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Intro to Pharmacology > Pharmacodynamics - Part 1 > Flashcards

Pharmacodynamics - Part 1 Flashcards

1
Q

What is the definition of pharmacodynamics?

A

The study of the impact of drugs on the body or drug actions.

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2
Q

No drug produces a _______ effect.

A

single

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3
Q

Drug actions occur because _______ binds to _______ ______.

A

drugs - cellular targets

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4
Q

When drugs bind to cellular targets this:

  • initiates ________ ________
  • pharmacological effect is due to the alteration of an intrinsic physiological process and ___ the creation of a _____ process.
A

biochemical reactions

NOT - new process

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5
Q

Every drug tends to have more than one ______, and thus more than one _____.

A

target

action

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6
Q

In this class, the term cellular target can be used interchangeably with what?

A

receptor

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7
Q

In drug action, we cannot create ____ ________.

We can either ______ the process or ________ it.

A

new processes

enhance or inhibit

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8
Q

Drug action essentially alters what?

A

Intrinsic physiological processes

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9
Q

Where are drug targets present?

A

Cell surface
Organelle within the cell
In the cytoplasm

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10
Q

There is a _______ number of receptors in a given cell.

This means that _______-mediated responses _______ upon ________ of all receptors.

A

finite
receptor
plateau
saturation

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11
Q

What are different drug targets?

A

Proteins/glycoproteins
Nucleic acids
Carbohydrates
Lipids

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12
Q

What are the different protein/glycoprotein drug targets?

A

Enzymes

receptors

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13
Q

What are the different nucleic acid drug targets?

A

DNA and RNA

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14
Q

What are the different Carb drug targets?

A

Glcyogen

Cell surface receptors

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15
Q

What is the lipid drug target?

A

Cell membranes

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16
Q

Most receptors or drug tragets are of what kind?

A

Proteins/glycoproteins.

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17
Q

Drug action occurs:
- when the concentration or quantity of the drug at the site of responsive tissue attains a certain _______ ________ level

A

critical minimal

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18
Q

The certain critical minimal level which equates “effective” level can be determined by __ general factors?
What are they?

A

4

  • affinity of the drug to the targets
  • Ability of the drug to cause changes
  • Responsiveness of the target to the changes
  • adaptability of the target-tissues/organs to the changes
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19
Q

The 4 general factors for determinign the effective level of drug concentration for drug action:

  • ______ of the drug to the targets
  • Ability of the drug to cause ______
  • ____________ of the target to the changes
  • ___________ of the target-tissues/organs to the changes
A

Affinity
changes
responsiveness
adaptability

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20
Q

What is critical for drug action to occur?

A

Drug needs to be present near the receptor, and in sufficient quantity

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21
Q

Describe a drug that would not cause a change.

A

Diagnostic compound that binds to receptor to track changes but doesnt cause any change.

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22
Q

Describe adaptability to drug action.

A

Change occurs, but cell adapts to the change.

- body might produce more receptor

23
Q

Why is drug adaptability important for drug action?

A

If the cell adjusts too quickly, drug action may not occur

24
Q

The affinity of drug targets refers to:

- the ______ of binding between the drug and receptor

A

strength

25
Q

What does the affinity of drug targets mean?

A

The strength of binding between the drug and receptor

26
Q

The number of occupied receptors is a function of the balance between ______ and _______ drug

A

free and bound

27
Q

What are the different intermolcular interaction important for drug affinity to a target?

A

Ionic, H-bond, VdW, Covalent

28
Q

Describe not easily breakable covalent bonds.

A

Some drugs bind to targets irreversibly and remove the target from its natural action completely
- ex: tamoxiffen cancer drug

29
Q

The majority of drug binding to targets is ________.

A

reversible

30
Q

For the majority of drugs, they _______ with natural compounds for the natural _______.

A

compete

target

31
Q

When a drug binds covalently and the bond is not easily breakable, this means?

A

The action is permanent

32
Q

Affinity is used to describe how ______ the interaction between the ______ and the _______ is.

A

strong
ligand
receptor

33
Q

What is the measure of drug affinity?

A

Dissociation constant - Kd

34
Q

kd is reciprocally related to what?

A

ka

35
Q

Using the standard A = B –> AB nomenclature, provide Kd and Ka.

A 
ka = AB/A + B
kd = A+B/AB
36
Q

The association constant can be thought of as the eqb constant in the ______ direciton; the dissociation constant can be thought of the eqb constant in the ______ direction.

A

forward

reverse

37
Q

At equilibrium, what is Kd equal to?

A

kd/ka = Kd

38
Q

Experimentally, related to Kd, a _______ ______ can be plotted.

A

binding curve

39
Q

What are the axes of the binding curve?

A

Y - fraction B bound

X - Concentration of A free

40
Q

How can one determine Kd from a binding curve?

A

When 50% of B (receptor) is bound by A (ligand), the binding curve value is equal to Kd.

41
Q

A translation to the right of the binding curve means what?

Left translation?

A

Right - binds worse, less affinity

Left - more affinity

42
Q

What is an issue with the binding curve?

A

Hard to determine the 50% mark by eye-balling

43
Q

What is the linear plot equivalent of a binding curve?

A

Scatchard plot

44
Q

What are the different parts of a scatchard plot?

A

Y - [fraction bound B/A]
X - [Fraction bound B]
y-intercept = 1/Kd
slope = -1/Kd

45
Q

Define the dissociation constant.

A

Measure of a drug’s affinity for a given receptor

Defined as the concentration of a drug required in solution to achieve 50% occupancy of its receptors.

46
Q

A higher affinity shows ______ concentration of drug required in solution to achieve 50% occupancy of its receptors.

A

less

47
Q

Define efficacy.

A

Degree to which a drug is able to produce the desired response.

48
Q

Define potency

A

Amount of drug required to produce 50% of the maximal response the drug is capable of inducing

49
Q

What is potency used for?

A

Compare compounds within the SAME class of drugs

50
Q

What is effective concentration 50% (ED50)?

A

Concentration of the drug which induces a specified clinical effect in 50% of subjects

51
Q

What is the Lethal dose 50% (LD50)?

A

concentration of the drug which induces death in 50% of subjects

52
Q

What is the therapeutic index?

A

Measure of the safety of a drug.
- provides the margin of safety
Margin between the therapeutic and lethal doses of a drug

53
Q

How is the therapeutic index calculated?

A

LD50/ED50

Intro to Pharmacology (23 decks)

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