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U4 APEX PHARMACODYNAMICS- COMPLETE Flashcards

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1
Q

Pharmacodynacmis is the study of

A

Effect site concentration and CLINICAL EFFECT

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2
Q

Describes the relationship between the DRUG DOSE AND PLASMA CONCENTRATION

A

Pharmacokinetics

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3
Q

Pharmacobiophasics unites

A

Pk and PD by examining the relationship between plasma concentration and effect site concentration

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4
Q

Pharmacokinetics studies primarily 2 things

A

Drug dose
Plasma concentration

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5
Q

Pharmacobiophasics studies primarily 2 things

A

Plasma concentration
Effect site concentration

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6
Q

Pharmacodynamics studies primarly 2 things

A

Effect site concentration

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7
Q

Mnemonic to remember each pharmk,pharmB, PharmD

A

KBD
DPEC

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8
Q

What the body does to the drug

A

Pharmakinetics

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9
Q

Relationship is affected by

A

ADME

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10
Q

The biophase aka

A

Effect site

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11
Q

What the drug does the body

A

Pharmacodynamics

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12
Q

Pharmacodynamics concepts
PEDAPIA LETS

A

Potency
Efficacy
Dose response curve slope
Agonist
Partial Agonist
Inverst agonist
Antagonist
LD50
ED50
Therapeutic index
Stereochemistry

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13
Q

On the dose response curve, the x-axis correlates with:

A

Potency

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14
Q

Dose requires to achieve a given clinical effect

A

potency

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15
Q

Intrinsic ability of a drug to elicit a given clinical effect.

A

Efficacy

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16
Q

Potency is on ___axis, efficacy on ____axis

A

x; y

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17
Q

What does the slope of the dose response curve tells us?

A

How many receptors must be occupied to elicit a clinical effect.

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18
Q

Dose response curve from multiple patients to learn abou tthe

A

individual variability of each patient.

