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#Pharmacotherapeudics > CNS Neurotransmission > Flashcards

CNS Neurotransmission Flashcards

1
Q

GABA is

A

inhib

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2
Q

glutamate is

A

excitatory

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3
Q

glutamate is turned in to ______ by _____

A

GABA

GAD

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4
Q

_____ and ______ inhib GAD

A

allyglycine and isonazid

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5
Q

_____ is the transporter that packages GABA into vessicles

A

VGAT

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6
Q

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

A

tetanus toxin (lock jaw)

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7
Q

____ transporters reuptake GABA, this is inhib by ____

A

GATs

tiagabine

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8
Q

_____ turns GABA into glutamate; inhib by ____

A

GABA-T

Vigabatrin

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9
Q

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

A

A & C

intrinsic choloride ion channels

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10
Q

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

A

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

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11
Q

Inotropic GABAa receptors are _____ actinq

A

fast

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12
Q

prolonged occupation by GABA will lead to ____

A

desensitization

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13
Q

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

A 
DHEA
Oleamide
DHDOC
Pregnenolone
THDOC
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14
Q

______ and _____ bind GABAa

A

muscimol and gaboxadol

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15
Q

_______ and _____ (drug classes) are modulators of GABAa

A

Benzos

and Berbiturates

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16
Q

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

A

chlorozepate
chlordiazepoxide
zolpidem

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17
Q

______ do not activate in the absence of GABA

A

benzos

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18
Q

benzos are highly ____ bound; and have a _____ absorption

A

protein

rapid and complete (b/c highly hydrophobic)

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19
Q

Benzos are metabolized by CYP___

A

3A4

20
Q

______ is the benzo antagonist/antidote

A

Flumazenil

21
Q

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

A

butalbital
methohexital
primidone
thipoental

22
Q

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

A

thiopental, pentobarbital, and methohexital

GABAa as an agonist (fast receptor)

23
Q

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

A

phenobarbital

24
Q

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

A

adipose tissue (highly hydrophillic bc enters CNS)

25
Q

barbs have an extensive _______ metabolism which can lead to tolerance

A

P450/liver

26
Q

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

A

propofol

etomidate

27
Q

Metabotropic/GABA_ receptors are found mostly _____

A

B

spinal cord

28
Q

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

A

K+

leads to inhibition of opening of Ca2+ channels

29
Q

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

A

Baclofen

30
Q

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

A

Intrathecal (for chronic dz(MS))

NOT w/oral

31
Q

name the 5 sx of Baclofen withdrawl

A 
hypersensitivty
rhabdomyolysis
puritis
delerium
fever
32
Q

ethanol targets _____ and ______

A

GABAa and glutamate

33
Q

chloral hydrate is

A

an older sedative/hypnotic

34
Q

Gamma Hydroxybutyric acid (GHB) is

A

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

35
Q

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

A

AMPA, Kainate, and NMDA

FAST EXCITATORY

36
Q

how do AMPA and Kainate work?

A

throughout CNS, activation=NA in and K out

37
Q

hwo does NMDA work

A

in hippocampus, cerebral cortex and spinal cord

K out, and NA and Ca in

38
Q

there are no drugs that target the the metabotropic _______ receptor

A

glutamate

39
Q

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

A

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

40
Q

name the 3 NMDA antagonists

A

memantine, amantadine, and riluzole

41
Q

Riluzole blocks _____ channels and is indicated for _____ dzs

A

Na

neurodegen

42
Q

memantine and amantadine are noncompet blockers on _____ receptor

A

NMDA

43
Q

memantine is for ____

and amantadine is for _____

A

alzheimers

parkinsons (dec dyskinesia)

44
Q

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

A

inactivated form of Na
reduces glutamate
indicated for seizures

45
Q

Felbamate inhibits ______ receptors and is indicated for ______

A

inhib NMDA

seizures

#Pharmacotherapeudics (15 decks)

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