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Updated: Jul 3, 2025

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
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Published on: March 28, 2017

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将CYP2C19的转换效应纳入临床药物遗传学的相关性

Maike Scherf-Clavel1, Heike Weber1,2, Stefan Unterecker1

  • 1Department of Psychiatry, Psychosomatics and Psychotherapy, Center of Mental Health, University Hospital of Würzburg, 97080 Würzburg, Germany.

Pharmacopsychiatry
|February 14, 2024
PubMed
概括

转化会影响CYP2C19的功能状态,改变代谢器表型,但不会改善药物度相关性. 对于服用影响CYP2C19的药物患者,建议对治疗药物进行监测.

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The elimination half-life and drug clearance of drugs following nonlinear kinetics can vary with dosage. The Michaelis-Menten parameters and drug concentration influence these factors. As the dose increases, the elimination half-life tends to lengthen, resulting in a reduction in clearance and a disproportionately larger area under the curve. The total clearance can be derived from the Michaelis-Menten equation for drugs following a one-compartment model.
A study on guinea pigs examined the...
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Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
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