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824 > exam 3 > Flashcards

exam 3 Flashcards

1
Q

ADME stands for

A

Absorption, Distribution, Metabolism, Excretion

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2
Q

Characteristics determined by concentration vs time profile

A

Onset, duration, intensity

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3
Q

Time between administration and pharmacological effect

A

Onset

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4
Q

How high the concentration is

A

Intensity

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5
Q

Length of time above MEC

A

duration

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6
Q

Minimum effective concentration

A

MEC

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7
Q

The study of the absorption, distribution, biotransformation, and elimination of xenobiotics

A

Pharmacokinetics

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8
Q

The study of the molecular, biochemical, and physiological effects of xenobiotics and their mechanisms of actions

A

Pharmacodynamics

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9
Q

Patho, pharmacodynamics, pharmacokinetics make up

A

pharmacotherapeutics

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10
Q

Most rapid onset route

A

Intravenous

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11
Q

Slowest onset route

A

Oral

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12
Q

Routes of administration

A

Ingestion, Inhalation, Dermal, Parenteral

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13
Q

IV, SC, IM, Intraperitoneal equal what route

A

Parenteral

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14
Q

Reduction of absorption impacts

A

intensity and duration

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15
Q

Reduction of speed of entry impacts

A

Onset

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16
Q

AI phenobarbital to hydroxyphenobarbital

A

Hydroxylation

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17
Q

AA procainamide to N-acetylprocainamide

A

acetylation

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18
Q

IA codeine to morphine

A

demethylation

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19
Q

AR

A

acetaminophen to reactive metabolite

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20
Q

Major routes of excretion

A

Renal (kidney) is primary
Biliary (feces)

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21
Q

Other routes of excretion

A

Pulmonary, salivary, mammary

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22
Q

Which antibiotic is a better choice in a patient with renal failure?

A

The one eliminated in bile not urine

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23
Q

Barriers that may reduce amount of drug that reaches site of action

A

gut wall metabolism, degraded in stomach, dose distributing away from target tissue, can’t enter membranes, enzymes

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24
Q

The fate of a drug once it enters the systemic circulation

A

Disposition

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25
Q

A chemical that is normally foreign to the body includes drugs, occupational chemicals, environmental compounds

A

Xenobiotic

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26
Q

___ percent of problems used to be from ADME, now its ___ percent

A

40%, 10%

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27
Q

___ barriers like the BBB can significantly reduce the amount of drug that enters the site of action

A

Tissue

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28
Q

Morphine is a metabolite of codeine and this metabolite is responsible for the analgesic effect when codeine is administered. In a patient who has a genetic defect such that they cannot metabolize codeine, the magnitude of pain relief would be expected to be _____ compared to normal patients.

A

Decreased

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29
Q

Factors that determine movement of a drug across membranes

A

Characteristics of membrane, mechanism of passage, swell time, physiochemical characteristics, pH of microenvironment, surface area

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30
Q

Why does most oral drug absorption occur in the small intestine?

A

Inner wall of small intestine covered by folds of kerckring plicae circulares, surface contain tiny villi and microvilli that increase surface area

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31
Q

food transit time in mouth

A

1 min

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32
Q

food transit time in esophagus

A

4- seconds

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33
Q

food transit time in stomach

A

2-4 hours

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34
Q

food transit time in small intestine

A

3-5 hours

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35
Q

food transit time in colon

A

10 hours to days

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36
Q

Carrier mediated transport examples

A

Facilitated diffusion and active transport

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37
Q

95% of drugs are absorbed by

A

passive transcellular diffusion

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38
Q

Transcellular permeability can be increased by

A

removing charged ionized groups, increasing lipophilicity, reducing size

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39
Q

The passive movement of drug through lipid membranes driven by concentration gradient

A

Transcellular diffusion

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40
Q

The passive movement of drug between cells via tight junctions driven by concentration gradient

A

Paracellular diffusion

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41
Q

A carrier mediated process that involves a transport protein which moves drug with a concentration gradient

A

facilitated diffusion

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42
Q

A carrier mediated process that involves a transport protein which moves drug against a concentration gradient

