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BIOM2402 > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

Module 1 (71 cards)

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1
Q

Pharmacodynamics:

A

The study of drugs on living tissue

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2
Q

In comparison to common-names and commercial names, common names are ___ capitalized

A

not

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3
Q

Agonists:

A

Activate receptors

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4
Q

Antagonists:

A

Inhibit receptors; bind to receptors without producing a response.

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5
Q

Antagonists prevent agonists from having an effect. T/F

A

True

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6
Q

Competitive antagonists can be overcome by:

A

Increasing dose of agonist

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7
Q

Non-competitive antagonists:

A

Can not be overcome by incr. Dose of agonist

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8
Q

Functional antagonists:

A

Inversely proportional effect on respective receptors

*Drugs that increase heart rate are functional antagonists of those that decrease heart rate

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9
Q

Emax:

A

When all receptors are occupied

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10
Q

EC50:

A

Half maximum response, point of inflection

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11
Q

K1:

A

Rate at which drug and receptor combine

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12
Q

K2:

A

Rate at which drug receptor complex comes apart

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13
Q

Drug Receptor Binding:

A

The affinity of the drug for the receptor

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14
Q

Response:

A

How well the activated receptor couples to downstream receptor pathways

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15
Q

The sigmoid curve:

Response moves to the right:

A

Less potent

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16
Q

The sigmoid curve:

Response moves to the left:

A

More potent

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17
Q

Within the dose-response curve, the potency is on the _ axis

A

potency: x-axis

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18
Q

Within the dose-response curve, the efficacy is on the _ axis

A

efficacy: y-axis

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19
Q

Drugs with a _____ therapeutic window are safe

A

Large

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20
Q

Drugs with a _____ therapeutic window are not safe

A

Small

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21
Q

Drugs with no therapeutic window:

A

The effect and adverse effect occur simultaneously

i.e. Chemotherapy

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22
Q

Therapeutic Index =

A

Amount that causes an effect : Amount that causes toxicity

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23
Q

The therapeutic window and therapeutic index are…

A

measures of safety

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24
Q

Maximum response requires maximum receptor occupancy. T/F

A

False

–> Spare receptors

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25
Prolonged exposure of receptors to drugs can lead to...
a loss in responsiveness
26
Receptor desensitisation:
Receptor stops responding to drug --> An uncoupling with the second messenger system
27
Receptor down-regulation:
Loss of target receptors on cell Receptors become internalised via endocytosis; OR Gets recycled and goes back to cellular surface
28
Analgesia:
Pain relief and sedation
29
Ligand-gated ion channels:
Nicotinic | Acetylcholine
30
G-protein coupled receptors
i.e. Beta-adrenoreceptor
31
Kinase-linked receptors:
Insulin receptor 3 different domains; receptor, transmembrane helix, and tyrosine kinase Serine, threonine and tyrosine
32
Multiple steps act to
Amplify signal
33
Nuclear receptors | i.e. Estrogen receptor
Can take hours - days to illicit effect, relies on gene transcription
34
Nuclear receptors class 1:
Present in the cytoplasm; Upon activation, they form dimers and migrate to the nucleus; *Ligands are mainly hormones.
35
Nuclear receptors class 2:
Present in the nucleus; Upon activation, they form dimers with retinoid X receptor; *Ligands are mainly lipids.
36
xxxMAB =
Antibody
37
xxxNIB =
Kinase
38
Some receptors exist in 2 states; ____ within equilibrium
resting or active
39
The active state elicits a response in the _____
absence of a ligand
40
An antagonist alone has no effect on the constitutive activity as it is not dependent on the binding of a drug. T/F
True
41
Inverse agonist:
decreases response as it shifts the activated state to the resting state
42
Partial agonists:
have affinity for both states of the receptor. Thus, it activates like a full agonist but also inactivates at the same time. The net effect is a lower maximum effect
43
Intrinsic activity:
The difference between affinity for the activated and resting state
44
Cooperativity:
when a receptor contains >1 binding site that are NOT independent of each other
45
Positive cooperative binding:
Binding of first molecule enhances the binding of the second molecule)
46
Negetive cooperative binding:
Binding of first molecule inhibits the binding of the second molecule)
47
Bioassay:
The comparison of an unknown to a set of standards using biological activity 1. Construct a curve of standard activity 2. Measure activity of unknown 3. Measure the concentration from curve
48
Type 1 error:
Where you get a difference when there is no difference.
49
Type 2 error:
Where you do not get a difference when there is one
50
Type 1 and Type 2 errors can be overcome by...
Increasing patient numbers
51
Non-deleterious drug reactions:
side effects within therapeutic range
52
Deleterious drug-reactions:
Toxic effect; effects above therapeutic range
53
Side effects occur within the...
Therapeutic range
54
Adverse effects occur within the...
Exceeded therapeutic range
55
Allergic reactions:
1. Anaphlaylactic 2. Cytolytic 3. Arthus 4. Delayed hypersensitivity
56
Anaphalaylactic reactions:
IgE activated mast cells to release mediators, i.e. histmaine
57
Cytolyic reactions:
IgG and IgM induce cell lysis
58
Arthus reactions:
IgG induce an inflammatory response through complement activation
59
Delayed hypersensitivity:
Inflammatory reaction due to production of lymphokines
60
Within receptor desensitization, the sigmoidal curve shifts to the...
Right
61
An example of receptor down-regulation is...
i.e. Insulin receptors --> Diabetes T2
62
Biased signalling occurs when:
An agonist can activate different pathways by binding to the same receptor
63
Only agonists can activate receptors. T/F
True
64
The two-state receptor model explains:
Why some agonists can decrease activity instead of increasing it
65
Spare receptors are unimportant for...
Antagonists
66
A non-competitive antagonists _____ maximum effect
Increases
67
Functional antagonists:
Activate biological pathways that act in opposite directions
68
Occupation is goverened by:
Affinity
69
Activation is goverened by:
Efficacy
70
Evidence shows that many full agonists were | capable of eliciting maximal responses at very low occupancies. This is an example of:
Spare receptors
71
Antagonists have an efficacy of ___
antagonists have zero efficacy

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