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Exam 1 Flashcards

0
Q

insulin works via?

A

receptor tyrosine kinase

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1
Q

glucocorticoids work via?

A

intracellular receptors

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2
Q

platelet growth factors work via?

A

receptor tyrosine kinases

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3
Q

nerve growth factors work via

A

receptor tyrosine kinases

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4
Q

platelet-derived growth factors work via?

A

receptor tyrosine kinases

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5
Q

kinase activity is a separate protein for?

A

cytokine receptors

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6
Q

NO is synthesized via what signaling pathway

A

cyclic GMP/guanylyl cyclase

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7
Q

decreased response because the enzymes that metabolize the drug are induced
(increased drug metabolism = decreased response)
is??

A

pharmacokinetic tolerance

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8
Q

decreased response due to change in receptor # or function is?

A

pharmacodynamic tolerance

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9
Q

what is physiologic tolerance?

A

when 2 agents w/ opposing physiologic effects are administered together

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10
Q

what is competitive tolerance

A

receptor antagonist w/ an agonist

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11
Q

what is potency

A

the dose required to produce a particular effect

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12
Q

a basic drug in an acidic medium will…?

A

become ionized & accumulate

then be eliminated

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13
Q

drugs with high first pass metabolism?

A

lidocaine, morphine

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14
Q

how does first pass metabolism influence oral availability

A

decreases

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15
Q

drugs with low first pass metabolism

A

diazepam, digitoxin

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16
Q

CNS & autonomic drugs, cardiovascular drugs target?

A

G protein coupled receptor

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17
Q

local anesthetics and anticonvulsants target?

A

voltage-gated ion channels

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18
Q

nicotine targets?

A

ligand-gated ion channel

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19
Q

benzodiazepienes target?

A

ligand gated ion channels

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20
Q

MAO inhibitors and cholinesterase inhibitors target?

A

enzymes

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21
Q

antidepressants target? (and 2 examples?)

A

transport proteins (DAT, SERT)

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22
Q

anticancer and antiviral drugs target?

A

nucleic acids

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23
Q

codeine is metabolized to what?

A

morphine (active metabolite)

