LECTURE 3

Question 1

List the different modes of drug permeation into the body

Answer 1

Intracellular junctions
Lipid cell membranes
Transporters
Endocytosis
Exocytosis

Question 2

How do you order a series of drugs according to their efficiency in passive diffusion?

Answer 2

More hydrophobic drugs = more lipophilic
– More efficient at passive diffusion
More hydrophilic drugs = more lipophobic
– Less efficient at passive diffusion

Question 3

List examples of hydrophilic groups

Answer 3

Alcohol
Carboxylic acid
Amine
Ketone
Amide
Ester

Question 4

Describe hydrophilic groups

Answer 4

lipophobic
Typically polar & capable of H-bond formation

Question 5

Describe hydrophobic groups

Answer 5

Lipophilic
Typically, non-polar hydrocarbons

Question 6

List examples of hydrophobic groups

Answer 6

Methyl
Chloro
Phenyl
Hexyl
Cyclohexyl

Question 7

List common H-bond donors

Answer 7

• OH, - NH

Question 8

List common H-bond acceptors

Answer 8

• O, - N

Question 9

What is the effect of protonation in a drug on its solubility in water?

Answer 9

Lower water solubility
– neutral or + charged group

Question 10

What is the effect of deprotonation in a drug on its solubility in water?

Answer 10

Higher water solubility
– negatively charged group