Mechanism of action of medications Flashcards

1
Q

mirtazapine

give specific receptors

A

NaSSantidepressant
noradernaline and serotonin specific antidepressant

HT2 antagonist
HT3 antagonist
H1 antagonist
alpha 1 and alpha 2 antagonist
moderate muscarinic antagonist

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2
Q

venlafaxine, duloxetine

A

SNRI

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3
Q

reboxetine

A

NaRI

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4
Q

st john’s wort

A

weak MAOI and weak SNRI

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5
Q

trazadone

give group and receptors

A

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

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6
Q

meclobemide

A

reversible MAOA inhibitor

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7
Q

aglomelatine

A

melatonergic agonist (MT1 and MT2)
5HT2C antagonist

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8
Q

buproprion

A

NDRI (noradrenaline dopamine reuptake inhibitor)
nACh antagonist

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9
Q

donepezil

A

reversible acetylcholinesterase inhibitor

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10
Q

tacrine

A

reversible anticholinesterase inhibitor

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11
Q

rivastigmine

A

reversible acetylcholinesterase inhibitor
butyrylcholinesterase inhibitor

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12
Q

galantamine

A

selective, competitive and reversible acetylcholinesterase inhibitor

also enhances intrinsic action of ACh on nACh receptors through allosteric action

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13
Q

memantine

A

non-competitive NMDA antagonist

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14
Q

valproate

A

GABA modulation
sodium channel inhibition
NMDA antagonist

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15
Q

gabapentin, pregabalin

A

binds to alpha2delta subunit of voltage gated Ca channels -> reduced glutamate and substance P release -> reduced neuronal excitability

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16
Q

topiramate

3 things

A

GABA modulator
NMDA antagonist
Na channel stabiliser

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17
Q

carbamazepine

A

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

18
Q

phenytoin

A

stabilises Na channels

19
Q

lamotrigine

4 things

A

NMDA receptor modulation
stabilises Na channels
blocks Ca channels
some GABA modulation

20
Q

lofexidine

A

alpha 2 agonist

(used in management of opioid withdrawal)

21
Q

buprenorphine

A

partial agonist at mu-opioid receptor

22
Q

naloxone

A

pure opioid antagonist
will reverse mu, delta and kappa

23
Q

naltrexone

A

long acting opioid antagonist (all 3 but particularly mu)

(long acting when compared to naloxone)

24
Q

atomoxetine

A

noradrenaline reuptake inhibitor

25
Q

varenicline

partial or full?

A

nicotine receptor partial agonist

26
Q

disulfiram

reversible or irreversible?

A

irreversible aldehyde dehydrogenase inhibitor

NB alcohol [alcohol dehydrogenase] -> aldedehyde [aldehyde dehydrogenase] -> acetate

aldehyde is what makes you feel terrible

27
Q

acamprosate

A

NMDA glutamate receptor antagonist
positive allosteric modulator of GABAa receptor

(positive allosteric modulators increase agonist affinity and/or efficacy)

28
Q

selegiline

A

selective, irreversible MAOB inhibitor

also MAOA at higher doses

29
Q

sildenafil

A

PDE5 (cGMP-specific phosphodiesterase type 5) inhibitor

30
Q

gaba A agonists

A

ethanol
benzos
z drugs
barbiturates e.g. phenobarbital

31
Q

gaba B agonists

A

baclofen
GHB

32
Q

gaba a antagonists

A

flumazanil

33
Q

dexamphetamine / lisdexamphetamine / methylphenidate

A

DNRI / NDRI
dopamine and noradrenaline reuptake inhibitor

34
Q

guanfacine

A

Selective agonist of α2A-adrenergic receptors. Binds to postsynaptic α2A-adrenergic receptors, mimicking NA

35
Q

clonidine

A

Agonist of α2-adrenergic receptors, mimic NA

36
Q

amisulpride

A

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)

37
Q

olanzapine

A

dopamine and 5HT2 antagonism

38
Q

aripiprazole

A

partial agonist at 5HT1 and D2
5HT2A antagonist

39
Q

clozapine

A

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

40
Q

lurasidone

A

ANTAGONIST @: D2 5HT2A 5HT7 alpha2A and alpha2c adrenoreceptors

(does not bind to histaminergic or muscarinic receptors)

41
Q

tetrabenzine

A

inhibition of vesicular monoamine transporter 2