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Pharmacology > Exam 2: Step 2 Mechanism of Action > Flashcards

Exam 2: Step 2 Mechanism of Action Flashcards

1
Q

fluoxetine

A

blocks SERT to increase serotonin

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2
Q

alteplase

A

binds fibrin in a fresh clot, then activates plasminogen to dissolve the clot

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3
Q

lamotrigine

A

inactivate Na channel

inhibit Ca channel

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4
Q

duloxetine

A

blocks SERT and NET

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5
Q

rasagiline

A

inhibits degradation of dopamine by MAO-B

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6
Q

valproic acid

A

inactivate Na channel
inhibit T-type Ca channel
inhibits breakdown of GABA

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7
Q

carbamazepine

A

inactivate Na channel

potentiate GABA response

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8
Q

ergotamine (PO) and dihydroergotamine (IV, IM, nasal, PR)

A

cerebral vasoconstriction

5-HT agonist in trigeminal nerve

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9
Q

phenytoin

A

inactivate Na channel

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10
Q

sumatriptan

A

selective agonist at 5-HT1B,D,F receptors

B - blood vessels - constrict
D - peripheral neurons - inhibit CGRP release
F - central neurons - inhibit neurotransmission

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11
Q

sertraline

A

blocks SERT

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12
Q

selegeline and rasagiline

A

inhibit DA degradation by MAO-B (which is mostly in the striatum)

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13
Q

ramelteon

A

melatonin receptor agonist

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14
Q

zonisamide

A

inactivate Na channel

inhibit T-type Ca channel

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15
Q

celecoxib

A

COX-2 inhibitor

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16
Q

benztropine

A

muscarinic antagonist on GABA-ergic neuron (for Parkinsonism tremor)

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17
Q

misoprostol

A

inhibits gastric acid secretion

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18
Q

carbidopa

A

inhibits peripheral L-AAD (decarboxylase enzyme) from converting of L-DOPA to DA

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19
Q

tolcapine

A

inhibits peripheral AND central COMT (methyltransferase enzyme) from converting L-DOPA to 3-O-MD

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20
Q

entecapone

A

inhibits peripheral COMT (methyltransferase enzyme) from converting L-DOPA to 3-O-MD

