Summary
It has been previously demonstrated that gabapentin, a gamma-amino butyric acid analogue, inhibits monoaminergic neurotransmitter release from rabbit caudate nucleus slices and from rat cortex. In humans this drug has been shown to have anti-epileptogenic activity. Serotonin may act as an inhibitory neurotransmitter and its interaction with blood platelets is thought to reflect its central actions. We investigated sleep stages, whole blood serotonin levels, and serum melatonin in healthy men after the administration of gabapentin. With increasing serum gabapentin levels six healthy subjects showed an increase in sleep stages 3 and 4 and in whole blood serotonin (P<0.05). Serum melatonin levels were not influenced.
On account of these results we speculate that gabapentin modulates the release of serotonin from blood platelets. The increase in peripheral serotonin points paradigmatically to an increase in the bioavailability of serotonin which may account for the increase in sleep stages 3 and 4.
Article PDF
Similar content being viewed by others
Avoid common mistakes on your manuscript.
References
Andersen MG, Young FG, Cohen DJ, Schlicht KR, Patel N (1981) Liquid-chromatographic determination of serotonin and tryptophan in whole blood and plasma. Clin Chem 27: 775–776
Bartoszyk GD (1978) Gabapentin and convulsions provoked by excitatory amino acids. Naunyn Schmiedebergs Arch Pharmacol 324: R24
Birkeland AJ (1982) Plasma melatonin levels and nocturnal transitions between sleep and wakefulness. Neuroendocrinology 34: 126–130
Brown GM, Grota LJ, Pulido O, Burns TG, Niles LP, Snieckus V (1983) Application of immunologic techniques to the study of pineal indolalkylamines. In: Reiter R (ed) Pineal research reviews. A Liss, New York, pp 207–246
Carlsson A (1976) The contribution of drug research to investigating the nature of endogenous depression. Pharmacopsychiatry 9: 2–10
Clarenbach P, Birmanns B, Jaursch-Hancke C (1986a) The effect of ritanserin on sleep and hormones in man. In: Koella W, Obal F, Schulz H, Visser P (eds) Sleep research. Karger, Basel, in press
Clarenbach P, Krätzschmar S, Rao ML (1986b) Effects of a GABA-analogue on sleep, serotonin and hormones in man. Proc 8th Eur Congr Sleep Res, Szeged, Hungary, Sept 1–5, Abstract No 64
Caudill WL, Houck GP, Wightman RM (1982) Determination of gamma-aminobutyric acid by liquid chromatography with electrochemical detection. J Chromatogr 227: 331–336
Cramer H, Rudolph J, Consbruch U, Kendel K (1974) On the effects of melatonin on sleep and behaviour in man. Adv Biochem Psychopharmacol 11: 187–191
Geeraerts F, Schimpfessel L, Crokaert R (1974) A simple routine method to preserve and determine blood serotonin. Experientia 30: 837–838
Hengy H, Kölle EU (1985) Determination of gabapentin in plasma and urine by highperformance liquid chromatography and pre-column labelling for ultraviolet detection. J Chromatogr 341: 473–478
Jouvet M (1969) Biogenic amines and the states of sleep. Science 163: 32–41
Rao ML, Fels K (1987) Beeinflussen Tryptophan und Serotonin beim Menschen die Melatonin-Ausschüttung und damit die Funktion des “Regulators der Regulatoren” (Zirbeldrüse); In: Kielholz P, Müller-Oerlinghausen B (eds) Advances in pharmacotherapy, vol 3. Karger, Basel, pp 87–99
Rao ML, Mager T (1987) Influence of the pineal gland on pituitary function in humans. Basal serum values of pituitary hormones and catecholamines in relation to melatonin. Psychoneuroendocrinology 12: 141–147
Rechtschaffen A, Kales A (1968) A manual of standardized terminology, techniques, and scoring system for sleep stages of human subjects. NIH Publication 204, US Government Printing Office, Washington DC
Reimann W (1983) Inhibition by GABA, baclofen and gabapentin of dopamine release from rabbit caudate nucleus: are there common or different sites of action? Eur J Pharmacol 94: 341–344
Schlicker E, Reimann W, Göthert M (1985) Gabapentin decreases monoamine release without affecting acetylcholine release in the brain. Drug Res 35: 1347–1349
Sizonenko PC, Moore DC, Paunier L, Baumanoir A, Nahory A (1979) Melatonin secretion in relation to sleep in epileptics. Prog Brain Res 25: 549–551
Sneddon JM (1973) Blood platelets as a model for monoamine-containing neurons. Prog Neurobiol 1: 153–198
van Praag HM (1977) Significance of biochemical parameters in the diagnosis, treatments, and prevention of depressive disorders. Biol Psychiatry 12: 101–131
Author information
Authors and Affiliations
Additional information
This work is part of the dissertation of M. V. submitted to the Faculty of Medicine of the University of Bonn, Federal Republic of Germany.
Rights and permissions
About this article
Cite this article
Rao, M.L., Clarenbach, P., Vahlensieck, M. et al. Gabapentin augments whole blood serotonin in healthy young men. J. Neural Transmission 73, 129–134 (1988). https://doi.org/10.1007/BF01243384
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF01243384