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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
Q

ibuprofen

A

reversible COX1 and COX2 inhibitor

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26
Q

phenytoin

A

inactivate Na channels

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27
Q

naproxen

A

reversible COX1 and COX2 inhibitor

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28
Q

acetaminophen

A

COX-2 and COX-3 inhibitor

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29
Q

vigabatrin

A

inhibits GABA transaminase (to increase GABA)

metabolite is phenobarbital (but ? importance)

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30
Q

phenobarbital

A

binds to site on GABA-A receptor, enhancing duration of chloride influx
at high doses, can DIRECTLY open channel

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31
Q

benzodiazepines

A

bind to site on GABA-A receptor to enhance chloride influx

Needs GABA to function, cannot directly open channel

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32
Q

clozapine
olanzapine
risperidone

A

5HT2 block&raquo_space;> 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

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33
Q

flumazenil

A

competitive ANTAGONIST at BZ site on GABA-A receptor

reverses effects of BZs and BZ agonists

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34
Q

metaclopramide

A

increases gastric emptying

antagonist at 5-HT3 and D2 receptors

35
Q

propranolol in migraine tx

A

unclear

???overall reduction in adrenergic tone

36
Q

buspirone

A

direct partial agonist at CNS 5-HT1a receptor

37
Q

L-DOPA

A

precursor for DA synthesis

38
Q

ropinirole and pramipexole

A

directly stimulate CNS D2 receptors

39
Q

zolpidem and eszoplicone

A

binds to alpha-1 subunit of GABA-A receptor, which is selective for sedation

40
Q

amandatine

A

enhance DA release

inhibit DA reuptake

41
Q

haloperidol

A

D2 block&raquo_space; 5HT2 block

D2 antagonist +++
5-HT2 block ++

42
Q

topiramate

A

inactivate Na channel
inhibit AMPA receptor
increase GABA activity

43
Q

onabotulinum toxin in migraine tx

A

cleaves snares to prevent release of CGRP from peripheral trigeminal nerve terminal

(calcitonin gene related peptide)

44
Q

aripiprazole

A

unlike other atypicals

PARTIAL AGONIST at D2 receptor = decreases DA activity in accumbens while increasing DA in the cortex

also 5HT2 block +++

45
Q

gabapentin

A

inhibit Ca channel

46
Q

chlorpromazine

A

D2 antagonist +

5-HT2 block ++
alpha-1 block +++ (bad in elderly)
ACh block +

47
Q

Abciximab
Tirofiban
Eptifibatide
(blue drugs, IV only, just need to know MOA)

A

block IIb/IIIa receptor on platelet to block fibrinogen bridge formation (platelet aggregation)

48
Q

fondaparinux

A

catalyzes antithrombin at factor 10a

49
Q

dabigatrain

A

direct factor 2a inhibitors

50
Q

heparin

A

catalyzes antithrombin at factor 10a and 2a

51
Q

Rivaroxaban and apixaban

A

direct factor 10a inhibitors

52
Q

enoxaparin

A

catalyzes antithrombin mostly at factor 10a but also at 2a

53
Q

amitryptyline

A

block SERT and NET…(mostly SERT)…

```
but also… anti-
muscarinic/cholinergic
histaminergic
alpha-1 adrenergic
side effects!!!
~~~

54
Q

G-CSF

A

stimulates progenitor cells committed to granulocyte lineage

mobilizes stem cells of all lineages into peripheral blood (enables harvesting for transplant)

55
Q

warfarin

A

inhibits VKORC enzyme
which blocks Gla formation
which prevents factors 10, 9, 7, and 2 from binding to platelets

56
Q

tranylcypromine

A

irreversibly inhibit monoamine oxidase, to prevent degradation of NE and serotonin

57
Q

epoetin

A

stimulates erythroid proliferation and differentiation

58
Q

clopidogrel and prasugrel

A

irreversibly block the ADP purine receptor (P2Y12) to prevent GP-IIb/IIIa activation and fibrinogen binding (platelet aggregation)

59
Q

GM-CSF

M for myeloid

A

stimulates proliferation of granulocytic, erythroid and megakaryotic progenitor cells

60
Q

ziprasidone

A

same as other atypicals (5HT2 block > D2 block)

5H2block ++++
D2 block +++

61
Q

lithium

A

unclear and complex

decrease IP3 second messenger?

62
Q

morphine, hydromorphone, oxymorphone

A

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
Q

fentanyl

A

same as morphine but faster acting

64
Q

methadone

A

MOR agonist with long half life

also has non-opioid analgesic MOAs

65
Q

meperidine

A

MOR agonist (same as morphine)

less potent, faster acting

66
Q

codeine

A

PRODRUG converted to morphine by CYP2D6 (beware of “poor metabolizers”)

67
Q

oxycodone and hydrocodone

A

direct analgesic properties

also partially metabolized to oxymorphone and hydromorphone (not CYP2D6 dependent)

68
Q

pentazocine

A

kappa receptor agonist acts at spinal and supra-spinal sites

and partial MOR ANTAGONIST

69
Q

buprenorphine

A

mixed partial MOR agonist

and kappa receptor ANTAGONIST

70
Q

dextromethorphan

A

active at DM receptor (antitussive, not analgesic)

71
Q

naloxone and naltrexone

A

competitive MOR ANTAGONIST

72
Q

tramadol

A

weak MOR agonist

inhibition of NE and 5-HT reuptake

73
Q

loperamide

A

acts on MOR in myenteric plexus of large intestine

74
Q

atropine

A

muscarinic ANTAGONIST.

crosses BBB

75
Q

nicotine and varenicline

A

direct nicotinic agonist

76
Q

ipratropium

A

muscarinic ANTAGONIST in lungs

does not cross BBB

77
Q

neostigmine

A

reversible anticholinesterase

does NOT cross BBB

78
Q

physostigmine

A

reversible anticholinesterase

crosses BBB

79
Q

donepezil

A

crosses BBB to increase acetylcholine at CNS synapses

to improve cognition and memory

80
Q

sarin

A

IRREVERSIBLE anticholinesterase

81
Q

vecuronium

A

NONDEPOLARIZING competitive nicotinic ANTAGONIST at skeletal muscle

82
Q

trimethaphan

A

ANTAGONIST at ganglion

block sympathetic/parasympathetic so that you (the ED PA) can control BP

83
Q

succinylcholine

A

depolarizing skeletal muscle nicotinic ANTAGONIST w/ VERY fast onset

84
Q

botulinum toxin in wrinkle tx

A

blocks acetylcholine release at cholinergic terminals = no muscle contraction

Pharmacology (6 decks)

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