Drug Metabolism Flashcards
Define Drug Metabolism:
A biochemical modification to pharmaceutical substance by livin organisms, ususally through activity of specialzed enzymes.
4 main sites of drug metabolism?
Liver
Lungs
Gut Lining
Kidneys
What is a prodrug?
A precursor to a drug which is converted to its active form by metabolism. e.g. Codeine
What are the 3 outcomes of metabolism on a drug?
Production of toxic metabolites
Activation (prodrugs)
Deactivation/loss of activity
What does the “wide substrate specificty” of metabolic enzymes mean?
It means many drugs can be metabolized by more than one enzyme
What are the 3 types of phase 1 metabolism reaction? [HOR}
Hydrolysis
or Oxidation
or Reduction
Whats the function of phase 1 metabolism?
To increase polarity of the compound and provide an active site for phase 2 to occur
What family of enzymes carries out phase 1 metabolism?
P-450 family of enzymes
Prefix for the enzymes in phase 1 metabolism?
CYP- is the prefix followed by no-letter-no.
3 enzymes in phase 1 metabolism?
CYP3A4
CYP2D6
CYP1A2
Where is CYP3A4 found?
In the Liver
What does CYP2D6 metabolize?
CYP2D6 metabolizes antidepressants, antipsychotics & ocnverts codeine to morphine
How does smoking affect CYP2D6?
CYP2D6 is induced by Smoking.
What does CYP1A2 metabolize?
Theophylline
Which phase 1 enzyme isnt induced by smoking?
CYP3A4 isnt induced by smoking