs; the main metabolic path was similar in rat, dog, hamster, mouse and rabbit. The metabolites of fluvoxamine are inactive with regard to aminergic uptake processes. 3 Fluvoxamine is neither sedative nor stimulating, shows a very low cardiotoxic effect and no affinity for the cholinergic receptor. On the basis of the pharmacological profile, a highly favourable therapeutic ratio of antidepressant effects vs disturbing side‐effects is predicted.