Module 4a Pharmaceutically Active Components

Question 1

Definition of Pharmacodynamics

Answer 1

The study of how a drug affects the organism/body

Question 2

Definition of Pharmacokinetics

Answer 2

The study of how the organism/body affect the drug.

The study of how absorption, distribution, metabolism, and excretion of drug from the body.

Question 3

What does Pharmacodynamics include?

Answer 3

Site of Action
Mechanism of Action
Receptor Binding
Post-receptor Effects
Chemical Interactions

Question 4

What can affect pharmacodynamics?

Answer 4

Disease/Disorder
Age
Drug-Drug Interactions

Question 5

What are three receptor subtypes?

Answer 5

Enzymes
Ion Channels
Membrane Receptors

Question 6

What are 4 chemical interactions involved with drug binding?

Answer 6

Electrostatic interaction (intermolecular forces)
Hydrophobic Interactions
Covalent Bonds
Stereospecific Interactions (enantiomers)

Question 7

What are 3 drug properties?

Answer 7

Affinity - how well the drug binds to the receptor

Efficacy - how well the drug produces its desired effect

Potency - term used to compare the relative affinity of competing drugs

Question 8

What are two categories of drugs?

Answer 8

Agonist - bind and activates receptors

Antagonist - bind, but do not activate receptors

Question 9

What are two types of antagonist drugs?

Answer 9

Competitive - bind reversibly

Non-competitive- either binds irreversibly or binds to create allosteric effects that diminish agonist’s ability to bind to a different receptor

Question 10

___________ affects the ability of the drug to give its desired effect.

Answer 10

Concentration

Question 11

What is Bioavailability?

Answer 11

How much of the administered drug is actually absorbed. Typically used for oral administration.

Question 12

What are 8 factors affecting bioavailability?

Answer 12

1. Molecular weight of the drug.
2. Drug Formulation
3. Drug Stability (pH sensitivity)
4. First Pass Metabolism (Liver)
5. Blood Flow
6. Gastric Emptying
7. Intestinal Motility
8. Drug Interactions

Question 13

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

Answer 13

Drug Solubility

Question 14

What are two common processes of metabolism?

Answer 14

Hydrolysis (esters, amides, nitriles)

REDOX reactions (Cytochrome P450 enzymes in the liver)

Question 15

What are 4 main routes for excretion?

Answer 15

1. Kidneys (majority of drugs)
2. Feces (unabsorbed drugs from the bile)
3. Lungs (inhaled anesthetic drugs)
4. Sweat (not very common)

Question 16

What is the Lipinski Rule of 5?

Answer 16

Describes drug potential for a new chemical entity (NCE).
Used as a tool to measure a NCE’s potential bioavailability.

Question 17

The Lipinski Rule of 5 is based on what four factors?

Answer 17

1. Hydrogen bond donors (typically amine and alcohols) - no more than 5.
2. Hydrogen bond acceptors (total # of N, O, and F) - no more than 10
3. Molecular Weight - less than 500
4. Calculated Partition Coefficient (cLogP) - no more than 5

*Violation of more than one of these rule predicts NCE is not orally available.

Question 18

Structural alerts of certain functional groups that have been linked to increase toxicity due to their metabolites. Name 5 examples listed in lecture.

Answer 18

1. Aromatic anilines
2. Nitroaromatics
3. Aliphatic Halides
4. Polycyclic Aromatics Hydrocarbons- 3 or more rings together
5. Thiophenes