Pharm NT I Flashcards

1
Q

what are the classes of NT

A

amino acids
small molecule
peptides
endocannabinoids

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2
Q

what are the excitatory aa NT

A

glutamate and aspartate

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3
Q

what are the inhibitory aa NT

A

GABA and Glycine

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4
Q

What are the small molecule transmitters

A

Ach
Monoamines
histamine

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5
Q

what are the monoamines

A
catecholamines: dopamine and norepi
and serotonin (5-HT)
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6
Q

what are the peptide NT

A

opiods
tachykinins
others

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7
Q

what are the opioid NT

A

enkephalins
endorphins
dynorphins

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8
Q

what are the tachykinins

A

substance P

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9
Q

Where are small moleules NT made

A

in the nerve terminals then loaded into vesicles ATP dependent

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10
Q

where are peptides made

A

cell body and packaged there

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11
Q

depolarization to the presynaptic nerve acticates what

A

vCaCh causing fusion vesicles and release

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12
Q

drugs that act in CNS modify what

A

the chemical synaptic transmission

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13
Q

presynaptic sites of drug action include what

A

NT synthesis, storage, metabolism and release

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14
Q

what is the primary postsynaptic site of drug action

A

NT receptor

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15
Q

what are the 3 criteria for classical NT

A

localization
release
synaptic mimicry

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16
Q

what is an exception to the synaptic mimicry rule

A

sometime more than one substance transmits information so no single agonist or antagonis can mimic stimulation

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17
Q

what messengers are not synthesized or stored in presynatpic terminal

A

endocannabinoids

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18
Q

what ion channels modulate neuronal firing rate

A

Ca and K

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19
Q

What are ionotropic R

A

ligand gated ion channels

causes conformational change that opens channel or closes it

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20
Q

what causes EPSP

A

influx Na or Ca

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21
Q

what causes IPSP

A

efflux of K or influx Cl

22
Q

what NT activate ionotropic R

A
glutamate
GABA
Ach
Glycine
Serotonin
23
Q

how to metabotropic R work

A

GPCR that indirectly modulate ion channels

24
Q

major functional effects GPCRs

A

signal amplification

25
Q

What are the second messengers in GPCRs

A

adenylate cyclase and cAMP
DAG
IP3
ion Ca K Na or Cl

26
Q

what NT activate metabotropic R

A
glutamate
GABA
Ach
dopamine
Norepi
Serotonin
Histamine
Neuropeptides
Endocannabinoids
27
Q

does glutamate cross bbb

A

no

but it is made in brain from glucose

28
Q

what inactivates glutamate

A

taken up by glial cells and converted to glutamine then transported to glutamatergic nerve cells and converted back to glutamate

29
Q

What R does glutamate activate

A

ionotropic

non-NMDA and NMDA

30
Q

what R mediate most EPSP in prain

A

the AMPA or non NMDA
GluR1 2,3,4
ligand gated Na K Ch
glutamate!!!

31
Q

overstimulation NMDA R in brain cause what

A

Ca influx triggering cell death

especially in ischemia and hypoxia

32
Q

what ion blocks NMDA channels until depolarized

A

Mg

33
Q

what is PCP

A

phencyclidine “angel dust” ketamine

34
Q

how does PCP work

A

noncompetetice antagonist at NMDA R

high does cause dissociative anesthesia

35
Q

R subtypes for the NMDA R

A

NR1, 2A,2B,2C,2D

36
Q

what metabotropic R does glutamate activate on postsynapse

A

decrease K conductance increasing IP3 and DAG

37
Q

effects of glutamate on presynaptic GPCR

A

dec Ca (inhibitiory) dec cAMP

38
Q

what can cause the aura of migraine headaches

A

excessive glutamate release

39
Q

why is NMDA R antagonist memantine used to Tx severe dementia in alzheimers

A

glutamade R mediated excitotoxicity may contribute to pathogenesis of the disease

40
Q

synthesis of GABA

A

locally from glucose, pyruvate, sometimes other aa

41
Q

inactivation GABA

A

rapid reuptake from plasma membrane transporters

also taken up by glial cells

42
Q

GABAa activates what R

A

ionotropic

ligand Cl Ch (hyperpolarization IPSP)

43
Q

GABAb

A

metabotropic
post synaptic (inc K)
presynaptic (dec Ca inhibitory)

44
Q

what balances excitatory activity of glutamate

A

GABA inhibition

45
Q

GABA dysfunction leads to

A

hyperexcited states

46
Q

where do benzodiazepines and barbituates work

A

GABAa

so enhance inhibitory effects of GABA

47
Q

what are the benzodiazepines

A

alpazolam
diazepam
midazolam
clonazepam

48
Q

benzodiazepines are used to Tx

A

anxiety disorder, panic, sedation and sleep disorders

49
Q

what is phenobarbital

A

barbituate

50
Q

what is phenobarbital used for

A

sedative hypnotics and antiepileptics