J Clin Pharmacol
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PHARMACOKINETICS AND PHARMACODYNAMICS

Tyramine Pharmacokinetics and Reduced Bioavailability with Food

Chad M. VanDenBerg, PharmD, Lawrence F. Blob, MD, Eva M. Kemper and Albert J. Azzaro, PhD

From Somerset Pharmaceuticals, Inc., Tampa, Florida (Dr. VanDenBerg, Ms. Kemper, Dr. Azzaro) and Potomac Clinical Trials, Jessup, Maryland (Dr. Blob).

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.


Key Words: Tyraminepharmacokineticsbioavailability

Address for reprints: Chad VanDenBerg, PharmD, 2202 N. West Shore Blvd. Ste. #450, Tampa, FL 33607.


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A. J. Azzaro, C. M. VanDenBerg, L. F. Blob, E. M. Kemper, M. Sharoky, D. A. Oren, and B. J. Campbell
Tyramine Pressor Sensitivity During Treatment With the Selegiline Transdermal System 6 mg/24 h in Healthy Subjects.
J. Clin. Pharmacol., August 1, 2006; 46(8): 933 - 944.
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