Adrenergic & Cholinergic Effects of CNS Drugs

Question 1

what are the major stimulatory NTs?

Answer 1

aspartate & glutamate

Question 2

what are the 2 major inhibitory NT’s?

Answer 2

GABA & Glycine

Question 3

whch part of the brain that is involved in regulating sleep and arousal contains the majority of the noradrenergic neurons?

Answer 3

locus ceruleus

Question 4

increased activity in the locus ceruleus may increase anxiety by releasing what NT in the amygdala and in other limbic areas?

Answer 4

NE

Question 5

stimulation of what receptors in the amygdala enhances memories for stimuli encoded under strong negative emotion?

Answer 5

beta-adrenergic

Question 6

What kind of receptor is the nicotinic receptor?

Answer 6

multimeric ion channel (activation leads to permissive entry of Na+ and Ca2+ and cellular depolariztion)

Question 7

The central effects of ACh are mixture of what 2 receptors?

Answer 7

muscarinic and nicotinic

Question 8

what 2 NTs are involved in regulation of arousal (wakefulness) and cognitition?

Answer 8

ACh & NE

Question 9

if you make drugs that are antagnoists for ACh & NE then this would produce what effect in the CNS?

Answer 9

sedation and mental clouding

Question 10

what determines the drug choice for antipsychotics?

Answer 10

the tolerability of the side effects

Question 11

the antipsychotics can produce activity at a number of receptor systems including acting as antagonists at what 3 types of receptors?

Answer 11

alpha-adrenergic receptors
muscarinic receptors
histaminergic H1 receptors

Question 12

what are some of the AEs of muscarinic cholinoreceptor blockade in the ANS?

Answer 12

loss of accommodation, dry mouth, difficulty urinating, constipation

Question 13

what are some of the AEs of blocking alpha-adrenergic receptors in the ANS?

Answer 13

Orthostatic hypotension, impotence, ejaculation failure

Question 14

what are the AEs of dopamine receptor blockade in the CNS?

Answer 14

parkinson’s syndrome, akathisia, dystonias

Question 15

what is the AE associated with supersensitivity of dopamine receptors in the CNS?

Answer 15

tardive dyskinesia

Question 16

what is the AE of muscarinic blockade in the CNS?

Answer 16

toxin-confusional state

Question 17

antidepressants typically block reuptake of what 3 NTs?

Answer 17

NE, serotonin, dopamine

Question 18

antidepressants typically act as antagonists at 4 receptors?

Answer 18

muscarinic, histaminic (H1), alpha-1, dopaminergic (D2), possibly serotonergic (5-HT2A)

Question 19

what are the typical AEs associated with blocking a NE transporter?

Answer 19

anxiety, increased pressor effects of sympathomimetic amines, diaphoresis, tachycardia, tremor

Question 20

what are the typical AEs associated with blocking alpha-1adrenergic receptors?

Answer 20

postural hypotension, dizziness, potentiation of the antihypertensive effect of other meds, reflex tachycardia

Question 21

what are the typical AEs associated with blocking muscarinic receptors?

Answer 21

central effects including memory and cognitive impairment, delirium in severe cases
-sinus tachycardia (via reflex tachycardia or by removal of vagal inhibitory influence)

Question 22

dopaminergic neurons originating in the substantia nigra normally inhibit which receptors which are the output from the striatum?

Answer 22

GABAergic output

Question 23

which type of neurons exert an excitatory effect on the striatum?

Answer 23

cholinergic

Question 24

what determines the net activity of the striatal GABA neurons?

Answer 24

determined by the balance of inhibitory D1, D2 dopaminergic neurons and excitatory muscarinic neurons.

Question 25

in Parkinson’s disease which type of neurons degenerate leading to over excitation of the GABAergic neurons and to the associated motor-dysfunction?

Answer 25

DOPAMINERGIC NEURONS

Question 26

which 2 receptors are present within the regulation of amygdala?

Answer 26

alpha & beta 1 adrenergic receptors

Question 27

What part of the brain is known as being important in the interface b/w memories and emotions?

Answer 27

amygdala

Question 28

what is intrusion?

Answer 28

re-experience of traumatic memories at night

Question 29

which type of blockade is responsive to treating intrusion?

Answer 29

beta-adrenergic blockade

Question 30

what is avoidance?

Answer 30

inability to talk about the experience

Question 31

what is hyperarousal (PTSD)?

Answer 31

insomnia, irritability or outbursts of anger

Question 32

therapy with what kind of blockade causes a response in pts with hyperarousal symptoms?

Answer 32

alpha-adrenergic blockade

Question 33

what are 2 drugs currently labeled for PTSD?

Answer 33

paroxetine and sertraline

Question 34

use of which 2 drugs would be part of script-driven trauma imagery viewing to recalibrate the emotions aroused by memory recall?

Answer 34

prazosin with propanolol (combo would target intrusive and sleep related symptoms)

Question 35

what are some of the AEs of lipophilic beta-blockers?

Answer 35

dizziness, confusion, lethargy, fatigue, weakness, catatonia, hallucinations, short-term memory impairment, emotional lability, insomnia

Question 36

the 1st Gen H1 antagonists are more lipophilic and produce both H1 blockade centrally causing what 2 things?

Answer 36

sedation and confusion

Question 37

1st gen H1 antagonists produce H1 blockade centrally and strong anticholinergic action centrally and peripherally including what adverse effects?

Answer 37

Anticholinergic AEs of 1st gen H1 Antagnonists:
xeroxtomia, dry nasal mucosa, pharyngeal dryness, thick sputum, convulsions, tachycardia, blurred vision, palpitations, constipation

Question 38

which betablocker is classically lipophilic?

Answer 38

Propanolol

Question 39

which betablocker is classically hydrophilic?

Answer 39

atenolol

Question 40

selecting what kind of antimuscarinic will minimize the central AEs of these drugs?

Answer 40

quaternary amine structure