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Catechol-O-methyltransferase (COMT) is an ubiquituous enzyme which in animals and in man takes part in the metabolism of biologically active or toxic catechols including catechol-structured drugs.The effects of endogenous catecholamines and catechol-structured drugs can be potentiated if the function of COMT is inhibited. This is likely to lead also to haemodynamic effects and changes in catecholamine metabolism.The first COMT inhibitors were toxic, unspecific and short-acting. Therefore the effects of COMT inhibition in man were widely unexplored in man before the intoduction of the second generation COMT inhibitors.The second generation COMT inhibitors entacapone and tolcapone have now established their role as effective agents in the treatment of Parkinson''s disease. This book summarizes a series of studies investitigating the effects of COMT inhibition on haemodynamics, catecholamine metabolism, including some interaction studies with drugs interfering with catecholamine disposition.This book gives also a short review of the literature on this topic and should be useful for professionals and students having interest in the COMT inhibition and COMT inhibitors.