Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmacology I > ADME > Flashcards

ADME Flashcards

1
Q

what does ADME stand for

A

-Absorption
- Distribution
- Metabolism
- Excretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what does ADME describe

A

the key kinetic principles

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

what is absorption

A

how a drug moves from its site of administration into the bloodstream

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

what is distribution

A

movement of the drug between blood and tissues

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

what is metabolism

A

conversion of drugs into more hydrophilic metabolites

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what is excretion

A

removal of drugs and/or metabolites from the body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

where are the majority of drugs absorbed

A

in the small intestine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

what conditions can slow the absorption of drugs

A
  • gastroparesis in DM
  • colectomies
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

what features predict drug movement

A
  • molecular size
  • degree of ionization
  • lipid solubility
  • protein binding
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

to pass through lipid membranes drugs must be:

A

non ionized

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

to be water soluble, drugs need to be:

A

ionized

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

what happens when a strong acid interacts with water

A

a complete irreversible reaction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

what happens when a weak acid interacts with water

A

a reversible reaction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

most drugs are either:

A

weak acids or weak bases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

what happens to an acidic drug in an acidic pH

A

it is non-ionized and protonated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

what happens to a acidic drug in a basic pH

A

ionized, deprotonated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

what happens to a basic drug in acidic pH

A

ionized, protonated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

what happens to a basic drug in a basic pH

A

non-ionized, deprotonated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

acids are _____ when protonated

A

non -ionized and fat soluble

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

bases are _____ when deprotonated

A

non-ionized

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

what is pKa

A

the pKa is the pH at which there are equal amounts of protonated and non-protonated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

when pH = pKa:

A

protonated equals non protonated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

when pH < pKa:

A

protonated form predominates

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

when pH > pKa:

A

non-protonated form predominates

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

only the ______ form of the drug can readily cross the lipid membrane

A

non-ionized

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

ratio of ________ and ______ influences the rate of absorption

A

non-ionized and ionized

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

what is ion trapping

A

because ionized molecules cant cross the membrane, can effectively trap them and enhance excretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

how do acidic environments of abscesses affect ionization state of local anestehtics

A
  • local anesthetics are basic and have a high pKa
  • abscesses have a lower pH
  • when a basic drug is in an acidic pH the protonated and ionized form predominates - water soluble
  • the anesthetic will hang in the abscessed fluid which makes it harder to cross membrane and harder to numb
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

what anesthetic would take the longest time to work in an abscessed area

A

bupivicaine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

what anesthetic would be the fastest to numb in an abscessed area

A

mepivacaine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

absorption is the movement of a drug from its site of administration into the ______

A

central compartment

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

absorption is the process of:

A

dissolution and diffusion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

what is bioavailability

A

fraction of drug that reaches the systemic circulation intact

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

what is the bioavailability of IV drugs

A

100%

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

bioavailability is affected by:

A

route of administration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

what is hepatic extraction ratio

A

fraction of drug in blood that is irreversibly removed during one pass through the liver

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

what is first pass clearance

A

extent to which a drug is metabolized by the liver during its first pass in the portal blood through the liver to systemic circulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

drugs with low hepatic extraction will have _____ first pass clearance

A

low

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

first pass effect occurs due to metabolism in:

A
  • gut bacteria
  • intestinal brush border enzymes
  • portal blood
  • liver enzymes
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

describe low hepatic extraction

A
  • low first pass clearance
  • change in hepatic enzymes wont have significant effect on first pass clearance
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

describe high hepatic extraction

A
  • high first pass clearance
  • bioavailability is lower
  • changes in enzyme function will have large effect on first pass effect
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

what is an example of a drug with high hepatic extraction

A

morphine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

what is an example of a drug that undergoes enterhepatic recirculation

A

clindamycin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

what are the 2 types of routes of administration

A

enteral and parenteral

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
45
Q

what is parenteral route of transmission

A

any drug that bypasses the GI system to get to the blood

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
46
Q

what are the advantages and disadvantages of enteral administration

A

-A: most common route, safest, easier, most economical
- D: limited absorption, emetogenic potention, subject to first pass, absorption may be affected by food or other drugs, irregularities in absorption or propulsion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
47
Q

what are the advantages and disadvantages of parenteral administration

A

-A: not subject to first pass, most rapid onset, ability to titrate, doesnt require patient cooperation
- D: greater patient discomfort, requires additional training to administer, concern for bacterial contamination, infection associated risks

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
48
Q

what are the infection associated risks with parenteral administration

A
  • extravasation
  • intra-arterial injection
  • limb loss
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
49
Q

in oral administration absorption is governed by:

