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Effect of the MDR1 C3435T variant and P-glycoprotein induction on dicloxacillin pharmacokinetics.
Author: BenetLeslie Z, HuangYong, PutnamWendy S, WooJonathan M
Original Abstract of the Article :
This study investigated 2 hypotheses about genotype-phenotype relationships for the efflux transporter, P-glycoprotein: (1) the presence of a synonymous C3435T variant in exon 26 of the MDR1 gene correlates to higher plasma concentrations of a P-glycoprotein substrate, dicloxacillin, and (2) the eff...See full text at original site
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引用元:
https://doi.org/10.1177/0091270004273492
データ提供:米国国立医学図書館(NLM)
The MDR1 C3435T Variant and P-Glycoprotein Induction
This study delves into the fascinating world of [pharmacogenetics], a field that explores how genetic variations influence drug responses. Specifically, it examines the impact of a genetic variant known as the MDR1 C3435T variant on the pharmacokinetics of dicloxacillin, a medication often used to combat bacterial infections.
The study's design is like a grand camel caravan crossing the desert. The researchers, like seasoned guides, administered dicloxacillin to 18 healthy volunteers, first without any additional intervention, and then again after they had been taking rifampin, a drug known to stimulate the activity of P-glycoprotein, a transporter that pumps out drugs from cells. This allowed them to compare the effects of the MDR1 C3435T variant in both a 'natural' state and under a condition where P-glycoprotein was stimulated. The results, my dear, were quite revealing.
Dicloxacillin Levels and the MDR1 C3435T Variant
The researchers discovered that the MDR1 C3435T variant did not significantly alter the levels of dicloxacillin in the bloodstream, suggesting it does not influence how our bodies process the drug.
Rifampin's Impact on Dicloxacillin
However, when rifampin was involved, the scene changed! The presence of rifampin led to a noticeable decrease in the maximum concentration of dicloxacillin in the blood, indicating that rifampin's stimulatory effect on P-glycoprotein led to increased elimination of the drug from the body. The researchers also observed that rifampin increased the formation and clearance of the dicloxacillin metabolite, 5-hydroxymethyl metabolite.
Health Implications and Daily Life
This research sheds light on the intricate interplay between genes, drug metabolism, and the effectiveness of medications. If you are prescribed dicloxacillin, remember to discuss with your doctor if you are taking rifampin or any other medications that might affect P-glycoprotein activity. Understanding the factors that influence drug absorption and elimination can lead to more tailored and effective treatments.
Dr.Camel's Conclusion
This study, like a well-planned oasis in the desert, offers valuable insights into the complex world of pharmacogenetics. It demonstrates that P-glycoprotein induction can significantly impact the pharmacokinetics of dicloxacillin, highlighting the importance of considering drug interactions and individual variations when prescribing medications.
Date :
- Date Completed 2005-07-29
- Date Revised 2018-12-01
Further Info :
Related Literature
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