Tyramine pressor sensitivity during treatment with the selegiline transdermal system 6 mg/24 h in healthy subjects.
The oral tyramine pressor test was administered to healthy males during treatment with a selegiline transdermal system (STS; 6 mg/24 h). The tyramine sensitivity factor (TSF) was calculated from the ratio of baseline and on-treatment tyramine pressor doses. The tyramine sensitivity factor value following 9 days of treatment with the selegiline transdermal system was 1.85 +/- 0.10. Extended treatment, 33 days, produced a small, clinically non-meaningful increase in this value. The tyramine sensitivity factor for the selegiline transdermal system was similar to that following treatment with 10 mg/d of oral selegiline capsules but more than 20 times less than observed during tranylcypromine treatment. A larger increase in the tyramine sensitivity factor was observed following extended selegiline transdermal system treatment at a higher dose (12 mg/24 h), which was significantly decreased following coadministration of tyramine capsules with a meal. These results suggest a wide tyramine safety margin for the selegiline transdermal system and provide evidence that the 6-mg/24-h selegiline transdermal system can be administered safely without dietary tyramine restrictions.
Azzaro
Albert J
AJ
Somerset Pharmaceuticals, Inc, Tampa, Florida, USA.
Vandenberg
Chad M
CM
Blob
Lawrence F
LF
Kemper
Eva M
EM
Sharoky
Melvin
M
Oren
Dan A
DA
Campbell
Bryan J
BJ
D000279:Administration, Cutaneous; D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D001794:Blood Pressure / Q000187:drug effects*; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D018565:Food-Drug Interactions; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D006973:Hypertension / Q000139:chemically induced* / Q000503:physiopathology; D008297:Male; D008875:Middle Aged; D008996:Monoamine Oxidase Inhibitors / Q000008:administration & dosage / Q000009:adverse effects*; D012016:Reference Values; D012642:Selegiline / Q000008:administration & dosage / Q000009:adverse effects*; D013997:Time Factors; D014191:Tranylcypromine / Q000008:administration & dosage / Q000009:adverse effects; D014439:Tyramine / Q000008:administration & dosage / Q000009:adverse effects*
D008996:Monoamine Oxidase Inhibitors; D012642:Selegiline; D014191:Tranylcypromine; D014439:Tyramine