knipp lecture

Question 1

Does cholesterol only have harmful effect on membranes?

Answer 1

No, it provides fluidity at lower levels

Question 2

statins can cause ….

Answer 2

too fluid of a membrane

Question 3

what are cell-based assays used for?

Answer 3

to test the drug’s ability to cross intestines membrane

Question 4

is intestinal transport passive or active

Answer 4

Passive (non-saturable)
-paracellular
-transcellular

Question 5

How is intestinal transport mediated?

Answer 5

carrier-mediated
-active
-facilitated diffusion

Question 6

what are the classes of metabolism

Answer 6

phase 1: metabolism of the main compound examples, decarboxylases, oxygenase, deamination
phase 2: metabolism through addition, conjugation
phase 3: transport- multidrug resistance

Question 7

where are the sites of drug metabolism?

Answer 7

first pass : GI epithelium/ liver
then in organs and in the bloodstream

Question 8

what are the objectives of drug metabolism?

Answer 8

-to eliminate the pharmacological activity of a drug
-to make a compound continuously more soluble until it cannot escape excretion, potentially by more then one route

Question 9

metabolism can activate a drug. true/ false

Answer 9

true ( although it is rare and in most cases a prodrug situation)

Question 10

What does phase I contain?

Answer 10

CYP ( oxidation, reduction)
-2D 2C 3A 1A 2B

Question 11

what does phase II contain?

Answer 11

conjugation
-SULT, methyl transferase, UGT, NAT

Question 12

What cytochrome family is phase I metabolism focused on

Answer 12

P450 and in particular CYP3A4