Mechanism of action of medications Flashcards
mirtazapine
give specific receptors
NaSSantidepressant
noradernaline and serotonin specific antidepressant
HT2 antagonist
HT3 antagonist
H1 antagonist
alpha 1 and alpha 2 antagonist
moderate muscarinic antagonist
venlafaxine, duloxetine
SNRI
reboxetine
NaRI
st john’s wort
weak MAOI and weak SNRI
trazadone
give group and receptors
SARI
serotonin antagonist and reuptake inhibitor
blocks SERT
5HT1A antagonist
5HT2A antagonist
5HT2C antagonist
the 5HT2 antagonism causes insomnia, sexual dysfunction and anxiety side effects
meclobemide
reversible MAOA inhibitor
aglomelatine
melatonergic agonist (MT1 and MT2)
5HT2C antagonist
buproprion
NDRI (noradrenaline dopamine reuptake inhibitor)
nACh antagonist
donepezil
reversible acetylcholinesterase inhibitor
tacrine
reversible anticholinesterase inhibitor
rivastigmine
reversible acetylcholinesterase inhibitor
butyrylcholinesterase inhibitor
galantamine
selective, competitive and reversible acetylcholinesterase inhibitor
also enhances intrinsic action of ACh on nACh receptors through allosteric action
memantine
non-competitive NMDA antagonist
valproate
GABA modulation
sodium channel inhibition
NMDA antagonist
gabapentin, pregabalin
binds to alpha2delta subunit of voltage gated Ca channels -> reduced glutamate and substance P release -> reduced neuronal excitability
topiramate
3 things
GABA modulator
NMDA antagonist
Na channel stabiliser
carbamazepine
stabilises Na channels
Na moving into nerve cells through these channels excites the nerves cells and increases their firing (excitation). Because seizures are caused by nerve cells over-firing, slowing or blocking the sodium channel leads to fewer seizures
phenytoin
stabilises Na channels
lamotrigine
4 things
NMDA receptor modulation
stabilises Na channels
blocks Ca channels
some GABA modulation
lofexidine
alpha 2 agonist
(used in management of opioid withdrawal)
buprenorphine
partial agonist at mu-opioid receptor
naloxone
pure opioid antagonist
will reverse mu, delta and kappa
naltrexone
long acting opioid antagonist (all 3 but particularly mu)
(long acting when compared to naloxone)
atomoxetine
noradrenaline reuptake inhibitor
varenicline
partial or full?
nicotine receptor partial agonist
disulfiram
reversible or irreversible?
irreversible aldehyde dehydrogenase inhibitor
NB alcohol [alcohol dehydrogenase] -> aldedehyde [aldehyde dehydrogenase] -> acetate
aldehyde is what makes you feel terrible
acamprosate
NMDA glutamate receptor antagonist
positive allosteric modulator of GABAa receptor
(positive allosteric modulators increase agonist affinity and/or efficacy)
selegiline
selective, irreversible MAOB inhibitor
also MAOA at higher doses
sildenafil
PDE5 (cGMP-specific phosphodiesterase type 5) inhibitor
gaba A agonists
ethanol
benzos
z drugs
barbiturates e.g. phenobarbital
gaba B agonists
baclofen
GHB
gaba a antagonists
flumazanil
dexamphetamine / lisdexamphetamine / methylphenidate
DNRI / NDRI
dopamine and noradrenaline reuptake inhibitor
guanfacine
Selective agonist of α2A-adrenergic receptors. Binds to postsynaptic α2A-adrenergic receptors, mimicking NA
clonidine
Agonist of α2-adrenergic receptors, mimic NA
amisulpride
D2/D3 selective antagonist
low affinity selective antagonist of ‘D2 like’ receptors (D2=D3>D4)
little affinity for D1 like’ receptors (D1 and D5)
little affinity for non dopaminergic receptors (serotonin, histamine, adrenergic, and cholinergic)
olanzapine
dopamine and 5HT2 antagonism
aripiprazole
partial agonist at 5HT1 and D2
5HT2A antagonist
clozapine
dopamine and serotonin antagonist (5HT2A)
high affinity for D4 (lesser extent D1 D2 D3 D5) which may explain fewer EPSEs
5HT1A partial agonist (may explain reduciton of negative symptoms)
M1 M2 M3 M5 histamin and alpha 1 antagonist
norclozapine works on the M1 and M4 receptors
lurasidone
ANTAGONIST @: D2 5HT2A 5HT7 alpha2A and alpha2c adrenoreceptors
(does not bind to histaminergic or muscarinic receptors)
tetrabenzine
inhibition of vesicular monoamine transporter 2