Term
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Definition
• Drug metabolism can produce metabolites that may be more active, equipotent, less active, toxic or with altered therapeutic activity as compared to the parent compound
• The type of metabolite generated is highly dependent on the chemical structure of the parent compound
• The metabolites may play significant role in both pharmacodynamic and pharmacokinetic properties of the drug
• DDIs involving metabolism should be carefully studied if there is production of active metabolites |
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Term
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Definition
o Options:
Half life = ~14 h -> Half life = 20-30h
10-40X more potent |
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Term
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Definition
| o The formation of oxidized analog is the primary inactivation pathway for 1,4-DHP type CCBs |
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Term
| Active à Inactive (Phase II) |
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Definition
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Term
| Active à Altered activity |
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Definition
o Altered activity can refer to altered therapeutic activity or toxicity
o Drug-induced hepatotoxicity is the most common type of toxicity seen with drugs
o Hepatotoxicity is potentiated by underlying liver disorders, age and external inhibitors/inducers of microsomal enzymes
o Other toxic reactions include; idiosyncratic reactions and drug/chemical induced carcinogenesis
o The toxic reactions are primarily due to generation of electrophiles or free radical containing metabolites
o General electrophilic reaction seen as a result of metabolism
o General free radical type reaction
o Drug-induced chemical carcinogenesis |
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