Adrenergic & Cholinergic Effects of CNS Drugs Flashcards
what are the major stimulatory NTs?
aspartate & glutamate
what are the 2 major inhibitory NT’s?
GABA & Glycine
whch part of the brain that is involved in regulating sleep and arousal contains the majority of the noradrenergic neurons?
locus ceruleus
increased activity in the locus ceruleus may increase anxiety by releasing what NT in the amygdala and in other limbic areas?
NE
stimulation of what receptors in the amygdala enhances memories for stimuli encoded under strong negative emotion?
beta-adrenergic
What kind of receptor is the nicotinic receptor?
multimeric ion channel (activation leads to permissive entry of Na+ and Ca2+ and cellular depolariztion)
The central effects of ACh are mixture of what 2 receptors?
muscarinic and nicotinic
what 2 NTs are involved in regulation of arousal (wakefulness) and cognitition?
ACh & NE
if you make drugs that are antagnoists for ACh & NE then this would produce what effect in the CNS?
sedation and mental clouding
what determines the drug choice for antipsychotics?
the tolerability of the side effects
the antipsychotics can produce activity at a number of receptor systems including acting as antagonists at what 3 types of receptors?
alpha-adrenergic receptors
muscarinic receptors
histaminergic H1 receptors
what are some of the AEs of muscarinic cholinoreceptor blockade in the ANS?
loss of accommodation, dry mouth, difficulty urinating, constipation
what are some of the AEs of blocking alpha-adrenergic receptors in the ANS?
Orthostatic hypotension, impotence, ejaculation failure
what are the AEs of dopamine receptor blockade in the CNS?
parkinson’s syndrome, akathisia, dystonias
what is the AE associated with supersensitivity of dopamine receptors in the CNS?
tardive dyskinesia
what is the AE of muscarinic blockade in the CNS?
toxin-confusional state
antidepressants typically block reuptake of what 3 NTs?
NE, serotonin, dopamine
antidepressants typically act as antagonists at 4 receptors?
muscarinic, histaminic (H1), alpha-1, dopaminergic (D2), possibly serotonergic (5-HT2A)
what are the typical AEs associated with blocking a NE transporter?
anxiety, increased pressor effects of sympathomimetic amines, diaphoresis, tachycardia, tremor
what are the typical AEs associated with blocking alpha-1adrenergic receptors?
postural hypotension, dizziness, potentiation of the antihypertensive effect of other meds, reflex tachycardia
what are the typical AEs associated with blocking muscarinic receptors?
central effects including memory and cognitive impairment, delirium in severe cases
-sinus tachycardia (via reflex tachycardia or by removal of vagal inhibitory influence)
dopaminergic neurons originating in the substantia nigra normally inhibit which receptors which are the output from the striatum?
GABAergic output
which type of neurons exert an excitatory effect on the striatum?
cholinergic
what determines the net activity of the striatal GABA neurons?
determined by the balance of inhibitory D1, D2 dopaminergic neurons and excitatory muscarinic neurons.
in Parkinson’s disease which type of neurons degenerate leading to over excitation of the GABAergic neurons and to the associated motor-dysfunction?
DOPAMINERGIC NEURONS
which 2 receptors are present within the regulation of amygdala?
alpha & beta 1 adrenergic receptors
What part of the brain is known as being important in the interface b/w memories and emotions?
amygdala
what is intrusion?
re-experience of traumatic memories at night
which type of blockade is responsive to treating intrusion?
beta-adrenergic blockade
what is avoidance?
inability to talk about the experience
what is hyperarousal (PTSD)?
insomnia, irritability or outbursts of anger
therapy with what kind of blockade causes a response in pts with hyperarousal symptoms?
alpha-adrenergic blockade
what are 2 drugs currently labeled for PTSD?
paroxetine and sertraline
use of which 2 drugs would be part of script-driven trauma imagery viewing to recalibrate the emotions aroused by memory recall?
prazosin with propanolol (combo would target intrusive and sleep related symptoms)
what are some of the AEs of lipophilic beta-blockers?
dizziness, confusion, lethargy, fatigue, weakness, catatonia, hallucinations, short-term memory impairment, emotional lability, insomnia
the 1st Gen H1 antagonists are more lipophilic and produce both H1 blockade centrally causing what 2 things?
sedation and confusion
1st gen H1 antagonists produce H1 blockade centrally and strong anticholinergic action centrally and peripherally including what adverse effects?
Anticholinergic AEs of 1st gen H1 Antagnonists:
xeroxtomia, dry nasal mucosa, pharyngeal dryness, thick sputum, convulsions, tachycardia, blurred vision, palpitations, constipation
which betablocker is classically lipophilic?
Propanolol
which betablocker is classically hydrophilic?
atenolol
selecting what kind of antimuscarinic will minimize the central AEs of these drugs?
quaternary amine structure
