RX318 EXAM 4 COMPILATION WITH COMPLETE SOLUTIONS!!

RX318 EXAM 4 COMPILATION WITH COMPLETE SOLUTIONS!!



Partition coefficient

Relative lipid/water distribution of a drug in its nonionized state (logP)



Substituent contributes more to water solubility than to lipid solubility

(-) π value

1 multiple choice option



Substituent contributes more to lipid solubility than to water solubility

(+) π value

1 multiple choice option



Log P value > +0.5

Water insoluble

1 multiple choice option



Log P value < +0.5

Water soluble

1 multiple choice option



Log D

Distribution coefficient of a drug between a lipid bilayer and a water layer at a specific
pH



Lipinski's Rule of 5 (bad oral bioavailability)

,- MW > 500

- calc Log P > 5

- H-bond donors > 5

- H-bond acceptors > 10



Rotatable bonds

Any single bond, not in a ring, bound to a nonterminal heavy atom



≤ 10 RotBs

Good oral bioavailability

1 multiple choice option



MW > 500

Bad oral bioavailability

1 multiple choice option



calc Log P > 5

Bad oral availability

1 multiple choice option



H-bond donors > 5

Bad oral availability

1 multiple choice option



H-bond acceptors > 10

Bad oral availability

1 multiple choice option

, Topological polar surface area

The sum of the surface area of polar atoms (usually O, N, and attached H) in a molecule



Sum of H-bond donors and acceptors ≤ 12

Good oral bioavailability

1 multiple choice option



Rule of 4 (4)

- MW < 400

- N+O ≤ 4

- Basic pKa < 8

- TPSA < 60Å




Rule of 4

Characteristics of drugs that are not P-gp substrates and are more likely to get into the
CNS




MW < 450

Successful CNS drug candidate

1 multiple choice option




cLog P < 5

Successful CNS drug candidate