Pharmacodynamics/Pharmacokinetics

Question 1

What is the most common route of membrane transport for Drugs INTO the cell?

Answer 1

Passive Diffusion

Question 2

What is the most common route of membrane transport for Drugs OUT OF the cell?

Answer 2

Active Transport

Question 3

What kinds of substances will be trapped in Acidic Compartments?

Answer 3

Weak Bases

Question 4

What kind of substances will be trapped in Basic compartments?

Answer 4

Weak Acids

Question 5

What is Bioavailability (F)? How is it calculated/measured?

Answer 5

Bioavailability (F) is the fraction of the Drug that reaches the bloodstream.

Bioavailability (F) = AUC(route used) / AUC (intravenous)

Question 6

How do you calculate the amount of drug absorbed?

Answer 6

Amount of Drug absorbed=

Salt Factor (S) * Bioavailability (F) * Drug Dose

Question 7

Is a Drug bioactive when it is bound to a protein? What is alpha a representation of in regards to this?

Answer 7

No, a Drug is not bioactive when it is bound to a protein, it is only bioactive when it is free.

Alpha is a variable representing = Free Drug / Protein-Bound Drug

Question 8

How do you calculate Therapeutic Index?

Answer 8

Therapeutic Index =

TD50 (Median Toxic Dose) / ED50 (Median Effective Dose)

Question 9

What is the name for the specific DNA sequence that a Transcription factor binds to within the promoter/enhancer region of a DNA sequence?

Answer 9

Transcription Factors bind to the Response Element within Promoters/Enhancers

Question 10

What specific area of a GPCR does the G Protein in the cytosol interact with?

Answer 10

A G Protein interacts with a GPCR typically around the cytoplasmic loop connecting the 5th (V) and 6th (VI) Transmembrane domains

Question 11

What specific Adenylate Cyclase do Gi Protein function to inhibit

Answer 11

Gi functions to inhibit Adenylate Cyclase 5, 6, and 13

Question 12

What do Gs and Gi Proteins share in common?

Answer 12

Although one activates Adenylate Cyclase and the other inhibits it, they both are able to exert their actions through the action of SRC Tyrosine Kinases

Question 13

What other way may Protein Kinase A be abbreviated besides PKA?

Answer 13

Protein Kinase A may be abbreviated PKA or R2C2

Question 14

What signaling molecules utilize Receptors Tyrosine Kinases with INTRINSIC tyrosine kinase Activity?

Answer 14

Growth factors utilize RTK’s with INTRINSIC Tyrosine Kinase activity. Including: Insulin, IGF-1, VEGF, EGF, NGF, PDGF

Question 15

What signaling molecules use RTK’s that DO NOT have intrinsic activity, and instead must use Cytosolic Tyrosine Kinases (JAK - Janus Kinases)?

Answer 15

Growth Hormone
Interferon
Leptin
EPO
IL 2-10, 15