1] Division of Clinical Pharmacology and Experimental Therapeutics, Medical Service, San Francisco General Hospital Medical Center, University of California, San Francisco, San Francisco, California, USA [2] Department of Pediatrics, San Francisco General Hospital Medical Center, University of California San Francisco, San Francisco, California, USA.
Clin Pharmacol Ther. 2013 Dec;94(6):687-94. doi: 10.1038/clpt.2013.159. Epub 2013 Aug 9.
The aim of the study was to examine genetic, pharmacokinetic, and demographic factors that influence sensitivity to nicotine in never-smokers. Sixty never-smokers, balanced for gender and race (white, black, and Asian), wore 7-mg nicotine skin patches for up to 8 h. Serial plasma nicotine concentrations and subjective and cardiovascular effects were measured, and genetic variation in the CYP2A6 gene, encoding the primary enzyme responsible for nicotine metabolism, was assessed. Nicotine toxicity requiring patch removal developed in nine subjects and was strongly associated with rate of increase and peak concentrations of plasma nicotine. Toxicity and subjective and cardiovascular effects of nicotine were associated with the presence of reduced-function CYP2A6 alleles, presumably reflecting slow nicotine metabolic inactivation. This study has implications for understanding individual differences in responses to nicotine medications, particularly when they are used for treating medical conditions in nonsmokers, and possibly in vulnerability to developing nicotine dependence.
本研究旨在探讨影响从不吸烟者对尼古丁敏感性的遗传、药代动力学和人口统计学因素。60 名从不吸烟者(按性别和种族平衡,包括白种人、黑种人和亚洲人)佩戴 7 毫克尼古丁贴片长达 8 小时。连续测量血清尼古丁浓度以及主观和心血管效应,并评估 CYP2A6 基因(编码主要负责尼古丁代谢的酶)的遗传变异。9 名受试者出现需要去除贴片的尼古丁毒性,这与血清尼古丁浓度的增加速度和峰值密切相关。尼古丁毒性以及主观和心血管效应与 CYP2A6 等位基因的功能降低有关,可能反映了尼古丁代谢失活的缓慢。本研究对于理解尼古丁药物反应的个体差异具有重要意义,特别是当它们用于治疗非吸烟者的医疗状况时,并且可能与尼古丁依赖易感性有关。