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Mechanisms of Drug Action > Drug-Receptor Interactions > Flashcards

Drug-Receptor Interactions Flashcards

1
Q

What can change the position of a concentration-binding curve?

A

Nothing

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2
Q

What does COX stand for?

A

Cyclooxygenase

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3
Q

What is the effect of aspirin on the COX enzyme?

A

The COX enzyme is acetylated irreversibly so the inflammation pathway is stopped

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4
Q

What kind of inhibitor is ibuprofen on COX enzymes?

A

Competitive reversible

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5
Q

What are the 2 ways drugs can produce side effects?

A
  • Drug good at reaching targets but targets are all over the body
  • Drug is bad at hitting its targets and the extra targets it hits produce side effects
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6
Q

Why does aspirin produce the side effect of stomach ulcers?

A

COX enzymes are found in mucosal cells in gut lining aka the drug target is found in the wrong place

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7
Q

How are side effects from morphine produced?

A

Due to the drug hitting other targets

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8
Q

Give 5 reasons drugs may show side effects and toxicity

A
  • Drugs are insufficiently selective
  • Target sites may be involved in many processes
  • Prolonged use of drug may cause changes in structure and function
  • Patient variability
  • Drug interactions
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9
Q

Define pharmacokinetics

A

The way the body deals with a drug e.g. how it is absorbed

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10
Q

Define pharmacodynamics

A

The effects of the drug on the body

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11
Q

Give an example of a drug which acts on ion channels

A

Tetrodotoxin

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12
Q

Give an example of a drug which acts on transporters

A

Cocaine

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13
Q

Give some features of metabotropic eceptors

A
  • Always have multiple subunits which transverse the plasma membrane
  • N terminus external, C terminus internal
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14
Q

What is an ionotropic receptor?

A

A receptor that responds to a ligand by opening an ion channel

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15
Q

What is a metabotropic receptor?

A

A type of receptor which acts as a second messenger

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16
Q

Do antagonists have efficacy?

A

No

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17
Q

What property is shared by both agonists and antagonists?

A

Affinity

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18
Q

What does KD represent?

A

The concentration of drug at which 50% of binding sites are occupied

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19
Q

Does a higher KD mean a higher affinity drug?

A

No, a lower KD means a higher affinity drug

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20
Q

What 5 conditions are required for the receptor occupancy equation (P) to be valid?

A
  • At equilibrium
  • [Drug] at receptors= that applied to system
  • 1 drug molecule combines with 1 receptor
  • Negligible amount of drug added is bound
  • Binding of 1 drug does not affect binding of another
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21
Q

What does saturable mean?

A

At some point all binding sites are filled

22
Q

What is the shape of a concentration-binding curve?

A

Rectangular Hyperbola

23
Q

Define pharmacological response

A

The ability of an agonist to produce a pharmacological effect in a cell/tissue

24
Q

What does the halfway point of a functional response curve represent?

A

EC50

25
Q

What is EC50?

A

The concentration of drug which produces half the maximum response the specified drug can provide

26
Q

What does a large gap between response and occupancy curves mean for a drug?

A

It has a high efficacy, the higher the efficacy the further apart the curves are

27
Q

If receptor number is reduced which direction does the conc-response curve shift?

A

Right

28
Q

What 3 things affect the position of a concentration-response curve?

A
  • affinity
  • efficacy
  • receptor no.
29
Q

Define potency

A

How much drug is needed to produce a particular response

30
Q

Define partial agonist

A

A drug which must occupy all receptors to evoke their maximum response (drug whose maximum response is less than the full response the tissue is capable of)

31
Q

Which value of ϵ represents full efficacy?

A

1

32
Q

Give an example of a partial agonist

A

Salbutamol

33
Q

Which receptors does salbutamol target?

A

β2 and β1 receptors

34
Q

Where are: β1 and β2 receptors located?

A

β1 are found in the heart

β2 are found in the lungs

35
Q

What is salbutamol used to treat?

A

Asthma

36
Q

Why does salbutamol in inhalers only affect the lungs and not the heart?

A

The heart contains a very small number of β2 receptors which salbutamol acts on, whilst the lungs have many β2 receptors

37
Q

What are the 4 types of drug antagonism?

A
  • Competitive
  • Non-competitive
  • Uncompetitive
  • Physiological
38
Q

What is an uncompetitive antagonist?

A

When binding of an antagonist occurs to an activated form of the receptor

39
Q

What is a competitive antagonist?

A

An antagonist that binds reversibly at the agonist recognition site, preventing access of normal ligand

40
Q

What is a non-competitive antagonist?

A

An antagonist that does not bind at the agonist site but inhibits agonist binding in another way

41
Q

Does the presence of a competitive agonist affect the maximum response achieved by an agonist?

A

No

42
Q

What is the difference between affinity and efficacy?

A

Affinity is the ability of a drug to bind to a receptor whereas efficacy is the ability of a drug to evoke a biological response

43
Q

What is receptor reserve?

A

The proportion of receptors that do not need to be occupied to produce a maximum response

44
Q

A more potent drug will produce a concentration response further left or right?

A

Left

45
Q

What is an uncompetitive agonist?

A

When binding occurs to an activated form of the receptor

46
Q

Does a very potent drug have a high or low EC50?

A

Low

47
Q

What is concentration-ratio?

A

The concentrations of agonist producing the same response in the absence and presence of antagonist

48
Q

What is the y axis of a schild plot?

A

log (dose ratio-1)

49
Q

What is the x axis of a schild plot?

A

log[antagonist]

50
Q

How is KB calculated from a schild plot?

A

the inverse log of where the line meets the x axis

51
Q

How is relative potency determined?

A
  • log concentration-response curves for each agonist must be plotted on the same graph
  • agonists then compared by equipotent molar ratios

Mechanisms of Drug Action (8 decks)

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