HTHSCI 2H03 Lecture 2: Drug Metabolism and Elimination

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Lecture'2:'Drug'Metabolism'and'Elimination
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Lecture'2:'Drug'Metabolism'and'Elimination
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Lecture'2:'Drug'Metabolism'and'Elimination
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Document Summary

Drugs that are fat soluble diffuse across plasma membranes and are absorbed into the bloodstream. Drugs that are non-polar are easily distributed through body tissues. As with absorption only free drug molecules are distributed. Only free (unbound) drug molecules can be distributed into body tissues. Blood flow, organ size, and physical properties (solubility) of the drug dictate distribution. Fat-soluble drugs - may be able to enter the cell itself, example: steroids can act on our dna itself. Good - give medication to mom without hurting fetus (in most cases) These facilitate the mechanical barriers discussed above - they prevent the passage of drugs through these barriers. Parenteral administration: drugs distribute to target tissues and exert a biological/therapeutic effect. Oral administration: drugs are first distributed to the liver via the hepatic portal circuit. A fraction of the dose is metabolized "first-pass effect" and no longer available to exert a biological response.

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