A Comparative Review of the Pharmacological and Toxicological Properties of Disulfiram and Calcium Carbimide

Peachey, John E.; Brien, J. F.; Roach, Carol; Loomis, Christopher W.

doi:10.1097/00004714-198101000-00005

Cited by 51 publications

(13 citation statements)

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“…DDC is metabolised to diethylamine, carbon disulfide (CS 2 ), DDC methyl ester, DDC glucuronide and DDC sulfate; a small amount of DDC is reoxidised to DSF. DSF, DDC and CS 2 are widely distributed throughout the body in lipids of various tissues, and the highest levels of these compounds are found in skeletal muscle [36]. Humans eliminate more than 90% of orally administered DSF within 3 days by renal clearance as DDC, DDC glucuronide and, to a small extent, as DDC sulfate, and via the breath as CS 2 [36].…”

Section: In Vitro Studiesmentioning

confidence: 99%

“…DSF, DDC and CS 2 are widely distributed throughout the body in lipids of various tissues, and the highest levels of these compounds are found in skeletal muscle [36]. Humans eliminate more than 90% of orally administered DSF within 3 days by renal clearance as DDC, DDC glucuronide and, to a small extent, as DDC sulfate, and via the breath as CS 2 [36]. Few publications showed the activity of DSF or its metabolites against TB.…”

Section: In Vitro Studiesmentioning

confidence: 99%

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Potential antimicrobial agents for the treatment of multidrug-resistant tuberculosis

Alsaad

Wilffert

Altena

et al. 2013

European Respiratory Journal

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Treatment of multidrug-resistant (MDR) tuberculosis (TB) is challenging because of the high toxicity of second-line drugs and the longer treatment duration than for drug-susceptible TB patients. In order to speed up novel treatment for MDR-TB, we suggest considering expanding the indications of already available drugs. Six drugs with antimicrobial activity (phenothiazine, metronidazole, doxycycline, disulfiram, tigecycline and co-trimoxazole) are not listed in the World Health Organization guidelines on MDR-TB treatment but could be potential candidates for evaluation against Mycobacterium tuberculosis.A systematic review was conducted to evaluate antituberculous activity of these drugs against M. tuberculosis. We searched PubMed, Google Scholar and Embase for English articles published up to December 31, 2012.We reviewed in vitro, in vivo and clinical antituberculous activity of these drugs in addition to pharmacokinetics and side-effects. Of the drugs effective against actively replicating M. tuberculosis, cotrimoxazole seems to be the most promising, because of its consistent pharmacokinetic profile, easy penetration into tissue and safety profile. For the dormant state of TB, thioridazine may play a potential role as an adjuvant for treatment of MDR-TB. A strategy consisting of pharmacokinetic/pharmacodynamic studies, dose finding and phase III studies is needed to explore the role of these drugs in MDR-TB treatment.@ERSpublications Six antimicrobial drugs are not listed in WHO guidelines on MDR-TB treatment but could offer potential for TB treatment

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Section: In Vitro Studiesmentioning

confidence: 99%

Section: In Vitro Studiesmentioning

confidence: 99%

Potential antimicrobial agents for the treatment of multidrug-resistant tuberculosis

Alsaad

Wilffert

Altena

et al. 2013

European Respiratory Journal

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“…However, results from more recent double-blinded, placebocontrolled clinical trials of both agents indicate that these alcohol-sensitizing agents are no more effective in reducing alcohol drinking than the placebo-control. [14][15][16] Nevertheless, the fact that supervised and carefully scheduled disulfiram is more effective than supervised naltrexone and unsupervised acamprosate 17 suggests that alcohol abuse can be controlled by ALDH inhibitors. Disulfiram itself is capable of inactivating many enzymes with active sulfhydryls including the cytosolic ALDH isozyme, ALDH-1.…”

Section: F D a A P P R O V E D P H A R M A C O L O G I C A L T R E mentioning

confidence: 99%

“…Figure 9. Structures of minor isoflavonoids found in an alcoholic extract of Radix puerariae: genistin (13), 7,4 0 -O-diglucosyldaidzein (14), genistein (15), and formononetin (16).…”

Section: B Daidzin Is the Major Anti-dipsotropic Principle Of Rpmentioning

confidence: 99%

Anti‐dipsotropic isoflavones: The potential therapeutic agents for alcohol dependence

Keung

2003

Medicinal Research Reviews

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Daidzin is the active principle of Radix puerariae (RP), an herbal remedy that has been used apparently safely and effectively for the treatment of "alcohol addiction" in China for more than a millennium. It has been shown to reduce alcohol consumption in all animal models tested to date. A link between daidzin's capacity to reduce alcohol consumption and its ability to increase liver mitochondrial monoamine oxidase (MAO): aldehyde dehydrogenase (ALDH-2) activity ratio has been established. Daidzin analogs that potently inhibit ALDH-2 but not MAO are the most anti-dipsotropic, whereas those that also inhibit MAO are not. On the basis of these findings, it was proposed that the liver mitochondrial MAO-ALDH-2 pathway is the primary site of action of daidzin and that a biogenic aldehyde derived from the action of MAO mediates its anti-dipsotropic action. Therefore, to design and synthesize more potent anti-dipsotropic analogs, structural features that would enhance ALDH-2 inhibition and/or decrease MAO inhibition needed to be evaluated. Structure-activity-relationship (SAR) studies have revealed that a sufficient set of criteria for a potent anti-dipsotropic analog is an isoflavone with a free 4'-OH function and a straight-chain alkyl at the 7 position that has a terminal polar function such as -OH, -COOH, or -NH2. The preferable chain lengths for the 7-O-omega-carboxy, 7-O-omega-hydroxy, and 7-O-omega-amino substituents are 5 < or = n < or = 10, 2 < or = n < or = 6, and n > or = 4, respectively. Analogs that meet these criteria have increased potency for ALDH-2 inhibition and/or decreased potency for MAO inhibition and are, therefore, likely to be potent anti-dipsotropic agents.

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“…An extremely high dose of disulfiram was needed to affect Hoxd-4 expression. However, disulfiram exhibits various side effects, particularly on the central nervous system (Peachey et al, 1981), and it is ambiguous whether the effect on Hoxd-4 expression is caused by suppression of RALDH. Even when embryos were exposed to disulfiram throughout early embryogenesis until the prim-5 stage, cartilages formed normally when the embryos were transferred to normal seawater.…”

Section: Unsusceptibility Of Hoxd-4 and Shh Expression To Disulfiram mentioning

confidence: 99%

Induction of Bent Cartilaginous Skeletons and Undulating Notochord in Flounder Embryos by Disulfiram and α, α'-Dipyridyl

2001

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A Comparative Review of the Pharmacological and Toxicological Properties of Disulfiram and Calcium Carbimide

Cited by 51 publications

References 0 publications

Potential antimicrobial agents for the treatment of multidrug-resistant tuberculosis

Potential antimicrobial agents for the treatment of multidrug-resistant tuberculosis

Anti‐dipsotropic isoflavones: The potential therapeutic agents for alcohol dependence

Induction of Bent Cartilaginous Skeletons and Undulating Notochord in Flounder Embryos by Disulfiram and α, α'-Dipyridyl

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