CNS Drug Mechanisms of Action

Question 1

Ethosuximide

Answer 1

blocks thalamic T-type Ca2+ channels

Question 2

Benzodiazepines

Answer 2

Facilitate GABA(A) action by increased frequency of Cl- channel opening

Question 3

Barbiturates

Answer 3

Facilitate GABA(a) action by increasing duration of Cl- channel opening, thus decreasing neuronal firing

Question 4

Non-benzodiazepine hypnotics

Answer 4

Act via BZ1 subtype of the GABA receptor- reversed by flumazenil

Question 5

Suvorexant

Answer 5

Orexin (hypocretin) receptor antagonist

Question 6

Ramelteon

Answer 6

Melatonin receptor agonist, binds MT1 and MT2 in suprachiasmatic nucleus

Question 7

Triptans

Answer 7

5-HT(1B/1D) agonists; inhibit trigeminal nerve activation; prevent vasoactive peptide release; induce vasoconstriction

Question 8

Bromocriptine

Answer 8

Dopamine agonist

Question 9

Amantadine

Answer 9

Increases DA release and decreases DA reuptake

Question 10

Carbidopa

Answer 10

Blocks peripheral conversion of L-DOPA to DA by inhibiting DOPA decarboxylase

Question 11

Entacapone

Answer 11

COMT inhibitor

Question 12

Tolcapone

Answer 12

COMT inhibitor

Question 13

Selegiline

Answer 13

MAO-B inhibitor

Question 14

Benztropine

Answer 14

Antimuscarinic adjunct to improve tremor and rigidity

Question 15

Trihexyphenidyl

Answer 15

Antimuscarinic adjunct to improve tremor and rigidity

Question 16

Rasagiline

Answer 16

MAO-B inhibitor

Question 17

Tetrabenazine

Answer 17

Inhibit vesicular monoamine transporter (VMAT)–> decreases DA vesicular packaging and release

Question 18

Reserpine

Answer 18

Inhibit vesicular monoamine transporter (VMAT)–> decreases DA vesicular packaging and release

Question 19

Riluzole

Answer 19

Decreases glutamate excitotoxicity; ALS treatment

Question 20

Memantine

Answer 20

NMDA receptor antagonist

Question 21

Tacrine

Answer 21

AChE inhibitor

Question 22

Baclofen

Answer 22

Activates GABA(A) receptors at level of spinal cord, inducing skeletal muscle relaxation

Question 23

Cyclobenzaprine

Answer 23

Centrally acting skeletal muscle relaxant

Question 24

Pentazocine

Answer 24

Kappa-opioid receptor agonist and mu-opioid receptor weak/ partial agonist; analgesia

Question 25

Butorphanol

Answer 25

Kappa-opioid receptor agonist and mu-opioid receptor partial agonist; analgesic

Question 26

Tramadol

Answer 26

Very weak opiod agonist; also inhibits 5-HT and NE reuptake

Question 27

Methylphenidate/ Dextroamphetamine/ methamphetamine

Answer 27

Increases catecholamines in the synaptic cleft (esp NE and DA)

Question 28

Typical antipsychotics

Answer 28

Block D2 receptors (increase cAMP)

Question 29

Buspirone

Answer 29

Stimulates 5-HT1A receptors

Question 30

TCAs

Answer 30

Inhibit NE and 5-HT reuptake

Question 31

Bupropion

Answer 31

Inhibits reuptake of NE and DA

Question 32

Mirtazapine

Answer 32

Alpha 2 antagonist (increases NE and 5-HT release), 5-HT 2&3 antagonist; H1 antagonist

Question 33

Trazodone

Answer 33

Primarily blocks 5-HT2, alpha 1, and H1 receptors; weakly inhibits 5-HT reuptake

Question 34

Varenicline

Answer 34

Nicotinic ACh receptor partial agonist

Question 35

Vilazodone

Answer 35

Inhibits 5-HT reuptake; 5-HT1A receptor partial agonist

Question 36

Vortioxetine

Answer 36

Inhibits 5-HT reuptake; 5-HT1A receptor agonist and 5-HT3 receptor antagonist