The SD of residuals (S y͉x) was 73 ng/L in the concentration range of 0 –5000 ng/L and 22 ng/L in the range of 0 –500 ng/L. The agreement between the GC/MS and MEIA assays indicated low interference from other estrogenic compounds and their metabolites in the latter assay. In conclusion, we have developed a GC/MS method for the quantification of estradiol in patient serum samples and serum-based...

Objective: To evaluate the effect of NIPRD-AM1 on CYP3A4 in order to generate clinically significant data for its safe and efficacious use. Materials and Methods: NIPRD-AM1 is a phytomedicine developed from aqueous root extracts of Nauclea latifolia Smith (Rubiaceae) for the treatment of uncomplicated malaria. The effect of NIPRD-AM1 on CYP3A4 was measured with and without the addition of NIPRD...

Ticagrelor is an orally administered, antiplatelet agent that inhibits ADP's prothrombotic effects on the platelet by antagonizing the P2Y 12 receptor. Ticagrelor is a reversibly binding direct-acting P2Y 12 antagonist and does not require metabolic activation to achieve its antiplatelet effect. CYP3A4 and CYP3A5 appear to be the enzymes predominantly responsible for the formation of the ticagr...

Although co-administration of amenamevir (a helicase–primase inhibitor) reportedly decreases exposure to midazolam, a CYP3A4 substrate, it remains unclear whether induces the metabolism calcineurin inhibitors (tacrolimus and cyclosporine) metabolized by CYP3A4. Herein, we illustrated two cases induction for amenamevir. The concentration/dose normalized body weight was defined as inhibitors. fir...

The effects of [4'-(6-allyl-methyl-amino-hexyloxy)-2'-fluoro-phenyl]-(4-bromophenyl)-methanone fumarate (Ro 48-8071), an inhibitor of 2,3-oxidosqualene:lanosterol cyclase (cyclase), were evaluated on CYP3A4 and CYP2B6 mRNA content in primary cultured human hepatocytes. In seven hepatocyte culture preparations, 24-h treatment with 3, 10, or 30 microM Ro 48-8071 produced median increases in CYP3A...

Although primary human hepatocytes are commonly used for induction studies, the evaluation method is associated with several problems. More recently, a reporter gene assay has been suggested to be an alternative, although the contribution of only transfected nuclear receptors can be evaluated. The aim of the present study was to establish a method by which the extent of in vivo CYP3A4 induction...

Introduction: Amiodarone is one of drug with narrow therapeutics index. This medicine was metabolized by CYP3A4 and CYP2C8. The changes in the activity this enzymes CYP2C8 polymorphism will affect effect. study aimed to determine impact on amiodarone responses. Method: review article search PubMed keywords: ‘amiodarone’ ‘polymorphism CYP3A4’ CYP2C8’. Results: We collect 46 references Conclusion...

Vitamin D(3) is critical for the regulation of calcium and phosphate homeostasis. In some individuals, mineral homeostasis can be disrupted by long-term therapy with certain antiepileptic drugs and the antimicrobial agent rifampin, resulting in drug-induced osteomalacia, which is attributed to vitamin D deficiency. We now report a novel CYP3A4-dependent pathway, the 4-hydroxylation of 25-hydrox...

Artemisinin drugs have become the first-line antimalarials in areas of multidrug resistance. However, monotherapy with artemisinin drugs results in comparatively high recrudescence rates. Autoinduction of cytochrome P450 (P450)-mediated metabolism, resulting in reduced exposure, has been supposed to be the underlying mechanism. To better understand the autoinduction and metabolic drug-drug inte...