An investigation of the formation of cytotoxic, protein-reactive and stable metabolites from carbamazepine in vitro
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Reactive metabolites of the anticonvulsant drugs and approaches to minimize the adverse drug reaction
2021, European Journal of Medicinal ChemistryCitation Excerpt :OXC is almost promptly transformed to the vital active metabolite called as 10,11-dihydro-10-hydroxy-5H-dibenz [b,f]azepine-5-carboxamide(10-hydroxy-10,11-dihydro-carbamazepine) [113,114]. Moreover, eslicarbazepine acetate (BIA 2–093) also follows the biotransformation pathway similar to the OXC (Fig. 28) [115]. The different entities were incorporated or removed by scientists to remove the structural feature of CBZ and its analogues associated with toxic effect.
Drug-Induced Liver Injury
2017, Zakim and Boyer's Hepatology: A Textbook of Liver DiseasePathogenetic analyses of carbamazepine-induced liver injury in F344 rats focused on immune- and inflammation-related factors
2016, Experimental and Toxicologic PathologyCitation Excerpt :Treatment with ketoconazole and troleandomycin unexpectedly up-regulated the level of ALT and AST in mice, whereas there was a down-regulation in rats. A previous study demonstrated that ketoconazole significantly reduced the metabolism-dependent irreversible binding of radiolabelled CBZ to human liver microsomes (Pirmohamed et al., 1992). These previous finding suggests a similarity of metabolic pathways that lead to CBZ-induced liver injury between rat and human.
High-content screening imaging and real-time cellular impedance monitoring for the assessment of chemical's bio-activation with regards hepatotoxicity
2015, Toxicology in VitroCitation Excerpt :As with the other drugs tested, cyclophosphamide (CP) is metabolized in liver. Indeed, its antineoplasic action is linked to the biotransformation processes but it can also lead to toxicity (Pirmohamed et al., 1992). Using classical cytotoxic tests on primary cultures of hepatocytes (Fig. 5A–D), we found no significant toxicity of this compound via MTT (IC50 = 21.31 mM) or neutral red tests (IC50 = 18.75 mM) whereas ATP monitoring (IC50 = 8.27 mM) and real-time cellular impedance detection (IC50 = 2.6 mM) showed a higher sensitivity with this drug.
Anticonvulsant agents
2013, Drug-Induced Liver DiseaseDrug-Induced Liver Injury
2012, Zakim and Boyer's Hepatology