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Autonomic physiology > Midterm 1 > Flashcards

Midterm 1 Flashcards

1
Q

the action of a drug on an individual

A

pharmacodynamics

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2
Q

substance used in the diagnosis, treatment, or prevention of an illness

A

drug

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3
Q

anti-emitic, specific muscarinic acetylcholine receptor antagonist of vestibular pathway, decreases ACh input

A

scopolamine

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4
Q

vestibular, sensory, emotional, chemoreceptors, GI tract are all things that project to what

A

vomition center

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5
Q

the way botox achieves specificity

A

local administration

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6
Q

the study of drug administration, absorbtion, distribution, action, and excretion

A

pharmacokinetics

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7
Q

routes of administration

A

oral, IV, intramuscular, inhalation, topical, subcutaneous, intraperitonial, intracranial

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8
Q

Problems with oral administration

A

acidic environment in stomach, first pass effect (liver metabolism often reduces efficacy, but not loarsitan)

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9
Q

first pass effect

A

drug must enter bloodstream: portal vein - liver - drug metabolism. Both acidic stomach env. and liver metabolism can reduce function of drug

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10
Q

works better after metabolism

A

loarsitan

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11
Q

MEC (desired response)

A

minimum effective concentration (always exists)

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12
Q

point at which drug exceeds threshold

A

onset of effect

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13
Q

point of drug being toxic

A

MEC (adverse response)

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14
Q

Difference between drug threshold and toxic threshold

A

therapeutic window

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15
Q

Time it takes for half of drug to leave system

A

Half-life (T1/2)

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16
Q

Repeated doses to achieve steady state leads to this curve shape

A

sigmoidal

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17
Q

Fast onset, large volumes, sterility problem, must be hydrophilic

A

IV

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18
Q

Steady absorbiton, hydrophobic, sterility problems, sometimes irritating

A

Intramuscular

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19
Q

Gaseous (volatile), fast onset, sometimes requires flame

A

Inhalation

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20
Q

slow, steady absorption, only hydrophobic

A

Topical

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21
Q

implantation of pellet, slow, steady absorption, sterility problems, removal problems

A

subcutaneous

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22
Q

injection into abdomen, fast availability, sterility problem, used for lab rats

A

Intraperitoneal

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23
Q

drug effectiveness/absorbtion graph

A

IV, IP, IM, oral(PO)

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24
Q

directly to CNS, sterility problem, (epidurals)

A

Intracranial

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25
Q

drug enters and exits body tissues

A

Equilibrium

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26
Q

Drug doesnt know where you want it to go

A

hydrophilic, hydrophobic, specific receptors, etc.

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27
Q

tissue drug has no effect in and gets trapped in, no receptors

A

drug reservoir

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28
Q

example of drug reservoir

A

adipose tissue

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29
Q

nonspecific assoiation, other drug reservoir that isnt drug reservoir, is reversible, amino acids attractive to drug

A

proteins

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30
Q

liver chemically alters drugs to make removal easier

A

metabolism

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31
Q

metaolized drug

A

metabolite

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32
Q

why is transformation from ph 2 to 7 necessary

A

make absorption possible, must be nonpolar to cross lipid bilayer

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33
Q

why weak bases are good oral candidates

A

protonation in stomach, becomes neutral

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34
Q

BBB is different in this way

A

tight junctions and astrocytic feet

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35
Q

R-CH2-CH3 –>(cytochrome P450) –> R-CH(OH)-CH3

A

oxidation

36
Q

R-NO2 –> R-NH2

A

reduction

37
Q

R-CO2R’–>esterases>R-CO2H+R’OH

A

hydrolysis

38
Q

R-OH + R –> R-O-R’

A

conjugation

39
Q

contains furanocoumarins which inhibit a P450 enzyme, increases levels of lipitor in bloodstream | can also block transporters in intestine which are responsible for uptake (allegra)

A

grapefruit juice

40
Q

urination, sweat, exhalation, liver–bile

A

excretion

41
Q

bifunctional role of receptor, one “thing” for which atropine and pilocarpine are competing in salivary glands (DATE, PERSON, THEORY NAME)

A

john langley (1878)- receptor theory

42
Q

coined the term “receptor,” lock and key metaphor (person and dates)

A

Paul Ehrlich (1854 - 1915)

