1-intro Flashcards

(78 cards)

1
Q

What kind of drugs are antihistamines??

A

Inverse agonists

Suppress activity / make it worse, unlike antagonist that stops it (not Necessarily making it worse)

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2
Q

Why gen 2 antihistamines non sedating

A

P-glycoprotein pumps remove it from the brain while gen 1 cant

Less in brain, less sedation

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3
Q

Pharmacodynamics

A

What drug does to body

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4
Q

Pharmacokinetics

A

what body does to the drug

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5
Q

Prodrug

A

not intrinsically active, activated by a metabolic step

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6
Q

off-target effect

A

influence on other receptors than the one target, they are often related receptors

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7
Q

G-protein coupled receptor

A

ligand bind to extracellular surface, conformational change, activates signalling cascade activated by G proteins

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8
Q

Gs

A

activates adenylate cyclase

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9
Q

what does adenylate cyclase do

A

catalyses ATP to cAMP

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10
Q

Gi

A

inhibits adenylate cyclase

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11
Q

Gq

A

activates phospholipase C

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12
Q

what does phospholipase C do

A

breakdown PIP2 to IP3 and DAG

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13
Q

what does IP3 and DAG do

A

triggers ER to release Ca2+

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14
Q

tyrosine kinase receptors

A

ligand binding causes auto-phosphorylation

dimerization of receptors (ligand binding)

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15
Q

Ion channel

A

fastest
makes electrical signals
ions flowing through proteins
LIGAND BINDING, VOLTAGE GATED

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16
Q

voltage gated ion channel

A

quick, milliseconds, movement of charged a.a. in transmembrane electric field charge position in response to changes in voltage

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17
Q

ligand gated

A

open or close in response to binding of a small molecule

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18
Q

agonism

A

binding of substrate to receptor that generates an effect

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19
Q

EC50

A

conc. of drug that yields 50% of its max effect, same as efficacy

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20
Q

Emax

A

max biological effect observed with the drug

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21
Q

efficacy

A

same as emax

Max biological effect observed with the drug

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22
Q

potency

A

concentration dependence, how much is needed for a certain effect.

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23
Q

what is potency related to

A

EC50

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24
Q

potency EC50 relationship

A

high potency, low EC50

low potency, high EC50

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25
partial agonist
can generate a fractional effect
26
full agonist
can generate a max effect
27
antagonist
cannot generate a biological effect, influences receptors response to agonist
28
inverse agonist
suppresses basal activity, opposite effect of agonist
29
competitive antagonism
more agonist required to generate given response
30
what does competitive antagonism shift
potency/EC50
31
What does non competitive antagoism shift (efficacy and potency
reduce efficacy, no change in potency
32
steroid hormone receptors | what type and mechanism of action
intracellular, slow, requires DNA binding
33
cell surface receptor mechanism of action
fast, intracellular signalling cascades
34
dose ratio
EC50(w/antagonist) / EC50(w/o antagonist)
35
irreversible competitive antagonism
cannot be displaced by increased agonist concentration, binds to same site as the agonist
36
allosteric potentiation
increase efficacy and/or potency of the agonist
37
mixed antagonist
combo of weakened efficacy and potency
38
orthosteric site
agonist binding site
39
does COX-1 or 2 have a bigger active site
COX-2
40
what do NSAIDS inhibit
COX1 and 2
41
what drug is tylenol
acetaminophen
42
extraction ratio/factor
clearance/blood flow
43
what does low extraction ratio mean
organ doesn't filter much so the drug stays in blood
44
what is high extraction ratio
organ clears out most of the blood, like the liver!
45
bioavailability
% of unprocessed drug that reaches systemic circulation after being administrated by a particular route
46
receptor reserve
when there are more receptors present than are required for a full biological effect
47
Effect formula
(Emax)/(1+ EC50/[drug])
48
first pass metabolism
drugs pass through hepatic circulation the liver (major metabolism) before entering heptic circulation
49
what is Kd
dissociation constant, when 50% receptors are bound
50
why can there be a mismatch between binding and effect?
receptor reserve (more receptors needed than required to make effect)
51
what is distribution
how drugs are partitioned into different body compartments
52
factors that effect distribution
1. binding to plasma proteins, these are "bound" (not free or pharmacologically active) 2. drug accumulation in tissues --> favored for lipophilic drugs and purfuse organs
53
are drugs bound to plasma proteins pharmacologically active?
NO ! they are not free
54
what does perfuse mean
more blood is supplied to the area
55
what kind of drugs collect more in tissues
lipophilic
56
volume of distribution formula
total amount of drug in body/[drug]
57
high volume of distribution means | and why
well distributed often highly lipophilic
58
low volume of distributed means
poorly distributed often lipophobic and bound to plasma proteins
59
what is biotransformation
metabolism in liver
60
phase 1 biotransformation
OXIDATION by CYP enzymes | mixed function oxidase system
61
phase 2 biotransformatin
add POLAR parts to make it more prone to excretion
62
does phase 1 or 2 biotransformation happen first
EITHER OR
63
capacity limited elimination
when [drug] is higher than their affinity of the enzyme that breaks it down
64
pharmacogenomics/genetics
how drugs affect people because of their genes ex: CYP enzymes vary a lot
65
therapeutic index
TD50/ED50 toxic dose/effective dose
66
is big or small therapeutic index better
BIG
67
relative risk reduction
1-(event rate in treatment group)/(event rate in control group)
68
is relative risk reduction good?
misleading because it does not convey baseline risk and doesn't capture the diff. b/w large reduction of something frequent vs. infrequent
69
absolute risk reduction formula
event rate in control group-event rate in treatment group
70
is absolute risk reduction good?
yes, describes # of cases prevented by drug instead of % relative to baseline (RRR)
71
numbers needed to treat formula
1/ARR 1/(event rate in control group-event rate in treatment group)
72
is numbers needed to treat good?
yes, it shows the population level drug benefit
73
what if you get a negative numbers needed to treat ???
it means event is higher in experimental than control group... BAD DRUG--> numbers needed to harm
74
numbers needed to harm
when you have a negative numbers needed to treat
75
meta-analysis
systematic review, data from multiple trials combined into a forest plot
76
Schild Plot
dose ratio vs. log[antagonist]
77
what is IIP3 role
bind to ER so calcium is released
78
what is DAG role
remains in membrane and activates PKC