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Apex > Unit 4 Pharmacology: Pharmacodynamics > Flashcards

Unit 4 Pharmacology: Pharmacodynamics Flashcards

1
Q

Pharmacodynamics is the study of:

A

Effect site concentration and clinical effect

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2
Q

Pharmacokinetics is the study of:

A

Drug dose and plasma concentration

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3
Q

Pharmacobiophasics is the study of:

A

Plasma concentration and effect site concentration

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4
Q

What 4 things affect pharmacokinetics?

A

Absorption
Distribution
Metabolism
Elimination

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5
Q

What 10 concepts are involved in pharmacokinetics

A 
Volume of distribution
Half-lives 
Metabolism 
Enzyme induction and inhibition
Clearance
Steady state
Context sensitive half-time
Degree of ionization
Protein binding
Ion trapping
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6
Q

What concept is involved in pharmacobiophasics?

A

Rate constants between the plasma and effect site

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7
Q

What 11 concepts are involved in pharmacodynamics?

A 
Potency
Efficacy
Dose response curve
Agonist
Antagonist 
Partial agonist
Inverse agonist
ED50
LD50
Therapeutic index
Stereochemistry
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8
Q

On the dose response curve the x-axis represent what?

A

Potency

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9
Q

Define potency

A

The dose required to achieve a given clinical effect

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10
Q

What 5 things is potency affected by?

A 
Absorption
Distribution
Metabolism 
Elimination
Receptor affinity
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11
Q

What is ED50? ED90?

A

They are measures of potency.
ED50: the dose required to achieve a given effect in 50% of the population
ED90: dose required to achieve given effect in 90% of population

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12
Q

What does it mean if the dose response curve has a left shift?

A

Increased affinity for receptor -> higher potency -> lower dose required

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13
Q

What does it mean if the dose response curve has a right shift?

A

Decreased affinity for receptor -> lower potency -> higher dose required

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14
Q

What is efficacy? Where is it on the dose response curve?

A

A measure of the intrinsic ability of a drug to elicit a given clinical effect.
The height of the plateau on the y-axis represents efficacy

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15
Q

What does the slope represent on the dose response curve? Steeper means what?

A

How many receptors must be occupied to elicit a clinical effect.
A steep slope implies that most of the receptors must be occupied before we observe the clinical response.

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16
Q

What is individual variability? What explain it?

A

A particular dose may provide excellent clinical effect in one patient, but not another.
It is explained by differences in pharmacokinetics and pharmacodynamics in patients

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17
Q

What is a agonist?

A

Binds to the receptor and turns on a specific cellular response

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18
Q

What does an agonist mimic?

A

An endogenous ligand

19
Q

Continuous administration of an agonist may cause _______ of the target receptors.

A

Down-regulation - a decrease in the number of receptors making it less sensitive to the drug

20
Q

What is a partial agonist?

A

Binds to a receptor but is only capable of partially turning on a cellular response. It is less efficacious than a full agonist.

21
Q

What is another name for a partial agonist?

A

Agonist-antagonist

22
Q

What unique effect occurs with the use of an agonist AND partial agonist?

A

The partial agonist can block the effects of an agonist by competing for biding sites

23
Q

What is an antagonist?

A

It blocks the receptor from anything that could turn on a cellular response.

24
Q

Which way is the dose response curve shifted with use of a competitive antagonist?

A

It is shifted right for the agonist. Giving more of the agonist can overcome the antagonist.

25
Q

How does a non competitive antagonist bond? Can it’s effects be overcome?

A

Permanently, usually through covalent bonds.

The effects of a noncompetitve antagonist can only be reversed by producing new receptors.

26
Q

Which way does a noncompetitive antagonist shift the dose response curve?

A

It shifts it DOWN, so that it resembles a partial agonist.

27
Q

What is an inverse agonist?

A

Binds to the receptor and causes an opposite effect to that of a full agonist.

28
Q

An inverse agonist has ___ efficacy.

A

Negative

29
Q

Define addition:

A

Effect of 2 drugs given at the same time are added to each other
1 + 1 = 2

30
Q

Define synergism:

A

Effects of 2 drugs given at the same time is greater than the sum of their individual effects.
1 + 1 = 3

31
Q

Define potentiation:

A

Effect of one drug is enhanced by a drug that has no effect of its own.
1 + 0 = 3

32
Q

Define antagonism:

A

Simultaneous administration of one drug cancels out the effect of a second drug.
1 + 1 = 0

33
Q

Define ED50:

What is it a measure of?

A

Effective Dose 50: the dose that produces the expected clinical response in 50% of the population.
It is a measure of potency.

34
Q

Define LD50:

A

Lethal Dose 50: the dose that will produce death in 50% of the population.

35
Q

Define Therapeutic Index:

Equation:

A

A measure of drug safety. It is the ratio of the LD50 to the ED50

Therapeutic index = LD50 / ED50

36
Q

What is stereochemistry?

A

The study of the 3-dimensional structure of molecules

37
Q

What is chirality?

A

A division of stereochemistry that deals with molecules that have a center of 3-D asymmetry

38
Q

What is an enantiomer?

A

Chiral molecules that are non-superimposable mirror images of one another

39
Q

How are enantiomers distinguished from one another?

A 
By the direction in which they rotate when exposed to polarized light.
Dextrorotatory enantiomer (+) rotates clockwise
Levorotatory enantiomer (-) rotates counterclockwise
40
Q

What letters are used to describe the orientation of a specific stereocenter within a molecule?

A

R and S

D&L and R&S

41
Q

What is a racemic mixture?

A

Mixture that contains 2 enantiomers in equal amounts

42
Q

How common are enantiomers? Racemic mixtures?

A

About 1/3 of the dugs we administer are enantiomers, and just about all of them are racemic mixtures

43
Q

Examples of enantiomers

A 
ketamine
Thiopental
Methohexital
Isoflurane
Desflurane 
Mepivacaine 
Prilocaine 
Bupivacaine 
Morphine 
Methadone 
Ibuprofen
Ketoralac

Apex (46 decks)

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