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Fundamental Of Disease > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

What is pharmacodynamics

A

The effects of drugs on the body

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2
Q

What happens when a drug binds to a receptor?

A

A change is brought about

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3
Q

Equation for receptor binding

A

L + R reversible LR

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4
Q

What is Kd?

A

Intrinsic factor in any pair of drug receptor complex. It varies with temperature.

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5
Q

The mass of action equation between bound and free receptors

A

Kd = (L)(R) / (LR)

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6
Q

As ligand concentration increases so does the concentration of…… (In diseases)

A

Bound receptors increase

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7
Q

As free receptor concentration increases so does……..

A

The receptor bound concentration does as well

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8
Q

Kd is defined as

A

50% of the available receptor occupied

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9
Q

Pharmacodynamics in relationship to dose response relationship curves

A

The relationship between the dose of the drug and the organisms response to the drug.

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10
Q

The response to a drug is proportional to……

A

Concentration of receptors that are. Bound by the drug.

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11
Q

What are the two types of dose responses curves?

A

Graded and quantum

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12
Q

Graded response curves

A

The effect of various doses on an individual

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13
Q

Quantal response curves

A

Effect of various doses of a drug on a population of individuals.

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14
Q

What are two important parameters that can be deduced from the graded response curve?

A

Potency and efficacy

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15
Q

What is the symbol denoted for potency?

A

EC 50

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16
Q

What is the symbol denoted for efficacy?

A

E max

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17
Q

What does the potency parameter mean?

A

Concentration at which the drug elicits 50% of its maximum response.

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18
Q

Agonist

A

If a drug-receptor binding results in the activation of the receptor.

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19
Q

Antagonist

A

Inhibits the drug from binding

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20
Q

In order for a drug to have a useful therapeutic effect to must?

A

Absorbed, distributed and eliminated

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21
Q

In order for drugs to have an effect they must.

A

Move for the site of administration to the site of action.

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22
Q

What is permeation?

A

Is the movement of drugs molecules from into and within the biological environment.

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23
Q

What are the four stages of permeation?

A

Aqueous diffusion
Lipid diffusion
Transport by special carrier
Endocytosis and pinocytosis

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24
Q

Aqueous diffusion

A

It is the movement of molecules through the watery extra cellular and intercellular spaces.

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25
Q

Lipid diffusion

A

Is the passive movement of molecules through the phospholipid membrane of cells and other lipid structures.

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26
Q

Special carriers

A

Drugs that do not readily diffuse through membeanes need endogenous substances to transport the molecules through the cells.

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27
Q

Endocytosis

A

The binding of the transported molecules to specialized components on the membrane(receptors) which cause the unfolding of the area of that membrane.

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28
Q

Endocytosis

A

Allows large proteins to get across membrane in the lipid form.

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29
Q

What was an example of endocytosis?

A

B12 and iron intrinsic factor

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30
Q

Exocytosis

A

The reverse process it is the expulsion of membrane encapsulated materials from the cells.

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31
Q

Frick’s Diffusion

A

Predicts the rate ochre movement of molecules across a barrier.

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32
Q

Receptors

A

Specific molecules in a biological system that drugs interact with to produce changes in the function of the system.

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33
Q

Receptor site

A

The binding region on a macromolecule and has relatively high and selective affinity for the drug.

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34
Q

Effectors

A

Molecules that translate the drug receptor integration into a change in a cellular activity.

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35
Q

Pharmacodynamics

A

Term used to describe the effects of a drug on the body.

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36
Q

Drug receptor binding

A

When a ligand binds to receptor a change is brought about .

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37
Q

Kd= koff/ kon

A

The intrinsic factor of any pair

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38
Q

What is the law of mass?

A

Kd

39
Q

What are the two types of dose response ?

A

Graded and Quantal

40
Q

Potency is

A

Concentration at which the drug elicits 50% of its maxiumum

41
Q

What is efficacy?

A

The maximum response produced by the drug and additional drug would yield no better response

42
Q

Spare receptor

A

When a drug does not use all its receptors but shows 100% maxiumum.

43
Q

There are two types of antagonist. What are there?

A

Receptors and non receptors

44
Q

Antagonist that bind to receptors are divided into two groups.

A

Active and allosteric

45
Q

Antagonist that do not bind to receptors are called non receptors. What are the tow groups of receptors?

A

Chemical and physiological

46
Q

What is a receptor antagonist?

A

A receptor antagonist bonds to either an active receptor or allosteric receptor.

47
Q

Properties of antagonist

A

antagonists have affinity but no efficacy for their cognate receptors, and binding will disrupt the interaction and inhibit the function of an agonist or inverse agonist at receptors

48
Q

What happen when an antagonist binds to an allosteric receptor?

A

antagonists have affinity but no efficacy for their cognate receptors, and binding will disrupt the interaction and inhibit the function of an agonist or inverse agonist at receptors

49
Q

The function of a non receptor anatagonist

A

It does not bind to the agonist receptor but binds to an allosteric receptor and stops the agonist from binding.

50
Q

How does non receptor work?

