The metabolism zonation in liver lobules is well known yet its incorporation into the mathematical models of acetaminophen (APAP) metabolism is still primitive - only the oxidation pathway via reaction with the cytochrome P450 (CYP450) has been considered, yet the zonal heterogeneity exhibits in all three pathways including sulphation, glucuronidation and oxidation. In this paper we present a novel computational method where an intracellular APAP metabolism model is integrated into a Finite Element Model (FEM) of sinusoids, and the zonal heterogeneity in three metabolism pathways are all incorporated. We demonstrate that the degradation of APAP, detoxification via glutathione (GSH) and the formation of hepatotoxicity, are all affected profoundly by the zonal difference. Specifically, glucuronidation plays a major role in the degradation of APAP. Generation of GSH, its conjugation with the toxic NAPQI and the spatial distribution of CYP450 combined together determine the toxicity of APAP. We suggest that the current platform be used for further hepatotoxicity study of APAP by incorporating other heterogeneity factors.
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http://dx.doi.org/10.1016/j.dmpk.2018.09.266 | DOI Listing |
Toxins (Basel)
December 2024
Nephrology and Renal Transplantation, Hospital Clínic de Barcelona, 08036 Barcelona, Spain.
Pain is a frequent and disturbing symptom among hemodialysis patients. Protein-bound uremic toxins (PBUTs) are related to cardiovascular and overall mortality, and they are difficult to remove with current hemodialysis treatments. The PBUT displacers, such as furosemide, tryptophan, or ibuprofen, may be promising new strategies for improving their clearance.
View Article and Find Full Text PDFCureus
November 2024
Gastroenterology and Hepatology, Rapides Regional Medical Center, Alexandria, USA.
Drug-induced liver injury (DILI) is a rare but significant cause of acute liver failure, often challenging to diagnose due to its clinical similarity to other liver conditions. Since most drugs are metabolized by liver enzymes, the liver is at risk for hepatotoxicity. Although DILI has a low incidence in clinical practice, it remains a critical consideration for patients on potentially hepatotoxic medications.
View Article and Find Full Text PDFJ Pharm Sci
December 2024
Janssen Research & Development, LLC, Discovery Pharmaceutics, San Diego, CA, USA.
Rat pharmacokinetic studies are commonly utilized in early discovery to support absorption, distribution, metabolism, and excretion optimization of active pharmaceutical ingredients (APIs). The aim of this work was to compare exposures from fit-for-purpose oral suspension and solution formulations in rats to guidance provided by the refined Developability Classification System (rDCS) with respect to identifying potential limits to oral absorption, formulation strategy selection, and to optimize oral bioavailability (BA). This investigation utilized six diverse APIs covering a large range of biorelevant solubility, metabolic stability, and oral BA in rats.
View Article and Find Full Text PDFMol Med
December 2024
Beijing Institute of Hepatology, Beijing Youan Hospital, Capital Medical University, No. 8, XitouTiao Road, Youwai Street, Fengtai District, Beijing, 100069, China.
Background: Acetaminophen (APAP)-induced acute liver injury (AILI) is the most prevalent cause of acute liver failure and mitochondrial dysfunction plays a dominant role in the pathogenesis of AILI. Mitochondrial transcription factor A (TFAM) is an important marker for maintaining mitochondrial functional homeostasis, but its functions in AILI are unclear. This study aimed to investigate the function of TFAM and its regulatory molecular mechanism in the progression of AILI.
View Article and Find Full Text PDFA 60-year-old polymorbid patient developed severe metabolic acidosis during weeks of treatment with flucloxacillin and paracetamol. The acidosis was triggered by an accumulation of 5-oxoproline due to pre-existing risk factors for glutathione deficiency as well as a ketoacidosis due to starvation. After treatment with N-acetylcysteine and hemofiltration, the acidosis completely resolved.
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