3

Question 1

Pill negatives

Answer 1

patient compliance, drug absorption is slower and rapid metabolism may cause failure to reach an optimum concentration.

Question 2

With pills,

Answer 2

OD is less likely due to absorption and time to react.

Question 3

With pill absorption,

Answer 3

time and surface area matter. Mouth and esophagus arenty too important, colon is not important, as the drug is gone by that time.

Question 4

Main site of pill absorption

Answer 4

stomach and small intestine.

Question 5

Most drugs have to be ——— enough to get throguh numerous cell membranes during absorption

Answer 5

lipophilic

Question 6

The larger the ——the more likely drug will be absorbed by passive diffusion

Answer 6

partition constant

Question 7

Pores are

Answer 7

always open

Question 8

ABC transporters (use ATP) can

Answer 8

kick drugs out of cells - can be overexpressed, creating drug resistance. Problem is that these aren’t specific for one drug, so they can leadto resistance of a group of drugs.

Question 9

SLC transporters (exchange Na+ or K+) important for

Answer 9

transport of certain drugs that are organic acids or bases

Question 10

Intravenous are faster to ———, can’t affect ——–

Answer 10

difuse

adverse effects/limit them easily

Question 11

Intramuscular/subcutaneous

Answer 11

i) Good if problems with enteric absorption or inactivation
ii) Many smaller drugs absorbed similarly as from the gut with these routes and bigger things as well as proteins can get in through gaps.

Question 12

For intramuscular/subcutaneous, ———— can retard absorption (diminish circulation)

Answer 12

Vasoconstriction

Question 13

Topical = Absorption of some ——– drugs enhanced by ——

Answer 13

lipophilic

solvents (DMSO)

Question 14

Water soluble drugs move through —-

Answer 14

endothelial gaps and are lsower

Question 15

Bigger proteins move into blood from

Answer 15

transcytosis - vesicles that form and are internalized.

Question 16

Restricted distribution into CNS- blood brain barrier

Answer 16

No gaps in endothelium, sheath surrounds, drugs efficiently transported out of endothelium back into blood stream

Question 17

Q/C = Vd, the volume of distributio

Answer 17

Q = initial mg of drug, C = mg/L of plasma sample after a bit.

Question 18

Vd higher than total fluid volume (41L)

Answer 18

means it’s going somewhere (sticking to protein, tissues), drug is getting metabolized, excreted, leading to low concentration in plasma

Question 19

The volume of distribution (VD) is the

Answer 19

theoretical volume that would be necessary to contain the total amount of an administered drug at the same concentration that it is observed in the plasma. It is defined as the distribution of a medication between plasma and the rest of the body after oral or parenteral dosing.

Question 20

Drug metabolism

Phase I: Add (uncover)

Answer 20

functional group (make more polar)

Usually done through oxidations (P450 enzymes, flavin monooxygenases

Question 21

Drug metabolism

Phase II:

Answer 21

Conjugation

Question 22

Smooth E.R. of hepatocytes:

Answer 22

membrane bound enzymes that metabolize drugs (microsomes)

Question 23

Morphine inactive,, but 6-glucuronide is

Answer 23

active form - done in smooth er of hepatocytes

Question 24

Non microsomal metabolism (in liver and other tissues)

Answer 24

Microsomal enzymes designed to remove foreign substances

Non-microsomal metabolism when drug mimics natural substance

Question 25

in glomerular filtration, ———– is a major filter

Answer 25

basement membrane

Question 26

Drugs that are filtered but not reabsorbed or secreted back clear at

Answer 26

130 mL/min

If Vd is 12 L, the drug will have a t1/2 of about 1 hr in the plasma

Question 27

2. Drugs that are actively secreted and not reabsorbed may clear as fast as

Answer 27

650 mL/min

If Vd is 12 L, the drug will have a t1/2 of about 13 min in the plasma