IOn the basis of both in vitro and in vivo experiments fluvoxamine has been characterized as a potential anti-depressant drug with almost exclusively 5-hydroxytryptamine (5-HT) uptake inhibiting properties. 2 Fluvoxamine is effective in inhibiting 5-HT uptake by blood platelets and brain synaptosomes. Due to inhibition of the membrane pump the compound prevents 5-HT depletion by the tyraminederivatives H 75/12 and H 77/77. As a result of the interference with the neuronal re-uptake mechanism for 5-HT, fluvoxamine produces a decreased 5-HT turnover in the brain. Effects of 5-hydroxytryptophan (5-HTP) are potentiated in mice and in combination with pargyline, fluvoxamine induces 5-HT-like behavioural effects. 3 In contrast to tricyclic antidepressants, noradrenaline uptake processes are either unaffected or only slightly inhibited by fluvoxamine. The noradrenaline depleting effects of tyramine derivatives are not influenced by fluvoxamine. Reserpine effects, such as ptosis are affected only at very high doses of the test compound. The antagonism by fluvoxamine of the reserpine-induced lowering of the pentamethylenetetrazole convulsive threshold can be regarded as due to an effect upon 5-HT uptake. In contrast to the effects of desmethylimipramine and imipramine, no stimulatory effects are found in rats when rapidly acting reserpine-like compounds are given following a dose of fluvoxamine.

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.

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