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Involvement of CYP2D6 and CYP2B6 on tramadol pharmacokinetics.
Pharmacogenomics. 2020 Jul; 21(10):663-675.P

Abstract

This study included 24 healthy volunteers who received a single 37.5 mg oral dose of tramadol. We analyzed 18 polymorphisms within CYP2D6, CYP2B6, CYP3A, COMT, ABCB1, SLC22A1 and OPRM1 genes by quantitative PCR, to study whether these polymorphisms affect its pharmacokinetics, pharmacodynamics and safety. CYP2D6 intermediate metabolizers (n = 6) showed higher tramadol plasma concentrations and lower clearance compared with normal and ultrarapid metabolizers. CYP2B6 G516T T/T (n = 2) genotype was also associated to higher tramadol plasma levels. No other polymorphism affected tramadol pharmacokinetics. Three volunteers experienced a prolonged QTc not associated with the genetic variants studied or altered phamacokinetic parameters. The correlation of CYP2B6 genotype with higher tramadol concentrations is remarkable since its influence on its elimination is also relevant and has been less studied to date. However, given our small sample size, it is important to interpret our results with caution.

Authors+Show Affiliations

Clinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, 28006, Spain.Clinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, 28006, Spain. UICEC Hospital Universitario de La Princesa, Plataforma SCReN (Spanish Clinical Reseach Network), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, 28006, Spain.Clinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, 28006, Spain. UICEC Hospital Universitario de La Princesa, Plataforma SCReN (Spanish Clinical Reseach Network), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, 28006, Spain.Clinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, 28006, Spain.Clinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, 28006, Spain.Clinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, 28006, Spain. UICEC Hospital Universitario de La Princesa, Plataforma SCReN (Spanish Clinical Reseach Network), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, 28006, Spain.Clinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, 28006, Spain. UICEC Hospital Universitario de La Princesa, Plataforma SCReN (Spanish Clinical Reseach Network), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, 28006, Spain. Pharmacology Department, Facultad de Medicina, Universidad Autónoma de Madrid, Madrid, 28049, Spain.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32538291

Citation

Saiz-Rodríguez, Miriam, et al. "Involvement of CYP2D6 and CYP2B6 On Tramadol Pharmacokinetics." Pharmacogenomics, vol. 21, no. 10, 2020, pp. 663-675.
Saiz-Rodríguez M, Ochoa D, Román M, et al. Involvement of CYP2D6 and CYP2B6 on tramadol pharmacokinetics. Pharmacogenomics. 2020;21(10):663-675.
Saiz-Rodríguez, M., Ochoa, D., Román, M., Zubiaur, P., Koller, D., Mejía, G., & Abad-Santos, F. (2020). Involvement of CYP2D6 and CYP2B6 on tramadol pharmacokinetics. Pharmacogenomics, 21(10), 663-675. https://doi.org/10.2217/pgs-2020-0026
Saiz-Rodríguez M, et al. Involvement of CYP2D6 and CYP2B6 On Tramadol Pharmacokinetics. Pharmacogenomics. 2020;21(10):663-675. PubMed PMID: 32538291.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Involvement of CYP2D6 and CYP2B6 on tramadol pharmacokinetics. AU - Saiz-Rodríguez,Miriam, AU - Ochoa,Dolores, AU - Román,Manuel, AU - Zubiaur,Pablo, AU - Koller,Dora, AU - Mejía,Gina, AU - Abad-Santos,Francisco, Y1 - 2020/06/15/ PY - 2020/6/17/pubmed PY - 2020/6/17/medline PY - 2020/6/16/entrez KW - CYP2B6 KW - CYP2D6 KW - pharmacokinetics KW - tramadol SP - 663 EP - 675 JF - Pharmacogenomics JO - Pharmacogenomics VL - 21 IS - 10 N2 - This study included 24 healthy volunteers who received a single 37.5 mg oral dose of tramadol. We analyzed 18 polymorphisms within CYP2D6, CYP2B6, CYP3A, COMT, ABCB1, SLC22A1 and OPRM1 genes by quantitative PCR, to study whether these polymorphisms affect its pharmacokinetics, pharmacodynamics and safety. CYP2D6 intermediate metabolizers (n = 6) showed higher tramadol plasma concentrations and lower clearance compared with normal and ultrarapid metabolizers. CYP2B6 G516T T/T (n = 2) genotype was also associated to higher tramadol plasma levels. No other polymorphism affected tramadol pharmacokinetics. Three volunteers experienced a prolonged QTc not associated with the genetic variants studied or altered phamacokinetic parameters. The correlation of CYP2B6 genotype with higher tramadol concentrations is remarkable since its influence on its elimination is also relevant and has been less studied to date. However, given our small sample size, it is important to interpret our results with caution. SN - 1744-8042 UR - https://www.unboundmedicine.com/medline/citation/32538291/Involvement_of_CYP2D6_and_CYP2B6_on_tramadol_pharmacokinetics L2 - https://www.futuremedicine.com/doi/10.2217/pgs-2020-0026?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -
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