Anxiolytics lecture MOAs

Question 1

Benzo: GABA-A modulator
5 drugs

Answer 1

alprazolam
clonazepam
diazepam
lorazepam
temazepam

Question 2

buspirone

Answer 2

5-HT1A partial agonist

Question 3

clobazam

Answer 3

less sedating benzo;
AED

Question 4

GABA-A modulator: sleep aid

Answer 4

eszopiclone
zolpidem

Question 5

AEDs - inhibits voltage-gated NA+ channels in order to decrease glutamate
(7 drugs)

Answer 5

carbamazepine & oxcarbazepine
lacosamide (Vimpat)
lamotrigine (Lamictal)
phenytoin (Dilantin)
topiramate
valproate

Question 5

phenobarbital

Answer 5

barbiturate - GABA-A modulator

Question 6

benzos MOA

Answer 6

Positive allosteric modulator (enhances action) of GABA (a major inhibitory neurotransmitter) at GABA-A receptor which is a chloride/Cl- channel)

Question 7

z-compounds MOA

Answer 7

Allosteric modulators of benzodiazepine site on GABA-A receptor (different receptor subtype than benzo site)

Question 8

z-compound drugs

Answer 8

• Zolpidem (Ambien) – t1/2 (2 h)
• EsZopiclone (Lunesta)- t1/2 (6 h)
• Zaleplon (Sonata) – t1/2 (1 h)

Question 8

flumazenil (Romazicon) - MOA

Answer 8

Benzodiazepine receptor antagonist on GABA-A receptor

Question 9

blockade of N-type or Q-type Voltage-Gated Ca2+ channels (decrease Glutamate release)
(3 drugs)

Answer 9

lamotrigine
pregabalin
gabapentin

Question 10

Decrease Synaptic Vesicular Release of glutamate

Answer 10

levetiracetam

Question 11

blockade of glutamate receptors postsynaptic

Answer 11

Felbamate (NMDA)
Topiramate (AMPA)

Question 12

increases GABA release & inhibits voltage gated Ca2+ channels to decrease glutamate release

Answer 12

gabapentin
pregabalin

Question 13

GABA-transaminase inhibitor
(GABA-T is what degrades GABA)
& inhibits voltage NA+ channels

Answer 13

valproate / divalproex

Question 13

Increased Responsiveness to GABA at GABA-A Receptors

Answer 13

BZDs &
Barbiturates

Question 14

phenytoin MOA

Answer 14

inhibits voltage-gated Na+ channels of excitatory neurons

Question 15

Phenobarbital (Luminal) - MOA

Answer 15

Barbiturate class;
Potentiates GABA effect

Question 16

MOA - Carbamazepine (Tegretol)/Oxcarbazepine (Trileptal)

Answer 16

inhibits voltage-gated Na+ channels of excitatory neurons

Question 17

MOA -
Valproate (Depacon)/Divalproex (Depakote)

Answer 17

multiple including
- inhibition of GABA breakdown
-inhibition of voltage-dependent Na+ channels.

Question 18

MOA- Topiramate (Topamax)

Answer 18

multiple including
- inhibition of voltage-gated Na+ channels in excitatory neurons
- inhibition of Glutamate AMPA receptors

Question 19

MOA-
Gabapentin (Neurontin) and Pregabalin (Lyrica)

Answer 19

inhibits voltage-gated Ca2+ channel, leads to decrease Ca2+ influx and decreases excitatory neurotransmitter release; may increase GABA levels by unknown mechanism

Question 20

potent inducers of hepatic CYP450 enzymes and glucuronosyltransferases (UGTs),

Answer 20

• Phenytoin
• Phenobarbital
• Carbamazepine

Question 21

CYP inhibitor

Answer 21

valproate

Question 22

MOA - benztropine

Answer 22

centrally active muscarinic antagonist

Question 23

MOA - carbidopa/levodopa

Answer 23

-dopamine precursor -Combination product to decrease peripheral conversion to dopamine

Question 24

MOA- donepezil

Answer 24

reversible AchE-inhibitor

Question 25

MOA - memantine

Answer 25

glutamate NMDA antagonist

Question 26

dopamine receptor agonist (PD: restless leg syndrome)

Answer 26

pramipexole ropinirole

Question 27

MAOB inhibitor (decreases metabolism of DA)

Answer 27

selegiline rasagiline

Question 28

MOA - benztropine & trihexyphenidyl

Answer 28

central acting antimuscarinic

Question 29

AChE-I's for Alzheimer's disease (3 drugs)

Answer 29

galantamine (Razadyne) donepezil (Atricept) rivastigmine (Exelon)

Question 30

NMDA type glutamate receptor antagonist

Answer 30

memantine (Namenda)