Block A Lecture 1: Introduction to Pharmacology

Question 1

What is pharmacology?

Answer 1

The study of the mechanisms of action, uses and unwanted effects of drugs on living tissues
(Lecture 1, Part 1, Slide 5)

Question 2

What is a drug?

Answer 2

A substance that modifies the activity of living tissue either positively or negatively
(Lecture 1, Part 1, Slide 5)

Question 3

What is physiology?

Answer 3

The science of how living tissues function
(Lecture 1, Part 1, Slide 5)

Question 4

What 2 effects can drugs have on physiology?

Answer 4

It can interfere with either normal or abnormal physiology
(Lecture 1, Part 1, Slide 5)

Question 5

What is therapeutics?

Answer 5

The study or use of pharmacological agents in disease states
(Lecture 1, Part 1, Slide 6)

Question 6

What can many therapies produce?

Answer 6

Unwanted adverse effects
(Lecture 1, Part 1, Slide 6)

Question 7

What is pathology?

Answer 7

The study of the causes and effects of a disease or injury or of disease in general
(Lecture 1, Part 1, Slide 7)

Question 8

What is an agonist?

Answer 8

A drug or naturally occurring body substance that directly causes a measurable response, which can either be excitatory or inhibitory, depending on what receptor is being activated
(Lecture 1, Part 1, Slide 10)

Question 9

What is affinity?

Answer 9

How strongly a substrate / drug binds to its enzyme / receptor
(Lecture 1, Part 1, Slide 10)

Question 10

What does efficacy mean?

Answer 10

The ability of a drug to activate the receptor (elicit a response)
(Lecture 1, Part 1, Slide 10)

Question 11

Do agonists have affinity, efficacy or both?

Answer 11

They have both affinity and efficacy
(Lecture 1, Part 1, Slide 10)

Question 12

What is a concentration-response curve?

Answer 12

A graph used to measure how effective an agonist is - with agonist concentration being on the X axis and the response elicited (as %age max of the tissue) on the Y axis
(Lecture 1, Part 1, Slide 11)

Question 13

What is an EC50 value?

Answer 13

The concentration of the drug (agonist) when it is acting at 50% of its maximum effective response
(Lecture 1, Part 1, Slide 11)

Question 14

What shape of curve should a good drug create on the concentration-response curve?

Answer 14

A sigmoidal (“S”) shaped curve
(Lecture 1, Part 1, Slide 11)

Question 15

What does a concentration-response curve graph allow?

Answer 15

Comparison of EC50 values
(Lecture 1, Part 1, Slide 12)

Question 16

Does a lower EC50 value equal a more or less potent drug?

Answer 16

More potent
(Lecture 1, Part 1, Slide 12)

Question 17

What are the 3 types of antagonism?

Answer 17

Pharmacological, Chemical and Physiological
(Lecture 1, Part 1, Slide 13)

Question 18

What is pharmacological antagonism?

Answer 18

When drugs counteract each other by acting on the same receptor type
(Lecture 1, Part 1, Slide 13)

Question 19

What is chemical antagonism?

Answer 19

When one drug antagonises the action of another by chemically combining with it
(Lecture 1, Part 1, Slide 13)

Question 20

What is physiological antagonism?

Answer 20

When two drugs counteract each other by producing opposing effects on different receptors
(Lecture 1, Part 1, Slide 13)

Question 21

Do antagonists have affinity, efficacy or both?

Answer 21

They have affinity but no efficacy - meaning no directly measurable effect
(Lecture 1, Part 1, Slide 13)

Question 22

Name the 3 ways that an antagonist can act in.

Answer 22

Competitive
Irreversible-competitive
Non-competitive
(Lecture 1, Part 1, Slides 15,16 and 17)

Question 23

What is competitive antagonism?

Answer 23

Drugs competing to bind the same receptor
(Lecture 1, Part 1, Slide 15)

Question 24

What does occupancy refer to?

Answer 24

The proportion of the receptors to which the agonist is bound to
(Lecture 1, Part 1, Slide 15)

Question 25

How can competitive antagonism be reversed?

