Mechanism of action of medications

Question 1

mirtazapine

give specific receptors

Answer 1

NaSSantidepressant
noradernaline and serotonin specific antidepressant

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

Question 2

venlafaxine, duloxetine

Answer 2

SNRI

Question 3

reboxetine

Answer 3

NaRI

Question 4

st john’s wort

Answer 4

weak MAOI and weak SNRI

Question 5

trazadone

give group and receptors

Answer 5

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

Question 6

meclobemide

Answer 6

reversible MAOA inhibitor

Question 7

aglomelatine

Answer 7

melatonergic agonist (MT1 and MT2)
5HT2C antagonist

Question 8

buproprion

Answer 8

NDRI (noradrenaline dopamine reuptake inhibitor)
nACh antagonist

Question 9

donepezil

Answer 9

reversible acetylcholinesterase inhibitor

Question 10

tacrine

Answer 10

reversible anticholinesterase inhibitor

Question 11

rivastigmine

Answer 11

reversible acetylcholinesterase inhibitor
butyrylcholinesterase inhibitor

Question 12

galantamine

Answer 12

selective, competitive and reversible acetylcholinesterase inhibitor

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

Question 13

memantine

Answer 13

non-competitive NMDA antagonist

Question 14

valproate

Answer 14

GABA modulation
sodium channel inhibition
NMDA antagonist

Question 15

gabapentin, pregabalin

Answer 15

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

Question 16

topiramate

3 things

Answer 16

GABA modulator
NMDA antagonist
Na channel stabiliser

Question 17

carbamazepine

Answer 17

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

Question 18

phenytoin

Answer 18

stabilises Na channels

Question 19

lamotrigine

4 things

Answer 19

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

Question 20

lofexidine

Answer 20

alpha 2 agonist

(used in management of opioid withdrawal)

Question 21

buprenorphine

Answer 21

partial agonist at mu-opioid receptor

Question 22

naloxone

Answer 22

pure opioid antagonist
will reverse mu, delta and kappa

Question 23

naltrexone

Answer 23

long acting opioid antagonist (all 3 but particularly mu)

(long acting when compared to naloxone)

Question 24

atomoxetine

Answer 24

noradrenaline reuptake inhibitor

Question 25

varenicline | partial or full?

Answer 25

nicotine receptor partial agonist

Question 26

disulfiram | reversible or irreversible?

Answer 26

irreversible aldehyde dehydrogenase inhibitor NB alcohol [alcohol dehydrogenase] -> aldedehyde [aldehyde dehydrogenase] -> acetate aldehyde is what makes you feel terrible

Question 27

acamprosate

Answer 27

NMDA glutamate receptor antagonist positive allosteric modulator of GABAa receptor (positive allosteric modulators increase agonist affinity and/or efficacy)

Question 28

selegiline

Answer 28

selective, irreversible MAOB inhibitor also MAOA at higher doses

Question 29

sildenafil

Answer 29

PDE5 (cGMP-specific phosphodiesterase type 5) inhibitor

Question 30

gaba A agonists

Answer 30

ethanol benzos z drugs barbiturates e.g. phenobarbital

Question 31

gaba B agonists

Answer 31

baclofen GHB

Question 32

gaba a antagonists

Answer 32

flumazanil

Question 33

dexamphetamine / lisdexamphetamine / methylphenidate

Answer 33

DNRI / NDRI dopamine and noradrenaline reuptake inhibitor

Question 34

guanfacine

Answer 34

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

Question 35

clonidine

Answer 35

Agonist of α2-adrenergic receptors, mimic NA

Question 36

amisulpride

Answer 36

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)

Question 37

olanzapine

Answer 37

dopamine and 5HT2 antagonism

Question 38

aripiprazole

Answer 38

partial agonist at 5HT1 and D2 5HT2A antagonist

Question 39

clozapine

Answer 39

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

Question 40

lurasidone

Answer 40

ANTAGONIST @: D2 5HT2A 5HT7 alpha2A and alpha2c adrenoreceptors (does not bind to histaminergic or muscarinic receptors)

Question 41

tetrabenzine

Answer 41

inhibition of vesicular monoamine transporter 2