Leys- Drug Resistance

Question 1

What is the primary site for drug metabolism?

Answer 1

Liver

Question 2

Increase in drug ____ allows the drug to be excreted.

Answer 2

hydrophilicity

Question 3

Metabolic products are less pharmologically ___ than the substrate drug

Answer 3

active

Question 4

____ prodrugs are concerted into their active forms

Answer 4

inactive

Question 5

What are the three potential outcomes of drug metabolism

Answer 5

o increase in drug hydrophilicity allowing drug to be excreted (liver)
o metabolic products are less pharmologically active than the substrate drug
o inactive prodrugs are converted into their active forms (liver)

Question 6

Mechanisms for drug resistance (DEAAA)

Answer 6

o Decreased permeability of drug
o Alteration of target site for drug
o Enzymatic inactivation of drug
o Active transport of drug out of cell (tends to increase resistance to many drugs)
o Amplification of the gene coding for the drugs target

Question 7

An ___ in DNA repair activity can ___ effectiveness of drugs that target DNA

Answer 7

increase

decrease

Question 8

What can an increase in DNA repair activity decrease?

Answer 8

effectiveness of drugs that target DNA

Question 9

What can cause multi-drug resistance?

Answer 9

increase in the amount of transporter proteins on the cell that pump many different drugs

Question 10

___ in the amount of transporter proteins on the cell can cause multi-drug ___

Answer 10

Increase

resistance