Pharmacology 2 Flashcards

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1
Q

Briefly - how do drugs act as a ligand for receptors

A
  • they recognize a transmitter or hormone
  • they trigger a cellular response
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2
Q

Briefly - how do drugs act as Endogenous ligand

A

neurotransmitter of hormone or other mediator

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3
Q

Which is the most common receptor drug target

A

GPCRs (receptors coupled to G proteins)

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4
Q

5 receptors targetted by drugs

A
  1. nuclear receptors
  2. Catalytic receptors e.g. receptor tyrosine kinases
  3. cytokine receptors
  4. ligand-gated ion channels
  5. Receptors coupled to G proteins (GPCR)
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5
Q

Examples of other type of drugs tnat don’t act on receptors

A
  • Cyclo-oxygenases (NSAIDS)
  • Voltage-gated ion channels (local anaesthetics)
  • Precursor synthesis (L-DOPA)
  • 5-HT transporter (fluoxetine (Prozac))
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6
Q

What tend to be receptor mediated actions? (4 things)

A
  1. of high potency/affinity
  2. Tissue selective
  3. Chemically-specific
  4. inhibited by specific antagonists (assuming drug is agonist)
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7
Q

How can we calculate the effect of a drug

A

% of receptors occupied (linear correlation for now)

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8
Q

How to calculate dissociation constant

A
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9
Q

how can you calculate what proportion of receptors are occupied by a drug

A

Proportion of Receptors occupied by Drug p = [D] / (kD + [D])

You can figure this out even if you don’t know how much receptor is around…

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10
Q

What does reflects the kD

A

Reflects the affinity of a drug for its receptor

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11
Q

What does it mean when [D] = kD

A

50% of receptors are occupied

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12
Q

hence, what does a low kD mean

A

high affinity, and vice versa

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13
Q

what is an agonist drug

A

mimics actions of the endogenous ligand

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14
Q

what is an antagonist drug

A

counters the actions of an agonist

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15
Q

What is the EC50

A

The concentration of a drug that is needed to reach 50% of the maximal effect

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16
Q

whta is the theory behind spare receptor

A

The maximum effect of a drug would be achieve with less than 100% receptor occupancy by the agonist drug

17
Q

What does a spare receptor theory means for the drug effect?

A

The maximum effect and EC50 will be achieve at a lower concentration than the regular curve

18
Q

difference in efficacy between full agonist, partial agonist and antagonist

A

Full agonist: high efficacy
Partial agonist: medium efficacy
antagonist: zero efficacy

19
Q

how can partial agonist block the effect of a full agonist?

A

They both act at the same receptors, so some are occupied by partia and some by full agonist - the effect is then less then 100% (considering that the full agonist alone would have 100% effect)

20
Q

What is the basal activity

A

The activity that receptors do by themselves, without the drug. independent of agonist/ligand

21
Q

What would be an inverse agonist

A

It has a negative efficacy, it depresses the basal activity of the receptors

22
Q

What specific condition is required for inverse agonist to have an effect

A

it only applies where unbound receptors produce a detectable basal signal

23
Q

Efficacy vs potenxy

A

Efficacy: How well an agonist stimulates a certain effect
- 2 agonists could have the same efficacy, but they might do so in different concentration range
Potency: concentration range at which an agonist achieve the max effect

24
Q

comment on efficacy and potency

A
  • C is less efficient than B
  • C is more potent than B
25
Q

What is a surmountable antagonist

A

a competitive antagonist that will bind with receptors, but an increase in the agonist concentration could still reach a maximum efficacy (the agonist can replace the antagonist when you increase the agonist concentration)

26
Q

What is an insurmountable antagonist

A

it is a competitive irreversible antagonism - meaning that agonist can’t compete when the antagonist is occupying a receptor

27
Q
A