PHARMACOLOGY-pharmacodynamics Flashcards

(48 cards)

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
What effect can occur with continuous administration of an antagonist
Up-regulation of the target receptors
26
How can a competitive antagonist action be overcome
By increasing the concentration of the agonist
27
How is the dose-response curve of an agonist affected by a competitive antagonist
Since more drug would be required to reach clinical effect, the curve would appear as a reduction in potency (right shift)
28
How is the dose-response curve of an agonist affected by a noncompetitive antagonist
The curve is shift down, resembling a partial agonist
29
How are the effects of noncompetitive antagonists reversed
By producing new receptors fyi administering increased agonist drugs will not cause the agonist to out-compete and displace the noncompetitive drug
30
What type of efficacy do inverse agonists have
Negative efficacy
31
What are the 4 possible responses with coadministration of drugs
Addition Synergism Potentiation Antagonism
32
Describe the behavior of addition with coadministration of drugs Given an example
Effect of two drugs given at the same time are added together 1+1=2 Morphine + dilaudid ASA + ibuprofen
33
Describe the behavior of synergism with coadministration of drugs Give an example
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
Describe the behavior of potentiation with coadministration of drugs Give an example
Effect of one drug is enhanced by the drug that has no effect of its own 1+0=3 PCN + probenecid
35
Describe the behavior of antagonism with coadministration of drugs Give an examples
Simultaneous administration of one drug negates the effect of the second drug 1+1=0 Midazolam + flumazenil Fentanyl + naloxone
36
Define ED50 (effective dose 50)
the dose that produces the expected clinical response in 50% of the population
37
Define LD50 (lethal dose 50)
The dose that produces death in 50% of the population
38
Define TD50 (toxic dose)
The dose that produces toxicity in 50% of the population
39
What is therapeutic index and what does it measure
The measure of drug safety | It's a ratio between either LD50 or TD50 to ED50
40
What is the ED50 a measure of
POTENCY | The dose that produces the expected clinical response in 50% of the population
41
Describe the margin of safety in a drug that has either a narrow or wide therapeutic index
Narrow TI = narrow margin of safety (lower TD50:ED50 ratio) | Wide TI = wide margin of safety (higher TD50:ED50 ratio)
42
Define chirality
Tetrahedral bonding of carbon to 4 DIFFERENT atoms
43
What are enantiomers
Chiral molecules that are non-superimposable mirror images of another This affects receptors that may be sterospecific
44
How are R and S enantiomers related.
They are mirror images of each other. Not superimposable
45
Give an example of drugs that have R and S enentiomers
Ketamine Isoflurane Morphine
46
How does manipulation of the ratio of R and S enantiomers affect a medication
It can manipulate certain side effects
47
What are racemic mixtures
They contain 2 enantiomers in equal amounts i.e. racemic epinephrine
48
How does the amount of chiral carbons relate to enantiomers
The more chiral carbons means the more enantiomers that can be created