Block A Lecture 1: Introduction to Pharmacology Flashcards

1
Q

What is pharmacology?

A

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

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2
Q

What is a drug?

A

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

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3
Q

What is physiology?

A

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

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4
Q

What 2 effects can drugs have on physiology?

A

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

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5
Q

What is therapeutics?

A

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

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6
Q

What can many therapies produce?

A

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

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7
Q

What is pathology?

A

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

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8
Q

What is an agonist?

A

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)

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9
Q

What is affinity?

A

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

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10
Q

What does efficacy mean?

A

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

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11
Q

Do agonists have affinity, efficacy or both?

A

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

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12
Q

What is a concentration-response curve?

A

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)

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13
Q

What is an EC50 value?

A

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

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14
Q

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

A

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

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15
Q

What does a concentration-response curve graph allow?

A

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

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16
Q

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

A

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

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17
Q

What are the 3 types of antagonism?

A

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

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18
Q

What is pharmacological antagonism?

A

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

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19
Q

What is chemical antagonism?

A

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

20
Q

What is physiological antagonism?

A

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

21
Q

Do antagonists have affinity, efficacy or both?

A

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

22
Q

Name the 3 ways that an antagonist can act in.

A

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

23
Q

What is competitive antagonism?

A

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

24
Q

What does occupancy refer to?

A

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

25
Q

How can competitive antagonism be reversed?

A

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

26
Q

What is reversible competitive antagonism described as?

A

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

27
Q

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

A

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)

28
Q

What is irreversible competitive antagonism?

A

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)

29
Q

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

A

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

30
Q

What is non-competitive antagonism?

A

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

31
Q

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

A

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)

32
Q

What is a full agonist?

A

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

33
Q

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

A

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

34
Q

What is a partial agonist?

A

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

35
Q

Why was synthetic chemistry a huge turning point in pharmacology?

A

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

36
Q

What did Paracelsus say?

A

“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)

37
Q

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

A

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

38
Q

What are the symptoms of botulinum toxin?

A

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

39
Q

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

A

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)

40
Q

What is iatrogenicity?

A

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)

41
Q

What is tetratogenicity?

A

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

42
Q

What is thalidomide?

A

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)

43
Q

What 3 ways are drugs studied?

A

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

44
Q

What are 4 examples of drug targets?

A

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

45
Q

What do receptors do?

A

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

46
Q

Why are receptors needed in physiology?

A

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