Clinical Pharmacology Tyramine Challenge Study to Determine the Selectivity of the Monoamine Oxidase Type B (MAO-B) Inhibitor Rasagiline
Tamar Goren 1*, Liat Adar 1, Nissim Sasson 1, and Yoni M. Weiss 1
1 Teva Pharmaceutical Industries Ltd



* To whom correspondence should be addressed. E-mail: tamar.goren@teva.com.il.


Abstract
Rasagiline is a selective, monoamine oxidase (MAO)-B inhibitor indicated for treatment of Parkinson’s disease. This double-blind, placebo-controlled study determined the tyramine sensitivity factor (TSF) and degree of MAO-A inhibition (ie, reduction in plasma dihydroxyphenylglycol) in healthy volunteers who received phenelzine (15 mg, 3 times daily; positive control), selegiline (5 mg, twice daily), or rasagiline (1-6 mg, once daily) for 14 days or rasagiline 2 mg/d for 30 days... Plasma dihydroxyphenylglycol concentrations suggested that rasagiline 1 mg/d had no effect, whereas rasagiline 2 mg/d had only minimal effect. In contrast, rasagiline 4 and 6 mg/d reduced dihydroxyphenylglycol to a degree approaching that achieved by the positive control phenelzine. Results demonstrate that rasagiline selectively inhibits MAO-B and is not associated with increased tyramine sensitivity at the indicated dose (1 mg/d). These data allowed removal of dietary tyramine restriction from rasagiline US labeling.

http://jcp.sagepub.com/cgi/content/a...270010369674v1