Week 2

Question 1

What is a medicine?

Answer 1

May contain more than 1 drug

- usually contains other substances such as stabilisers, solvents etc

Question 2

What does enteric coating mean?

Answer 2

Has a candy like coating, meaning it can travel through gut and protect against pH level so it makes it to destination

Question 3

What type of drugs end with ‘olol’

Answer 3

Beta blockers or B-adrenoreceptor blockers

Question 4

What type of drugs end with ‘caine’

Answer 4

Local anaesthetic

Question 5

What type of drugs end with ‘dipine’

Answer 5

Calcium channel blockers

Question 6

What type of drugs end with ‘mab’

Answer 6

Monoclonal antibodies

Question 7

What type of drugs end with ‘pril’

Answer 7

ACE inhibitors

Question 8

What type of drugs end with ‘statin’

Answer 8

HMG-CoA reductase inhibitors

• Anti colesterol

Question 9

What type of drugs end with ‘azoles’

Answer 9

antifungal agents

Question 10

Explain pharmacodynamics

Answer 10

What the drug does to the body

Question 11

Explain pharmcokinetics

Answer 11

What the body does to the drug

• literally the movement of drugs into and around the body

Question 12

Define pharmacodynamics

Answer 12

the way in which drugs interact with the body in order for therapeutic action to occur

Question 13

what are some specific targets for drugs?

Answer 13

• osmostic effects
• pH changes
• chelating agents
• disruption of cells

Question 14

What are some molecular targets for drug action?

Answer 14

• Receptors
• Ion channels
• Enzymes
• Carriers/transporters

Question 15

What can cause adverse effects?

Answer 15

Can be due to the drug acting:

• at the same/similar target elsewhere in the body
• at a different (but related) target

Question 16

How can drug selectivity be achieved?

Answer 16

• modifications to drug structure
• limiting access of drug
• route

Question 17

What is a ligand?

Answer 17

another name for a drug

Question 18

What is a recognition site?

Answer 18

another name for receptor

Question 19

What does antagonist mean?

Answer 19

a drug that is administered to occupy a receptor to prevent endogenous process occurring

Question 20

What is an agonist?

Answer 20

A drug that activates a receptor/response once landing on receptor

Question 21

Define affinity

Answer 21

ability to bind at a receptor site

Question 22

Define Efficacy

Answer 22

ability of a substance which has bound at a receptor site to generate a ‘stimulus’, hence to produce a biological effect

Question 23

Define Potency

Answer 23

relates to the dose or concentration at which a drug produces an effect

Question 24

How do drugs attach to receptors?

Answer 24

They mimic endogenous ligands

Question 25

How to antagonists work with receptors?

Answer 25

They block the actions of endogenous ligands

Question 26

What type of drug has affinity but on efficacy?

Answer 26

Antagonist

Question 27

What type of drug has both affinity and efficacy?

Answer 27

Agonist

Question 28

What are the 3 steps to determining how well a drug will work?

Answer 28

1. Binding 2. Activation 3. Transduction

Question 29

What is the timescale for Ligand-gated ion channels (ionotropic receptors)?

Answer 29

Milliseconds Examples: Nicotinic ACh receptors

Question 30

What is the timescale for G-protein-coupled receptors (metabotropic)?

Answer 30

Seconds Example: Muscarinic ACh receptor

Question 31

Which has a faster receptor - effector reaction? Ligand gated ion channels or G-protein coupled receptors?

Answer 31

Ligands gated ion channels

Question 32

What is the equation for dose-response

Answer 32

DR = D+R magnitude of response is determined by amount of DR complexes formed

Question 33

What is an orthosteric site?

Answer 33

the receptor site that an agonist lands in

Question 34

What is an allosteric site?

Answer 34

a secondary receptor site that can influence the response of an agonist.

Question 35

What is an allosteric agonist?

Answer 35

helps to amplify the agonist response

Question 36

Why is a log scale better than a linear scale?

Answer 36

It has a relative scale that accurately defines trends relative to the scale of the subject

Question 37

What is the EC50?

Answer 37

The half maximal effective concentration

Question 38

What does the EC50 - The half maximal effective concentration - mean

Answer 38

What concentration is required to see 50% of the maximal response

Question 39

What is Emax?

Answer 39

the maximal response when all receptors are occupied

Question 40

What is a full agonist?

Answer 40

produces a maximum response which is equal to the maximum response of tissue - the maximal response you can achieve from an agonist

Question 41

What is a partial agonist?

Answer 41

produces a maximum response which is less that the maximum response of the tissue

Question 42

what are the characteristics of a partial agonist?

Answer 42

- have affinity - sometimes more than a full agonist | - have efficacy - but it's lower than that of a full agonist

Question 43

What are the characterises of antagonists?

Answer 43

- Have affinity for the site - > eg. compatitive antaginist - antagonists binding to the site do not produce a biological effect - have affinity but no efficacy

Question 44

What are the various types of antagonists?

Answer 44

- competitive - non-competitive - irreversible

Question 45

What are the types of antagonism?

Answer 45

Physiological - opposing the effects of a second present drug Chemical - combines with a inactivates drug Pharmacokinetic - reduces active drug at receptor site Allosteric - bind to a different site on the receptor to affect ligand binding or stimulation of a response Competitive - binds to the same site as the agonist

Question 46

what are examples of common agonists?

Answer 46

- ventolin - morphine - adrenaline

Question 47

what are examples of common antagonists?

Answer 47

- narcan | - claratyne

Question 48

What is the therapeutic index?

Answer 48

provides an indication of effective drug dose vs toxicity on administration - used as a risk benefit tool

Question 49

Do we want the therapeutic index to be high or low?

Answer 49

High we want a high ratio

Question 50

What is the equation for therapeutic index?

Answer 50

Toxic dose 50/effective dose 50

Question 51

What are examples of drugs with a narrow therapeutic index?

Answer 51

- Warfarin - Carbamazepine - Digoxin - Lithium - Phenytoin - Tacrolomus - Amphotericin