Pharmaceutical Sciences Encyclopedia 2010
DOI: 10.1002/9780470571224.pse120
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The Role of Drug Metabolism in Toxicity

Abstract: Drug toxicity and the factors that govern it are quite complex. In drug discovery, toxicity can depend on factors that may be species‐specific, thus forcing toxicologists to determine the relevance of toxicity in animals to that in humans. The article presents some key characteristics of the common enzymes encountered in metabolic clearance of drugs.

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Cited by 4 publications
(6 citation statements)
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“…If the reactive species formed in the CYP are able to escape the active site and bind covalently to other proteins or nucleic acids, this can culminate in adverse drug reactions and toxicity. 116 Indeed, in the majority of cases, toxicity is caused by the actions of such reactive metabolites, rather than by the parent chemicals. 116 Generation of such ROMs is also a major reason for the failure of many drugs in pre- and postclinical trials.…”
Section: Cytochrome P450 Enzymesmentioning
confidence: 99%
See 1 more Smart Citation
“…If the reactive species formed in the CYP are able to escape the active site and bind covalently to other proteins or nucleic acids, this can culminate in adverse drug reactions and toxicity. 116 Indeed, in the majority of cases, toxicity is caused by the actions of such reactive metabolites, rather than by the parent chemicals. 116 Generation of such ROMs is also a major reason for the failure of many drugs in pre- and postclinical trials.…”
Section: Cytochrome P450 Enzymesmentioning
confidence: 99%
“… 116 Indeed, in the majority of cases, toxicity is caused by the actions of such reactive metabolites, rather than by the parent chemicals. 116 Generation of such ROMs is also a major reason for the failure of many drugs in pre- and postclinical trials. 69 …”
Section: Cytochrome P450 Enzymesmentioning
confidence: 99%
“…The American Academy of Pediatrics estimates that compliance in children is as low as 53%, indicating that children frequently fail to take medications properly. Noncompliance can lead to: (1)persistent symptoms, (2) need for additional doctor visits or even hospitalizations, (3) worsening of condition, (4) need for additional medications, (5) increased healthcare costs and (6) development of drug-resistant organisms in cases of infectious diseases [2].…”
Section: Introductionmentioning
confidence: 99%
“…Sweet, umami, and bitter tastes are triggered by the binding of molecules to G protein-coupled receptors on the cell membranes of taste buds. Saltiness and sourness are perceived when alkali metal or hydrogen ions enter taste buds, respectively [4].As taste senses both harmful and beneficial things, all basic tastes are classified as either aversive or appetitive, depending upon the effect the things they sense have on our bodies [5].Sweetness helps to identify energy-rich foods, while bitterness serves as a warning sign of poisons [6].…”
Section: Introductionmentioning
confidence: 99%
“…By coordinating the right type of coating material it is possible to completely mask the taste of a bitter drug, while at the same time, not adversely affecting the intended drug release profile 50 . Any nontoxic polymer that is insoluble at pH 7.4 and soluble at acidic pH would be an acceptable alternative for taste masking 51 . This technology involves softening the active blend using the solvent mixture of watersoluble polyethylene glycol, using methanol and expulsion of softened mass through the extruder or syringe to get a cylinder of the product into even segments using heated blade to form tablets.…”
Section: >10andpercent;mentioning
confidence: 99%