PHARMACOLOGY-pharmacodynamics Flashcards

1
Q

Pharmacodynamics is the study of…

A

effect site concentration and clinical effect

What the drug does to the body

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2
Q

What is pharmacokinetics

A

What the body does to the drug

i.e. plasma concentration, absorption, distribution, metabolism, elimination

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3
Q

What is pharmacobiophasics

A

The specific area of the body where the drug engages tis receptor

Drug concentration in the biophase (not plasma) determines its clinical effect

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4
Q

What does the dose-response curve illustrate

A

The relationship between the drug dose and its clinical effects.
Describes potency, efficacy, and slope

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5
Q

Define potency

A

The dose required to achieve a given clinical effect

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6
Q

What do the ED 50 and ED90 measure and represent

A
Measure = potency
Represent = the dose required to achieve a given effect in 50% and 90% of the population
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7
Q

Define efficacy

A

Ability of a drug to elicit a given clinical effect

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8
Q

When is risk for drug toxicity increased

A

Once a drug dose reaches maximum efficacy but additional administration are given…

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9
Q

What does the slope of the dose-response curve depict

A

How many receptors must be occupied to elicit a clinical effect

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10
Q

Define “individual variability”

A

Differences between PK and PD between patients

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11
Q

What pharmacokinetic factors affect potency

A

absorption, distribution, metabolism, elimination, and receptor affinity

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12
Q

What does a left-shift in the dose-response curve represent (3)

A

Increase affinity for receptor
Higher potency
Lower dose required

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13
Q

What does a right-shift in the dose-response curve represent (3)

A

Decreased affinity for receptor
Lower potency
Higher dose require

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14
Q

What does a higher plateau on the dose-response curve imply

A

Greater efficacy of a drug

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15
Q

What does a low plateau on the dose-response curve imply

A

Lower efficacy of a drug

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16
Q

What happens once the plateau phase is reached on the dose-response curve

A

Additional drug canNOT produce additional effects and increase the risk of toxicity

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17
Q

What does a steep slope of the dose-response curve imply

A

That most receptors must be occupied before we observe the clinical response

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18
Q

How does a full agonist drug work

Example drug

A

It instructs the receptor to produce its maximal response by mimicking an endogenous ligand

Ex = norepinephrine, dopamine, propofol, alfentanil

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19
Q

How does a partial agonist work.

Example drug

A

They are capable of partially activating a cellular response when binding to a receptor. It is less efficacious than a full agonist
Ex = nalbuphine

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20
Q

How does an antagonist work

A

By binding to a receptor and preventing an agonist from binding. It prevents the receptor from having any response

21
Q

What is the difference between competitive and noncompetitive antagonism

A
Competitive = reversible
Noncompetitive = NOT reversible, permanently binds receptor via covalent bonds
22
Q

What are examples of drugs that are competitive antagonists

A

Atropine

Nondepolarizing NMBD

23
Q

What are examples of drugs that are noncompetitive antagonists

A

Aspirin

Phenoxybenzamine

24
Q

How does an inverse agonist work

Example of drug

A

By binding to the receptor and causing the opposite effect of the full agonist
Ex = propranolol

25
Q

What effect can occur with continuous administration of an antagonist

A

Up-regulation of the target receptors

26
Q

How can a competitive antagonist action be overcome

A

By increasing the concentration of the agonist

27
Q

How is the dose-response curve of an agonist affected by a competitive antagonist

A

Since more drug would be required to reach clinical effect, the curve would appear as a reduction in potency (right shift)

28
Q

How is the dose-response curve of an agonist affected by a noncompetitive antagonist

A

The curve is shift down, resembling a partial agonist

29
Q

How are the effects of noncompetitive antagonists reversed

A

By producing new receptors

fyi administering increased agonist drugs will not cause the agonist to out-compete and displace the noncompetitive drug

30
Q

What type of efficacy do inverse agonists have

A

Negative efficacy

31
Q

What are the 4 possible responses with coadministration of drugs

A

Addition
Synergism
Potentiation
Antagonism

32
Q

Describe the behavior of addition with coadministration of drugs
Given an example

A

Effect of two drugs given at the same time are added together
1+1=2
Morphine + dilaudid
ASA + ibuprofen

33
Q

Describe the behavior of synergism with coadministration of drugs
Give an example

A

Effect of two drugs given at the same time is GREATER than the sum of their individual effects
1+1=3
Propofol + midazaolam
Levodopa + carbidopa

34
Q

Describe the behavior of potentiation with coadministration of drugs
Give an example

A

Effect of one drug is enhanced by the drug that has no effect of its own
1+0=3

PCN + probenecid

35
Q

Describe the behavior of antagonism with coadministration of drugs
Give an examples

A

Simultaneous administration of one drug negates the effect of the second drug
1+1=0
Midazolam + flumazenil
Fentanyl + naloxone

36
Q

Define ED50 (effective dose 50)

A

the dose that produces the expected clinical response in 50% of the population

37
Q

Define LD50 (lethal dose 50)

A

The dose that produces death in 50% of the population

38
Q

Define TD50 (toxic dose)

A

The dose that produces toxicity in 50% of the population

39
Q

What is therapeutic index and what does it measure

A

The measure of drug safety

It’s a ratio between either LD50 or TD50 to ED50

40
Q

What is the ED50 a measure of

A

POTENCY

The dose that produces the expected clinical response in 50% of the population

41
Q

Describe the margin of safety in a drug that has either a narrow or wide therapeutic index

A

Narrow TI = narrow margin of safety (lower TD50:ED50 ratio)

Wide TI = wide margin of safety (higher TD50:ED50 ratio)

42
Q

Define chirality

A

Tetrahedral bonding of carbon to 4 DIFFERENT atoms

43
Q

What are enantiomers

A

Chiral molecules that are non-superimposable mirror images of another
This affects receptors that may be sterospecific

44
Q

How are R and S enantiomers related.

A

They are mirror images of each other. Not superimposable

45
Q

Give an example of drugs that have R and S enentiomers

A

Ketamine
Isoflurane
Morphine

46
Q

How does manipulation of the ratio of R and S enantiomers affect a medication

A

It can manipulate certain side effects

47
Q

What are racemic mixtures

A

They contain 2 enantiomers in equal amounts i.e. racemic epinephrine

48
Q

How does the amount of chiral carbons relate to enantiomers

A

The more chiral carbons means the more enantiomers that can be created