6/10 Intro To PD

Question 1

Drug define

Answer 1

A chemical substance of known structure, other than a nutrient or essential dietary ingredient, which, when administered to a living organism, produces a biological effect

Question 2

Pharmacodynamic

Answer 2

Effect of drug on the body

Question 3

Pharmacokinetic

Answer 3

Effect of body on drug

Question 4

Main types of drug targets

Answer 4

Carrier molecules / transporters
Enzymes
Ion channels
Receptors

Question 5

Define pro drug

Answer 5

Biologically inactive compound which can be metabolised in the body to produce a drug

Question 6

Types of enzymes

Answer 6

Inhibitor, false substrate, pro-drug

Question 7

Ion channels

Answer 7

Protein molecules that span across the cell membrane allowing the passage of ions from one side of membrane to other side

Question 8

Drug that binds to receptor and blocks the effect of endogenous chemical mediator

Answer 8

Antagonist

Question 9

Agonist

Answer 9

Drug that finds to the receptor and generates an effect

Question 10

Fastest receptor

Answer 10

Ligand-gated ion channels
Milliseconds

Question 11

G- protein coupled receptors
Time scale and example

Answer 11

Time = seconds

Example = muscarinic, ACh receptor

Question 12

Kinase- linked receptors
Time scale and example

Answer 12

Time = hours
Cytokine receptors

Question 13

Nuclear receptors
Time scale and example

Answer 13

Hours
Oestrogen receptor

Question 14

Ligand-gated ion channel receptors
Time scale and example

Answer 14

Time-milisecond
Example = nicotinic, ACh receptor

Question 15

What cellular responses do nuclear receptors regulate?

Answer 15

Responses to hormones such as vitamin D3

Question 16

Advantage of drug to have high specificity for its target?

Answer 16

Because it reduces the incidence of side effect

• if drug binds non-specifically to lots of different targets, it can have lots of different effects

Question 17

Define affinity

Answer 17

How avidly a drug binds to its target site

Question 18

Define efficacy

Answer 18

The drugs ability to activate the receptor once it has bound to it

Question 19

Law of mass action

Answer 19

States the rate of a chemical reaction is proportional to the product of the concentrations of the reactants

Question 20

High concentration of drug means it has Lower affinity why? Law of mass

Answer 20

Because system in equilibrium- adding more drug pushes equilibrium over to the right, producing more drug-receptor complex

Question 21

How to study the relation between drug concentration and effect can be studied by using?

Answer 21

A relevant bioassay

e.g. Organ bath

Question 22

Define potency

Answer 22

Measure of drug activity expressed in terms of the amount required to produce an effect of given intensity

Question 23

Measure of efficacy

Answer 23

E MAX

Question 24

Measure of potency

Answer 24

EC50

Question 25

Partial agonist define

Answer 25

Drug with agonist effects but where a submaximal effect is produced due to a reduced efficacy compared to a full agonist

Question 26

Competitive antagonism

Answer 26

An antagonist and another drug compete for the same binding site

Question 27

Efficacy

Answer 27

Parameter that describes the ‘strength’ of the agonist-receptor complex in evoking a tissue response

Question 28

Potency

Answer 28

Concentration/amount of the drug required to produce a defined effect

Question 29

Why can’t you construct a concentration - response curve of an antagonist

Answer 29

Antagonist has no efficacy

Question 30

When does particu agonist act as an antagonist?

Answer 30

In the presence of a full agonist