Azzaro Albert J, Vandenberg Chad M, Blob Lawrence F, Kemper Eva M, Sharoky Melvin, Oren Dan A, Campbell Bryan J
Somerset Pharmaceuticals, Inc, Tampa, Florida, USA.
J Clin Pharmacol. 2006 Aug;46(8):933-44. doi: 10.1177/0091270006289852.
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.
在使用司来吉兰透皮系统（STS；6毫克/24小时）治疗期间，对健康男性进行了口服酪胺升压试验。酪胺敏感性因子（TSF）由基线和治疗期间酪胺升压剂量的比值计算得出。使用司来吉兰透皮系统治疗9天后的酪胺敏感性因子值为1.85±0.10。延长治疗至33天，该值有小幅增加，但在临床上无意义。司来吉兰透皮系统的酪胺敏感性因子与口服司来吉兰胶囊10毫克/天治疗后的相似，但比反苯环丙胺治疗期间观察到的低20多倍。在更高剂量（12毫克/24小时）下延长司来吉兰透皮系统治疗后，酪胺敏感性因子有更大增加，在酪胺胶囊与食物同时服用后显著降低。这些结果表明司来吉兰透皮系统有较宽的酪胺安全范围，并提供了证据表明6毫克/24小时的司来吉兰透皮系统可在无饮食酪胺限制的情况下安全给药。
