Premium
Tyramine Pharmacokinetics and Reduced Bioavailability with Food
Author(s) -
VanDenBerg Chad M.,
Blob Lawrence F.,
Kemper Eva M.,
Azzaro Albert J.
Publication year - 2003
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 - 10.1177/0091270003253425
Subject(s) - tyramine , bioavailability , meal , pharmacokinetics , pharmacology , oral administration , chemistry , medicine , endocrinology , food science
Tyramine challenge studies have demonstrated that it requires approximately twice the amount of tyramine administered with a meal compared to administration after a fast to elicit the same effect, suggesting a reduction in bioavailability of tyramine when administered with food. The pharmacokinetics of tyramine when administered in a fasted versus a fed state were studied. A single 200‐mg dose of tyramine was administered orally to healthy subjects both after an overnight fast and during a meal. Systemic exposure to tyramine was reduced by 53% ( p < 0.05), and the maximum concentration of tyramine was reduced by 72% ( p < 0.05) when the dose was administered during a meal. Tyramine maximum serum concentration was observed between 20 minutes and 1 hour when the dose was administered after an overnight fast and appeared to be delayed and/or prolonged by administration during a meal. Tyramine oral clearance was 135 ± 55.4 L/min, maximum observed serum concentration was 37.7 ± 26.01 ng/mL, and tyramine elimination half‐life was 0.533 (range: 0.330–0.668) hours after administration to fasted subjects. Tyramine bioavailability was significantly reduced when administered with a meal compared to after a fast. The results suggest that larger amounts of dietary tyramine will be required to induce a pressor response equivalent to that following encapsulated tyramine administered in the fasted state.