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Biomedical Pharmacology > Lecture 1: Introductory Principles > Flashcards

Lecture 1: Introductory Principles Flashcards

1
Q

Pharmacodynamics

A

The branch of pharmacology concerned with effects of drugs, and the mechanism of their action. The effect of a drug on the body

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2
Q

Pharmacokinetic

A

The branch of pharmacology concerned with the movement of drugs through the body. The effect of body on a drug

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3
Q

Agonist

A

Any substance that can produce a functional response at a target site

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4
Q

Antagonist

A

A substance that stop a normal physiological response from occurring e.g. blocking neurotransmitter release

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5
Q

Occupancy

A

How much of a drug blocking receptors or recognition sites

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6
Q

Affinity

A

Ability to bind The higher the affinity the higher the occupancy

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7
Q

Efficacy

A

The functional response

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8
Q

Potency

A

The concentration of a drug needed to get an effect

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9
Q

What are the targets for drug action?

A

Receptors, Ion channels, enzymes and transporters/carrier molecules

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10
Q

Receptors

A

A recognition molecule for an endogenous chemical mediator Sensing element in the system of chemical communication that coordinates function of all different cells in body, the chemical messengers

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11
Q

Ion channels

A

Gateways in cell membrane Selectively allow passage of particular ions Ligand gated ion channel: only open when one or more agonist molecules are bound Voltage-gated channel: gated by changes in the transmembrane potential

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12
Q

How does drugs affect ion channel function?

A

Bind to channel protein itself or by indirect interaction involving a G protein A drug may directly block a pore or a drug may bind to part of an ion channel

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13
Q

Enzymes

A

Pharmacologically active drugs that can be activated by the correct enzyme in the area it needs to be activated

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14
Q

Transporters/carrier molecules

A

Transport of ions and many organic molecules across renal tubule, the intestinal epithelium and the blood brain barrier

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15
Q

What does activation mean?

A

The receptor is affected by the bound molecule and will elicit a tissue response

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16
Q

What does the occupation of receptors Increase?

A

The affinity of a drug for any target

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17
Q

What can agonist mimic the effect of?

A

Endogenous molecule

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18
Q

What does agonist possess?

A

Significant efficacy

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19
Q

What does antagonist have?

A

Zero efficacy

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20
Q

What does the law of mass action give rise to?

A

Dissociation constant

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21
Q

What does the law relate?

A

That the rate of chemical reaction is proportional to the concentration of the reacting substance

22
Q

What is the dissociation constant?

A

A constant between free drug/free receptor concentration and drug/receptor concentration in other equation

23
Q

What happens when you increase concentration of drug?

A

Shift equilibrium to right (elevation in drug receptor complex)

24
Q

What does it mean if a drug has high affinity for its receptors?

A

Low dissociation constant

25
Q

What is kd?

A

The concentration at which half of the receptors are occupied by drugs

26
Q

What is high affinity of a drug for a receptor?

A

High occupancy of drug binding to receptor

27
Q

High affinity drug

A

Low kd

28
Q

Low affinity drug

A

High kd

29
Q

What are key considerations for binding?

A

Total binding Non specific binding Specific binding

30
Q

What is proportional to degree of radioactivity that can be measured within test solution?

A

Amount of binding you have to a receptor

31
Q

How can specific binding be measured?

A

Substractive process

32
Q

What does the binding curve define?

A

Relationship be ween concentration and the amount of drug bound

33
Q

What does scarchard plot give?

A

Straight line from which the binding parameters K and Bmax can be calculated

34
Q

What experiment can be used to determine efficacy and potency?

A

The bioassay experiment

35
Q

What is an example of bioassay?

A

Organ bath

36
Q

Why doesn’t concentration-response curve give direct estimates of affinity of drugs for receptors?

A

Relationship between receptor occupancy and response is usually non-linear

37
Q

E-max

A

Measure of efficacy - the maximal response that the drug can produce

38
Q

EC-50

A

Effective concentration that produces 50% is the maximum response - a measure of potency

39
Q

Potency

A

A measure of drug activity, governed by both affinity and efficacy

40
Q

Efficacy

A

The ability of a drug to cause a functional response as a result of binding to its receptor

41
Q

What efficacy do partial agonists have?

A

Less than 1

42
Q

What are full agonists?

A

Compounds that are able to elicit a maximal response following receptor occupation and activation

43
Q

What are partial agonist?

A

Compounds that can activate receptors but are unable to elicit the maximal response of the receptor system

44
Q

What does occupancy and affinity show?

A

How a drug binds to receptor

45
Q

What does efficacy and potency show?

A

What happens when the drug is bound to receptor

46
Q

What is reversible competitive antagonism?

A

Bind to receptors reversibly A parallel shift to the right of dose-response curve The maximum response is not depressed Both free to associate/dissociate from target site Raising the agonist concentration can restore the agonist occupancy

47
Q

What is irreversible competitive antagonism?

A

Produces a parallel shift to the right Depresses the maximum response Effectively remove receptors

48
Q

How do you quantify antagonism?

A

An antagonist has no efficacy Hence need a suitable agonist, the action of which can be inhibited by the antagonist of interest Antagonist potency can be expressed in the form of PA2 value

49
Q

What is the PA2 value?

A

Negative logarithm of the molar concentration of antagonist which will reduce the response of a tissue to a double dose of agonist to that of a single dose of agonist

50
Q

The schools plot

A

Conduct an organ bath experiment examining tissue response to an agonist in the presence of increasing concentrations of antagonist

51
Q

What is the dose ratio?

A

Dose needed in presence of antagonist compared to dose needed with no antagonist

52
Q

What are other times of antagonism?

A
  1. Chemical antagonism 2. Pharmacokinetic antagonism 3. Physiological antagonism

Biomedical Pharmacology (19 decks)

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