The effect of hair color on the incorporation of codeine into human hair
The effect of hair color on the incorporation of codeine into human hair
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DOI：
10.1093/jat/27.8.545
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发表时间：
2003-11-01
影响因子：
2.5
通讯作者：
Slawson, MH
中科院分区：
文献类型：
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作者：
Rollins, DE;Wilkins, DG;Slawson, MH
黑色素对毛发中外源性物质结合的影响将影响毛发检测确定的药物浓度的解释。本研究的目的是确定可待因作为滥用药物的模型化合物是否会随着黑色素浓度的变化而掺入黑色、棕色、金色或红色头发中。这些数据将有助于解释头发中的可待因浓度，并有助于阐明头发颜色对药物掺入的潜在影响。年龄在21-40岁的男性和女性黑人（n= 6）、棕色（n= 12）、金发（n= 8）或红发（n= 6）白人和非白人黑发（n= 12）白人入组本研究。每名受试者口服磷酸可待因糖浆，剂量为30 mg，每日3次，持续5天。治疗期结束后24小时，给予30 mg可待因剂量，测定受试者的可待因浓度-时间曲线下面积（AUC）。在给药前和给药后1、4、5、6和7周，测量最靠近头皮顶点区域的前3 cm毛发中的可待因和黑色素。确定每个受试者头发的定量和定性黑色素谱，以提供头发颜色的客观测量。测量可待因的血浆浓度，以消除可待因的生物利用度和清除率差异，这些差异可能是导致可待因毛发浓度差异的因素。受试者被要求不要在头皮的顶部区域剪发或对头发使用任何形式的化学处理，但允许采取其他正常的卫生措施。给药后5周的平均（± SE）毛发可待因浓度为：黑发1429（± 249）pg/mg;棕发208（± 17）pg/mg;金发99（± 10）pg/mg;红发69（± 11）pg/mg。在黑发中，亚洲人的可待因浓度为2564（± 170）pg/mg，白人为865（± 162）pg/mg。在第4、6和7周观察到相似的浓度关系。观察到可待因和黑色素的毛发浓度之间的强相关性（R2= 0.73）。可待因浓度与黑色素浓度的归一化减少了观察到的毛发颜色差异。这些数据表明，可待因毛发检测结果的解释和报告受到毛发颜色的影响。在该给药方案后，拟定的联邦指南临界值200 pg/mg可待因将导致100%的黑发受试者和50%的棕发受试者报告为阳性，金发或红发受试者报告为阴性。应在人体中仔细研究这些药物与毛发的结合，以确保对药物浓度的适当解释。
The influence of melanin on the binding of xenobiotics in hair will impact the interpretation of drug concentrations determined by hair testing. The purpose of this study was to determine if codeine, as a model compound of abused drugs, would be incorporated into black, brown, blond, or red hair as a function of melanin concentration. Such data would assist in the interpretation of codeine concentrations in hair and help elucidate the potential influence of hair color on incorporation of drugs. Male and female Caucasians with black (n= 6), brown (n= 12), blond (n= 8), or red hair (n= 6) and non-Caucasians with black hair (n= 12) aged 21–40 years were enrolled in the study. Each subject was administered oral codeine phosphate syrup in a dosage of 30 mg three times a day for five days. Twenty-four hours after the end of the treatment period, a 30-mg codeine dose was administered and the subject's plasma area under the concentration time curve (AUC) for codeine was determined. Codeine and melanin were measured in the first 3 cm of hair closest to the vertex region of the scalp prior to and 1, 4, 5, 6, and 7 weeks after dosing. The quantitative and qualitative melanin profiles were determined for each subjects hair to provide an objective measure of hair color. The plasma concentrations of codeine were measured to eliminate differences in the bioavailability and clearance of codeine as factors that might account for the differences in codeine hair concentrations. The subjects were asked not to cut their hair in the vertex region of the scalp or to use any form of chemical treatment on their hair, but otherwise normal hygienic measures were permitted. The mean (± SE) hair codeine concentrations 5 weeks after dosing were 1429 (± 249) pg/mg in black hair; 208 (± 17) pg/mg in brown hair; 99 (± 10) pg/mg in blond hair; and 69 (± 11) in red hair pg/mg. In black hair, codeine concentrations were 2564 (± 170) pg/mg for Asians and 865 (± 162) pg/mg for Caucasians. Similar concentration relationships were observed at weeks 4, 6, and 7. A strong relationship between the hair concentrations of codeine and melanin (R2= 0.73) was observed. Normalization of the codeine concentration with the melanin concentration reduced the hair color differences observed. These data demonstrate that the interpretation and reporting of hair test results for codeine are influenced by hair color. After this dosing protocol, the proposed federal guideline cutoff of 200 pg/mg of codeine would result in 100% of subjects with black hair and 50% of subjects with brown hair being reported as positive, and subjects with blond or red hair would be reported as negative. The incorporation of these drugs into hair should be studied carefully in humans to ensure the appropriate interpretation of drug concentrations.