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Wolford NUAN 5232 - Pharm: Pharmacodynamics > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

The study of what the drug does to the body?

A

Pharmacodynamics

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2
Q

The amount of drug at the receptor is a function of:

A

Dose, Time, & Pharmacokinetics

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3
Q

What is a ligand?

A

Anything that binds

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4
Q

Law of Mass Action

A

D+R=DR Complex
Concentration of ligand + Concentration of receptors = Drug-Receptor Complex
(the higher the concentration the greater the tendency to form)

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5
Q

The interaction of a ligand/drug binding depends on 2 things:

A

Affinity & Intrinsic activity

attraction & effect when it interacts

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6
Q

Dose-Response Curve

A

Relates dose and effect

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7
Q

EC50

A

Max possible drug effect

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8
Q

Potency

A

Quantity of drug to produce a specific effect

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9
Q

Factors affecting potency?

A

Absorption, Distribution, Metabolism, Excretion, Affinity

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10
Q

Effective dose (ED)

A

Dose required to produce a specific effect
(lower ED = higher potency)
Moves left on dose-response curve.
Affinity moves the curve to the left.

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11
Q

Median effective dose (ED50)

A

Dose required to produce an effect in 50% of patients.

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12
Q

ED90

A

Dose required to produce an effect in 90% of patients.

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13
Q

Median Lethal Dose (LD50)

A

Dose required to produce death in 50% of patients!!!

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14
Q

Slope of the concentration-effect curve is?

A

The range of doses that are useful for achieving a clinical effect.

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15
Q

A steeper slope on the concentration-effect curve means?

A

The more binding of receptors is required to achieve effect.

The steeper the slope means smaller increases will = greater intensity of effect.

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16
Q

Efficacy measures:

A

intrinsic ability of a drug to produce an effect.

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17
Q

How is efficacy depicted on a graph?

A

By the plateau of the dose-response curve.

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18
Q

Therapeutic Index indicates?

A

The difference between the desired effect and undesirable effects.

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19
Q

What is the therapeutic window?

A

Desired effect with minimal toxicity.

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20
Q

What pharmacodynamic effect would you expect from a high metabolizer CYP2D6 of codeine?

A

High pain response. More is metabolized. Patient is knocked out.

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21
Q

What happens when you give codeine to a low metabolizer of CYP2D6?

A

Patient doesn’t feel anything.

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22
Q

What is the active portion of the form that readily crosses the biologic membranes?

A

Nonionized

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23
Q

LIst 4 types of Pharmacokinetic variations:

A
  1. Absorption
  2. Distribution
  3. Metabolism
  4. Excretion
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24
Q

List 3 types of Pharmacodynamic variations:

