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.