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The Effect of CYP2B6, CYP2D6, and CYP3A4 Alleles on Methadone Binding : A Molecular Docking Study
Joint Authors
Ismail, Rusli
Choong, Yee Siew
Kamal, Nik Nur Syazana Bt Nik Mohamed
Tye, Gee Jun
Lim, Theam Soon
Source
Issue
Vol. 2013, Issue 2013 (31 Dec. 2013), pp.1-7, 7 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2013-09-09
Country of Publication
Egypt
No. of Pages
7
Main Subjects
Abstract EN
Current methadone maintenance therapy (MMT) is yet to ensure 100% successful treatment as the optimum dosage has yet to be determined.
Overdose leads to death while lower dose causes the opioid withdrawal effect.
Single-nucleotide polymorphisms (SNP) in cytochrome P450s (CYPs), the methadone metabolizers, have been showen to be the main factor for the interindividual variability of methadone clinical effects.
In this study, we investigated the effect of SNPs in three major methadone metabolizers (CYP2B6, CYP2D6, and CYP3A4) on methadone binding affinity.
Results showed that CYP2B6*11, CYP2B6*12, CYP2B6*18, and CYP3A4*12 have significantly higher binding affinity to R-methadone compared to wild type.
S-methadone has higher binding affinity in CYP3A4*3, CYP3A4*11, and CYP3A4*12 compared to wild type.
R-methadone was shown to be the active form of methadone; thus individuals with CYP alleles that binds better to R-methadone will have higher methadone metabolism rate.
Therefore, a higher dosage of methadone is necessary to obtain the opiate effect compared to a normal individual and vice versa.
These results provide an initial prediction on methadone metabolism rate for individuals with mutant type CYP which enables prescription of optimum methadone dosage for individuals with CYP alleles.
American Psychological Association (APA)
Kamal, Nik Nur Syazana Bt Nik Mohamed& Lim, Theam Soon& Tye, Gee Jun& Ismail, Rusli& Choong, Yee Siew. 2013. The Effect of CYP2B6, CYP2D6, and CYP3A4 Alleles on Methadone Binding : A Molecular Docking Study. Journal of Chemistry،Vol. 2013, no. 2013, pp.1-7.
https://search.emarefa.net/detail/BIM-457325
Modern Language Association (MLA)
Kamal, Nik Nur Syazana Bt Nik Mohamed…[et al.]. The Effect of CYP2B6, CYP2D6, and CYP3A4 Alleles on Methadone Binding : A Molecular Docking Study. Journal of Chemistry No. 2013 (2013), pp.1-7.
https://search.emarefa.net/detail/BIM-457325
American Medical Association (AMA)
Kamal, Nik Nur Syazana Bt Nik Mohamed& Lim, Theam Soon& Tye, Gee Jun& Ismail, Rusli& Choong, Yee Siew. The Effect of CYP2B6, CYP2D6, and CYP3A4 Alleles on Methadone Binding : A Molecular Docking Study. Journal of Chemistry. 2013. Vol. 2013, no. 2013, pp.1-7.
https://search.emarefa.net/detail/BIM-457325
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-457325