Chapter 4

Question 1

What is bio transformation

Answer 1

Is breaking down of a drug into its metabolites via the action of various enzymes

Question 2

What is metabolite

Answer 2

This is the product from enzymatic transformation of a drug

Question 3

Where does bio transformation typically occur

Answer 3

In liver, but can be in places like stomach or kidneys

Question 4

Explain phase 1 of bio transformation

Answer 4

Involves p450 enzymes and produces water soluble mtabolites

Question 5

What are Active metabolites

Answer 5

These are metabolites that have useful pharmacological effects

Question 6

What happens in phase 2 of bio transformation

Answer 6

It involves the process of conjugation for metabolites produced in phase 1 that makes them less able to passively diffuse across memebranes

Question 7

What are agonist

Answer 7

They activate neurotransmitter receptors

Question 8

Partial agonists define

Answer 8

Activate receptors but to a lesser degree that full agonist drugs
Used in treatment of drug addiction

Question 9

Ceiling effect

Answer 9

Not strongly enough to cause overdose but stimulates the recptors

Question 10

Antagonist

Answer 10

Fail to activate a neurotransmitter receptor or blocks it.
Work on ionotropic receptors

Question 11

Competitive antagonist

Answer 11

Bind and block neurotransmitter binding

Question 12

Non competitive antagonist

Answer 12

Will bind and inactivate channel.

Question 13

Allosteric regulators

Answer 13

Substances that bind to protein but do not activate the protein
Upregulate or downregulate receptor response to nt

Question 14

Positive modulators

Answer 14

Bind to allosteric sites on receptor and increase ability of nt to bind or activate the receptor

Question 15

Negative modulators

Answer 15

Bind to allosteric sites and decrease the ability of neurotransmitter to bind and/or activate the receptor.

Question 16

Chronically asmisnistration

Answer 16

Repeated use of drug making ne adapt to it

Question 17

Tolerance

Answer 17

Caused by chronic use
Is a drug adaptation that requires escalating drug doses to get desired effects

Question 18

Pharmacokinetic tolerance

Answer 18

Changes in metabolic process.
Also called drug dispositional tolerance

Question 19

Pharmacodynamic tolerance

Answer 19

Changes at the synapse
Changes in the number of neurotransmitter receptors. (The receptors get worn out)
Occurs when there is a reduced response to drug’s site of action
Can be seen in drugs like ecstasy.

Question 20

Behavioral tolerance

Answer 20

Reduced behavioral response to drug’s effect.
Involves cognitive adaptation to chronic drug use.
E.g., people performing better under influence of alcohol

Question 21

Conditioned or contingent tolerance

Answer 21

Also cognitive adaptation
Associate environmental stimuli with drug taking.

Question 22

Cross-tolerance

Answer 22

Drugs acting on similar receptors or neurotransmitters.
So if tolerant to heroin, you get tolerant to drugs in same class.

Question 23

Sensitization

Answer 23

Chronic use cause increase in responsiveness to drug

Question 24

Drug dependence

Answer 24

Occurs when a user needs a drug in order to function normally.
Becomes apparent after withdrawal symptoms are seen

Question 25

Withdrawal syndrome

Answer 25

Set of physicali and psychological symptoms that occur when a person stops using a drug use after dependence

Question 26

Physical dependence

Answer 26

Presence of physical withdrawal symptoms after cessation. For example, pain, diarhea

Question 27

Psychological dependence

Answer 27

Changepresence of psychological withdrawal symptoms, e.g., changes in mood and strong drug cravings