Adrenergic and Cholinergic effects of drugs

Question 1

excitatory neurotransmitters

Answer 1

glutamate

aspartate

Question 2

inhibitory neurotransmitters

Answer 2

GABA
glycine
beta alanine
taurine

Question 3

highest concentration of NE in the brain

but found throughout the brain

Answer 3

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

Question 4

adrenergic receptora are all of which overall type

Answer 4

metabotropic

-GPCR’s

Question 5

alpha one has which type of G protein subtype

Answer 5

Gq-calcium based signalling-stimulatory outcomes

Question 6

alpha two has which type of G protein

Answer 6

Gi-cAMP based signalling-inhibitory outcomes

*inhibitory autoreceptors and post-synaptic modulators

Question 7

Beta receptors use which type fo g protein

Answer 7

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

Question 8

locus ceruleus involved in regulating what?

Answer 8

sleep and arousal

attention and vigilence

Question 9

overactivity in locus ceruleus could potentially lead to,

Answer 9

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

Question 10

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

Answer 10

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

Question 11

ACH receptors used in CNS

Answer 11

both Muscarnic and Nicotinic

*not necessarily where drugs re muscarinic ligands

Question 12

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

Answer 12

nicotinic ACHreceptor

Question 13

M1, M3, M5 are all coupled to

Answer 13

Gq GPCR–> stimualtory

Question 14

M2 and M4

Answer 14

Gi receptor-> inhibitory

Question 15

nicotinic subtype found in autonomic ganglia

Answer 15

Nn

Question 16

nicotinic subtype found at NMJ

Answer 16

Nm

Question 17

ACH functions in the brain

Answer 17

motivation
learning
memory

Question 18

NE regulate what in the brain

Answer 18

arousal
attention
vigilance
memory

Question 19

descending NE fibers also modulate what

Answer 19

afferent pain signals

Question 20

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

Answer 20

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

Question 21

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

Answer 21

histamine

Question 22

atypical antipsychotics all

Answer 22

do no possess uniform pharmacology or MOA

Question 23

main MOA’s for these centrally acting antipsychotics

Answer 23

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

Question 24

dopa blockade side effects

Answer 24

parkinsonism, akathisia, dystonia

amenorrhea-galactorrhea, infertility, impotence

Question 25

combined serotinin and histamine blockade side effect

Answer 25

weight gain

Question 26

muscarinic cholioceptor blockade side effects

Answer 26

loss of accomodation xerostomia difficulty urinating constipation

Question 27

alpha blockade side effects

Answer 27

orthostatic hypotension impotence ejaculation failure

Question 28

supersensitivity of dopa receptors side effects

Answer 28

tardive dyskinesia

Question 29

side effects from blockade of NE transporter

Answer 29

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

Question 30

alpha one blockade side effects

Answer 30

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

Question 31

effects of muscarinic blockade

Answer 31

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

Question 32

net activity of striated GABA neurons is determined by

Answer 32

relative balance of D1 and D2 receptors and excitatory muscarinic neurons

Question 33

in parkinsons--D2

Answer 33

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

Question 34

tx of perkinsons involves

Answer 34

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

Question 35

drugs for parkinsons

Answer 35

L dopa | benztropine, diphenhydramine, trihexyphenidyl

Question 36

side effects of the three antimuscarinic agents used in early parkinsons

Answer 36

sedation, mental confusion, constipation, urinary retention, cycloplegia

Question 37

intrusion

Answer 37

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

Question 38

intrusion responds to

Answer 38

beta blockade

Question 39

avoidance

Answer 39

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

Question 40

hyperarrousal

Answer 40

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

Question 41

hyperarousal responds to

Answer 41

alpha blockade

Question 42

SSRI's labeled for PTSD

Answer 42

paroxetine and sertraline

Question 43

PTSD targeting intrusive or sleep related symptoms

Answer 43

prazosin propranolol combination of the 2*

Question 44

peripheral drugs having CNS effects

Answer 44

>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

Question 45

name some quaternary anti-cholinergics

Answer 45

glycopyrrolate | propantheline