Pharmacodynamics Flashcards

1
Q

What do drugs do?

A
  • alter the rate of bodily functions

- modulate intrinsic physiological functions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Law of Mass Action

A

-rate of association of a molecule to a surface is equal to the rate of dissociation of the molecule from the surface

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Adsorption isotherm depends on the interaction of which 2 molecules?

A

ligand and receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Receptor occupation theory

A

a bimolecular interaction where a drug binds reversibly to the receptor so equilibrium is reached

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Orthosteric agonist

A

a drug agonist activating the same receptor site as that acted upon by a physiological agonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What happens to a dose-response curve when transferred to a logarithmic plot?

A

sigmoidal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

How do you find potency of drug using a dose response curve?

A

50% response across and then down to the dose concentration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is the intrinsic activity of a drug?

A

the ability of a ligand to activate a receptor and the signal transduction system linked to that receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is the equation for intrinsic activity and how can you interpret the results?

A

Emax of an agonist/Emax of full agonist
alpha=1 – full agonist
alpha >0,<1 – partial agonist
alpha=0 – antagonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Why would an agonist be classified as a partial agonist?

A
  • slow on/off receptor kinetics

- partial receptor activation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What are spare receptors?

A

The percentage of receptors that are left over after reaching maximal efficacy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Which has more of an effect on signal transduction activation: affinity for receptor or intrinsic activity?

A

affinity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

The potency of a drug is dependent on what?

A
  • affinity (binding of the receptor)

- efficacy (response elicited by drug-bound receptor)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What are common allosteric antagonists?

A

activating antibodies (IgG)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Allosteric antagonists have uniformly ______ intrinsic activity.

A

less

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What is an allosteric antagonist’s potency compared to agonists?

A

can be more or less potent

17
Q

Clinical dose range

A

20-80% of dosage curve

18
Q

All competitive antaganists are __________

A

orthosteric

19
Q

Antagonists are generally ______ lipid soluble, higher relative ________, and _______ molecular weight

A

more; affinity (for receptor); larger

20
Q

what is DR10?

A

dose required to increase ED50 by 10-fold

21
Q

What are the 2 forms of non-competitive agonists?

A

orthosteric irreversible antagonism: “suicide molecule”

allosteric antagonism: conformational change that does not allow binding of ligand (hormone or drug)

22
Q

“Suicide molecules” are _______-dependent

A

concentration

23
Q

What kind of drug has pharmacological effects than far outlast their duration in the plasma?

A

“suicide” molecules/orthosteric irreversible antagonism

24
Q

How can the body reactivate its receptor after an orthosteric irreversible antagonist/”suicide” molecule binds?

A

using lysosomal degradation of the covalently bound receptor and synthesize new receptors

25
Q

How do you calculate therapeutic index?

A

LD50/ED50

26
Q

How do you calculate margin of safety?

A

LD01/ED99

27
Q

What is a constitutively active receptor?

A

receptor has a basal activity level that can be increased in presence of agonist, but not needed

28
Q

What is an inverse agonist?

A

binds to constitutively active receptor causing an uncoupling and decrease in signal transduction in a dose-dependent manner

29
Q

What are the types of bias in signal transduction pathways?

A
  • balanced signaling bias
  • Agonist (ligand) bias
  • Receptor bias
  • Tissue bias