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Pharmacology Exam 1 (Lauren) > L1 Pharmacodynamics > Flashcards

L1 Pharmacodynamics Flashcards

1
Q

What is pharmacodynamics?

A

What drugs do to the body

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2
Q

What is pharmacokinetics?

A

What the body does to drugs

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3
Q

What is pharmacogenomics?

A

Study of the genetic variations that cause differences in how individuals respond to drugs

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4
Q

What is an agonist?

A

Binds to the receptor and initiates a response that can be full or partil

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5
Q

What is an antagonist

A

Binds to the receptor but does NOT initiate a response

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6
Q

What are allosteric activators and inhibitors?

A

Bind to a site OTHER than the active site and alter response

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7
Q

What is responsible for drug specificvit?

A

The receptor

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8
Q

What determines the quantitative relationship between drug concentration and pharmacological effect?

A

The receptor

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9
Q

Can a receptor respond to multiple shapes and charges?

A

No, the interaction between a drug and receptor is very specific. Only a specific shape and chemical charge will fit

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10
Q

Is ionic/electrostatic interaction reversible?

A

Yes

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11
Q

Is covalent binding reversible?

A

NO

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12
Q

What is an example of drugs that do hydrophobic interactions?

A

Lipid soluble drugs like local anesthetics and anticonvulsants

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13
Q

What is this type of interaction:

Nonpolar region of a drug binds to a non-polar region of the receptor

A

Hydrophobic interaction

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14
Q

What is this kind of interaction:

Atoms from two molecules share electrons

A

Covalent binding

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15
Q

What is the classic example of a drug that binds covalently and irreversibly?

A

Aspirin binding to the COX enzyme

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16
Q

Are drugs constantly binding and unbinding from their receptors?

A

YES unless it’s covalently bound

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17
Q

What is “the ability of a drug to bind to a receptor”

A

Affinity

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18
Q

At equilibrium, how many of the receptors are bound?

A

Half

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19
Q

What is Kd

A

The concentration of free drug at which 50% of the drug is bound to its receptor

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20
Q

What is the other name for “equilibrium dissociation constant”

A

Kd

21
Q

What does Kd measure?

A

The affinity

22
Q

What kind of drug has affinity and intrinsic activity?

A

Full agonists

Alpha=1

23
Q

What is efficacy/intrinsic activity?

A

The ability of a drug to initiate a response

24
Q

What kind of drug has affinity but no intrinsic activity?

A

Antagonists

Alpha=0

25
Q

What is Emax?

A

The maximal response

26
Q

Are efficacy and potency related in any way?

A

NO

Just because you have a maximum effect doesn’t mean you have a potent drug, it could just be that you have a lot of it

27
Q

What is EC50

A

The plasma concentration of the drug that produces 50% of the maximal effect

28
Q

If EC50 is low, what does that say about the potency of the drug?

A

Lower the EC50, the more potent the drug

29
Q

What is ED50

A

The dose with 50% maximal effect

Goes hand in hand with EC50

30
Q

Why do we use a semi log scale when making a dose response curve?

A

It expands the scale at low concentrations where the response increases rapidly (therapeutic effect), and it contracts at high concentrations where response is not changing as quickly (toxicity)

31
Q

What can we calculate by using a semi log plot of a dose response curve?

A

Kd and EC50/ED50

32
Q

What is potency?

A

The dose required to produce a given effect

33
Q

What does a graded dose response curve measure

A

The response in an individual

34
Q

What does a steep slope mean on a graded dose response curve?

A

The drug has a small therapeutic window (risky)

35
Q

What does a quantal dose-respond curve tell you?

A

The frequency within a population that a response occurs

36
Q

What can we calculate from a quantal dose-respond curve?

A

ED50

LD50

TD50

37
Q

What is the therapeutic ratio/index/window?

Not calculation

A

The range of doses with high efficacy and low probability of adverse effects

38
Q

How do you calculate the therapeutic ratio/index/window

A

TR=LD50/ED50

So if TR=4, then you can multiply ED50 by 4 and still be pretty safe?

39
Q

How do you calculate the margin of safety?

A

Margin of safety= LD1/ED99

40
Q

The higher the margin of safety the ______ the drug

A

Safer

41
Q

A margin of safety that is less than 1 means:

A

It is a very risky drug

42
Q

Are efficacy and intrinsic activity the same thing?

A

YES

43
Q

If a tissue type has lots of spare receptors, how do you adjust the dose?

A

LOWER the dose

44
Q

What does it mean if you can elicit a maximum response without occupying all the available receptors?

A

The tissue has Spare receptors

45
Q

If a tissue has spare receptors, how will EC50 relate to Kd

A

EC50 will be lower than Kd

You got 50% maximal effect by binding fewer receptors

46
Q

What happens to the concentration response curve (EC50) if there are spare receptors?

A

It is shifted to the left

47
Q

What happens to Kd if there are spare receptors?

A

NOTHING

48
Q

If EC50 is lower than Kd, then_____

A

There are spare receptors and you need to use a lower dose

Pharmacology Exam 1 (Lauren) (7 decks)

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