CNS Neurotransmission

Question 1

GABA is

Answer 1

inhib

Question 2

glutamate is

Answer 2

excitatory

Question 3

glutamate is turned in to ______ by _____

Answer 3

GABA

GAD

Question 4

_____ and ______ inhib GAD

Answer 4

allyglycine and isonazid

Question 5

_____ is the transporter that packages GABA into vessicles

Answer 5

VGAT

Question 6

GABA release (in response to Ca2+ influx) is inhib by

Answer 6

tetanus toxin (lock jaw)

Question 7

____ transporters reuptake GABA, this is inhib by ____

Answer 7

GATs

tiagabine

Question 8

_____ turns GABA into glutamate; inhib by ____

Answer 8

GABA-T

Vigabatrin

Question 9

Ionitropic recptors are GABA_ and GABA_; these work by opening ______

Answer 9

A & C

intrinsic choloride ion channels

Question 10

Metabotropic receptors are GABA_, these work by _______, which means they ______

Answer 10

B
G-protein coupled receptors(2nd messenger)\
these have LONGER activity (DOA)

Question 11

Inotropic GABAa receptors are _____ actinq

Answer 11

fast

Question 12

prolonged occupation by GABA will lead to ____

Answer 12

desensitization

Question 13

GABAa modulators bind to allosteric sites and causes inc receptor activation… name the 5

Answer 13

DHEA
Oleamide
DHDOC
Pregnenolone
THDOC

Question 14

______ and _____ bind GABAa

Answer 14

muscimol and gaboxadol

Question 15

_______ and _____ (drug classes) are modulators of GABAa

Answer 15

Benzos

and Berbiturates

Question 16

name the three benzos that don’t end in zepam or zolam

Answer 16

chlorozepate
chlordiazepoxide
zolpidem

Question 17

______ do not activate in the absence of GABA

Answer 17

benzos

Question 18

benzos are highly ____ bound; and have a _____ absorption

Answer 18

protein

rapid and complete (b/c highly hydrophobic)

Question 19

Benzos are metabolized by CYP___

Answer 19

3A4

Question 20

______ is the benzo antagonist/antidote

Answer 20

Flumazenil

Question 21

what are the 4 barbiturates that don’t have “barb” in their name

Answer 21

butalbital
methohexital
primidone
thipoental

Question 22

anesthetic barbiturates include _____, ____, and ______; these act on GABA_ as a _______

Answer 22

thiopental, pentobarbital, and methohexital

GABAa as an agonist (fast receptor)

Question 23

_________ is an anticonvulsant barbiturate, its has less direct agonism and leads to less sedation, amnesia, and LOC than other Barbs

Answer 23

phenobarbital

Question 24

chronic use of barbs can lead to high uptake in ______, leading to inc Vd and long elimination of 1/2 life

Answer 24

adipose tissue (highly hydrophillic bc enters CNS)

Question 25

barbs have an extensive _______ metabolism which can lead to tolerance

Answer 25

P450/liver

Question 26

______ and ______ enhance activation of GABAa by GABA and at high doses act as agonists

Answer 26

propofol | etomidate

Question 27

Metabotropic/GABA_ receptors are found mostly _____

Answer 27

B | spinal cord

Question 28

GABAb receptors work by G proteins which activate ___ channels leading to ____ of voltage gated Ca2+ channels

Answer 28

K+ | leads to inhibition of opening of Ca2+ channels

Question 29

_____ is a GABAb agonist that is used 1rily for muscle strains/spasticity dos.

Answer 29

Baclofen

Question 30

w/ Baclofen tolerance develops with ______ route, but not typically by ______ route

Answer 30

Intrathecal (for chronic dz(MS)) | NOT w/oral

Question 31

name the 5 sx of Baclofen withdrawl

Answer 31

``` hypersensitivty rhabdomyolysis puritis delerium fever ```

Question 32

ethanol targets _____ and ______

Answer 32

GABAa and glutamate

Question 33

chloral hydrate is

Answer 33

an older sedative/hypnotic

Question 34

Gamma Hydroxybutyric acid (GHB) is

Answer 34

a gaba isomer used to induce narcolepsy (date rape drug)

Question 35

name the 3 inotropic glutamate receptors; what is the response?

Answer 35

AMPA, Kainate, and NMDA | FAST EXCITATORY

Question 36

how do AMPA and Kainate work?

Answer 36

throughout CNS, activation=NA in and K out

Question 37

hwo does NMDA work

Answer 37

in hippocampus, cerebral cortex and spinal cord | K out, and NA and Ca in

Question 38

there are no drugs that target the the metabotropic _______ receptor

Answer 38

glutamate

Question 39

Excitotoxicity is caused by _______ or _______ and is implicated in 5 dzs/disorders/processes

Answer 39

(inc Ca2+ intracellularly); inc release or dec reuptake of glutamate neurodegen dz, epilepsy, stroke, trauma, hyperalgesia

Question 40

name the 3 NMDA antagonists

Answer 40

memantine, amantadine, and riluzole

Question 41

Riluzole blocks _____ channels and is indicated for _____ dzs

Answer 41

Na | neurodegen

Question 42

memantine and amantadine are noncompet blockers on _____ receptor

Answer 42

NMDA

Question 43

memantine is for ____ | and amantadine is for _____

Answer 43

alzheimers | parkinsons (dec dyskinesia)

Question 44

lamotrigine stabilizes _______of _____ channels reducing _______..... it's indicated for ______

Answer 44

inactivated form of Na reduces glutamate indicated for seizures

Question 45

Felbamate inhibits ______ receptors and is indicated for ______

Answer 45

inhib NMDA | seizures