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Terms in this set (12)
Michaelis Menten Equation
V=(Vmax x [drug]/Km + [drug])
What is Vmax?
[Drug] causing fastest turnover of enzyme
What is Km?
[Drug substrate] causing that makes enzyme turnover at 1/2 its maximum rate (Vmax/2)
Phase-I mediated enzyme reactions
Role of Phase I metabolism
Expose/create chemically reactive group from drug to facilitate further processing in Phase II
What happens to drug formed during Phase I?
Made water soluble for hepatic or renal excretion
Which family of Phase I enzymes is usually responsible for oxidation?
Cytochrome P450 enzymes
What type of enzymes are Cytochrome P450?
On-demand - induced only when drug is detected
Eg. of Phase II enzyme
What do UDP-glucuronosyl transferases do?
Conjugate water-soluble glucuronide to drug (this also deactivates drug)
Two reasons for drug metabolism
Deactivate pharmacological activity
Create water soluble metabolite for excretion
What happens to pharmacological activity of a drug if its enzyme is induced?
Activity decreases as drug is rapidly broken down
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