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21
Q

aspirin

A

IRREVERSIBLE COX-1 and COX-2 inhibitor

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22
Q

levetiracetam

A

interfere w/ glutamate vesicle fusion (SV2A ligand) in presynaptic terminal

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23
Q

ethosuximide

A

inhibit T-type Ca channel in thalamic neuron

T-type Ca channels involved in absence seizures

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24
Q

primidone

A

inactivate Na channel

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25
ibuprofen
reversible COX1 and COX2 inhibitor
26
phenytoin
inactivate Na channels
27
naproxen
reversible COX1 and COX2 inhibitor
28
acetaminophen
COX-2 and COX-3 inhibitor
29
vigabatrin
inhibits GABA transaminase (to increase GABA) metabolite is phenobarbital (but ? importance)
30
phenobarbital
binds to site on GABA-A receptor, enhancing duration of chloride influx at high doses, can DIRECTLY open channel
31
benzodiazepines
bind to site on GABA-A receptor to enhance chloride influx | Needs GABA to function, cannot directly open channel
32
clozapine olanzapine risperidone
5HT2 block >>> D2 block (opposite of typical antipsychotics) 5-HT2 antagonist which facilitates dopamine release in cortex = less negative symptoms D2 antagonist selectively in mesolimbic pathway = less positive symptoms without causing EPS
33
flumazenil
competitive ANTAGONIST at BZ site on GABA-A receptor reverses effects of BZs and BZ agonists
34
metaclopramide
increases gastric emptying antagonist at 5-HT3 and D2 receptors
35
propranolol in migraine tx
unclear ???overall reduction in adrenergic tone
36
buspirone
direct partial agonist at CNS 5-HT1a receptor
37
L-DOPA
precursor for DA synthesis
38
ropinirole and pramipexole
directly stimulate CNS D2 receptors
39
zolpidem and eszoplicone
binds to alpha-1 subunit of GABA-A receptor, which is selective for sedation
40
amandatine
enhance DA release | inhibit DA reuptake
41
haloperidol
D2 block >> 5HT2 block D2 antagonist +++ 5-HT2 block ++
42
topiramate
inactivate Na channel inhibit AMPA receptor increase GABA activity
43
onabotulinum toxin in migraine tx
cleaves snares to prevent release of CGRP from peripheral trigeminal nerve terminal (calcitonin gene related peptide)
44
aripiprazole
unlike other atypicals PARTIAL AGONIST at D2 receptor = decreases DA activity in accumbens while increasing DA in the cortex also 5HT2 block +++
45
gabapentin
inhibit Ca channel
46
chlorpromazine
D2 antagonist + 5-HT2 block ++ alpha-1 block +++ (bad in elderly) ACh block +
47
Abciximab Tirofiban Eptifibatide (blue drugs, IV only, just need to know MOA)
block IIb/IIIa receptor on platelet to block fibrinogen bridge formation (platelet aggregation)
48
fondaparinux
catalyzes antithrombin at factor 10a
49
dabigatrain
direct factor 2a inhibitors
50
heparin
catalyzes antithrombin at factor 10a and 2a
51
Rivaroxaban and apixaban
direct factor 10a inhibitors
52
enoxaparin
catalyzes antithrombin mostly at factor 10a but also at 2a
53
amitryptyline
block SERT and NET...(mostly SERT)... | ``` but also... anti- muscarinic/cholinergic histaminergic alpha-1 adrenergic side effects!!! ```
54
G-CSF
stimulates progenitor cells committed to granulocyte lineage mobilizes stem cells of all lineages into peripheral blood (enables harvesting for transplant)
55
warfarin
inhibits VKORC enzyme which blocks Gla formation which prevents factors 10, 9, 7, and 2 from binding to platelets
56
tranylcypromine
irreversibly inhibit monoamine oxidase, to prevent degradation of NE and serotonin
57
epoetin
stimulates erythroid proliferation and differentiation
58
clopidogrel and prasugrel
irreversibly block the ADP purine receptor (P2Y12) to prevent GP-IIb/IIIa activation and fibrinogen binding (platelet aggregation)
59
GM-CSF | M for myeloid
stimulates proliferation of granulocytic, erythroid and megakaryotic progenitor cells
60
ziprasidone
same as other atypicals (5HT2 block > D2 block) 5H2block ++++ D2 block +++
61
lithium
unclear and complex decrease IP3 second messenger?
62
morphine, hydromorphone, oxymorphone
glucuronidated into 2 metabolites that can cross BBB: Morphone-6-G full MOR agonist Morphine-3-G no affinity to MOR but neuroexcitatory @ NMDA receptor (can cause seizures)
63
fentanyl
same as morphine but faster acting
64
methadone
MOR agonist with long half life also has non-opioid analgesic MOAs
65
meperidine
MOR agonist (same as morphine) less potent, faster acting
66
codeine
PRODRUG converted to morphine by CYP2D6 (beware of "poor metabolizers")
67
oxycodone and hydrocodone
direct analgesic properties also partially metabolized to oxymorphone and hydromorphone (not CYP2D6 dependent)
68
pentazocine
kappa receptor agonist acts at spinal and supra-spinal sites and partial MOR ANTAGONIST
69
buprenorphine
mixed partial MOR agonist | and kappa receptor ANTAGONIST
70
dextromethorphan
active at DM receptor (antitussive, not analgesic)
71
naloxone and naltrexone
competitive MOR ANTAGONIST
72
tramadol
weak MOR agonist | inhibition of NE and 5-HT reuptake
73
loperamide
acts on MOR in myenteric plexus of large intestine
74
atropine
muscarinic ANTAGONIST. crosses BBB
75
nicotine and varenicline
direct nicotinic agonist
76
ipratropium
muscarinic ANTAGONIST in lungs does not cross BBB
77
neostigmine
reversible anticholinesterase does NOT cross BBB
78
physostigmine
reversible anticholinesterase crosses BBB
79
donepezil
crosses BBB to increase acetylcholine at CNS synapses to improve cognition and memory
80
sarin
IRREVERSIBLE anticholinesterase
81
vecuronium
NONDEPOLARIZING competitive nicotinic ANTAGONIST at skeletal muscle
82
trimethaphan
ANTAGONIST at ganglion block sympathetic/parasympathetic so that you (the ED PA) can control BP
83
succinylcholine
depolarizing skeletal muscle nicotinic ANTAGONIST w/ VERY fast onset
84
botulinum toxin in wrinkle tx
blocks acetylcholine release at cholinergic terminals = no muscle contraction

Pharmacology (6 decks)

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