43
Q

molecules that bind receptors

A

ligands

44
Q

cause a positive response (biological), can initiate second messenger response

A

agonist

45
Q

binds with high affinity, but doesn’t have biological effect (nothing turned on in cell), no second messenger pathway, blocks normal chemical binding, blocked cellular activity

A

antagonist

46
Q

one example antagonist can be used for response

A

narcan for heroin overdose

47
Q

Gs

A

stimulates adenylyl cyclase - takes ATP and forms cAMP, alters PKA, catalytic subunits run free and phosphorylate downstream targets

48
Q

Gi

A

inhibits adenylyl cyclase

49
Q

Gq

A

stimulates PLC - DAG–>PL(K?)C

50
Q

Go

A

couples directly to ion channels

51
Q

how many transmembrane domains do G protein receptors have?

A

7

52
Q

nicotine is agonist for this type of channel

A

ligand-gated ion channel

53
Q

transporter: just takes one

A

uniporter

54
Q

transporter: picks up one from inside, one from outside, and swaps them

A

antiporter

55
Q

transporter: takes multiple things at once and moves them to other side of membrane

A

symporter

56
Q

transporter: uses ATP

A

ATP-driven transporter

57
Q

proteins which interact with DNA following binding of a ligand (e.g. estrogen)

A

Transcriptional activator

58
Q

receptor where each monomer has half of the receptor sites, presence of ligand bring 2 monomers together, they phosphorylate each other, then phosphorylates downstream intracellular target

A

Tyrosine Kinase Receptor

59
Q

Drug binding to receptor is:

A

reversible

60
Q

computer runs water molecule over protein surface, this helps us determine:

A

protein shape

61
Q

how much drug wants to get into and stay in binding pocket | “ability of drug to bind receptor”

A

affinity

62
Q

4 factors that determine drug affinity

A

steric interactions, ionic bonds, hydrogen bonds, hydrophobic interactions (all reversible), covalent bonds rare

63
Q

Concentration at which 50% of receptors are bound

A

Kd (affinity constant), logarithmic curve, smallest concentration that achieves Kd has highest affinity, Kd is inflection point

64
Q

concentration of competitor at which we lose 50% of first drug binding

A

IC50

65
Q

binding assay demonstration

A

once receptors are filled, more drugs wont bind

66
Q

how fast drug associates with receptor

A

k1- forward rate constant

67
Q

how long it takes drug to come off of receptor

A

k-1 - reverse rate constant

68
Q

k-1/ k1

A

reflects affinity

69
Q

ability of drug bound to receptor to induce intracellular activity

A

efficacy

70
Q

intrinsic efficacy of 1

A

full agonist

71
Q

intrinsic efficacy btw 0 and 1

A

partial agonist

72
Q

intrinsic efficacy of 0

A

antagonist

73
Q

regions responsible for making associations with drug - influences affinity

A

binding domain

74
Q

region that interacts with drug that “turns on” receptor (conformational change)

A

activation domain

75
Q

____ is a measure of how well a drug binds; ____ is a measure of how well a drug can produce desired effect

A

affinity, efficacy

76
Q

dose response curves can tell you response to drug, but neither ___ or ____ specifically

A

affinity, efficacy

77
Q

concentration of drug at which 50% of population exhibits a response after a certain period

A

EC50, lower EC50 is a better drug

78
Q

receptor expression, ligand affinity, and intrinsic efficacy, all constitute:

A

drug effectiveness

79
Q

receptor expression is not ___ within population, or even within people

A

constant

80
Q

with sudden high concentrations of agonist, receptor becomes phosphorylated, inactivated, and internalized/sequestered

A

desensitization

81
Q

with chronic levels of agonist, receptors become phosphorylated multiple times, inactivated, and internalized, having been tagged for degradation, B- arrestin involved

A

downregulation

82
Q

administration of 2nd drug to allow re-sensitization of 1st drug’s receptors

A

drug vacation

83
Q

drug binding and biological response are ___ correlated

A

directly

84
Q

Therapeutic index

A

TD50/ED50 (2 is not safe drug, doubling dose causes side effects in 1/2 of population

85
Q

Therapeutic window

A

TD50 - ED50

86
Q

3 categories of neurotransmitters of ANS

A

ACH, catecholamines (NE and E), and indolamines (serotonin)

Autonomic physiology (2 decks)

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