A

active transport

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43
Q

A process in which a cell engulfs and internalizes a particle

A

Endocytosis

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44
Q

Primary site of absorption after oral administration because of high surface area

A

small intestine

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45
Q

altered by food or drugs, influences extent and rate of drug absorption

A

gastrointestinal transit time

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46
Q

carrier mediated is different than passive because its

A

saturable and subject to drug drug interactions

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47
Q

Selectively move substrates across cell membranes

A

transporter proteins

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48
Q

remove drugs from cells that have entered via passive diffusion, can reduce the amount of drug that accumulates in certain tissue such as the brain

A

Efflux transporters

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49
Q

Slowing gastric emptying would be expected to have which effect on the absorption of a drug absorbed by passive diffusion?

A

it will take longer to reach peak concentration

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50
Q

Which moves mechanisms down a concentration gradient?

A

Paracellular, transcellular, facilitated diffusion

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51
Q

Co-administration of an inhibitor of the efflux protein p-glycoprotein would have what effect on the oral absorption of a drug that is a substrate for pgp?

A

The inhibitor will increase the amount of drug absorbed

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52
Q

which of the following would not increase transcellular permeability? remove ionized groups, decrease lipophilicity, reduce molecular size

A

decreasing lipophilicity

53
Q

under passive diffusion rate of transport increases as concentration _____

A

increases

54
Q

move solutes out of the cell

A

efflux transporters

55
Q

Consequences of efflux transporter p glycoprotein

A

Limited drug absorption, enhanced drug elimination, limited distribution

56
Q

For large molecules, depend on particle size, frequently used for nanoparticle drug delivery

A

endocytosis

57
Q

The movement of drug molecules across biological membranes into various tissues in the body

A

Distribution

58
Q

The movement of drug molecules across vascular endothelial cells and into interstitial space

A

Transvascular transport

59
Q

A transvascular transport process driven by pressure

A

Convection

60
Q

A transvascular transport process driven by a concentration gradient

A

Diffusion

61
Q

The concentration of a drug within a tissue due to pH differences that lead to ionization of the drug in the tissue environment

A

drug trapping

62
Q

The initial movement of drug from highly perfused tissues to poorly perfused tissues

A

Redistribution

63
Q

slower distribution, driven by pressure, convection

A

perfusion

64
Q

driven by concentration gradient, diffusion

A

permeability rate limited

65
Q

binding of drug to plasma protein

A

restricts distribution

66
Q

most drug in tissue is bound to

A

nonspecific sites and not receptors

67
Q

only ___ is phamacologically active

A

free drug

68
Q

different ph environments causes

A

drug trapping

69
Q

BBB properties

A

tight junctions, negative head groups, high pgp concentration

70
Q

how drugs enter cns

A

existing transporter, directly to CNS, disruption of BBB, appropriate physiochemical properties

71
Q

efflux activity can be so extensive drug in brain doesnt reach

A

measurable concentrations

72
Q

___ molecules dont cross membrane to fetus

A

large polar

73
Q

driving force for convection

A

pressure

74
Q

driving force for diffusion drug movement

A

concentration gradient

75
Q

A drug that is only distributed into vascular space will exhibit a monoexponential blood concentration vs time curve after intravenous administration t of f

A

true

76
Q

Which drug is most likley to undergo transvascular transport via convection

A

the biggest dalton one

77
Q

A decrease in plasma protein binding will result in an

A

increase in amount of drug in tissue (only free drug crosses)

78
Q

A change in the structure of a drug molecule such that is is no longer transported by pgp will have what effect on CNS concentration?

