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Impact of Heterotropic Allosteric Modulation on the Time-Dependent Inhibition of Cytochrome P450 3A4.
Drug Metab Dispos
October 2023
Lilly Research Laboratories; Eli Lilly and Company, Indianapolis, Indiana.
The current study was designed to investigate the influence of allosteric effectors on the metabolism of the prototypical cytochrome P450 (CYP) 3A4 substrate midazolam (MDZ), and on the determination in vitro time-dependent inhibition (TDI) of CYP3A4 using human liver microsomes (HLM). As the concentration of midazolam increased to 250 M in HLMs, homotropic cooperativity resulted in a decrease in the 1'-hydroxymidazolam to 4-hydroxymidazolam ratio to a maximum of 1.1.
View Article and Find Full Text PDFIn vitro evaluation of fenfluramine and norfenfluramine as victims of drug interactions.
Pharmacol Res Perspect
June 2022
Zogenix, Inc, Emeryville, California, USA.
Fenfluramine (FFA) has potent antiseizure activity in severe, pharmacoresistant childhood-onset developmental and epileptic encephalopathies (e.g., Dravet syndrome).
View Article and Find Full Text PDFBoromycin has Rapid-Onset Antibiotic Activity Against Asexual and Sexual Blood Stages of .
Front Cell Infect Microbiol
April 2022
Institute of Tropical Medicine, University of Tübingen, Tübingen, Germany.
Boromycin is a boron-containing macrolide antibiotic produced by with potent activity against certain viruses, Gram-positive bacteria and protozoan parasites. Most antimalarial antibiotics affect plasmodial organelles of prokaryotic origin and have a relatively slow onset of action. They are used for malaria prophylaxis and for the treatment of malaria when combined to a fast-acting drug.
View Article and Find Full Text PDFDevelopment and validation of an LC-MS/MS screening method for macrolide and quinolone residues in baby food.
J Environ Sci Health B
May 2021
Chemistry Department, Instituto Nacional de Controle de Qualidade em Saúde, Fundação Oswaldo Cruz (Fiocruz), Rio de Janeiro, Rio de Janeiro, Brazil.
A simple, rapid and sensitive screening method by liquid chromatography-tandem mass spectrometry (LC-MS/MS) was developed for the identification of 7 macrolides (clarithromycin, erythromycin, oleandomycin, spiramycin, tilmicosin, troleandomycin and tylosin) and 8 quinolones (ciprofloxacin, difloxacin, enrofloxacin, flumequine, moxifloxacin, nalidixic acid, norfloxacin and ofloxacin) in meat and egg-based baby foods. Sample preparation was performed using an alkaline modified QuEChERS (Quick, Easy, Cheap, Effective, Rugged, Safe) extraction method without additional clean-up steps. A simplex-lattice mixture experimental design was used in the optimization of the QuEChERS extraction solvent.
View Article and Find Full Text PDFGrapefruit juice enhances the systolic blood pressure-lowering effects of dietary nitrate-containing beetroot juice.
Br J Clin Pharmacol
February 2021
School of Cardiovascular Medicine and Sciences, Department of Clinical Pharmacology, King's College London British Heart Foundation Centre of Research Excellence, London, UK.
Aims: Dietary nitrate from sources such as beetroot juice lowers blood pressure (BP) via the nitrate-nitrite-nitric oxide (NO) pathway. However, NO and nitrite are inactivated via reoxidation to nitrate, potentially limiting their activity. Cytochrome P450-3A4 inhibition with troleandomycin prevents nitrite re-oxidation to nitrate in rodent liver.
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