Exam 2: Step 2 Mechanism of Action Flashcards
fluoxetine
blocks SERT to increase serotonin
alteplase
binds fibrin in a fresh clot, then activates plasminogen to dissolve the clot
lamotrigine
inactivate Na channel
inhibit Ca channel
duloxetine
blocks SERT and NET
rasagiline
inhibits degradation of dopamine by MAO-B
valproic acid
inactivate Na channel
inhibit T-type Ca channel
inhibits breakdown of GABA
carbamazepine
inactivate Na channel
potentiate GABA response
ergotamine (PO) and dihydroergotamine (IV, IM, nasal, PR)
cerebral vasoconstriction
5-HT agonist in trigeminal nerve
phenytoin
inactivate Na channel
sumatriptan
selective agonist at 5-HT1B,D,F receptors
B - blood vessels - constrict
D - peripheral neurons - inhibit CGRP release
F - central neurons - inhibit neurotransmission
sertraline
blocks SERT
selegeline and rasagiline
inhibit DA degradation by MAO-B (which is mostly in the striatum)
ramelteon
melatonin receptor agonist
zonisamide
inactivate Na channel
inhibit T-type Ca channel
celecoxib
COX-2 inhibitor
benztropine
muscarinic antagonist on GABA-ergic neuron (for Parkinsonism tremor)
misoprostol
inhibits gastric acid secretion
carbidopa
inhibits peripheral L-AAD (decarboxylase enzyme) from converting of L-DOPA to DA
tolcapine
inhibits peripheral AND central COMT (methyltransferase enzyme) from converting L-DOPA to 3-O-MD
entecapone
inhibits peripheral COMT (methyltransferase enzyme) from converting L-DOPA to 3-O-MD
aspirin
IRREVERSIBLE COX-1 and COX-2 inhibitor
levetiracetam
interfere w/ glutamate vesicle fusion (SV2A ligand) in presynaptic terminal
ethosuximide
inhibit T-type Ca channel in thalamic neuron
T-type Ca channels involved in absence seizures
primidone
inactivate Na channel
ibuprofen
reversible COX1 and COX2 inhibitor
phenytoin
inactivate Na channels
naproxen
reversible COX1 and COX2 inhibitor
acetaminophen
COX-2 and COX-3 inhibitor
vigabatrin
inhibits GABA transaminase (to increase GABA)
metabolite is phenobarbital (but ? importance)
phenobarbital
binds to site on GABA-A receptor, enhancing duration of chloride influx
at high doses, can DIRECTLY open channel
benzodiazepines
bind to site on GABA-A receptor to enhance chloride influx
Needs GABA to function, cannot directly open channel
clozapine
olanzapine
risperidone
5HT2 block»_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
flumazenil
competitive ANTAGONIST at BZ site on GABA-A receptor
reverses effects of BZs and BZ agonists
metaclopramide
increases gastric emptying
antagonist at 5-HT3 and D2 receptors
propranolol in migraine tx
unclear
???overall reduction in adrenergic tone
buspirone
direct partial agonist at CNS 5-HT1a receptor
L-DOPA
precursor for DA synthesis
ropinirole and pramipexole
directly stimulate CNS D2 receptors
zolpidem and eszoplicone
binds to alpha-1 subunit of GABA-A receptor, which is selective for sedation
amandatine
enhance DA release
inhibit DA reuptake
haloperidol
D2 block»_space; 5HT2 block
D2 antagonist +++
5-HT2 block ++
topiramate
inactivate Na channel
inhibit AMPA receptor
increase GABA activity
onabotulinum toxin in migraine tx
cleaves snares to prevent release of CGRP from peripheral trigeminal nerve terminal
(calcitonin gene related peptide)
aripiprazole
unlike other atypicals
PARTIAL AGONIST at D2 receptor = decreases DA activity in accumbens while increasing DA in the cortex
also 5HT2 block +++
gabapentin
inhibit Ca channel
chlorpromazine
D2 antagonist +
5-HT2 block ++
alpha-1 block +++ (bad in elderly)
ACh block +
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)
fondaparinux
catalyzes antithrombin at factor 10a
dabigatrain
direct factor 2a inhibitors
heparin
catalyzes antithrombin at factor 10a and 2a
Rivaroxaban and apixaban
direct factor 10a inhibitors
enoxaparin
catalyzes antithrombin mostly at factor 10a but also at 2a
amitryptyline
block SERT and NET…(mostly SERT)…
```
but also… anti-
muscarinic/cholinergic
histaminergic
alpha-1 adrenergic
side effects!!!
~~~
G-CSF
stimulates progenitor cells committed to granulocyte lineage
mobilizes stem cells of all lineages into peripheral blood (enables harvesting for transplant)
warfarin
inhibits VKORC enzyme
which blocks Gla formation
which prevents factors 10, 9, 7, and 2 from binding to platelets
tranylcypromine
irreversibly inhibit monoamine oxidase, to prevent degradation of NE and serotonin
epoetin
stimulates erythroid proliferation and differentiation
clopidogrel and prasugrel
irreversibly block the ADP purine receptor (P2Y12) to prevent GP-IIb/IIIa activation and fibrinogen binding (platelet aggregation)
GM-CSF
M for myeloid
stimulates proliferation of granulocytic, erythroid and megakaryotic progenitor cells
ziprasidone
same as other atypicals (5HT2 block > D2 block)
5H2block ++++
D2 block +++
lithium
unclear and complex
decrease IP3 second messenger?
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)
fentanyl
same as morphine but faster acting
methadone
MOR agonist with long half life
also has non-opioid analgesic MOAs
meperidine
MOR agonist (same as morphine)
less potent, faster acting
codeine
PRODRUG converted to morphine by CYP2D6 (beware of “poor metabolizers”)
oxycodone and hydrocodone
direct analgesic properties
also partially metabolized to oxymorphone and hydromorphone (not CYP2D6 dependent)
pentazocine
kappa receptor agonist acts at spinal and supra-spinal sites
and partial MOR ANTAGONIST
buprenorphine
mixed partial MOR agonist
and kappa receptor ANTAGONIST
dextromethorphan
active at DM receptor (antitussive, not analgesic)
naloxone and naltrexone
competitive MOR ANTAGONIST
tramadol
weak MOR agonist
inhibition of NE and 5-HT reuptake
loperamide
acts on MOR in myenteric plexus of large intestine
atropine
muscarinic ANTAGONIST.
crosses BBB
nicotine and varenicline
direct nicotinic agonist
ipratropium
muscarinic ANTAGONIST in lungs
does not cross BBB
neostigmine
reversible anticholinesterase
does NOT cross BBB
physostigmine
reversible anticholinesterase
crosses BBB
donepezil
crosses BBB to increase acetylcholine at CNS synapses
to improve cognition and memory
sarin
IRREVERSIBLE anticholinesterase
vecuronium
NONDEPOLARIZING competitive nicotinic ANTAGONIST at skeletal muscle
trimethaphan
ANTAGONIST at ganglion
block sympathetic/parasympathetic so that you (the ED PA) can control BP
succinylcholine
depolarizing skeletal muscle nicotinic ANTAGONIST w/ VERY fast onset
botulinum toxin in wrinkle tx
blocks acetylcholine release at cholinergic terminals = no muscle contraction