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24
metabolism of diazepam
diazepam --> nordiazepam (longer half-life) --> oxazepam
25
acetaminophen metabolite?
N-acetyl-p-benzoquinone imine (toxic metabolite)
26
affinity is designated by?
Kd
27
what reactions are the most common phase I reactions?
oxidation
28
whats the most common phase II reaction?
conjugation
29
CYP2D6 polymorphism results in
decreased codeine metabolism to morphine --> less analgesic effect
30
acidic mediums trap which drugs?
basic drugs
31
basic mediums trap which drugs?
acidic drugs
32
what cytochrome metabolizes > 50% of drugs?
CYP 3A4
33
which CYP metabolizes alcohol?
CYP 2E1
34
alcohol's effect of CYP2E1 (2)
induction- more activity ---> EtOH tolerance | induction of CYP2E1 also increases acetaminophen metabolism
35
primary enzymes in Phase I metabolism?
Cytochrome P 450 (CYPs)
36
two CYP-independent oxidation reactions?
alcohol dehydrogenase | monoamine oxidase
37
grapefruit juice inhibits what enzyme?
CYP450 3A4
38
Examples of substrates inhibited by grapefruit juice?
Acetaminophen, diazepam, lidocaine
39
Quinidine inhibits what enzyme?
CYP 2D6
40
examples of substrates inhibited by quinidine?
Codeine, oxycodone
41
what is a common endogenous compound used in Phase II conjugation reaction?
glucuronic acid
42
Phase II conjugation reaction w/ glucuronic acid?
UDP-glucuronic acid + R-OH ---> glucuronic acid-R + UDP
43
renal excretion is influenced by 3 factors:
glomerular filtration rate active tubular secretion or reabsorption passive diffusion across tubular epithelium (all of these can be impacted by pathology)
44
describe enterohepatic circulation
conjugated metabolites released into the bile are cleaved by bacterial enzymes in the SI, releasing the drug for reabsorption
45
effect of enterohepatic circulation on drug half-life | and an example?
increases the drug's half-life | example: estrogen in BC
46
biotransformation of drugs?
lipid-soluble, non-ionized ---> water-soluble, ionized metabolites
47
large Vd signifies? re: distribution
extensive distribution, binds to peripheral tissues (not plasma- not bioavailable)
48
small Vd signifies? re: distribution
drugs that are highly concentrated in the plasma
49
examples of drugs with large Vd?
Acetaminophen, Propranolol
50
examples of drugs with small Vd?
Heparin, Warfarin
51
spare receptors effect on the concentration-response curve
shifted left to smaller concentrations
52
competitive antagonist effect on the curve
dose response curve shifts to the right
53
noncompetitive agonist effect on the curve
Emax and Bmax decrease
54
partial agonist effect on curve
lower Bmax and Emax than the full agonist
55
graded dose response curve measures?
response in an individual
56
on a graded dose response curve, the position on the X-axis indicates
potency
57
contraindications for gastric lavage (4)
more than 4 hours since ingestion of most poisons more than 30 min since ingestion of corrosive not used for hydrocarbon solvents or if coma, stupor, delirium are present
58
methods of increasing excretion rate to treat toxicity (4)
osmotic diuretics, alter urine pH, hemodialysis, hemoperfusion
59
single/multiple exposure to a poison over 1-2 days
acute toxicity
60
repeated exposures to a poison <3 mo.
subacute toxicity
61
repeated exposures to a poison > 3 mo.
chronic toxicity
62
nicotine toxicity mechanism
interference w/ receptor-ligand interactions
63
local anesthetic toxicity mechanism
interference w/ membrane fxn
64
toxicity mechanism of cyanide
interference w/ cellular energy fxn
65
toxicity mechanism of organophosphates
binding to biomolecules
66
toxicity mechanism of ethylene glycol
perturbation in calcium homeostasis
67
toxicity mechanism of MPTP
toxicity from selective cell loss
68
toxicity mechanism of carcinogens
non-lethal alterations in somatic cells
69
toxicity mechanism of dioxins
interference w/ cellular transcription factors
70
toxicity mechanism of Acetaminophen
induction of programmed cell death
71
Poisoning treatments that reduce absorption or increase elimination (3)
``` Activated charcoal Ammonium chloride (acidifies urine- basic drugs) Sodium bicarbonate (alkalinizes the urine- acidic drugs) ```
72
chelator of arsenic, gold, mercury, and acute lead
Dimercaprol
73
chelator of copper
Penicillamine
74
chelator of iron
Deferoxamine
75
tx for lead poisoning
calcium disodium edatate
76
tx for acetaminophen poisoning (drug)
Acetylcysteine
77
antidote for cholinesterase inhibitor
Atropine
78
sx of organophosphate poisoning
SLUD | Salivation, Lacrimation, Urination, Defecation
79
Kayser-Fleischer rings indicate?
copper accumulation
80
competitive agonist effect on curve (2)
increased Kd | right shift
81
noncompetitive antagonist effect on curve (2)
Emax and Bmax decrease
82
efficacy of partial agonists?
lower
83
Administration of agonist and allosteric activator effect the curve how?
same Emax, shift left
84
Administration of agonist and competitive antagonist affect the curve how?
shift right | No Emax
85
Administration of Agonist & Noncompetitive Antagonist affect the curve how?
No Emax
86
decreased response because the enzymes that metabolize the drug are induced
pharmacokinetic tolerance
87
examples of pharmacokinetic tolerance
barbiturates, EtOH, warfarin
88
decreased response due to change in receptor number or function
``` pharmacodynamic tolerance (desensitization, receptor down-regulation) ```
89
example of pharmacodynamic tolerance
B-adrenergic agonists (Albuterol)
90
occurs when two agents with opposing physiologic effects are administered together
physiologic tolerance
91
example of physiologic tolerance?
histamine and norepinephrine | vasodilation and vasoconstriction
92
administration of receptor antagonist along with receptor agonist results in?
competitive tolerance
93
example of competitive tolerance
Yohimbe & clonidine
94
two methods of desensitization?
1. continuous exposure to an agonist --> conversion of an ion channel to an altered, closed state 2. receptor coupling effector is phosphorylated to an inactive form
95
chronic administration of agonists can result in?
down-regulation = degradation of receptors

Pharm 1 (3 decks)

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