Chapter 4

Question 1

DEFINE

What are the 4 steps in Pharmacokinetics?

Answer 1

1. Absorption
2. Distribution
3. Biotransformation
4. Elimination

Question 2

EXPLAIN

What is occuring in the absorption step of Pharmacokinetics?

Answer 2

Drug is administered and is absorbed into the blood stream

Question 3

EXPLAIN

What is occuring in the Distribution step of Pharmacokinetics?

Answer 3

Drug is passed through the bloodstream and into the organs, penetrating the membrane

Question 4

EXPLAIN

What is occuring in the Biotransformation step of Pharmacokinetics?

Answer 4

The drug is broken down into metabolites by enzymes

Question 5

EXPLAIN

What is occuring in the Elimination step of Pharmacokinetics?

Answer 5

The drug and/or metabolites are eliminated from the body

Question 6

LIST

What are the 8 routes of administration?

Answer 6

1. Inhalation
2. Intramuscular
3. Intravenous
4. Oral
5. Nasal and Mucosal membrane
6. Subcutaneous (into the fatty tissue)
7. Sublingual
8. Transdermal (absorbed through an external patch)

Question 7

EXPLAIN

What does the Henderson-Hassleback Equation calculate?

Answer 7

The ratio of unionized to neutral drug molecules in a drug

Question 8

EXPLAIN

If a drug has a pKa close to the local pH, will it have more neutral or ionized molecules than those with a pKa further than from the local pH?

Answer 8

it will be more neutral

Question 9

DEFINE

Liberation

in the drug processing

Answer 9

The process of drug molecules seperating from the delivering form

want drugs to absorb in intestines

Question 10

DEFINE

Distribution

Answer 10

The passage of a drug from the bloodstream to sites in the body

Question 11

DEFINE

Bioavailability

Answer 11

The ability of a drug to reach a site of action

Question 12

DEFINE

Nonspecific Binding

Answer 12

The binding of a drug to site thats are not the intended target
* protein binding
* Depot binding

Question 13

DEFINE

What is the Blood-brain Barrier?

Answer 13

The barrier that surrounds the blood vessels in the brain to prevent substances in the blood from entering the brain

Question 14

DEFINE

What is passive diffusion?

Answer 14

The diffusion of molecules across the Blood-Brain Barrier

Question 15

LIST

What are the 3 requirements for being able to do passive diffusion?

Answer 15

1. Lipid/Fat soluble
2. Neutral charge
3. Small

Question 16

DEFINE

Active Transport

Answer 16

The use of membran channels or transporters that allow the passage of chemicals

Question 17

DEFINE

Biotransformation

Answer 17

The conversion of a drug into one or more metabolites

Question 18

EXPLAIN

How many phases are there in biotransformation?

Answer 18

2

Question 19

EXPLAIN

What happens in phase 1 of biotransformation?

Answer 19

• CYP450 family of enzymes
• Usually generates atleast 1 water soluble motabolites

Question 20

EXPLAIN

What happens in phase 2 of biotransformation?

Answer 20

• Catabolism via conjugation
• Become bigger, charged as less lipid soluble

conjugation: transfer of genetic material between bacterial cells

Question 21

DEFINE

First-Pass metabolism

Answer 21

Metabolism that occurs before a drug enters circulation

Question 22

DEFINE

Active Metabolite

Answer 22

A drug’s metabolite that has its own physiological effect

Question 23

DEFINE

Prodrug

Answer 23

A physiologically weak or inactive compounds metabolized in the body to produce an active drug

Question 24

DEFINE

Elimination Rate

Answer 24

An amount of drug eliminated from the body over time

Question 25

# LIST What are the 2 types of elimination?

Answer 25

1. Zero-Order Kinetics (Constant) 2. First-Order Kinetics (Non-Constant/Half life)

Question 26

# EXPLAIN How does zero-life kinetics work?

Answer 26

the drug is eliminated at the same rate no matter how much how much of the drug is in the system

Question 27

# EXPLAIN How does first-order kinetics work?

Answer 27

The drug is eliminated in half lives, eliminating half of what is currently in the system each cycle

Question 28

# DEFINE Steady-State Drug Concentration

Answer 28

A sustained concentration of a drug in the body over multiple doses | Slow release formulation using its half life

Question 29

# DEFINE Binding Affinity

Answer 29

How well a drug binds to its receptor

Question 30

# DEFINE Receptor Efficacy

Answer 30

The effect a drug has on its receptor

Question 31

# LIST What are the 4 types of Receptor Efficacy?

Answer 31

1. Agonist 2. Partial Agonist 3. Antagonist 4. Inverse Agonist

Question 32

# DEFINE Agonist | Receptor Efficacy

Answer 32

The drug activiates the neurotransmitter receptor as expected

Question 33

# DEFINE Partial Agonist | Receptor Efficacy

Answer 33

The drug has a weaker efficacy for activating receptors

Question 34

# DEFINE A**nta**gonist | Receptor Efficacy

Answer 34

The drug fails to activate a receptor and prevents another neurotransmitter from activating the receptor * **Competitive**: Prevents NT binding * **Noncompetitive:** Does not prevent binding; still cannot activate

Question 35

# DEFINE Inverse agonist | Receptor Efficacy

Answer 35

Produces the opposite effect of the natural ligand

Question 36

# DEFINE Allosteric Binding Site

Answer 36

A binding site on a receptor that is different than where the neurotransmitter binds

Question 37

# LIST What are the 5 types of drug tolerances?

Answer 37

1. Pharmacokinetics 2. Pharmacodynamic 3. Behavioural 4. Conditioned 5. Cross

Question 38

# DEFINE Pharmacokinetic Tolerence

Answer 38

Reduces the amount of drug reaching the target organ

Question 39

# DEFINE Pharmacodynamic Tolerance

Answer 39

Reduces the responsiveness of target organ to the drug

Question 40

# DEFINE Behavioural Tolerance

Answer 40

Reduced drug effect from learned behaviour and enviromental cues

Question 41

# DEFINE Conditioned Tolerance

Answer 41

Conditioned physiological responses counteract the drugs effects

Question 42

# DEFINE Cross Tolerance

Answer 42

The frequent use of one drug that leads to a tolerance for other drugs with similar biological functions

Question 43

# DEFINE Withdrawal Syndrome

Answer 43

A collection of responses that occur when a drug is no longer administered | Both physical and psychological