Codeine is bioactivated to morphine, a strong opioid agonist, by the hepatic cytochrome P450 2D6 (CYP2D6); hence, the efficacy and safety of codeine are governed by CYP2D6 activity. Polymorphisms are a major cause of CYP2D6 variability. We summarize evidence from the literature supporting this association and provide therapeutic recommendations for codeine based on CYP2D6 genotype. This documen...

The CYP2D6 enzyme is crucial for the metabolism of tamoxifen. The CYP2D6 gene is highly polymorphic, and individuals can be extensive, intermediate, or poor tamoxifen metabolizers. The aim of this study was to determine the frequencies of the CYP2D6 *3, *4, and *10 alleles in women with breast cancer who were treated with tamoxifen and analyze the association of enzyme activity with prognostic ...

It has earlier been shown that the isoenzymes CYP2D6 and CYP3A4 are involved in Oand N-demethylation of diltiazem (DTZ), respectively. Apparently, CYP3A4 plays a more prominent role than CYP2D6 in the overall metabolism of DTZ. However, previous observations indicate that the opposite might be true for the pharmacologically active metabolite desacetyl-DTZ (M1). Thus, the aim of the present in v...

BACKGROUND The gene encoding the phase I enzyme cytochrome P4502D6 (CYP2D6) has been previously investigated for its potential predictive role in the efficacy of breast cancer treatments such as tamoxifen, but its role in breast cancer susceptibility is unclear. This study aims to evaluate the association between germ line variations in CYP2D6 and breast cancer susceptibility. METHODS DNA sam...

Upon characterization of baculovirus-expressed cytochrome P-450 (CYP) 2C19, it was observed that this enzyme metabolized (1/2) bufuralol to 1*hydroxybufuralol, a reaction previously understood to be selectively catalyzed by CYP2D6. The apparent Km for this reaction was 36 mM with recombinant CYP2C19, approximately 7-fold higher than for recombinant CYP2D6. The intrinsic clearance for this react...

BACKGROUND Extrapyramidal syndromes (EPS) are clinically relevant side effects of metoclopramide which are often not anticipated. PATIENTS AND METHODS Two patients who received metoclopramide developed an acute dystonic reaction. Symptoms disappeared after biperiden or trihexyphenidyl were given. Molecular analysis of the CYP2D6 gene was performed using a PCR-based method. RESULTS Both pati...

BACKGROUND Frailty is a clinical phenotype that is associated with adverse health outcomes. Since frail patients may be more prone for adverse drug events and about 15-20 % of commonly prescribed drugs are metabolized by CYP2D6, we hypothesized that CYP2D6 metabolism is decreased in frail patients compared with healthy subjects. METHODS The (13)C-dextromethorphan breath test (DM-BT) was used ...

The genetically determined capacity of the cytochrome P450 CYP2D6 is suspected to be involved in the activation of tobacco carcinogens. From a multicentric case-control study carried out to analyze the interaction between host and environmental factors on tobacco-related cancers, we reported recently that the effect of tobacco on lung cancer risk rose with increasing CYP2D6 activity, and the ef...

The CYP2D6 gene encodes an enzyme important in the metabolism of many commonly used medications. Variation in CYP2D6 is associated with inter-individual differences in medication response, and genetic testing is used to optimize medication therapy. This report describes a retrospective study of CYP2D6 allele frequencies in a large population of 104,509 de-identified patient samples across all r...