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Oc P > 01 Principles > Flashcards

01 Principles Flashcards

1
Q

Affinity definition

A

potential for drug-receptor binding

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2
Q

Receptor definition

A

cellular binding site with a biological effect

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3
Q

Intrinsic activity definition

A

capacity to produce a beneficial biological effect

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4
Q

Agonist definition

A

substances that STIMULATE a receptor to produce a physiologic reaction (has intrinsic activity)

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5
Q

Antagonist definition

A

substances that INTERFERE with activity of a receptor and its endogenous substrate; does not produce a physiologic reaction itself (does not have intrinsic activity)

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6
Q

Allostery definition

A

bound ligand changes configuration of the molecule to influence specificity at a second site

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7
Q

Efficacy definition

A

[affinity] x [intrinsic activity]

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8
Q

Efficacy v. Potency

A

efficacy is dose independent; potency is dose dependent

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9
Q

What is the efficacy of an antagonist?

A

zero (because there is no intrinsic activity)

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10
Q

EC50 definition

A

effective concentration in 50% of subjects

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11
Q

ED50 definition

A

effective dose in 50% of subjects

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12
Q

IC50 definition

A

inhibitory concentration in 50% of subjects (antagonists)

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13
Q

Hypersensitivity definition

A

result of chronic antagonism

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14
Q

Maximum Dose definition

A

the MINIMUM amount of drug to produce the MAX therapeutic effect

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15
Q

Partial Agonist definition

A

LOW intrinsic activity with a therapeutic potency and affinity

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16
Q

Pharmacodynamics definition

A

how the drugs affect the body (MOA)

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17
Q

Pharmacokinetics definition

A

how the body affects the drug (ADME)

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18
Q

ADME definition

A

absorption, distribution, metabolism, elimination

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19
Q

Pharmacotherapeutics definition

A

how the drug affects disease processes

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20
Q

Concentration v. Dose

A

concentration is laboratory; dose is clinical

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21
Q

How is Pharmacodynamics measured?

A

potency, efficacy, affinity, toxicity

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22
Q

How is Potency related to EC50 and IC50?

A

potency is INVERSELY related to EC50 for agonists and IC50 for antagonists

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23
Q

Posology definition

A

science of drug dosing

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24
Q

Potency definition

A

biological response to a given dose

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25
Q

Resistance definition

A

loss of pharmacological effect

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26
Q

Selectivity definition

A

the ability to produce a desired effect versus an adverse effeict

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27
Q

Specificity definition

A

ability to act at a specific receptor

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28
Q

Tachyphylaxis definition

A

rapidly decreasing therapeutic response (can only be used short term)

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29
Q

Teratogenesis definition

A

congenital malformation

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30
Q

Bioavailability definition

A

amount of active drug to reach target tissue

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31
Q

Therapeutic Index definitioin

A

TD50:ED50 ratio (clinical) or LD50:ED50 ratio (laboratory)

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32
Q

LD50 definition

A

lethal dose for 50% treated (used in animal studies)

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33
Q

TD50 definition

A

toxic dose for 50% treated

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34
Q

What therapeutic index is safe?

A

high therapeutic indices are safest because it takes much more drug to create adverse effect than it does to treat

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35
Q

What therapeutic index is likely to produce a toxic effect?

A

low therapeutic indices are more likely to create toxic effect because the dose it takes to treat is nearly the dose that causes adverse toxicity

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36
Q

DPA definiton

A

diagnostic pharmaceutical agent

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37
Q

TPA definition

A

therapeutic pharmaceutical agent

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38
Q

What are six drug types?

A

supplemental, supportive, prophylactic, symptomatic, diagnostic, therapuetic

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39
Q

Supplemental drug definition

A

addition of a substance that is normally required but is insufficient in the patient

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40
Q

What is an example of a supplemental drug?

A

insulin

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41
Q

Supportive drug definition

A

aimed at resolving clinical signs

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42
Q

What is an example of a supportive drug?

A

glucose

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43
Q

Prophylactic drug definition

A

preventative/protection against potential issues

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44
Q

What is an example of a prophylactic drug?

A

low dose aspirin

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45
Q

Symptomatic drug definition

A

offers relief for patient symptoms, but does not cure

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46
Q

What is an example of a symptomatic drug?

A

olopatadine, artificial tears

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47
Q

Diagnostic drug definition

A

drug used only by doctor for diagnostic purposes

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48
Q

What is an example of a diagnostic drug?

