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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
Q

What factors influence the efficacy/toxicity of a drug? (List 5)

A
  1. Decreased total body water
  2. Decreased body mass
  3. Decreased cardiac output
  4. Decrease in plasma protein binding
  5. Decreased renal function
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26
Q

What is stereochemistry?

A

The description of structures in 3 dimensions.

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27
Q

What is an Isomer?

A

Compounds with the same molecular formula.

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28
Q

What are stereoisomers?

A

?

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29
Q

What are enantiomers?

A

?

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30
Q

What must all enantiomers contain?

A

a Chiral carbon.

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31
Q

What does chiral mean?

A

A molecule that has a non-superposable mirror image.

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32
Q

How can enantiomers be different?

A

Absorption, distribution, clearance, potency, & toxicity.

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33
Q

What direction do d or + enantiomers rotate polarized light?

A

to the RIGHT

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34
Q

What direction do l or - enantiomers rotate polarized light?

A

to the LEFT.

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35
Q

S & R designation

A

?

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36
Q

D and L designation

A

?

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37
Q

What is a racemic mixture?

A

Two enantiomers present in equal proportions 50:50

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38
Q

What does stereospecific mean?

A

The ability of a drug to bind to a receptor.

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39
Q

Affinity and intrinsic activity depend on?

A

the drugs chemical structure

40
Q

Examples of racemic mixtures: (list four)

A
  1. Ketamine
  2. Bupivacaine
  3. Cisatracurium
  4. Albuterol
41
Q

What does hyperactive mean?

A

low doses of medication leads to higher than expected effect.

42
Q

What does hypersensitive mean?

A

describes when a patient is allergic to a drug.

43
Q

What does Hyporeactive mean?

A

high doses of medication are required to evoke a desired effect.

44
Q

What is the definition of TOLERANCE?

A

Hyporeactivity that is acquired from chronic exposure to a drug.

45
Q

What is the definition of Cross-tolerance

A

tolerance to a drug that develops through continued use of another drug with similar pharmacologic effects.

46
Q

What is the definition of Tachyphylaxis?

A

tolerance that develops rapidly only after a few doses.

47
Q

What is cellular tolerance?

A

Neuronal adaption (i.e. opiods, barbiturates, and alcohol tolerance)

48
Q

What happens in cellular tolerance?

A
  1. decrease in receptors
  2. Enzyme induction
  3. Decreased neurotransmitter release
49
Q

What is the definition of Immunity?

A

Hyporeactivity induced by the presence of antibodies

50
Q

What is the definition of Idiosyncrasy?

A

An unusual effect occurring in an individual, regardless of intensity or dosage.

51
Q

What is an Additive effect?

A

A second drug acting with the first drug will produce an effect equal to an algebraic summation (1+1=2).

52
Q

What is a Synergistic effect?

A

Two drugs interacting to produce a much greater effect (1+1=4)

53
Q

What is an Antagonistic effect?

A

Two drugs interacting to cause a lesser effect (i.e. opioid agonist + opioid antagonist = lesser effect.)

54
Q

What is a Receptor?

A

Any cellular protein macromolecule to which a drug binds to bring about a response.

55
Q

What is an Agonist?

A

An activator which mimics the expected receptor response.

56
Q

What is a Full Agonist?

A

An agonist that has a high efficacy. (Max response is possible!)

57
Q

What is a Partial Agonist?

A

a drug that has an affinity for a receptor but has low efficacy. Insufficient stimulus to generate a maximal response.

58
Q

What is an Antagonist?

A

a drug that binds to a receptor without activating the receptor!!! (i.e. Naloxone, Atropine, Metoprolol, Propranolol, Esmolol, Flumazenil)

59
Q

What is a Competitive Antagonist?

A

Binds to a receptor at the same site without activating it. (Competes)

60
Q

What direction does the dose-effect curve shift when a competitive antagonist is present?

A

It shifts to the RIGHT

61
Q

What is a “competitive”/”surmountable” agonist?

A

An inhibition that can be overcome by increasing the concentration of the agonist.

62
Q

What is a Competitive reversible antagonist?

A

an antagonist that binds reversibly to the receptor . Must be great in number than the agonist. (i.e. non-depolarizing neuromuscular blocking agents.)

63
Q

What is a Noncompetitive irreversible antagonist?

A

an antagonist that binds permanently via a covalent bond to the active site on the receptor.

64
Q

What is a Noncompetitive pseudo-irreversible antagonist?

A

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
Q

Can you overcome Noncompetitive antagonists?

A

NO!

66
Q

What direction is the dose-effect curve shifted with noncompetitive antagonists?

A

Downward

67
Q

What is an Allosteric Non-competitive Antagonist?

A

Binds to a distinctly separate binding site.

68
Q

What is Allosteric Potentiation?

A

enhances the affinity of the normal agonist at its binding site.

69
Q

What does Allosteric mean?

A

?

70
Q

What are the 2 major functions of receptors?

A
  1. Ligand Binding

2. Signal Transduction

71
Q

What are the 2 function domains of receptors?

A
  1. Ligand-Binding domain

2. Effector domain

72
Q

Where are receptors located? (2)

A
  1. on the lipid membrane of the cell surface

2. in the cytosol or nucleus

73
Q

What is up-regulation?

A

increase in the number of receptor due to a lack of use.

74
Q

What is down-regulation?

A

decrease in the number of receptors due to excessive stimulation from an agonist or overuse of the receptor.

75
Q

Why should you not stop Beta Blocker abruptly?

A

?

76
Q

How are receptors named?

A

by the name of the ligand that binds to it (i.e. GABA receptors)

77
Q

What is the relationship between receptor density and receptor function

A

density dictates function.

78
Q

What are the 6 receptor superfamilies?

A
  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
Q

What is the normal resting membrane potential for when channels remain closed?

A

-60 to -80 mV

80
Q

What is a Ligand Gated Ion Channel?

A

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
Q

What is a Cation?

A

A positive charged ion (excitatory)

82
Q

What is an Anion?

A

?

83
Q

What type of Ligand-Gated Ion Channel do barbituates target

A

GABAa agonists

84
Q

What is the major excitatory neurotransmitter in the CNS?

A

Glutamate

85
Q

What two categories of can Glutamate react on?

A

LGIC & G protein

86
Q

3 types of glutamate ionotropic receptor channels?

A
  1. AMPA
  2. NMDA
  3. Kainate receptor
87
Q

What is the major inhibitory neurotransmitter in the brain?

A

GABA

88
Q

Can GABA cross the blood-brain barrier?

A

NO

89
Q

How do Benzo’s, barbiturates, propofol, etomidate effect GABAz receptors?

A

They enhance GABA inhibition in the CNS.

90
Q

What superfamily of receptors is extremely complex?

A

G protein - Coupled receptors (reactions take place WITHIN the cell)

91
Q

What type of receptors bind to all alpha and beta adrenergic drugs?

A

G Proteins

92
Q

What type of seratonin type receptors don’t couple with G protein receptors?

A

serotonin subtype 3

93
Q

Secondary messengers are linked by what receptors

A

G proteins

94
Q

What does tissue-specific mean?

A

a second messenger can produce different effects in different tissues

95
Q

Start 3/10/15

Name 3 ways a drug response is terminated?

A
  1. Metabolism
  2. Excretion
  3. Redistribution (TEST Q)
96
Q

What is redistribution?

A

a highly lipid-soluble drug that acts on the brain or CV system is arm. rapidly by IV injection OR by inhalation.

97
Q

What is the main reason a drug response is terminated?

A

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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