Chem test 4

Question 1

the study of how a drug affects the organism

Answer 1

Pharmacodynamics

Question 2

Pharmacokinetics

Answer 2

the study of how the organism affects the drug

Question 3

Receptor subtypes include:

Answer 3

Enzymes
Ion Channels
Membrane receptors

Question 4

Drugs bind due to what chemical interactions

Answer 4

Covalent bonds
Hydrophobic interactions
Electrostatic interactions (intermolecular forces)
Stereospecific interactions (enantiomers)

Question 5

Affinity is

Answer 5

how well the drug binds to the receptor

Question 6

how well the drug produces its desired effect is the definition of

Answer 6

Efficacy

Question 7

term used to compare the relative affinity of competing drugs

Answer 7

Potency

Question 8

Pharmacodynamics includes the effects of drugs on the body and their:

Answer 8

Site of Action
Mechanism of Action
Receptor Binding
Postreceptor Effects
Chemical Interactions

Question 9

Pharmacokinetics studies

Helps to better understand the following:

Answer 9

ADME

Drug administration
Therapeutic dosing
Time intervals between drug dosing
Toxic dosing

Question 10

Absorption rate determines time to

Answer 10

maximal concentration at the receptor to produce peak effect.

Question 11

how much of the administered drug is actually absorbed. (typically used for oral administration)

Answer 11

Bioavailability

Question 12

Factors affecting bioavailability include:

Answer 12

molecular weight of the drug
Intestinal motility
Drug stability (especially pH sensitivity)
Drug interactions
Blood flow
Drug formulation
Gastric emptying (food slows this process)
First pass metabolism (typically in the liver)

WISDBFGF

Question 13

Effectiveness of the movement of the drug throughout the body is influenced by

Answer 13

Blood
Total body water
Extracellular fluids
Lymphatic fluids
Cerebrospinal fluids
Protein-binding

Question 14

Why is drug solubility important?

Answer 14

Drug solubility properties help determine ability of drug to be distributed to the desired receptor site.

Question 15

Metabolism is the breakdown of drugs into metabolites, what does this do?

Answer 15

Prodrugs – convert from inactive form to active form
Typically inactivates the drug ahead of excretion

Question 16

Common processes of metabolism

Answer 16

Hydrolysis (esters, amides, and nitriles)
REDOX reactions (Cytochrome P450 enzymes in the liver)

Question 17

Most drugs fail during the ________ phase

Answer 17

discovery

Question 18

what percent of drugs fail in clinical testing?

Answer 18

90%

Question 19

What is the Lipinski rule of 5?

Violation of more than one “rule” predicts _______

Answer 19

• Hydrogen bond donors (typically amines and alcohols)
• Hydrogen bond acceptors (total number of N, O, and F)
  Want less than 10 total donors and acceptors
• Molecular weight (MW) max is 500
• Calculated Partition Coefficient (C log P)(a ratio of the solubility of the drug in oil versus water) threshold is 5

a new chemical entity is non-orally available

Question 20

Low MW drugs with a low cLogP can _____________

Answer 20

easily cross membranes.

Question 21

Potential drug compounds must have a mix of ____________

Answer 21

hydrophilic and lipophilic groups

Question 22

what are the Structural alerts – certain functional groups that have been linked to increased toxicity due to their metabolites:

Answer 22

Thiophenes
Aromatic anilines
Polycyclic aromatic hydrocarbons
Aliphatic halides
Nitroaromatics

Question 23

Drug efficacy is directly related to

Answer 23

the concentration of the drug at its site of action.

Question 24

Absorption of drugs into the bloodstream is dependent on

Answer 24

the acid/base properties of the drug and the pH at the site of absorption

Question 25

What happens to transport at high drug concentrations?

Answer 25

transport plateaus due to limited number of transport proteins available
Can lead to competition with structurally similar compounds.

Question 26

Small Drugs are how many Da?

Answer 26

(< 50 Da)

Question 27

Lipophilic Drugs are how many Da?

Answer 27

(50 – 500 Da)

Question 28

Transport and drug distribution is affected by

Answer 28

the size and charge of the drug molecule

Question 29

What kind of transport is used for small drugs?

Answer 29

bulk flow

Question 30

What kind of transport is used for lipophilic drugs?

Answer 30

passive transport

Question 31

What kind of transport is used for ionized drugs?

Answer 31

active transport