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Interaction of the benzodiazepines with the GABAA receptor
Published in Adam Doble, Ian L Martin, David Nutt, Calming the Brain: Benzodiazepines and related drugs from laboratory to clinic, 2020
Adam Doble, Ian L Martin, David Nutt
Chlormethiazole, which exhibits sedative, hypnotic and anticonvulsant properties together with neuroprotective effects in certain animal models of stroke (Green et al, 2000), clearly potentiates GABA-mediated transmission (Harrison and Simmonds, 1983; Cross et al, 1989; Hales and Lambert, 1991b). However, chlormethiazole also inhibits excitatory amino acid transmission but at significantly higher concentrations (Empson et al, 2000).
Psychopharmacology EMIs
Published in Michael Reilly, Bangaru Raju, Extended Matching Items for the MRCPsych Part 1, 2018
Acamprosate.Buprenorphine.Chlordiazepoxide.Clonidine.Clomethiazole.Diazepam.Disulfiram.Lofexidine.Methadone.Naltrexone.
Topic 6 Addictions and Substance Misuse
Published in Melvyn W.B. Zhang, Cyrus S.H. Ho, Roger C.M. Ho, Basant K. Puri, Get Through, 2016
Melvyn W.B. Zhang, Cyrus S.H. Ho, Roger C.M. Ho, Basant K. Puri
NICE guidance on the treatment for acute alcohol withdrawal: Benzodiazepine should be considered to offer. Both diazepam and chlordiazepoxide have UK marketing authorization for the management of acute alcohol withdrawal symptoms. The alternatives to benzodiazepines include carbamazepine, which could be used in the management of alcohol-related withdrawal symptoms, but it does not have UK marketing rights. Clomethiazole can be used in the management of alcohol-related withdrawal symptoms for patients who are determined to discontinue drinking and in the inpatient setting, as it could lead to fatal respiratory depression when combined with alcohol in patients with cirrhosis. It does have UK marketing rights.
Metabolic profiling in liver microsomes and mice of E28, a potent FLT3 inhibitor
Published in Xenobiotica, 2022
Yan Tan, Xiandeng Li, Minghai Tang, Huan Wang, Yong Chen, Haoyu Ye, Jiajia Zhao, Rui Wu, Panhong Wei, Leilei Du, Li Wan
The metabolic phenotype of E28 was researched using specific chemical inhibitors. The selective inhibitors and their concentrations were selected as follows: α-naphthoflavone (CYP1A2 inhibitor, 1 µM), pilocarpine (CYP2A6 inhibitor, 25 µM), ticlopidine (CYP2C19 inhibitor, 25 µM), quinidine (CYP2D6 inhibitor, 10 µM), clomethiazole (CYP2E1 inhibitor, 50 µM), ketoconazole (CYP3A4 inhibitor, 1 µM), and sulphaphenazole (CYP2C9 inhibitor, 20 µM). E28 (1 μM) were incubated with 0.5 mg/mL HLMs in the presence of selective P450 enzymes inhibitor in the reaction mixture containing NADPH-generating system for 60 min at 37 °C. All other incubation conditions and sample preparation procedures were the same as described in section 2.3 (In vitro metabolic stability in liver microsomal incubation). The reaction without chemical inhibitors (methanol instead of inhibitors) with the identical method of incubation, and was terminated at two-time points (0, 60 min), as negative and positive control respectively.
A study on distribution and stability of drugs at the interface of a scutellarin-loaded emulsion
Published in Pharmaceutical Development and Technology, 2021
Mingxi Ma, Shengxin Huang, Jiabi Zhu, Fei Xiong
Because of the importance of the interfacial properties of the drug, a three-phase model should be more appropriate than the two-phase one. The three-phase model was established by Teagarden et al. (1988) and they studied the distribution of prostaglandin E1 (PGE1) in a lipid emulsion. Levy et al. (1994) saw the interface layer between the oil phase and the aqueous phase formed by phospholipids clearly using a freeze-etching electron microscope. Nordén et al. (2001) found that through the interaction with phospholipid interface, Clomethiazole, a drug with surface activity, can greatly change the properties of phospholipid stable emulsion. Klang et al. (2011) suggested that the release properties of the medicine and the microstructure of the droplets could be improved by adding cyclodextrin to the interfacial film.
Effects of catalpol on the activity of human liver cytochrome P450 enzymes
Published in Xenobiotica, 2019
Lu Liu, Xiangang Cao, Tingxin Li, Xiaohua Li
Catalpol, coumarin and testosterone were obtained from the National Institute for the Control of Pharmaceutical and Biological Products (Beijing, China). d-Glucose-6-phosphate, Glucose-6-phosphate dehydrogenase, corticosterone, S-mephenytoin and NADP+ were obtained from Sigma Chemical Co. (St. Louis, MO). Phenacetin, acetaminophen, 4-hydroxymephenytoin, 7-hydroxycoumarin, 4′-hydroxydiclofenac, sulfaphenazole, quinidine, tranylcypromine, chlorzoxazone, 6-hydroxychlorzoxazone, paclitaxel, 6β-hydroxytestosterone and clomethiazole were obtained from Toronto Research Chemicals (Toronto, ON). Furafylline and montelukast were obtained from Beijing Aleznova Pharmaceutical (Beijing, China). Diclofenac, dextromethorphan and ketoconazole were purchased from ICN Biomedicals (Aurora, OH). Pooled HLMs were purchased from BD Biosciences Discovery Labware (Woburn, MA). All other reagents and solvents were of analytical reagent grade.