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The metabolism of serotonin (5-HT) in platelets is altered in several mental disorders and by various neurotransmitters. Since ethanol impairs the function of both nerves and platelets, the effect of ethanol on 5-HT metabolism was studied in normal platelets and in platelets from patients ingesting ethanol. Ingestion of ethanol by 3 subjects produced blood ethanol levels of 65–76 μM. Platelet MAO activity in each decreased by 50% and platelet serotonin levels increased 50–100%. Ethanol, incubated with normal platelets in vitro, competitively inhibited MAO activity. With phenylethylamine as substrate, the Km of MAO was 23 μM and the Ki of ethanol was 33 mM. With tyramine, Km and Ki were 94 μM and 571 mM, respectively.5-HT uptake by platelets increased 50–100% during ethanol ingestion over control values. By contrast in vitro addition of ethanol to normal platelets inhibited initial 5-HT uptake : Km and Ki were 0.0004 mM and 89.6 mM, respectively. The efflux of 5-HT from platelets was 3–5 times control values during ethanol ingestion and with addition of ethanol to normal platelets. Acetaldehyde at a concentration of 2 mM did not alter MAO activity or 5-HT uptake or efflux. The inhibitory effects of ethanol on MAO and 5-HT uptake were not altered by reserpine, aspirin, or tricyclic antidepressants. The results indicate that ethanol substantially alters 5-HT metabolism by human platelets. Inhibition by ethanol of MAO activity and 5-HT transport may contribute to ethanol-induced platelet and neuronal dysfunction.

Effects of Ethanol on Platelet Serotonin Metabolism