A
  • surface area for absorption
  • blood flow to site of absorption
  • dosage form administered
  • ionization status ( lipo vs hydrophilic)
  • concentration at site of absorption
50
Q

what orally administered drugs have enteric coating

A

drugs destroyed by gastric secretions, low PH, or that cause gastric irritation

51
Q

what is the risk associated with enteric coating on orally administered drugs

A

risk of bezoar formation

52
Q

orally administered drugs have ____ release

A

delayed

53
Q

what are the parenteral routes of administration

A
  • intravenous
  • intramuscular
  • subcutaneous
  • intradermal
  • inhalation
  • intranasal
  • intrathecal/epidural
  • topical
  • subgingival
54
Q

describe intravenous injections and their bioavailability

A
  • 100%
  • immediate onset, bypasses GI absorption
  • best for emergencies
55
Q

describe intramuscular injections and their bioavailability

A
  • 75-100%
  • irritatnig drugs given this route
  • not as rapid response as IV
  • depot preparations (sustained release)
56
Q

describe subcutaneous injections and their bioavailability and give examples

A
  • 75-100%
  • slower absorption than IV or IM
  • little risk of intravascular injection
  • ex: insulin, mechanical pumps, heparin
57
Q

describe intradermal injections and examples

A

-small amounts of drug
- tuberculosis skin test, local anesthetics

58
Q

describe inhalation route and its bioavailability

A
  • 5-100%
  • almost as rapid as IV (method of abuse)
  • delivered directly to lung (good selectivity) - minimal systemic side effects
  • gases, aerosols of solutions and powders - good for respiratory conditions
59
Q

describe intranasal administrations and their bioavailability

A
  • 5-100%
  • vasopressin for tx of diabetes insipidus, calcitonin (osteoporosis)
  • method of drug abuse
60
Q

describe intrathecal/epidural injections and examples

A
  • subarachnoid space of spinal cord into CSF
  • lumbar puncture-baclofen in MS, regional anesthetic in delivery, morphine drip
61
Q

describe topical route of administration and the bioavailability

A
  • skin, oral mucosa, sublingual, rectal
  • avoids 50% of first pass metabolism
  • when local effect is desired but can provide systemic effects
  • sublingual (100%), rectal (50%) bypasses liver - good bioavailability
  • transdermal controlled release
62
Q

what are examples of transdermal controlled release drugs

A
  • scopolamine
  • nitroglycerin
  • nicotine
  • fentanyl
63
Q

describe subgingival route of administration

A
  • perio specific uses: doxycycline (atridox)
  • minocycline (arestin)
64
Q

what happens in distribution

A

the administered drug leaves the blood stream and enters other compartments

65
Q

what is distribution dependent on

A
  • cardiac output
  • capillary permeability
    -blood flow
66
Q

what organs get the most to least blood distribution and what is the number of each

A
  • kidney: 360 mL/min/100gm
  • liver: 95 mL/min/100gm
  • heart: 70 mL/min/100gm
  • brain: 55 mL/min/100gm
67
Q

what are the 3 main compartments

A
  • central
  • peripheral
  • special compartments
68
Q

what is in the central compartment

A

well perfused organs and tissues such as heart, blood, liver, brain, kidney. drug equilibrates rapidly

69
Q

what is in the peripheral compartment

A
  • less well perfused organs/tissues such as adipose, skeletal, muscle
70
Q

what is in the special compartments

A
  • CSF, CNS, pericardial fluid, bronchial secretions, middle ear
71
Q

what are the 2 proteins that bind drugs and what types of drugs do they both bind

A
  • albumin: acidic drugs
  • A-glycoprotein: basic drugs
72
Q

where do drugs accumulate in tissue

A
  • organs
  • muscle
    -adipose
  • bone
73
Q

what is an exmaple of a drug that accumulates in adipose tissue

A

fentanyl

74
Q

what is an example of a drug that accumulates in bone and what does this cause

A

tetracycline- causes staining in the teeth

75
Q

what is redistribution and what is an example

A
  • from site of action into other tissues or sites
  • propofol
76
Q

describe the distribution in the CNS

A
  • blood brain barrier exists
  • efflux transporters
  • inflammatory processes
77
Q

what is the volume of distribution

A

volume of fluid in which a drug would need to be dissolved to have the same concentration in plasma
- not a real volume

78
Q

volume of distribution is the relationship between:

A

dose and resulting Cp

79
Q

what drugs tend to have a larger Vd

A

lipophilic drugs

80
Q

what drugs have a lower Vd

A

protein bound drugs

81
Q

where are drugs found with a Vd of more than 5 L

A

confined to plasma

82
Q

where are drugs found that have a Vd of 5-15L

A

distributed to extracellular fluid (RBCs and plasma)

