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Flashcards in Anxyolytics/Sleeping Drugs Deck (24)
1

What are the parts of the brain and their respective symptoms that are activated from the Amygdala in response to fear? 

1) Anterior Cingulate Cortex and Orbitofrontal Cortex = Fear affect and thoughts of fear

2) PAG = avoidance and motor responses - flight or flight or freeze

3) Hypothalamus = increased Cortisol, increased CAD, T2DM, Stroke

4) Respiratory Parabrachial Nucleus = increased RR, Dyspnesa, Asthma

5) Locus Coerulus and Cardiovascular = increased atherosclerosis, ischemia, BP, HR variability with chronic activation

6) Hippocampus -- remembering fear

2

What is Worry? What neironal circuits are involved with worry? 

Worry = anxious misery, apprehensive expectation, obsessions

 

Cortico-Striato-Thalamo-Cortical Circuit that starts in Prefrontal Cortex 

3

What are the classifications of Drugs used for Anxiety? 

Antidepressants - SSRI/SNRI/Tricyclics/ Atypicals

Benzodiazepines

Non-Benzodiazepine - Buspirone

 

Anticonvulsants

4

What is firstline treatment for GAD? 

Cognitive Therapy and then Antidepressants like SSRI/SNRI bc less side effects and administer 1x/day

5

What are some problems/side effects with SSRI? 

Sexyal Dysfunction, Fatigue, Drowsiness

Slow Onset 2-6 weeks 

6

What is Buspirone? How does it work? When is it used? 

Buspirone - 5HT1A PArtial Agonist

good for use when SSRI not tolerated and good for anxiety with very little side effects 

2Nd Choice for Tx for GAD behind SSRI

May be more effective on cognitive aspects of anxiety vs somatic (which BZD are better for) 

7

What are the Pros and Cons of Busprione? 

Pros - NO SYMPTOMS OF: Ataxia, confusion, memory problems, no abuse potential, no dependence, and not interactions w EtOH

 

Cons - Side effects: dizziness, HA, Nausea, Drowsiness

 

8

How do neurosteroids work? What are they? 

Metabolites of Progesterone / Pregnenolone that form in glial cells in the brain and are released with stress and SSRIS

 

Positive Modulation of GABA-A receptors giving tonic inhibition in post-syn neuron

9

What is the GABA receptor's structure? What does it do? 

GABA-gated Chloride Channel with 5 subunits that are 4 TMD each

 

Binding of GABA open channel and increase Chloride 

 

 

10

What are the purposes/binding/effects of the different subunits of the GABA channel? 

Alpha 1 subunit associated with sedation and binding of Ehtanol and volatile anasthetics

 

Alpha 2 subunit associated with anxiety and where Benzodiazepines bind

 

All these things bind to increase channel opening probabiliy

11

What can you give in the event of a BZD Overdose? How does it work? 

Flumenazil!!!

 

Antagonists effects of Agonists but by itself does not affect the receptor 

...Inverse Agonist reduce GABA stimulated Cl Flux

12

What are the BZD used for anxiety? 

What are the BZD used for sedation/hypnosis? 

Anxiety - Diazepam (long acting metabolites so dont have to taper), Oxazepam (elderly, conjugation only)

 

Sedation - Temazepam, Triazolam, Midazolam

13

How are BZD taken care of in the liver? Whichones have special reactions?  

Most are oxidized in the liver and their products are still active (Nordiazepam) and then have Phase 2 Glucuronide conjugation reaction to Oxazepam leading to elimination

 

Oxazepam, Temazepam, and Lorazepam can be directly conjugated and eliminated 

 

14

What are withdrawal symptoms of BZD? 

Tachycardia

STartle Response

GI discomfort

Rebound insomnia

Anxiety (vs reemergence) 

seizures

essentially, accentuated symptoms from original anxious bout 

15

What does Orexin/Hypocretin do? 

Loss of Orexin B signaling leads to narcolepsy 

 

 

16

What is narcolepsy? How do you treat it? 

Sudden, irregular and uncontrollable tendency to fall asleep

can be accompanied by cataplexy 

 

from loss of lateral hypothalamic neurons that produce Hypocretin

 

Treatment - Stimulants, Antidepressants, Modafinil

17

How are BZD used for sleep? What are some effects? 

Used and are effective and safe but can get tolerance and some dependence

 

Side Effects: Ataxia, confusion, memory disturbances

*Hip fractures in elderly! 

*Additive to other CNS depressants like EtOH which can be fatal

Generally do NOT depress HR and Respiration 

18

What are the other drugs used for sleep that are the best? What do they do? Why are they so great? 

PAMs = Positive Allosteric Modulators - Alpha 1 Subunit 

Positive Allosteric Modulators for GABA channel at the Alpha 1 subunit!!!!!

 

Zolpidem

Zaleplin

exZoplicone 

 

NO REBOUND!!!!!!!!! Good for long term use 

19

What does Melatonin do? 

Good for resetting natural clock by acting on Suprachiasmatic nucleus

used for sleep induction or jetlag to reset clock

 

20

Again, what are the Z drugs? How do the work? What's up w/half-lives? 

Eszopiclone, Zolpidem, Zaleplon

bind at GABA rec A1 site and are positive allosteric modulators

 

Half-life approximates duration of sleep 

21

What are the benzos used for sleep? 

Temazepam, Estazolam, Triazolam

22

How is Trazadone used for sleep and what does it do? 

SEdating atypical antidepressant that's given for sleep in MUCH lower doses than depression 

Depression dosin is 150-600 mg and Hypnotic dosing is 25-150 mg 

 

Acts at H1, Alpha1 and 5HT2A 

Little action at Serotonin transporters at the lower doses 

23

Summary for Anxiolytic drugs: First and Second line usage? After that it's BZD and what are effects of BZD? 

 

Other drugs you could use? 

SSRI first line bc few Side effects and Buspirone second choice but both are slow

Then BZD act fast but large abuse potential, withdrawal symptoms, ETOH interactions, Ataxia, memory disturbances - ACT AT GABA ALPHA2 

 

Gabapentin and Tiagibine alternatives 

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