Answer 25

By increasing the concentration of the agonist, enabling it to out-compete the antagonist and restore tissue responses (Lecture 1, Part 1, Slide 15)

Question 26

What is reversible competitive antagonism described as?

Answer 26

Surmountable - as it can be reversed (Lecture 1, Part 1, Slide 15)

Question 27

What are the 2 key features in the concentration response graph of competitive antagonism?

Answer 27

A shift of the agonist concentration response curve to the right (without changing the slope or max response) A linear relationship between agonist and antagonist concentration (as long as it is reversible) (Lecture 1, Part 1, Slide 15)

Question 28

What is irreversible competitive antagonism?

Answer 28

When the bond between the antagonist and the receptor is so strong that even increasing concentrations of agonists cannot displace the antagonist (Lecture 1, Part 1, Slide 17)

Question 29

What is usually the reason that a competitive antagonism is irreversible?

Answer 29

Covalent bonding between the antagonist and the receptor (Lecture 1, Part 1, Slide 17)

Question 30

What is non-competitive antagonism?

Answer 30

Antagonists which act at sites other than the agonist binding site (Lecture 1, Part 1, Slide 17)

Question 31

How can an agonist and an antagonist have the same effect?

Answer 31

By acting on different receptors and receptor locations e.g hyoscine antagonist reducing muscle contraction and morphine being an agonist for opioid receptors - causing a reduction in acetylcholine and therefore contractions (Lecture 1, Part 1, Slide 18)

Question 32

What is a full agonist?

Answer 32

An agonist which can produce a maximal response from a tissue (Lecture 1, Part 1, Slide 19)

Question 33

What does it mean for an agonist to produce a maximal response?

Answer 33

It makes the tissue produce the largest response it possibly can (Lecture 1, Part 1, Slide 19)

Question 34

What is a partial agonist?

Answer 34

An agonist which can only produce a sub-maximal response (Lecture 1, Part 1, Slide 19)

Question 35

Why was synthetic chemistry a huge turning point in pharmacology?

Answer 35

As it enabled new synthetic drugs to be created (Lecture 1, Part 2, Slide 3)

Question 36

What did Paracelsus say?

Answer 36

"All things are poisons for there is nothing without poisonous qualities. It is only the dose which makes a thing a poison" (Lecture 1, Part 2, Slide 5)

Question 37

What is the the margin between the therapeutic (desired) and toxic (undesired) effects called?

Answer 37

The therapeutic range (Lecture 1, Part 2, Slide 6)

Question 38

What are the symptoms of botulinum toxin?

Answer 38

Muscle paralysis and respiratory failure (Lecture 1, Part 2, Slide 7)

Question 39

What 5 things can botulinum toxin (Botox) be used to treat?

Answer 39

Removal of facial wrinkles Severe underarm sweating Cervical dystonia ( a neurological disorder causing severe neck and shoulder muscle contractions) Blepharospasm - uncontrollable blinking Strabismus - misaligned eyes (Lecture 1, Part 2, Slide 8)

Question 40

What is iatrogenicity?

Answer 40

The capacity of a drug to produce a disease from the side effects or inappropriate prescribing of the drug (Lecture 1, Part 2, Slide 9)

Question 41

What is tetratogenicity?

Answer 41

The capacity of a drug to produce abnormalities of the unborn child or foetus (Lecture 1, Part 2, Slide 9)

Question 42

What is thalidomide?

Answer 42

A drug used to treat morning sickness in pregnant women, the R (right hand) form is the therapeutic form whereas the S (Left hand) form is teratogenic (Lecture 1, Part 2, Slide 10)

Question 43

What 3 ways are drugs studied?

Answer 43

In vivo Ex vivo High throughput screening (Lecture 1, Part 2, Slide 11)

Question 44

What are 4 examples of drug targets?

Answer 44

Ion channels (open or closed) Enzymes Transporters / carriers Receptors (Lecture 1, Part 2, Slide 12)

Question 45

What do receptors do?

Answer 45

They receive and transduce signals that may be integrated into biological systems (Lecture 1, Part 2, Slide 13)

Question 46

Why are receptors needed in physiology?

Answer 46

Co-ordinates the activities of the bodies cells and organs (Lecture 1, Part 2, Slide 14)