Week 10
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Polymorphism – Drug interaction
Results in an exaggerated effect or minimal effect on the substrate Inhibitor: An enzyme inhibitor is a molecule, which binds to enzymes and decreases their activity. Inducer: An enzyme inducer is a type of drug that increases the metabolic activity of an enzyme either by binding to the enzyme and activating it, or by increasing the expression of the gene coding for the enzyme
Polymorphism – Drug interaction extensive metabolizers (inhibitors)
Extensive Metabolizers (EM) - Inhibitors Extensive metabolizer —– level of substrate drug is normally low due to rapid metabolism by the enzyme. An inhibitor to the enzyme will inhibit the extensive metabolism and cause significant elevations in the substrate drug.
Polymorphism – poor metabolizers - inhibitors
In a poor metabolizer, the level of substrate drug remains high because the metabolism of the substrate is much less than normal. When an inhibitor is added, the additional inhibition of metabolism is not much greater than is already occurring in the PM. The effect of inhibitor is less in a PM than in normal metabolizers.
Polymorphism – Drug interaction extensive metabolizers (Inducers)
Level of substrate drug is lower than in a normal metabolizer due to rapid metabolism. The addition of an inducer does not cause a greater difference in the level of substrate because the metabolism is already increased greatly. The drug interaction might not occur.
Polymorphism – poor metabolizers - Inducers
Level of substrate drug is higher than expected in normal metabolizer because of the lower metabolism of substrate. The addition of inducer will cause a significant increase in the metabolism of the substrate -much lower level of substrate than expected in a normal metabolizer. Drug interaction may occur to a greater extent. Drug interaction may result in substrate levels like those of normal metabolizers.