LLerena A, Herraíz A G, Cobaleda J, Johansson I, Dahl M L
Department of Clinical Pharmacology, Karolinska Institute, Huddinge University Hospital, Sweden.
Clin Pharmacol Ther. 1993 Dec;54(6):606-11. doi: 10.1038/clpt.1993.197.
Debrisoquin and S-mephenytoin hydroxylation phenotypes were determined in 72 Spanish psychiatric patients treated with neuroleptic or antidepressant agents. One patient (1.4%) was classified as a poor metabolizer of S-mephenytoin. Between both neuroleptic- and antidepressant-treated patients, the distribution of the debrisoquin metabolic ratio was shifted toward higher values compared with 54 drug-free healthy subjects. Forty percent of patients treated with neuroleptics and 5% of patients treated with antidepressants were classified as poor metabolizers of debrisoquin. CYP2D6 genotype analysis in 36 neuroleptic-treated patients confirmed that the high metabolic ratios were attributable to inhibition of CYP2D6 and not to overrepresentation of subjects with poor metabolizer genotypes. In 48 selected Spanish drug-free subjects, CYP2D6 genotype predicted the phenotype with 95% accuracy. Neuroleptics and antidepressants interfere at therapeutic doses with phenotyping for CYP2D6 but not for S-mephenytoin hydroxylation capacity. In psychotropic-treated patients, genotyping provides a valuable tool for prediction of the CYP2D6 phenotype.
对72名接受抗精神病药或抗抑郁药治疗的西班牙精神病患者进行了异喹胍和S-美芬妥英羟化表型测定。一名患者(1.4%)被归类为S-美芬妥英代谢不良者。与54名未服用药物的健康受试者相比,在接受抗精神病药和抗抑郁药治疗的患者中,异喹胍代谢率的分布均向更高值偏移。40%接受抗精神病药治疗的患者和5%接受抗抑郁药治疗的患者被归类为异喹胍代谢不良者。对36名接受抗精神病药治疗的患者进行的CYP2D6基因型分析证实,高代谢率是由于CYP2D6受到抑制,而非代谢不良基因型受试者比例过高所致。在48名选定的未服用药物的西班牙受试者中,CYP2D6基因型预测表型的准确率为95%。抗精神病药和抗抑郁药在治疗剂量下会干扰CYP2D6的表型分析,但不影响S-美芬妥英的羟化能力。在接受精神药物治疗的患者中,基因分型为预测CYP2D6表型提供了一个有价值的工具。