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Inhibition of Platelet Monoamine Oxidase Type B by Selegiline
Author(s) -
Hein Esa H.,
Anttila Markku I.,
Nyman Leena M.,
Pyykkö Kaija A.,
Vuorinen Jouni A.,
Lammintausta Risto A. S.
Publication year - 1997
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1997.tb04341.x
Subject(s) - selegiline , pharmacology , monoamine oxidase b , bioavailability , monoamine oxidase , monoamine oxidase inhibitor , oral administration , medicine , crossover study , chemistry , enzyme , parkinson's disease , biochemistry , alternative medicine , disease , pathology , placebo
Selegiline is an irreversible inhibitor of monoamine oxidase type B (MAO‐B). No comparative data are available on the MAO‐B inhibition caused by orally and intravenously administered selegiline. This study aimed to clarify this matter and to investigate the dose—response of MAO inhibition caused by orally administered selegiline. Sixteen healthy volunteers were given selegiline as a single intravenous dose (0.5 mg) and in three low oral doses (0.5 mg, 1.0 mg, and 1.5 mg) in an open‐label randomized crossover trial. The MAO‐B inhibition after the 0.5‐mg intravenous dose was 79.6 ± 15.1%. The dose—response of the three oral doses causing MAO‐B inhibition was logistic. To check whether this equation could be applied to higher doses, eight of the volunteers were given 5‐mg and 10‐mg oral doses. The MAO‐B inhibition after these doses (84.9 ± 11.9% and 95.6 ± 4.5%, respectively) fitted well with the logistic model. With this equation obtained, it was calculated that a 3.4‐mg oral dose of selegiline would be needed to obtain the same degree of MAO‐B inhibition as after the intravenous dose of 0.5 mg. Therefore, the ratio of MAO‐B inhibitory potential of intravenously and orally given selegiline is approximately 7 to 1, which fits well with the low bioavailability of the drug after oral administration.