A
  1. Genetics
  2. Patient physiology (Age)
  3. Drug interactions
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25
What factors influence the efficacy/toxicity of a drug? (List 5)
1. Decreased total body water 2. Decreased body mass 3. Decreased cardiac output 4. Decrease in plasma protein binding 5. Decreased renal function
26
What is stereochemistry?
The description of structures in 3 dimensions.
27
What is an Isomer?
Compounds with the same molecular formula.
28
What are stereoisomers?
?
29
What are enantiomers?
?
30
What must all enantiomers contain?
a Chiral carbon.
31
What does chiral mean?
A molecule that has a non-superposable mirror image.
32
How can enantiomers be different?
Absorption, distribution, clearance, potency, & toxicity.
33
What direction do d or + enantiomers rotate polarized light?
to the RIGHT
34
What direction do l or - enantiomers rotate polarized light?
to the LEFT.
35
S & R designation
?
36
D and L designation
?
37
What is a racemic mixture?
Two enantiomers present in equal proportions 50:50
38
What does stereospecific mean?
The ability of a drug to bind to a receptor.
39
Affinity and intrinsic activity depend on?
the drugs chemical structure
40
Examples of racemic mixtures: (list four)
1. Ketamine 2. Bupivacaine 3. Cisatracurium 4. Albuterol
41
What does hyperactive mean?
low doses of medication leads to higher than expected effect.
42
What does hypersensitive mean?
describes when a patient is allergic to a drug.
43
What does Hyporeactive mean?
high doses of medication are required to evoke a desired effect.
44
What is the definition of TOLERANCE?
Hyporeactivity that is acquired from chronic exposure to a drug.
45
What is the definition of Cross-tolerance
tolerance to a drug that develops through continued use of another drug with similar pharmacologic effects.
46
What is the definition of Tachyphylaxis?
tolerance that develops rapidly only after a few doses.
47
What is cellular tolerance?
Neuronal adaption (i.e. opiods, barbiturates, and alcohol tolerance)
48
What happens in cellular tolerance?
1. decrease in receptors 2. Enzyme induction 3. Decreased neurotransmitter release
49
What is the definition of Immunity?
Hyporeactivity induced by the presence of antibodies
50
What is the definition of Idiosyncrasy?
An unusual effect occurring in an individual, regardless of intensity or dosage.
51
What is an Additive effect?
A second drug acting with the first drug will produce an effect equal to an algebraic summation (1+1=2).
52
What is a Synergistic effect?
Two drugs interacting to produce a much greater effect (1+1=4)
53
What is an Antagonistic effect?
Two drugs interacting to cause a lesser effect (i.e. opioid agonist + opioid antagonist = lesser effect.)
54
What is a Receptor?
Any cellular protein macromolecule to which a drug binds to bring about a response.
55
What is an Agonist?
An activator which mimics the expected receptor response.
56
What is a Full Agonist?
An agonist that has a high efficacy. (Max response is possible!)
57
What is a Partial Agonist?
a drug that has an affinity for a receptor but has low efficacy. Insufficient stimulus to generate a maximal response.
58
What is an Antagonist?
a drug that binds to a receptor without activating the receptor!!! (i.e. Naloxone, Atropine, Metoprolol, Propranolol, Esmolol, Flumazenil)
59
What is a Competitive Antagonist?
Binds to a receptor at the same site without activating it. (Competes)
60
What direction does the dose-effect curve shift when a competitive antagonist is present?
It shifts to the RIGHT
61
What is a "competitive"/"surmountable" agonist?
An inhibition that can be overcome by increasing the concentration of the agonist.
62
What is a Competitive reversible antagonist?
an antagonist that binds reversibly to the receptor . Must be great in number than the agonist. (i.e. non-depolarizing neuromuscular blocking agents.)
63
What is a Noncompetitive irreversible antagonist?
an antagonist that binds permanently via a covalent bond to the active site on the receptor.
64
What is a Noncompetitive pseudo-irreversible antagonist?
an antagonists that binds to the receptor and the binding is so tight that it dissociates so slowly from the receptor that it is essentially irreversible in action.
65
Can you overcome Noncompetitive antagonists?
NO!
66
What direction is the dose-effect curve shifted with noncompetitive antagonists?
Downward
67
What is an Allosteric Non-competitive Antagonist?
Binds to a distinctly separate binding site.
68
What is Allosteric Potentiation?
enhances the affinity of the normal agonist at its binding site.
69
What does Allosteric mean?
?
70
What are the 2 major functions of receptors?
1. Ligand Binding | 2. Signal Transduction
71
What are the 2 function domains of receptors?
1. Ligand-Binding domain | 2. Effector domain
72
Where are receptors located? (2)
1. on the lipid membrane of the cell surface | 2. in the cytosol or nucleus
73
What is up-regulation?
increase in the number of receptor due to a lack of use.
74
What is down-regulation?
decrease in the number of receptors due to excessive stimulation from an agonist or overuse of the receptor.
75
Why should you not stop Beta Blocker abruptly?
?
76
How are receptors named?
by the name of the ligand that binds to it (i.e. GABA receptors)
77
What is the relationship between receptor density and receptor function
density dictates function.
78
What are the 6 receptor superfamilies?
1. ion channel receptors 2. G protein couples receptors (GPCRs) 3. Ligand regulated transmembrane enzymes 4. Nuclear regulated transmembrane non-enzymes 5. Nuclear hormone receptors 6. Intracellular enzymes
79
What is the normal resting membrane potential for when channels remain closed?
-60 to -80 mV
80
What is a Ligand Gated Ion Channel?
activated by the binding of a ligand (drug or neurotransmitter) binding to a specific site causing the channel to open and alter the cell membrane potentials.
81
What is a Cation?
A positive charged ion (excitatory)
82
What is an Anion?
?
83
What type of Ligand-Gated Ion Channel do barbituates target
GABAa agonists
84
What is the major excitatory neurotransmitter in the CNS?
Glutamate
85
What two categories of can Glutamate react on?
LGIC & G protein
86
3 types of glutamate ionotropic receptor channels?
1. AMPA 2. NMDA 3. Kainate receptor
87
What is the major inhibitory neurotransmitter in the brain?
GABA
88
Can GABA cross the blood-brain barrier?
NO
89
How do Benzo's, barbiturates, propofol, etomidate effect GABAz receptors?
They enhance GABA inhibition in the CNS.
90
What superfamily of receptors is extremely complex?
G protein - Coupled receptors (reactions take place WITHIN the cell)
91
What type of receptors bind to all alpha and beta adrenergic drugs?
G Proteins
92
What type of seratonin type receptors don't couple with G protein receptors?
serotonin subtype 3
93
Secondary messengers are linked by what receptors
G proteins
94
What does tissue-specific mean?
a second messenger can produce different effects in different tissues
95
Start 3/10/15 | Name 3 ways a drug response is terminated?
1. Metabolism 2. Excretion 3. Redistribution (TEST Q)
96
What is redistribution?
a highly lipid-soluble drug that acts on the brain or CV system is arm. rapidly by IV injection OR by inhalation.
97
What is the main reason a drug response is terminated?
The CNS effects after bolus injection of an IV anesthetic are terminated primarily by redistribution! (Test Q.)

Wolford NUAN 5232 - Pharm: Pharmacodynamics (1 decks)

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