pharmacology 2 Flashcards
1
Q
What happens to oral absorption as molecules become larger in size?
A
Oral absorption decreases with increasing molecular weight
According to Lipinski’s rules for optimal oral absorption a drug should be <500g/mol
2
Q
What determines drug absorption?
A
Drug size
Drug solubility
Drug ionisation
Membrane transporters
3
Q
How can solubility of lipids be measured in drugs?
A
Log(P)
Polar Surface Area
4
Q
What membrane proteins can affect oral absorption most dramatically?
A
p-Gp
5
Q
What gene encodes p-Gp?
A
ABCB1
6
Q
How are prodrugs used to improve bioavailability?
A
Hydrophilic groups can be masked by adding metabolism-sensitive lipophilic substituents.
7
Q
What is drug distribution?
A
The reversible transfer of a drug from
one location (e.g. blood) to another
(e.g. heart, brain or lung tissue)