A

higher cns concentration (pgp only transports out bc its efflux)

79
Q

Kidney route excretion process

A

GABEPVDC

80
Q

Mechanisms of renal excretion

A

Filtration, active tubular secretion, tubular reabsorption, biotransformation

81
Q

Determinants of filtration

A

MW <5000, number of nephrons, protein binding, renal blood flow

82
Q

Filtration happens in

A

glomerulus of bowmans capsule

83
Q

test for renal disease

A

if protein in urine then its a sign of disease

84
Q

Active tubular secretion location

A

Proximal convoluted tubule

85
Q

active tubular secretion graph

A

linear then hits a max

86
Q

drugs that under go ATS an exhibit

A

Stereoselective renal secretion

87
Q

clearance vs mw relationship

A

indirect

88
Q

dose and urinary excretion relationship

A

indirect

89
Q

The active transport of drug from blood to renal tubule in proximal tubule

A

active tubular secretion

90
Q

Movement of solute from inside renal tubule back into the blood

A

tubular reabsorption

91
Q

reabsorption of drug from small intestine after drug has been excreted through bile into intestine

A

enterohepatic recirculation

92
Q

food stimulates release of bile with drug in it

A

dose dumping

93
Q

Primary routes of drug excretion

A

renal and hepatic

94
Q

secondary routes of drug excretion

A

pulmonary, salivary, mammary

95
Q

Most important mechanisms of renal excretion

A

filtration, active tubular secretion, tubular reabsorption sometime biotransformation

96
Q

glomerular filtration is largely influenced by

A

molecular size and plasma protein binding

97
Q

Drugs which undergo active tubular secretion exhibit

A

saturation at high concentration and subject to competition

98
Q

tubular reabsorption is passive and driven by

A

concentration gradient and ph sensitive

99
Q

carrier mediated tubuar reabsorption

A

process is saturable

100
Q

hepatic elimination involves

A

metabolism and biliary excretion

101
Q

when a part of a dose is eliminated before entering circulation

A

first pass effect

102
Q

pgp and mdr1

A

actively secrete drug from hepatocyte into bile

103
Q

primary factors determining biliary secretion are

A

molecular weight and polarity

104
Q

Which is most likely subject to competitive drug drug interactions

A

tubular secretion

105
Q

As mw increases in renal elimination, filtration

A

decreases

106
Q

plot mw and drug excreted in bile

A

direct relationship

107
Q

Effect of enterohepatic recirculation on half life of a drug

A

increases half life

108
Q

decrease in plasma protein binding in glomerular filtration results in

A

increase of renal elimination

109
Q

which vitamin undergoes bioactivation in the kidney

A

vitamin d

110
Q

phase 1 metabolism

A

biotransformation of xenobiotics that includes oxidation, hydroxylation, to introduce or expose a functional group

111
Q

phase 2 metabolism

A

involves conjugation with a polar group yielding a polar metabolite that can be excreted in bile or urine influenced by availability of co substrate

112
Q

Most important organ where biotransformation takes place

A

liver

113
Q

frequently but not always subsequent to phase 1

A

phase 2

114
Q

two components in cytochrome p450 system

A

cyp450 reductase and cyp450

115
Q

indentification of cyp450 important for predicting

A

drug drug interactions

116
Q

cyp450 generates

A

reactive oxygen species with detrimental cellular effects

117
Q

critical determinant in ability to bind to cyp450 and binding affinity

A

geometric shape/conformation

118
Q

potent inhibitors of cyp450 that serve as sixth axial ligand for iron in heme

A

nitrogenous compounds

119
Q

covalent binding renders cyp450 inoperable and new cyp450 must be synthesized to restore metabolism

A

mechanism based inhibitors, suicide inhibition

120
Q

induction of metabolism results from

A

activating transcription factors

121
Q

when drugs induce the same cyp450

A

autoinduction

122
Q

inducers of drug metabolizing enzymes exhibit

A

cross talk

123
Q

increases polarity and size of drug molecules and reduces pharmacologic effect

A

phase 2 metabolism

124
Q

variablity in diet, other drugs, disease, environment can be more important than

A

genetic variability

125
Q

which pathway increases mw

A

phase 2

126
Q

which pathway results in metabolite eliminated in bile

A

phase 2

127
Q

Which inhibits cyp4a4

A

ritonavir

128
Q

what type of cyp450 inhibitor produces the longest lasting inhibition

A

mechanism based inhibition

129
Q

inducers of cyp450 are selective for one enzyme or enzyme family t o f

A

false

824 (12 decks)

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