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Flashcards in Intro to Pharmacodynamics Deck (27):
1

What kind of curve are you going to get when you plot a drug dose arithmetically?

Hyperbolic Curve

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2

What kind of curve are you going to get when you plot a drug dose as a logarithm?

Sigmoidal Curve

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3

The maximal effect that can be produced by the drug is ___________.

Emax

4

The does of drug that produces 50% of its maximal effect is ___________.

ED50

5

Which question does a Graded Response answer?

What is on the "y-axis"?

"How much?"

Effect of the drug is on the "y-axis"
- i.e. Arterial Pressure Change 

6

Which question does a Quantal Response answer?

 

"Binary" Responses

All or non / Yes-no

"Does the response occur or not?"
"In how many?"

Requires a Pre-Defined Response: Death falling asleep, 10% reduction in blood pressure

7

What is the name of the curve that measures the number or % of individuals responding at a dose of a drug and only at that does?

Non-Cumulative Quantal Dose Response Curve

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8

What is the name of the curve that measures the number or % of individuals responding to a dose of a drug AND at all doses lower than that dose?

Cumulative Quantal Dose Response Curve

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9

How do you calculate the Therapeutic index?

What does that value tell you?

TI = TD50 / ED50

The Higher the TI, the SAFER the drug

TD50 - Median Toxic Dose

10

The range of doses of a drug or of its concentration in a bodily system that provides for the safe and effective therapy is referred to as __________ . 

Therapeutic Window

11

Differentiate between narrow and wide therapeutic windows.

Wide: Not expecting to seem many Adverse Side Effects

12

Name the three parameters that describe the interaction of a drug with a receptor.

1. Affinity

2. Selectivity

3. Intrinsic Activity

13

What does the affinity of a drug with its receptor tell you?

High Affinity --> Good drug-receptor interaction; LESS drug is needed to produce a response

Low Affinity --> Poor drug-receptor interaction; MORE drug needed to produce a response

14

What does the selectivity of a drug with its receptor tell you?

A more selective drug would affect FEWER targets over a specific concentration range

15

What does the intrinsic activity of a drug with its receptor tell you?

Agonists and Antagonist

Antagonists --> Block the response so that it DOES NOT have intrinsic activity

16

Describe the different types of Agonists.

1. Full Agonists

2. Partial Agonists (Emax is lower here than in FULL agonists)

3. Inverse Agonists

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17

Action at the SAME receptor as the endogenous ligands is what type of Actagonism?

Pharmacologic (Receptor) Antagonism

Can have Agonist AND Allosteric Site Binding

18

What type of antagonism is present when chemical antagonist makes the other drug unavailable?

Chemical Antagonism

19

What type of Antagonism occurs between endogenous pathways regulated by different receptors?

Physiologic Antagonism

20

How do you control the drug effects when beneficial and adverse effects are mediated by the same receptors/signal transduction pathway on the same cell types?

TIGHT dose control 

Ex: Insulin and DM1

21

How do you control the drug effects when beneficial and adverse effects are mediated by the same receptors/signal transduction pathway on different cell types?

AVOID systemic administration

Ex: B2 agonist acts on Bronchi, Blood Vessels and the Liver

22

How do you control the drug effects when beneficial and adverse effects are mediated by different types of receptors?

HIGHLY selective drugs are going to have LESS side effects

23

Which axis will you look at to get the ED50 measurement? What does ED50 tell you?

X-AXIS

 

Tells you how potent the drug will be! Lower ED50 means the drug will be MORE potent

24

Describe the relationship between KD and Affinity.

INVERSE

(Low KD = High Affinity)

25

Which axis will you look at to get the Emax measurement? What does Emax tell you?

Y-AXIS

 

Tells you the efficacy of the drug! Higher Emax means you will have a more effective drug

26

What type of Antagonism takes place when you have an increase in EC50 and no change in Emax?

Competitive Antagonism

27

What type of Antagonism takes place when you have an increase in Emax and no change in EC50?

Non-Competitive Antagonism