A

By inhibiting the agonist directly (antibodies) by inhibiting a downstream molecule in the activation pathway by activating a pathway that opposes the action of the agonist.

51
Q

Chemical antagonist

A

Inactivates an agonist before it has an opportunity to act

52
Q

Example of a chemical antagonist

A

Chemical neutralisation

53
Q

Physiological effect

A

Causes a physiological effect opposite to that induced by the agonist.

54
Q

Competitive receptor antagonist

A

Binds reversibly to the active site of a receptor. It does not stablises a conformation required for receptor activation.

55
Q

Example of a competitive receptor antagonist

A

Pravastatin

56
Q

Non competitive antagonist

A

Can bind to either the active site or allosteric site.

57
Q

Are non competitive antagonist irreversible

A

Yes

58
Q

Does high concentration of the agonist affect non competitive antagonist

A

No it does not

59
Q

What is the role of a non competitive allosteric antagonist ?

A

Prevents an agonist from working even if the agonist is bound to the active site.

60
Q

A receptor is bound to A Non competitive antagonist can it be useful again ?

A

No

61
Q

What effect does a competitive receptor have on potency?

A

It reduces the potency

62
Q

What effect does a non competitive receptor have on potency?

A

Nothing , non competitive receptors effect effacy and not potency

63
Q

Example of a non competitive antagonist

A

Aspirin

64
Q

How does aspirin work?

A

Irreversibly acetylates cyclo -oxygenase which generates thromboxane A2 in platelets . This prevents platelets from clotting.

65
Q

How long does aspirin remains In the body?

A

7- 10 days

66
Q

How long does it take to make platelets

A

7-10 days

67
Q

The role of a chemical antagonist

A

Involves a direct chemical interaction between the agonist and the antagonist in a way which renders the agonist pharmacologically inactive.

68
Q

What is an example of a chemical antagonist?

A

Protea mine binds stoichiomatically to the acidic heparin classes of anticoagulants.

69
Q

What type of antagonist is Dimercaprol?

A

A chelator if lead and some other toxic metals. Is used to treat toxicity from mercury, arsenic or gold

70
Q

What’s a physiological antagonist

A

Binds to a different receptor molecule producing an effect opposite to that produced by the agonist.

71
Q

Example of a physiological antagonist?

A

Beta adrenergic antagonist used in the treatment

72
Q

Specifity

A

Makes drugs selective to particular to certain tissues

73
Q

Affinity

A

The tendency of a drug to bind to its receptor

74
Q

Drug potency

A

Is when a drug has a high affinity for receptors and occupy a high
proportion of receptors at Low concentrations.

75
Q

Partial agonist

A

Drugs with intermediate levels of efficacy with 100% receptor occupancy.

76
Q

What are full agonist

A

Have sufficient efficacy to elicit maximal tissue response maximal tissue response

77
Q

What does drug dose response relationships show?

A

They show that biological responses are graded and will continuously increase up to a maximum as the administered dose is continuously increased.

78
Q

What is TD50?

A

Toxic dose which 50% of subjects showed a toxic response.

79
Q

ED50

A

Effective dose which causes response in 50% of subjects and is used to determine the potency of drugs

80
Q

LD 50

A

Lethal dose which causes death in 50% of cases

81
Q

Therapeutic index

A

Ratio of TD50 and ED50

82
Q

Which has a high therapeutic index Aspirin or Heparin

A

Heparin

83
Q

What is reversible competitive antagonism?

A

When the combination of competitive antagonist and the receptor is loose.

84
Q

What is irreversible competitive antagonism?

A

When the combination of the competitive antagonist and the receptor is covalent bonded

85
Q

Non competitive antagonism

A

This involves the antagonist acting at a site beyond the receptor for the agonist.

86
Q

Example of a non competitive antagonist

A

Hexamethonium and the nicotine acetylcholine receptor.

87
Q

The effect of an antagonist on an agonist dose response relationship

A

Reduces the potency of the agonist without affecting the efficacy.

88
Q

The effect of a non competitive antagonist on a drug dose curve

A

Does not effect the potency but effects the efficacy.

89
Q

Pharmacokinetic antagonist

A

Reduces the effect of the active drug of action

90
Q

Examples of drugs that exert a physiological antagonism effect

A

Histamine and salbutamol . Histamine constricts the respiratory airways while salbutamol relaxes it.

Describes the interaction of two agonist that act independently of each other but happen to cause opposite effects.

91
Q

Tolerance

A

Developed when it becomes necessary to increase the dose of a drug to obtain an effect previously obtained with a smaller dose.

92
Q

Tolerance can occur due to?

A

Change in receptors caused by desensitization
Loss of receptors by internalization of receptors
Exhaustion of mediators
Increased metabolic degradation of the drug.
Physiological adaptions
Active extrusions of drugs from the cells.

93
Q

What is tachyphylaxis?

A

This is a quick onset of acquired tolerance following its initial administration. Usually due to quick lost of efficacy of the drugs at the receptors responsible for eliciting the effect upon a drug binding.

Fundamental Of Disease (19 decks)

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