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Aldehyde Oxidases as Enzymes in Phase I Drug Metabolism
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Cristiano Mota, Teresa Santos-Silva, Mineko Terao, Enrico Garattini, Maria João Romão, Silke Leimkühler
Human AOX1 is a cytosolic protein and it is recognized to play an important role in phase I drug metabolism, being involved in the oxidation of several antiviral, hypnotic, and antiepileptic agents (Baral et al., 2014; Bolis et al., 2017; Coelho et al., 2012; Fratelli et al., 2013; Garattini and Terao, 2011; Pryde et al., 2010; Pryde et al., 2012). AOX1 substrates are often intermediates or products of cytochrome-P450 dependent metabolism (Barr and Jones, 2011; Garattini and Terao, 2012; Kitamura and Sugihara, 2014; Obach et al., 2004). Furthermore, hAOX1 is inhibited by various types of drugs, including estrogen receptor modulators (raloxifene) and atypical antipsychotic agents (phenothiazines such as thioridazine and loxapine), which supports the involvement of the enzyme in drug interactions (Barr and Jones, 2011; Obach et al., 2004; Sanoh et al., 2015).
Synthesis, crystal structure, hirshfeld surface analysis, molecular docking and molecular dynamics studies of novel olanzapinium 2,5-dihydroxybenzoate as potential and active antipsychotic compound
Published in Journal of Experimental Nanoscience, 2022
V. Natchimuthu, Mohnad Abdalla, Manasi Yadav, Ishita Chopra, Anushka Bhrdwaj, Khushboo Sharma, S. Ravi, Krishnan Ravikumar, Khalid J. Alzahrani, Tajamul Hussain, Anuraj Nayarisseri
Antipsychotic medication, also known as neuroleptics is a class of psychotropics primarily manoeuvred for short- or long-term treatments of psychotic disorders (bipolar depression, delusions, paranoia, schizophrenia, etc.). Studies have revealed that Olanzapine, a novel atypical antipsychotic drug elicits a high response with low dosage on the patients suffering from psychotic ailments. It consists of a thieno-benzodiazepinyl structure and exhibits a similar in vitro binding profile with an atypical anti-psychotic agent; an FDA-approved drug, Clozapine [1,2]. According to the Biopharmaceutical Classification System (BCS), Olanzapine belongs to class II (low solubility, high permeability) cadre, and is highly effective in positive, negative, and cognitive symptoms for acute and relapsing schizophrenics. This drug is marketed under the trademark, Zyprexa by Eli Lilly and Company [3,4].
Clozapine, ziprasidone, and sertindole-induced morphological changes in the rat heart and their relationship to antioxidant enzymes function
Published in Journal of Toxicology and Environmental Health, Part A, 2018
Aleksandra Nikolić-Kokić, Nikola Tatalović, Jelena Nestorov, Milica Mijović, Ana Mijusković, Marko Miler, Zorana Oreščanin-Dušić, Milan Nikolić, Verica Milošević, Duško Blagojević, Mihajlo Spasić, Čedo Miljević
Atypical antipsychotics AAP, also referred to as second-generation antipsychotics constitute, a group of pharmaceutical agents used to treat psychiatric conditions, primarily schizophrenia and schizophrenia-related disorders. However, in recent years these potent medications were also utilized for treatment of a broad range of symptoms and disorders, including bipolar disorder and depression as well as personality disorders and obsessive-compulsive disorder. Clozapine was the first AAP developed in 1958 and after 30 years of investigations and clinical trials, it was approved by the FDA (Crilly 2007). Currently, clozapine is considered to be one of the most effective antipsychotic drug for treatment-resistant schizophrenia (Leucht et al. 2009). Despite its effectiveness, clozapine usage is limited due to the risk of several potentially fatal adverse reactions including myocarditis and sudden death (Haas et al. 2007). Myocarditis was reported as clinically important complication observed in patients on clozapine therapy without preexisting cardiovascular diseases (Haas et al. 2007). In contrast to clozapine, ziprasidone, and sertindole are AAP that generally are considered as a low risk for development of myocarditis and heart failure (Ward et al. 2013). However, ziprasidone and sertindole were found to induce prolongation of QT interval and TdP in some patients (Naguy 2016; Nielsen et al. 2015a, 2015b)