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BIOM2402 > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

Module 1

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
Q

Prolonged exposure of receptors to drugs can lead to…

A

a loss in responsiveness

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26
Q

Receptor desensitisation:

A

Receptor stops responding to drug

–> An uncoupling with the second messenger system

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27
Q

Receptor down-regulation:

A

Loss of target receptors on cell

Receptors become internalised via endocytosis;
OR
Gets recycled and goes back to cellular surface

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28
Q

Analgesia:

A

Pain relief and sedation

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29
Q

Ligand-gated ion channels:

A

Nicotinic

Acetylcholine

30
Q

G-protein coupled receptors

A

i.e. Beta-adrenoreceptor

31
Q

Kinase-linked receptors:

A

Insulin receptor
3 different domains; receptor, transmembrane helix, and tyrosine kinase

Serine, threonine and tyrosine

32
Q

Multiple steps act to

A

Amplify signal

33
Q

Nuclear receptors

i.e. Estrogen receptor

A

Can take hours - days to illicit effect, relies on gene transcription

34
Q

Nuclear receptors class 1:

A

Present in the cytoplasm;

Upon activation, they form dimers and migrate to the nucleus;

*Ligands are mainly hormones.

35
Q

Nuclear receptors class 2:

A

Present in the nucleus;
Upon activation, they form dimers with retinoid X receptor;

*Ligands are mainly lipids.

36
Q

xxxMAB =

A

Antibody

37
Q

xxxNIB =

A

Kinase

38
Q

Some receptors exist in 2 states; ____ within equilibrium

A

resting or active

39
Q

The active state elicits a response in the _____

A

absence of a ligand

40
Q

An antagonist alone has no effect on the constitutive activity as it is not dependent on the binding of a drug. T/F

A

True

41
Q

Inverse agonist:

A

decreases response as it shifts the activated state to the resting state

42
Q

Partial agonists:

A

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
Q

Intrinsic activity:

A

The difference between affinity for the activated and resting state

44
Q

Cooperativity:

A

when a receptor contains >1 binding site that are NOT independent of each other

45
Q

Positive cooperative binding:

A

Binding of first molecule enhances the binding of the second molecule)

46
Q

Negetive cooperative binding:

A

Binding of first molecule inhibits the binding of the second molecule)

47
Q

Bioassay:

A

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
Q

Type 1 error:

A

Where you get a difference when there is no difference.

49
Q

Type 2 error:

A

Where you do not get a difference when there is one

50
Q

Type 1 and Type 2 errors can be overcome by…

A

Increasing patient numbers

51
Q

Non-deleterious drug reactions:

A

side effects within therapeutic range

52
Q

Deleterious drug-reactions:

A

Toxic effect; effects above therapeutic range

53
Q

Side effects occur within the…

A

Therapeutic range

54
Q

Adverse effects occur within the…

A

Exceeded therapeutic range

55
Q

Allergic reactions:

A
  1. Anaphlaylactic
  2. Cytolytic
  3. Arthus
  4. Delayed hypersensitivity
56
Q

Anaphalaylactic reactions:

A

IgE activated mast cells to release mediators, i.e. histmaine

57
Q

Cytolyic reactions:

A

IgG and IgM induce cell lysis

58
Q

Arthus reactions:

A

IgG induce an inflammatory response through complement activation

59
Q

Delayed hypersensitivity:

A

Inflammatory reaction due to production of lymphokines

60
Q

Within receptor desensitization, the sigmoidal curve shifts to the…

A

Right

61
Q

An example of receptor down-regulation is…

A

i.e. Insulin receptors –> Diabetes T2

62
Q

Biased signalling occurs when:

A

An agonist can activate different pathways by binding to the same receptor

63
Q

Only agonists can activate receptors. T/F

A

True

64
Q

The two-state receptor model explains:

A

Why some agonists can decrease activity instead of increasing it

65
Q

Spare receptors are unimportant for…

A

Antagonists

66
Q

A non-competitive antagonists _____ maximum effect

A

Increases

67
Q

Functional antagonists:

A

Activate biological pathways that act in opposite directions

68
Q

Occupation is goverened by:

A

Affinity

69
Q

Activation is goverened by:

A

Efficacy

70
Q

Evidence shows that many full agonists were

capable of eliciting maximal responses at very low occupancies. This is an example of:

A

Spare receptors

71
Q

Antagonists have an efficacy of ___

A

antagonists have zero efficacy

BIOM2402 (4 decks)

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