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Pharmacology Test 1 > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

What are drugs?

A
  • any substance that brings about therapeutic change

- can vary in size from very small (MW <10) to very large (MW >10,000); too large|small creates issues

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2
Q

Pharmacodynamic

A

effect the drug has on the body

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3
Q

Agonism

A
  • inducer/stimulator
  • mimic actions of endogenous compounds
  • interacts with a receptor to produce a response
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4
Q

Partial Agonism

A
  • best can do is less than agonist

- still stimulates but not as well

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5
Q

Inverse Agonism

A
  • stimulate baseline level to 0
  • binds to the same receptor as an agonist, but produces the OPPOSITE effect
  • requires that the receptor has a basal level of activity in absence of ligand
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6
Q

Antagonism

A
  • blockers: don’t stimulate anything

- no internal activity of its own; only BLOCK

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7
Q

Receptors determine relationship

A
  • # receptors occupied by drug (affinity: how tightly bound)

- total # receptors there are = max level

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8
Q

Effect (equation)

A

[D] x Emax
__________
[D] + EC50

Emax: maximal effect
EC50: drug concetration that elicits half-max response (inflection curve of the S on a chart)

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9
Q 
Potency Ratio (equation)
(Potency comparison between two drugs)
A

EC50 Drug A
____________
EC50 Drug B

  • difference in potency between two drugs
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10
Q

Potency Definition

EC50 Relationship

A
  • measure of how much drug is required to elicit a response

- —- HIGH EC50=LOW potency (inverse relationship!)

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11
Q

Efficacy

A

DIRECT RELATIONSHIP TO Emax
-higher Emax = greater efficacy

EFFICACY is not POTENCY

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12
Q

Efficacy and Potency uses

A
  • Efficacy = what drug/selection choice (also take into consideration drug side effects)
  • Potency = dose/how much in needed
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13
Q

Antagonists

A
  • block actions of endogenous agonists
  • function’s “invisible”
  • monitor antagonist by effect on known agonist
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14
Q

Competitive Antagonists

A
  • reversible binding
  • highest affinity wins
  • can be overcome by adding more agonist

***Emax UNCHANGED, EC50 INCREASES (makes agonist appear less potent)

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15
Q

Noncompetitive Antagonists

A
  • irreversible binding
  • prevents agonist from reaching Emax
  • can not be overcome by adding more agonist

***Emax REDUCED (due to the reduced number of receptors) EC50 UNCHANGED (makes agonist appear less efficacious; makes appear as partial agonist)

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16
Q

Spare Receptors

A
  • when there are more receptors than needed to achieve Emax (max response)
  • no different from non-spare receptors
  • target max response with less drug
  • ** Increase the sensitivity of the tissue toward the drug
  • ——increase likelihood of a drug being bound when present at low concentrations
17
Q

How are spare receptors revealed?

A

by using irreversible antagonists to prevent agoinst binding to a portion of receptors

  • makes appear competitive because of spare receptors
  • antagonist wont block all receptors to begin with; will need to increase [antagonist] and see if you get a noncompetitive response over time
18
Q

Limitations of Graded Dose Response Curves

A
  • difficult to construct when pharmacological response is an “either-or” situation
  • a quantitative dose-response relationship in a single individual may have limited applicability to other individuals, due to inter-individual variability
  • clinical trials Y/N: can’t measure shades of grey
19
Q

Quantal Dose-Response Curve

A
  • dose required to produce a specified response in a large number of individuals
  • ** provide the median effective dose (ED50) at which 50% of the individuals exhibit the specified quantal response***
  • dose in which 50% of people in the study responded
  • ** provides a convenient way to compare the ED50 and TD 50 of drugs in a clinical setting
20
Q

Toxic Dose

A
  • dose required to produce a particular toxic response in 50% of people
21
Q

Therapeutic Index

A
  • margin of safety of a drug; determined in part by dose-response curve and comparing ED50 and TD50
  • higher TI = better/safer
  • TI below 5% difference = v. toxic drug
22
Q

Therapeutic Index (equation)

A

TD50
_____
ED50

Pharmacology Test 1 (8 decks)

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