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19
Q

Measure of potency 2

A

ED 50 and E90

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20
Q

The curve shifts to left meaning as far as affinity , potency , dose

A

Increase affinity for receptor, HIGHER POTENCY, lower dose required

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21
Q

The curve shifts to right meaning as far as affinity , potency , dose

A

Decrease affinity for receptor, LOWER POTENCY, Higher dose required

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22
Q

The height of the plateau on the y-axis represents

A

efficacy

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23
Q

Higher plateau means _____efficacy

A

Greater

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24
Q

Lower plateau means _______ efficacy

A

Lower

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25
A steep slope on the dose-response curve implies
Most of the receptors must be occupied before we observe the clinical response.
26
Once the effect is observed, small increase in the dose can have a
Profound clinical effect.
27
Medications with steep slope
NMB and inhaled anesthetics.
28
A drugs that binds to a receptor follows which law?
LAW of mass action
29
There is rate constant for
Drug binding and a rate constant for dissociation from the receptor.
30
Remember that efficacy is measured by the
height of the y-axis on the dose response curve.
31
Mimics an endogenous ligand
agonist
32
Instructs the receptor to produce its maximal response
A full agonist
33
Different drugs may produce the same clinical effect but each may require a different dose to do so. this is difference in
potency
34
Continuous administration of an AGONIST may cause (UP or down)
DOWN=REGULATION of the target receptors.
35
Examples of full agonist at the beta receptor
NE
36
It is less efficacious than a full agonist
Partial agonist
37
A partial agonist is also called
Agonist-antagonist
38
It can block the effects of an agonist by competing for binding sites
Partial agonist.
39
Giving a partial opioid agonist to an opioid addicted patient can
Precipitate withdrawal
40
Nalbuphine what you should no?
provides pain relief but there is a ceilling to its efficacy.
41
Sits in the receptor and prevents an agonist from binding to it, does not tell the cell to do anything.
Antagonists
42
By definition no efficacy
Antagonist
43
Continuous ADMINISTRATION of an ANTAGONISTS may cause
UPREGULATION Of target receptors.
44
Competitive antagonism is (reversible vs irreversible)
reversible
45
If a pt receives a competitive antagonist, the dose response curve for the agonist shifts to
shifts to the right.
46
Increasing the concentration of the agonist in a competitive antagonism can
overcome competitive antagonism (the agonist can achieve the same efficacy) but since it requires more drug molecules to achieve the desired clinical effect, the dose response would reflect a reduction in potency.
47
Example of competitive antagonism: Rocuronium competes with
Ach at the NMJ. Increasing the concentration of one susbtance increase its ability to compete for the binding site on the receptors/.
48
NONCompetitive antagonism is (reversible vs irreversible)
Not reversible (irreversible)
49
Permanently bind to a receptor through covalent bonds and their effect cannot be overcome by increasing concentration of agonist.
Noncompetitive antagonists.
50
Noncompetitive antagonists shifts dose response curve for the agonist
down, so that it resembles a partial agonist
51
The effects of noncompetitive antagonists can be only reversed by
producing new receptors. This explains why these drugs have long duration of action.
52
Example of noncompetitive antagonists?
ASA inhibits the COX-1 enzyme for the entire life of the platelet.
53
Has negative efficacy
Inverse Agonist
54
Binds to the receptor and causes an opposite effect to that of a full agonist
Inverse agonist.
55
Epinephrine is a
Full agonist
56
Epinephrine (Full agonist) binds to beta 1 receptor to _______while propranolol (an inverse agonist) binds to the beta-1 receptor to_____
increase cAMP, Decrese cAMP
57
G protein modulates
cAMP production
58
G protein: An agonist completely
activates the receptor and increase cAMP production
59
G proteins; A partial agonist
Partailly activates the receptors, it increases cAMP production, but not as much as a full agonist.
60
G Proteins: An inverse agonist
Activates the receptor, but because it causes the opposite effect of the agonist, it decreases cAMP production
61
G proteins: Antagonists
blocks the ability of the agonist to bind with the receptor, but it does not increase or decrease cAMP production .
62
A new induction agent has a median effective dose of 125 mg and the median lethal dose of 1500 mg. Calculate the TI of the drug?
LED (how to remember) LD50/ ED50 = TI 1500mg/125mg = 12 mg
63
What is the ED50?
dose that produces the expected clinical response in 50% of the population .
64
ED50 is a measure of
Potency
65
LD 50 is the dose that will
produce death in 50% of the population
66
The Therapeutic index is a measure of
Drug safety
67
TI is the ratio of
TI= LD50/ ED 50
68
A drug with narrow therapeutic index has a
narrow margin of safety : Examples VA and chemotherapy
69
A drug with WIDE therapeutic index
has a wide margin of safety.
70
Chirality is a division of
Stereochemistry
71
Deals with molecules that have a center of
3D symmetry
72
A molecule with 1 chiral carbon will exist as
2 enantiomers
73
The more chiral carbons in a molecue, the ____enantiomers that are created
More
74
A racemic mixture contains
2 enantiomers in equal amounts.
75
Study of 3 D structures of molecules
Stereochemistry.
76
Enantiomers are
chiral molecules that are NON-SUPERIMPOSABLE MIRROR IMAGES of one another.
77
Enantiomers are distinguished from each other by
the direction they rotate when exposed to polarized light.
78
The D means
Dextrorotary enantiomer
79
The dextrorotary enantiomer (+) rotates
Clockwise (think Positive DC)
80
The L means
Levorotary enantiomer
81
The Levorotary enantiomer (-) rotates
Counterclockwise (Negative Lcount)
82
What is a racemic mixtures
Contains 2 enantiomers in equal amount. About 1/3 of the drugs we administer are enantiomers, and just about all of these are prepared as racemic mixtures.
83
Drugs that exists as enantiomers often function as
2 different drugs, with different affinities for the target receptors and different side effects.
84
Clinical examples of racemic mixtures: bupivacaine
S-bupivacaine (Levobupivacaine) is less cardiotoxic than the R-bupivacine or the racemic mixtures
85
Clinical examples of racemic mixtures: Ketamine
S enantiomer of ketamine is less likely to cause emergene delirium than the R form, the S form is also more potent.
86
Examples of racemic mixtures VA
Isoflurane Desflurane
87
Examples of racemic mixtures IV anesthetics
Ketamine Thiopental Methohexital
88
Examples of racemic mixtures : Amide LAs
Mepivacaine Bupivacaine Prilocaine
89
Examples of racemic mixtures: Pain meds
IBuprofen Ketorolac Methadone Morphine

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