Small Molecule Drug Metabolism

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I. Why are drugs metabolized    

Small molecule drugs are xenobiotics, foreign molecules, that the human body attempts to deal with through a number of responses.  Some drugs are excreted from the human body intact.  Most drugs, however, need to be modified structurally to facilitate excretion.  These modification processes are called drug metabolism.  Drug metabolism is a detoxification function the human body possesses to defend itself from environment hostility.  When a person is sick, however, the body needs some kind of medication to fight the disease.  Ideally, a drug should reach the site of action intact, cure the disease, and leave the body after it completes its mission.  However, drug developers often face the dilemma that a potential drug is either metabolized/excreted from the body too fast, that the drug can not reach its therapeutic effect, or too slow, that it stays in the body for a long time, causing side effects.  (Remember the drug is a xenobiotic that the normal human body doesn't need.)  The study of drug metabolism, therefore, serves primarily two purposes: to elucidate the function and fate of the drug, and to manipulate the metabolic process of a potential drug.

 

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