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Y1 - ICPP > Lecture 18 - Review Of Pharmacodynamics > Flashcards

Lecture 18 - Review Of Pharmacodynamics Flashcards

1
Q

What is 0.0001 in exponential/scientific notation?

A

1x10^-4

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2
Q

What is 10^3 in log notation?

A

Log(base 10)1000 = 3

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3
Q

What is a ligand?

A

A substance that can interact with a target protein or receptor

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4
Q

What is an agonist?

A

A ligand that can interact/bind to a target protein, activating stimulating a biological response

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5
Q

What is an antagonist?

A

Ligands that have a affinity for a receptor or target protein that dont produce a biological response

Antagonists block the action of agonists

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6
Q

What is affinty?

A

A measure of strength of the interaction between a ligand/drug binds to a receptor

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7
Q

What measurement is used to define affinty?

A

Kd

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8
Q

What is Kd?

A

The concentration of ligament at which 50%of all available receptors are bound

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9
Q

What does a high value of Kd mean?

What does a low value of Kd mean?

A

High Kd = low affinity of drug (high conc of drug needed to occupy 50% of receptors)

Low Kd = high affinity of drug (low conc of drug needed to occupy 50% of receptors)

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10
Q

What is intrinsic efficacy?

A

The ability of a ligand to generate the active form of the receptor

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11
Q

What is the notation for the active form of a receptor?

A

R*

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12
Q

What is ligand efficacy?

A

The ability of a ligand to cause a measurable biological response

Comprises ligand efficacy and tissues ability to produce response

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13
Q

What is potency?

A

Essentially how good a drug is at evoking a response

The concentration of a drug that evokes 50% of its maximal response (Emax = EC50)

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14
Q

What does a low EC50 mean?

What does a high EC50 mean?

A

Low = More potent (less drug required to generate 50% of max response)

High = Less potent (more drug required to generate 50% of max response)

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15
Q

What is Emax?

A

The concentration of drug needed to reach the maximum response

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16
Q

What is Bmax?

A

Concentrations of drug required to reach maximum receptors bound

17
Q

What is a partial agonist?

A

Ligands that evoke responses that are always lower than the maximum response of a full agonist

18
Q

How does a full agonists Intrinsic activity compartment to a partial agonists?

A

Partial agonist = lower intrinsic activity

Full agonist = higher intrinsic activity

19
Q

What is the difference between an agonists intrinsic efficacy and an antagonists intrinsic efficacy?

A

Antagonists = no intrinsic efficacy but affinty

Agonist = intrinsic efficacy and affinity

20
Q

How would a drug with a high intrinsic efficacy Emax compare to a drug with low intrinsic activity?

A

High intrinsic activity = higher Emax

The larger the max point on a response curve the higher the intrinsic activity

21
Q

On a response/conc graph how can you determine which drug has the highest potency?

A

The drug furthest to the left which reaches its EC50 the quickest

22
Q

On a response/conc curve how can you estimate the affinity of a partial agonist?

A

For a partial agonist EC50 and its affinity are very similar

23
Q

What values can be determined from a Porportions of receptor bound - Conc graph for a drug?

A

Kd (affinity)
Bmax (max binding capacity)

24
Q

What values can be determined from a Response - Conc graph for a drug?

A

EC50 (potency)
Emax (intrinsic activity)

25
Q

What values will be different if there are spare receptors?
How will these values differ?

A

Kd
EC50

When EC50 is less/smaller than Kd

26
Q

What is Functional antagonism?

A

Antagonism of a cellular/tissue event being mediated by one mechanism by another mechanism

27
Q

What are the 3 types of drug antagonism?

A

Reversible competitive antagonism

Irreversible competitive antagonism

Non competitive anatongism

28
Q

What is reversible competitive anatagonism?

A

Same binding site (orthosteric site) as endogenous ligand

Interaction is a relatively weak bond (associates and dissociates)

29
Q

What is irreversible competitive antagonism?

A

Same binding site (orthosteric site) as endogenous ligand

Interaction is very strong (often covalent) antagonist dissociates very slowly or never

30
Q

What is non competitive antagonism?

A

Antagonist binds at a site away from the orthosteric site known as the Allosteric site

Y1 - ICPP (23 decks)

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