A

fluorescein

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49
Q

Therapeutic drug definition

A

works to eliminate the cause of whatever problem the patient is having

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50
Q

What is an example of a therapeutic drug?

A

methotrexate

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51
Q

What are the receptor motif super families? (5)

A

nuclear, g-protein-coupled, ion channels, enzymatic, calcium release

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52
Q

What are characteristics of a Nuclear receptor?

A

LIPID SOLUBLE, with cholesterol backbones, ready to gain access into the cell nucleus

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53
Q

What are examples of Nuclear receptors?

A

steroids, hormones

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54
Q

What is the most common receptor type targeted by ophthalmic drugs?

A

g-protein-coupled

55
Q

How do G-protein-coupled receptors work?

A

receptors inside the cell interact with proteins to cause conformational change that leads to opening of channels

56
Q

What are examples of G-protein-coupled receptors?

A

ACh(M), rhodopsin

57
Q

What are characteristics of Ion Channel receptors?

A

they are a tube in the cell membrane that is opened up by binding

58
Q

What are examples of Ion Channel receptors?

A

ACh(N), glutamate, GABA

59
Q

How do Enzymatic receptors work?

A

drug binds to the receptor which activates its enzymatic activity (usually in the cell membrane)

60
Q

What are examples of Enzymatic receptors?

A

insulin, epidermal growth factor

61
Q

How do Calcium Release receptors work?

A

stimulation of the receptor results in release of Ca++

62
Q

What effect occurs with the release of Ca++?

A

in small can fuel production of nitric oxide (vasodilator), or in large amounts can cause apoptosis

63
Q

What type of receptor is ACh(M)?

A

g-protein-coupled

64
Q

What type of receptor is ACh(N)?

A

ion channel

65
Q

Explain how drugs are designed according to the lock and key model.

A

when they leak out of the blood vessels, they designed to only bind to specific endogenous receptors, producing a cascade of events to evoke the desired effect

66
Q

How does inflammation affect the lock and key model?

A

inflammation causes blood vessels to become dilated and “leaky” so that the drug will accumulate in the inflamed area, thus the drug will produce effect in that particular affected area rather than diffusing throughout the whole body

67
Q

What are the modes of action of Agonists? (5)

A

direct, indirect, mixed, inverse, partial

68
Q

How do direct agonists work?

A

direct agonists stimulate a receptor and produce the desired effect through its actions on the receptor

69
Q

How do indirect agonists work?

A

indirect agonists are intermediaries that interact with a receptor to promote a natural effect in the body

70
Q

Cocaine is an example of what type of agonist?

A

indirect agonist (it binds to neurons to inhibit reuptake of catecholamines, but it is the norepinephrine that stimulates the true effect)

71
Q

How do mixed agonists work?

A

they use both agonist and antagonist properties

72
Q

How do inverse agonists work?

A

they STIMULATE a receptor which actually decreases activity

73
Q

How do partial agonists work?

A

they have sub-maximal stimulation of receptors and efficacy

74
Q

Which type of agonists are touted for reduced dependency and withdrawal effects?

A

partial agonists

75
Q

What are the three characteristics of antagonists?

A

binding integrity, binding site selectivity, mode of action

76
Q

What are the types of antagonist binding integrity?

A

reversible, or irreversible

77
Q

Which type of antagonist binding uses covalent bonds?

A

irreversible antagonists

78
Q

What are the types of binding site selectivity? (3)

A

competitive, non-competitive, uncompetitive

79
Q

Competitive Antagonist definition

A

binding site is the same as the endogenous agonist

80
Q

Non-Competitive Antagonist definition

A

binds at another site to produce allostery so that the endogenous agonist cannot bind

81
Q

Uncompetitive Antagonist definition

A

binds at another site to produce allostery so that the endogenous agonist is still bound and locked in so that it cannot dissociate and be restimulated

82
Q

What are the modes of action for antagonists? (3)

A

biological, chemical, physiological

83
Q

Which type of antagonist binding requires presence of an agonist?

A

uncompetitive

84
Q

What factors influence absorption of a drug?

A

first pass metabolism, barriers (degree of vascularity at administration site), patient (age, gender, weight, pregnancy, health)

85
Q

What is first pass metabolism?

A

the drug is ingested and absorbed through the gut into the blood, travelling directly into the liver so it is there metabolized rather than having a therapeutic effect

86
Q

What influences the distribution of a drug?

A

route of administration

87
Q

How do you calculate the Volume of Distribution (Vd)?

