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PAR2031 - Pharmacology > Week 2 > Flashcards

Week 2 Flashcards

1
Q

What is a medicine?

A

May contain more than 1 drug

- usually contains other substances such as stabilisers, solvents etc

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2
Q

What does enteric coating mean?

A

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

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3
Q

What type of drugs end with ‘olol’

A

Beta blockers or B-adrenoreceptor blockers

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4
Q

What type of drugs end with ‘caine’

A

Local anaesthetic

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5
Q

What type of drugs end with ‘dipine’

A

Calcium channel blockers

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6
Q

What type of drugs end with ‘mab’

A

Monoclonal antibodies

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7
Q

What type of drugs end with ‘pril’

A

ACE inhibitors

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8
Q

What type of drugs end with ‘statin’

A

HMG-CoA reductase inhibitors

  • Anti colesterol
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9
Q

What type of drugs end with ‘azoles’

A

antifungal agents

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10
Q

Explain pharmacodynamics

A

What the drug does to the body

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11
Q

Explain pharmcokinetics

A

What the body does to the drug

  • literally the movement of drugs into and around the body
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12
Q

Define pharmacodynamics

A

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

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13
Q

what are some specific targets for drugs?

A
  • osmostic effects
  • pH changes
  • chelating agents
  • disruption of cells
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14
Q

What are some molecular targets for drug action?

A
  • Receptors
  • Ion channels
  • Enzymes
  • Carriers/transporters
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15
Q

What can cause adverse effects?

A

Can be due to the drug acting:

  • at the same/similar target elsewhere in the body
  • at a different (but related) target
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16
Q

How can drug selectivity be achieved?

A
  • modifications to drug structure
  • limiting access of drug
  • route
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17
Q

What is a ligand?

A

another name for a drug

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18
Q

What is a recognition site?

A

another name for receptor

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19
Q

What does antagonist mean?

A

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

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20
Q

What is an agonist?

A

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

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21
Q

Define affinity

A

ability to bind at a receptor site

22
Q

Define Efficacy

A

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

23
Q

Define Potency

A

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

24
Q

How do drugs attach to receptors?

A

They mimic endogenous ligands

25
Q

How to antagonists work with receptors?

A

They block the actions of endogenous ligands

26
Q

What type of drug has affinity but on efficacy?

A

Antagonist

27
Q

What type of drug has both affinity and efficacy?

A

Agonist

28
Q

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

A
  1. Binding
  2. Activation
  3. Transduction
29
Q

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

A

Milliseconds

Examples:
Nicotinic ACh receptors

30
Q

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

A

Seconds

Example:
Muscarinic ACh receptor

31
Q

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

A

Ligands gated ion channels

32
Q

What is the equation for dose-response

A

DR = D+R

magnitude of response is determined by amount of DR complexes formed

33
Q

What is an orthosteric site?

A

the receptor site that an agonist lands in

34
Q

What is an allosteric site?

A

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

35
Q

What is an allosteric agonist?

A

helps to amplify the agonist response

36
Q

Why is a log scale better than a linear scale?

A

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

37
Q

What is the EC50?

A

The half maximal effective concentration

38
Q

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

A

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

39
Q

What is Emax?

A

the maximal response when all receptors are occupied

40
Q

What is a full agonist?

A

produces a maximum response which is equal to the maximum response of tissue

  • the maximal response you can achieve from an agonist
41
Q

What is a partial agonist?

A

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

42
Q

what are the characteristics of a partial agonist?

A
  • have affinity - sometimes more than a full agonist

- have efficacy - but it’s lower than that of a full agonist

43
Q

What are the characterises of antagonists?

A
  • Have affinity for the site
  • > eg. compatitive antaginist
  • antagonists binding to the site do not produce a biological effect
  • have affinity but no efficacy
44
Q

What are the various types of antagonists?

A
  • competitive
  • non-competitive
  • irreversible
45
Q

What are the types of antagonism?

A

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

46
Q

what are examples of common agonists?

A
  • ventolin
  • morphine
  • adrenaline
47
Q

what are examples of common antagonists?

A
  • narcan

- claratyne

48
Q

What is the therapeutic index?

A

provides an indication of effective drug dose vs toxicity on administration

  • used as a risk benefit tool
49
Q

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

A

High

we want a high ratio

50
Q

What is the equation for therapeutic index?

A

Toxic dose 50/effective dose 50

51
Q

What are examples of drugs with a narrow therapeutic index?

A
  • Warfarin
  • Carbamazepine
  • Digoxin
  • Lithium
  • Phenytoin
  • Tacrolomus
  • Amphotericin

PAR2031 - Pharmacology (13 decks)

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