Adrenergic and Cholinergic effects of drugs Flashcards

1
Q

excitatory neurotransmitters

A

glutamate

aspartate

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2
Q

inhibitory neurotransmitters

A

GABA
glycine
beta alanine
taurine

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3
Q

highest concentration of NE in the brain

but found throughout the brain

A

hypothalamus (locus ceruleus?)
central nucleus of amygdala
dentate gyrus of hippocampus

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4
Q

adrenergic receptora are all of which overall type

A

metabotropic

-GPCR’s

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5
Q

alpha one has which type of G protein subtype

A

Gq-calcium based signalling-stimulatory outcomes

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6
Q

alpha two has which type of G protein

A

Gi-cAMP based signalling-inhibitory outcomes

*inhibitory autoreceptors and post-synaptic modulators

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7
Q

Beta receptors use which type fo g protein

A

Gs-stimulatory-and use adenylate cylase-cAMP driven mechanisms

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8
Q

locus ceruleus involved in regulating what?

A

sleep and arousal

attention and vigilence

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9
Q

overactivity in locus ceruleus could potentially lead to,

A

anxiety, by releasing NE in the amygdala-emotion related to danger

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10
Q

stimulation of beta adrenergics by NE in the amygdala and other limbic areas can cause

A

PTSD-enhancement of memories for stimuli encoded under strong negative emotion-stimuli predicting danger

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11
Q

ACH receptors used in CNS

A

both Muscarnic and Nicotinic

*not necessarily where drugs re muscarinic ligands

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12
Q

mutlimeric ion channel leads to permissive Na+/Ca2+ entry and cellula depolarization

A

nicotinic ACHreceptor

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13
Q

M1, M3, M5 are all coupled to

A

Gq GPCR–> stimualtory

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14
Q

M2 and M4

A

Gi receptor-> inhibitory

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15
Q

nicotinic subtype found in autonomic ganglia

A

Nn

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16
Q

nicotinic subtype found at NMJ

A

Nm

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17
Q

ACH functions in the brain

A

motivation
learning
memory

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18
Q

NE regulate what in the brain

A

arousal
attention
vigilance
memory

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19
Q

descending NE fibers also modulate what

A

afferent pain signals

20
Q

drugs that are antagonists affecting either ACH or NE will have what side effects potentially

A

sedation and mental clouding-> both of these NT’s affect arousal and cognition

21
Q

another NT’s that maintains wakefulness acting centrally in the brain

A

histamine

22
Q

atypical antipsychotics all

A

do no possess uniform pharmacology or MOA

23
Q

main MOA’s for these centrally acting antipsychotics

A
antagonism at
dopa 1-5 receptors
serotonin 1q/2a
alpha 2>>1
muscarinic receptor antagonism 
histamine H1 antagonist
24
Q

dopa blockade side effects

A

parkinsonism, akathisia, dystonia

amenorrhea-galactorrhea, infertility, impotence

25
Q

combined serotinin and histamine blockade side effect

A

weight gain

26
Q

muscarinic cholioceptor blockade side effects

A

loss of accomodation
xerostomia
difficulty urinating
constipation

27
Q

alpha blockade side effects

A

orthostatic hypotension
impotence
ejaculation failure

28
Q

supersensitivity of dopa receptors side effects

A

tardive dyskinesia

29
Q

side effects from blockade of NE transporter

A

anxiety, increased BP via inc. pressor effects of sympathomimetics, sweating, direct tachycardia, tremor

30
Q

alpha one blockade side effects

A

postural hypotension, dizziness, dec BP by potentiating other antiHTN meds, reflex tachycardi

31
Q

effects of muscarinic blockade

A

memory and cognitive impairment, delirium, blurred vision, dec salivation, dry mouth, dec peristalsis, constipation, precipitation of narrow angle glaucoma, sinus tach (unopposed beta), urinary hesitancy and retention

32
Q

net activity of striated GABA neurons is determined by

A

relative balance of D1 and D2 receptors and excitatory muscarinic neurons

33
Q

in parkinsons–D2

A

d2 neurons degenerate-> leaving only the excitatory muscarinic neurons-tremor-muscarinic cholinergics unopposed to activate excitatory GABAergic neurons

34
Q

tx of perkinsons involves

A

L-DOPA: augment residual dopa pathways (would oppose exciattion by muscarinic stimulation)
Benztropine, Benadryl, Trihexyphenidyl-> inhibits muscarinic excitation

35
Q

drugs for parkinsons

A

L dopa

benztropine, diphenhydramine, trihexyphenidyl

36
Q

side effects of the three antimuscarinic agents used in early parkinsons

A

sedation, mental confusion, constipation, urinary retention, cycloplegia

37
Q

intrusion

A

re-experience of traumatic memories at night (nightmares) and during the day (fashbacks)

38
Q

intrusion responds to

A

beta blockade

39
Q

avoidance

A

inability to talk about the experience or return to the site, numbing of general responsiveness (emotional numbing, detachment, or estrangment from others), sense of foreshortened future

40
Q

hyperarrousal

A

insomnia,, irritability, or outbursts of anger, difficulty concentrating, hypervigillence, exxaggerated startle response

41
Q

hyperarousal responds to

A

alpha blockade

42
Q

SSRI’s labeled for PTSD

A

paroxetine and sertraline

43
Q

PTSD targeting intrusive or sleep related symptoms

A

prazosin
propranolol
combination of the 2*

44
Q

peripheral drugs having CNS effects

A

> liphophillic beta blockers such as propranolon (atenolon is not lipophillic)
1st gen anti-histamines-also strong anticholinergic acitivity in the periphery
liphophillic muscarinic antagonists -select drugs with quaternary amine structure

45
Q

name some quaternary anti-cholinergics

A

glycopyrrolate

propantheline