Search results for "Disulfiram"
showing 7 items of 7 documents
The potential of aldehyde dehydrogenase 2 as a therapeutic target in cardiovascular disease.
2018
Mitochondrial aldehyde dehydrogenase (ALDH-2) plays a major role in the ethanol detoxification pathway by removing acetaldehyde. Therefore, ALDH-2 inhibitors such as disulfiram represent the first therapeutic targeting of ALDH-2 for alcoholism therapy. Areas covered: Recently, ALDH-2 was identified as an essential bioactivating enzyme of the anti-ischemic organic nitrate nitroglycerin, bringing ALDH-2 again into the focus of clinical interest. Mechanistic studies on the nitroglycerin bioactivation process revealed that during bioconversion of nitroglycerin and in the presence of reactive oxygen and nitrogen species the active site thiols of ALDH-2 are oxidized and the enzyme activity is los…
Aldehyde dehydrogenase and HSP90 co-localize in human glioblastoma biopsy cells.
2013
The concept of a stem cell subpopulation as understood from normal epithelial tissue or bone marrow function has been extended to our understanding of cancer tissue and is now the target of treatment efforts specifically directed to this subpopulation. In glioblastoma, as well as in other cancers, increased expression of aldehyde dehydrogenase (ALDH) has been found localized within a minority sub-population of tumor cells which demonstrate stem cell properties. A separate body of research associated increased expression of heat-shock protein-90 (HSP90) with stem cell attributes. We present here results from our initial immunohistochemistry study of human glioblastoma biopsy tissue where bot…
O-18 - TDM in patients with substance related disorders
2012
The effect of pharmacotherapy of substance-related disorders is moderate at best. Therapeutic drug monitoring (TDM) could be an instrument to improve the outcomes. Since TDM for these drugs is not well established, the authors built a literature based rating scale to evaluate the necessity of TDM for the use of these pharmacological agents. Methods A literature research was performed for acamprosate, bupropion, buprenorphine, clomethiazole, disulfiram, methadone, naltrexone, and varenicline. A rating scale including 22 items, divided in five categories (efficacy, toxicity, pharmacokinetics, patient characteristics and cost effectiveness) was established for evaluation and related to the amo…
Therapeutic Drug Monitoring for Drugs Used in the Treatment of Substance-Related Disorders: Literature Review Using a Therapeutic Drug Monitoring App…
2011
Background The efficacy of drugs for the treatment of substance-related disorders is moderate at best. Therapeutic drug monitoring (TDM) could be an instrument to improve outcomes. Because TDM for most of those drugs is not established, the authors reviewed the literature and built a rating scale to detect the potential added value of TDM for these pharmacologic agents. Methods A literature search was performed for acamprosate, bupropion, buprenorphine, clomethiazole, disulfiram, methadone, naltrexone, and varenicline. The rating scale included 22 items and was divided in five categories: efficacy, toxicity, pharmacokinetics, patient characteristics, and cost-effectiveness. Three reference …
Influence of disulfiram on oxidative drug demethylation.
1970
In clinical antiepileptie therapy it has been observed that the simultaneous administration of diphenylhydantoin and various other drugs causes toxic reactions to diphenylhydantoin. I t was found that disulfiram (Olesen, 1966) as well as ehloramphenieol (Christensen and Skovsted, 1969) cause toxic effects in patients treated with diphenylhydantoin. They are attributed to an increased concentration of diphenylhydantoin in the plasma. Analogous observations show that chloramphenieol enhances the clinical effects of tolbutamide and dicoumarol (Christensen and Skovsted, 1969). Since diphenylhydantoin is metabolized chiefly by p-hydroxylation to 5-(p-hydroxyphenyl)-5-phenyl-hydantoin (Butler, 19…
Synthesis of substituted carbamo(dithioperoxo)thioates as potential BCA2-inhibitory anticancer agents
2015
A new, simple, one-step synthetic route to carbamo(dithioperoxo)thioates from commercially available starting materials is described. The key step of this new synthetic approach involves the tetrabromomethane-promoted reaction between secondary amines, carbon disulfide and alkyl thiols under basic conditions at room temperature. New compounds from this series selected for anticancer screening showed selective sub-micromolar activity within BCA2-expressing human breast cancer cell lines.
A conceptually new treatment approach for relapsed glioblastoma: Coordinated undermining of survival paths with nine repurposed drugs (CUSP9) by the …
2013
Kast, Richard E. et al.