A

Vd = dose/[drug in plasma]

88
Q

What influences the metabolism of a drug?

A

health of metabolizing organ(s)

89
Q

How is drug metabolism measured?

A

drug half life

90
Q

What routes of drug elimination exist?

A

fecal, urinary, sweat, respiration, saliva

91
Q

How is Drug Clearance calculated?

A

Clearance = [drug volume eliminated] / time

92
Q

How will a “red eye” affect volume of distribution?

A

Vd is increased due to the increased vascularity of the tissue causing the drug to more easily get into systemic circulation

93
Q

How does patient age affect dosing?

A

age usually requires a higher dose

94
Q

How does fat affect drug absorption?

A

when overweight patients take lipid-based drugs, the drug can accumulate in the body fat without producing an effect

95
Q

What does a high volume of distribution suggest?

A

the drug does not readily stay in the bloodstream, which may predispose patients to toxicity (often in patients with liver or renal disease)

96
Q

How does dehydration affect volume of distribution?

A

it decreased vD since the low plasma volume artificially enhances drug plasma concentration

97
Q

Which layer of the tears is both water and lipid soluble?

A

mucin layer

98
Q

What are the layers of the tear film? (anterior to posterior)

A

lipid, aqueous, mucin

99
Q

What type of drugs will dissolve on the first layer of tear film?

A

lipid-soluble drugs

100
Q

Which layer will dissociate charged drugs into solution?

A

aqueous

101
Q

In an inflammatory state, what happens to the tear film?

A

aqueous becomes more acidic, which prevents dissociation and action of the drug

102
Q

What can prevent dissociation of a charged drug?

A

lower pH of aqueous

103
Q

What are the two strongest barriers to drug passage in the eye?

A

corneal epithelium and RPE

104
Q

What structure in the eye lacks tight junctions, making it a poor barrier to drug passage?

A

corneal endothelium

105
Q

What prevents systemic drugs from causing toxicity in the eye?

A

while drugs can come through the choroid, they cannot cross the RPE

106
Q

What is the primary site of drug elimination in the eye?

A

ciliary body

107
Q

What is the surface volume of tear film?

A

10-30 microliters

108
Q

What is the volume of a drop?

A

25-56 microliters

109
Q

What is the rate of basal tear flow?

A

0.5-2.2 microliters/minute

110
Q

How long does it take to completely replace tear film?

A

5-20 minutes

111
Q

How do conjunctiva and sclera facilitate drug passage?

A
112
Q

How does iris pigment affect ocular drug absorption?

A

pigment is lipophilic and becomes a depot for the drug; darker eyes require more drops and have great sustained effect

113
Q

What is normal tear pH?

A

7.1-7.6 (slightly basic)

114
Q

Which type of drugs accumulate in aqueous media?

A

charged drugs

115
Q

Which types of drugs readily leave aqueous environments to cross lipid barriers?

A

uncharged drugs

116
Q

What is the volume of the anterior chamber?

A

200 microliters

117
Q

How long does it take for aqueous to be recycled in the anterior chamber?

A

50 minutes

118
Q

What is the most metabolically active part of the crystalline lens?

A

anterior epithelium

119
Q

How do steroids affect drug clearance?

A

decrease blood aqueous barrier permeability, reducing drug clearance

120
Q

Which model of drug kinetics lconcentration dependent?

A

1st order

121
Q

Which model of drug kinetics is concentration independent?

A

zero order

122
Q

Which model of drug kinetics do most drugs follow?

A

1st order

123
Q

Which model of drug kinetics has a linear rate of elimination?

A

zero order

124
Q

Which model of drug kinetics has an exponential rate of elimination?

A

1st order

125
Q

Which model of drug kinetics has a rate limiting barrier or saturable carrier?

A

zero order

126
Q

Which model of drug kinetics has a constant amount of clearance?

A

zero order

127
Q

Which model of drug kinetics has a constant proportion of clearance?

A

1st order

128
Q

Which model of drug kinetics has a non-saturable carrier?

A

1st order

129
Q

Which model of drug kinetics has a saturable carrier at high concentrations only?

A

mixed order

130
Q

Alcohol and ASA follow which model of drug kinetics?

A

zero order

131
Q

Steady State definition

A

drug in = drug out

132
Q

Which model of drug kinetics requires a greater demand for dose modification?

A

zero order

133
Q

How can plasma equilibrium be elevated?

A

increasing the dose, or increasing dosing frequency

Oc P (3 decks)

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