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Discovering interactions in polypharmacy: Impact of metamizole on the metabolism of quetiapine.
Br J Clin Pharmacol
November 2024
Department of Psychiatry, Psychotherapy and Psychosomatics, University Hospital RWTH Aachen, Aachen, Germany.
Aims: Metamizole is quite an old drug with analgesic, antipyretic and spasmolytic properties. Recent findings have shown that it may induce several cytochrome P450 (CYP) enzymes, especially CYP3A4 and CYP2B6. The clinical relevance of these properties is uncertain.
View Article and Find Full Text PDFPharmacokinetics-Based Pediatric Dose Evaluation and Optimization Using Saliva - A Case Study.
J Clin Pharmacol
July 2024
Pediatric Pharmacology and Pharmacometrics, University Children's Hospital Basel (UKBB), University of Basel, Basel, Switzerland.
Understanding pharmacokinetics (PK) in children is a prerequisite to determine optimal pediatric dosing. As plasma sampling in children is challenging, alternative PK sampling strategies are needed. In this case study we evaluated the suitability of saliva as alternative PK matrix to simplify studies in infants, investigating metamizole, an analgesic used off-label in infants.
View Article and Find Full Text PDFDiscovery of GPX4 inhibitors through FP-based high-throughput screening.
Eur J Med Chem
February 2024
The Center for Chemical Biology, Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; University of Chinese Academy of Sciences, 19 Yuquan Road, Beijing, 100049, China. Electronic address:
Ferroptosis is a form of non-apoptotic cell death, regulated by phospholipid hydroperoxide glutathione peroxidase 4 (GPX4), a selenoprotein with a selenocysteine residue (sec) in the active site. GPX4 is a promising target for cancer cells in therapy-resistant conditions via ferroptosis, which can reduce the level of lipid reactive oxygen species (ROS). So far, all existing GPX4 inhibitors covalently bind to GPX4 via a reactive alkyl chloride moiety or masked nitrile-oxide electrophiles with poor selectivity and pharmacokinetic properties and most were obtained by cell phenotype-based screening.
View Article and Find Full Text PDFPharmacotherapeutic monitoring of dipyrone in northeastern Brazilian donkeys (Equus asinus).
Res Vet Sci
November 2023
Department of Animal Science, Universidade Federal Rural do Semi-Árido, 572, Rua Francisco Mota, Presidente Costa e Silva, Mossoró, RN 59.625-900, Brazil. Electronic address:
This study aimed to monitor the effects of dipyrone following multiple administrations in northeastern donkeys. Ten castrated male donkeys, aged 6.4 ± 3 years and weighing 130.
View Article and Find Full Text PDFTime course of CYP3A activity during and after metamizole (dipyrone) in healthy volunteers.
Br J Clin Pharmacol
August 2023
Department of Clinical Pharmacology and Pharmacoepidemiology, Heidelberg University Hospital, Im Neuenheimer Feld 410, 69120, Heidelberg, Germany.
Aims: In patients of all ages, metamizole is a frequently used analgesic. Recently, metamizole has been identified as an inducer of, among others, cytochrome P450 (CYP) 3A activity, but the time course of this interaction has not been evaluated.
Methods: Using repeated oral microdoses (30 μg) of the CYP3A index substrate midazolam, we assessed changes in midazolam pharmacokinetics (area under the concentration-time curve from 2-4 h: AUC and estimated partial metabolic clearance: eCl ) before, at steady-state, and after discontinuation of 3 × 1000 mg metamizole/day orally for 8 days.
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