83
Q

where are drugs found that have a Vd larger than 42 L

A

distributed to all tissues in the body especially adipose

84
Q

increased Vd = _____ likelihood that the drug is in the tissue

A

increased

85
Q

decreased Vd = _____ likelihood that the drug is confined to the circulatory system

A

increased

86
Q

drugs are removed either:

A

metabolized/biotransformed and eliminated or excreted unchanges

87
Q

drugs must be _______ to be removed

A

water soluble

88
Q

lipid solubility is good for _____ and bad for ______

A

absorption and distribution; excretion

89
Q

what does biotransformation do

A

converts drugs into polar metabolites
- lipophilic into hydrophilic

90
Q

what does the liver accomplish metabolism of drugs through

A

P-450

91
Q

where is the cytochrome P-450 system locatde

A

liver, kidney, intestines

92
Q

what are the main most common cytochromes in the cytochrome P-450 system

A
  • CYP 3A4
  • CYP 2D6
  • CYP 2C9
  • CYP 1A2
93
Q

describe phase 1 of metabolism

A
  • catabolic
  • exposes functional group on parent compound
  • usually results in loss of pharmacologic activity
  • activation of prodrugs
94
Q

what is an example of a prodrug that is activated in phase 1 of metabolism

A

fosphenytoin to phenytoin

95
Q

what are the possible interactions with P450

A
  • substrates
  • inhibitors
  • inducers
96
Q

what is an example of a substrate in the P450 system

A

warfarin

97
Q

what is an example of an inhibitor in the P450 system

A

bactrim

98
Q

what do inducers in P450 do

A

the drug sends a message to the nucleus to make more CYP protein which lowers the concentration of another drug thus decreasing that drugs efficacy

99
Q

describe the genetic polymorphisms of the CYP isoenzymes

A
  • great genetic variability in function
  • may be poor metabolizers or rapid metabolizers
  • this can lead to subtherapeutic effect such as codeine and tramadol
  • or this can lead to toxicity such as in diazepam, alprazolam
100
Q

describe phase 2 of metabolism

A
  • occurs after functional groups are exposed
  • anabolic: adds water soluble molecules to structure
  • much less inter- patient variability
101
Q

what are the major reactions in phase II of metabolsim

A
  • glucuronidation
  • glutathione conjugation
  • sulfate conjugation
  • acetylation
102
Q

what are the primary routes of excretion

A

kidney, lung and feces

103
Q

what is excretion

A
  • removal of an unchanged drug
  • polar compounds -> lipid soluble compounds
104
Q

what are the 3 processes of excretion in the kidneys

A
  • glomerular filtration
  • active tubular secretion
  • passive tubular reabsorption
105
Q

describe the process of excretion in the kidneys

A
  • dependent on renal function
  • only unbound drug filtered
  • non-ionized weak acids and bases are passively reabsorbed
  • alkaline urine traps ionized acidic molecules and increases excretion
106
Q

describe excretion through the lungs and what is it affected by

A
  • primarily inhaled anesthesia or volatile liquid
  • affected by respiratory rate and blood flow
107
Q

describe excretion through feces

A
  • unabsorbed orally administered meds
  • metabolites excreted in the bile
  • un-reabsorbed metabolites secreted into the intestinal tract
108
Q

what is the main factor that determines rate of passive transport

A

lipid solubility

109
Q

how many molecules bind per molecule of albumin

A

2

110
Q

extensive protein binding can _____ drug elimination

A

slow

111
Q

competition for protein binding can sometimes lead to:

A

interactions

112
Q

which protein is more commonly bound

A

albumin

113
Q

acids get trapped in ____ environments

A

basic

114
Q

gut absorption depends on factors such as:

A
  • GI motility
  • GI pH
  • particle size
  • interaction with gut contents
115
Q

what catabolic reactions take place in phase I of metabolism

A

oxidation, reduction, hydrolysis

116
Q

which phase of metabolism results in more active products

A

phase I

117
Q

which phase of metaboslim involves the P450 system

A

phase I

118
Q

what is the end result of phase II metaboslim

A

conjugated, inactive and polar products for excretion

119
Q

unless they’re protein bound most drugs are filtered through:

A

the glomerulus

120
Q

weak acids and bases are actively secreted into:

A

the renal tubule

121
Q

lipid soluble drugs are ______ not efficiently excreted

A

passively reabsorbed

122
Q
A

Pharmacology I (12 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions