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Pharmacology > Pharmacodynamics I > Flashcards

Pharmacodynamics I Flashcards

1
Q

What is pharmacodynamics?

A

Biochemical and physiological effects and mechanisms (what drugs do to the body)

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2
Q

What is pharmacokinetics?

A

Absorption, distribution, metabolism, and elimination of drugs (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 drug response among individuals or populations

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4
Q

What is an agonists?

A

Bind to the receptor and initiates a response

Full or partial

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5
Q

What is an antagonist?

A

Bind to the receptor but does NOT initiate a response
(blocks)
Inhibits response to an agonist

Competitive or noncompetitive

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6
Q

What are allosteric activators/inhibitors?

A

Bind to different receptor site than agonist and alters the response to agonist

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7
Q

What is responsible for drug selectivity?

A

The receptor

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8
Q

Are receptors:

a) Selective or nonselective
b) Reversible or irreversible
c) Endogenous or exogenous
d) Saturable or insaturable

A

a) Selective
b) Reversible
c) Endogenous
d) Saturable

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9
Q

What determines the quantitative relationship between drug concentration?

A

The receptor

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10
Q

Do enantiomers fit into and stimulate/block the same receptors?

A

No

Enantiomers fit a specific receptor and stimulate or block different receptors

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11
Q

Do stereoisomers have the same activity levels?

A

No

May have more or fewer binding sites, which in turn alters activity levels

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12
Q

Are electrostatic interactions (ionic) reversible or irreversible?

A

Reversible

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13
Q

What are two examples of electrostatic interactions (ionic)?

A

Hydrogen bonding

Van der Waals forces

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14
Q

What is a hydrophobic interaction?

A

When a nonpolar region of a drug binds to a nonpolar region of the receptor

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15
Q

What is an example of a hydrophobic interaction?

A

Lipid soluble drugs (local anesthetics, anticonvulsants)

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16
Q

Is covalent binding reversible or irreversible?

A

Irreversible, very strong bond

Atoms from 2 molecules share electrons

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17
Q

What is an example of covalent binding?

A

Aspirin

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18
Q

Define affinity (Kd)

A

The ability of a drug to bind to a receptor

19
Q

What is the affinity at equilibrium?

A

Half the receptors

are bound; half the receptors are free

20
Q

Kd is a measure of

A

Affinity

21
Q

What is the relationship between Kd and the affinity the drug has for its receptor?

A

The lower the Kd the higher the affinity the drug has for its receptor

22
Q

Define efficacy (α)

A

The ability of a drug to initiate a response

100% response, α = 1
0% response, α = 0

23
Q

What determines the extent of a drug effect?

A

The number of receptors bound

24
Q

What determines the maximum effect (Emax) of a drug?

A

Efficacy

25
Q

What has affinity and intrinsic activity?

A

Full agonists

α = 1

26
Q

What has affinity but no intrinsic activity?

A

Antagonists

α = 0

27
Q

What has affinity but lower intrinsic activity?

A

Partial agonists

0 < α < 1

28
Q

The Emax is a function of

A
  1. The amount of drug
  2. The number of available receptors
  3. The ability to evoke a response (efficacy)
29
Q

Are efficacy and potency related?

A

No

30
Q

What does EC50 represent?

A

Drug concentration (plasma) that produces 50% of the maximal effect

31
Q

What is the relationship between EC50 and drug potency?

A

Lower the EC50, the more potent the drug

32
Q

A semi-log plot compares

A

log of the drug concentration (x-axis) vs. the response (y-axis)

33
Q

What are 3 benefits to using a semi-log plot?

A
  1. Transforms the hyperbolic curve into a sigmoid curve
  2. Expands the scale at low concentrations where the response increases rapidly (therapeutic effect)
  3. Contracts at high concentrations where the response is not changing as quickly (toxicity)
34
Q

What is a semi-log plot used for?

A

Used to calculate Kd and EC50 and to compare the effects of different drugs at a specific receptor

35
Q

Define potency

A

Dose required to produce a given effect

36
Q

Graded Dose-Response Curves measure

A

A response in an individual

37
Q

A steep slope indicates

A

A rapid response, risky

Small therapeutic window

38
Q

Define threshold dose

A

A dose below which there is no response

39
Q

Quantal Dose-Response Curves are used to measure

A

The frequency with which a response will occur to a given dose within a population

“all-or-none” effect

40
Q

Define therapeutic ratio

A

Range of doses with high efficacy and

low probability of adverse effects

41
Q

How is the therapeutic ratio calculated?

A

Difference between LD50 and ED50

TR = LD50/ED50

42
Q

Define margin of safety

A

Factor by which the ED99 concentration needs to be multiplied by to get the LD1 concentration

The higher the margin of safety, the safer the drug

43
Q

How is the margin of safety calculated?

A

Margin of safety = LD1/ED99

44
Q

Which drug has the greatest margin of safety, A or B?

Drug A) 10 mg/kg is effective in 99% of the population
and 100 mg/kg is toxic in 1%

Drug B) 40 mg/kg is effective in 99% and 50 mg/kg is toxic in 1% of the population

A

Drug A

Margin of safety = LD1/ED99
Drug A - 100/10 = 10
Drug B - 50/40 = 1.25

Drug A can be increased 10 fold without being concerned about toxicity

Drug B can only be increased by a small amount before being concerned about toxicity

Pharmacology (25 decks)

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