Active Metabolities

Many medications owe their effects to “active metabolites.” Discuss the effects that an active metabolite can have on the activity of a drug. Pick 3 drugs (you are encouraged to perform literature searches on your own) that are known to have active metabolites (prodrugs included) and discuss them in a few paragraphs (~250 words for each drug you choose, but limit your essay to 750 words total)–include their chemical structure as well.

Hints: focus on the enzymes and mechanisms responsible for producing those metabolites (e.g. is the active drug formed at a certain pH within the body? does CYP metabolism generate the active component?, etc…), and how the pharmacological effects of those metabolites compare to the parent drug (affinity, efficacy, higher permeation of the BBB, longer clearance/elimination times from the body, etc…). Cite at least TWO references.

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