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Intro to Pharmacology > Pharmacodynamics - Part 2 > Flashcards

Pharmacodynamics - Part 2 Flashcards

1
Q

Chirality:

- A chiral molecule is a type of molecule that has a non-_________ mirror image.

A

superimposable

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2
Q

What is the feature that is most often the cause of chirality in molecules?

A

Presence of an asymmetric carbon atom

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3
Q

The first step for naming molecules is to identify _________.

A

stereocenters

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4
Q

R nomenclature means ________.

S means ________-________.

A

clockwise

counter-clockwise

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5
Q

Some drug targets/receptors have no ________ and can interact with any _______ and give a similar _______.
These are termed what?

A

selectivity
isomer
efficacy
Non-selective

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6
Q

When a receptor is non-selective, what does this mean?

A

The molecule’s (Drug’s) geometry is not involved in binding

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7
Q

Conversely, a receptor can be very selective meaning what?

A

It will interact with one stereoisomer better than the other(s).

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8
Q

Adverse effects generally occur due to what?

A

Non-specific binding

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9
Q

What are the two terms related to isomers that give rise to different biological effects.

A

Eutomer

Distomer

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10
Q

What is a eutomer?

A

Eutomer is the isomer with higher affinity of activity.

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11
Q

What is a distomer?

A

Isomer with lower affinity or activity

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12
Q

What is the eudismic ratio?

A

Indicates how much of the eutomer there is relative to the distomer - the higher the ratio, the greater the amount of eutomer
(Describes the difference in pharmacological activity between the two enantiomers of a drug.)

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13
Q

What is a racemic mixture?

A

When a drug is synthesized, often contains both enantiomers in a racemic mixture.
I.e. a eudismic mixture

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14
Q

When would a racemic mixture not be used?

A

When one enantiomer causes adverse effects.

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15
Q

Two drugs have the same concentration, one producers a greater effect than the other.
This drug is termed what?

A

More efficacious

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16
Q

Two drugs of a similar class produce biological effects, but one requires a lower dose. This drug is what?

A

More potent

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17
Q

What is used to measure efficacy?

A

Dose-response curve

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18
Q

Describe a dose response curve.

A

Y - %biological effect
X - [Drug] - can be log scale
dose at 50% of biological effect is ED50

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19
Q

Describe the relationship between efficacy and potency with the dose response curve.

A

Potency - x-axis translations

Efficacy - y-axis translations

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20
Q

A drug that undergoes a translation to the left on the dose-response curve is what?

A

More potent

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21
Q

A drug that undergoes an upwards translation on the dose-response curve is what?

A

More efficacious

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22
Q

The lower the _____, the higher the potency.

A

ED50

23
Q

What is the equation for the therapeutic index?

A

TI = TD50/ED50

24
Q

TI is _______.

A

unitless

25
Q

A drug with a TI of 1 would be?

A

Bad

26
Q

A drug with a large TI has a ______ margin of safety

A

higher

27
Q

What are the two theoires (that we focus on) explaining the mechanisms of drug action?

A

Occupation theory

Rate theory

28
Q

Occupation theory:

- Biological effect is elicited/initiated when the ______ occupies the _______ site.

A

ligand

binding

29
Q

What is the occupation theory?

A

Biological effect is elicited/initiated when the ligand occupies the binding site.

30
Q

The occupation theory states that for a drug to act, it needs to have a ______.

A

target

31
Q

Occupation theory

- intermolecular reaction is ______ formed and ______.

A

readily

reversed

32
Q

Occupation theory:

- the level of biological effect is proportional to what?

A

the number of occupied sites

33
Q

According to the occupation theory, the more sites that are occupied, the _____ the biological effect that is observed.

A

higher

34
Q

According to the occupation theory, the occupation of one receptor ______ affect the other receptor’s ability to bind other ligands.

A

doesn’t

35
Q

A key point of the occupation theory is that drug receptors are _________ of one another.

A

independent

36
Q

Occupation theory explains the _____ ______ _____ well.

A

dose response curve

37
Q

Drug action and occupation theory:

  • Explains the level of _____ _______
  • Allow _______ _____ to be used during pre-clinical studies
  • Allow ______ testing based on biochemical assays
  • Allow chemists to predict and design new drugs based on the _______ ________ (target interactions)
A

biological effect
biochemical assays
drug
structural features

38
Q

Modified occupation theory:

  • The interaction of a drug and its receptor involves ____ step(s)
  • The ________ of the drug and the receptor, called _______ - explained by the ___ value
  • The initiation of _______ effect, called ______ or _______ ________
A

2
complexation
affinity
Kd

biological
efficacy
intrinsic activity

39
Q

According to the occupation theory,

the lower the Kd value, the ______ the interaction.

A

tighter

40
Q

_______ _______ (alpha) is the ability of the complex to generate the response ranging from 0 to 1 or 100%.

A

intrinsic activity

41
Q

What is the intrinsic activity?

A

Ability of the complex to generate the response - ranging from 0-100%.

42
Q

Occupancy theory could not explain what?

A

When two drugs bind to the same receptor but produce different biological effects.

43
Q

The occupation theory was good at explaining what?

A

The lower the Kd, the lower the dosage required.

44
Q

Rate theory:

- the activation of a receptor is proportional to the total ______ of _______ of the drug with its target per unit time

A

number

encounters

45
Q

According to the rate theory, the pharmacological activity of a drug is a function of what, but not of what?

A

Rate of association and dissociation
NOT
the number of occupied receptors.

46
Q

According to rate theory, agonists do what?

A

Associated and dissociate very fast

47
Q

According to rate theory, antagonists do what?

A

Associate fast, dissociate very slow

48
Q

When are the rate and occupancy theory equivalent?

A

At equilibrium

49
Q

What can the rate theory not account for?

A

The characteristics of different types of compounds.

50
Q

What is an agonist?

A

Ligand that produces the same effect as the natural compound (ex: NT) that would bind to that receptor.

51
Q

What is an antagonist?

A

Prevents the intrinsic reaction mechanism - does not cause the cell to do something else, just prevents it from doing something.

52
Q

What is a good trick for remembering dissociation and association rates for an antagonist for rate theory

A

Unwelcome guest

comes in easily, hard to get out

53
Q

The induced-fit theory, macromolecular perturbation theory and activation-aggregation theory have what in common?

A

Conformational changes

Intro to Pharmacology (23 decks)

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