Sedative, hypnotics, and anxiolytics Part 1 Flashcards

1
Q

Sedative

A

Calms anxiety, decreases excitement and activity, does not produce drowsiness, or impair performance

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2
Q

Anxiolytic

A

Anti Anxiety, relieves anxiety without sleep or sedation

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3
Q

Hypnotic

A

Induces sleep, implies restful, refreshing sleep, not “hypnotized!”, natural sleep

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4
Q

Narcotic

A

Actually means “sleep producing”, now refers to opioids or illegal drugs

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5
Q

Reticular formation

A

Extends through the central core of the medulla, pons, and midbrain

It is an intricate system composed of loosely clustered neurons in what is otherwise white matter

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6
Q

Stages of sleep

A

Wakefulness

Non-rapid eye movement (NREM) slow-wave sleep

Rapid-eye movement (REM) sleep

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7
Q

NREM Sleep

A

Stage 1 (dozing)
Stage 2 (unequivocal sleep)
Stage 3 (voltage increase, frequency decreases)
Stage 4 (delta waves)

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8
Q

REM sleep

A

similar to awake in EEG

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9
Q

Sleep deprivation

A

Total sleep
Delta sleep
REM

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10
Q

Factors that regulate sleep

A

Age

Sleep history

Drug Ingestion

Circadian Rhythms: “Normal sleep cycle”

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11
Q

Neurotransmitters

A

regulators of sleep

GABA: main target for current medication

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12
Q

Neuromodulators

A

GH
Prolactin
Cortisol
Melatonin: “hormone of darkness”
Endogenous peptides

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13
Q

GABAergic Neurotransmission

A

GABAa receptors
GABAb receptors
GABA Transporters
GABA-T (Transaminase)
SLIDE 11

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14
Q

GABAa receptor/Chloride Ion Channel Complex

A

Orthostatic site: GABA alpha1 and beta2

Allosteric sites: benzodiazepines site alpha 1 and gamma 2

Barbiturate
Ethanol
Glucocorticoid

Channel pore (picrotoxin)

Most common

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15
Q

Benzodiazepines

A

facilitate GABA action (alpha 1-5) increase frequency, require intact GABA system

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16
Q

Non-benzodiazepines

A

zolpidem, zaleplon, eszopiclone–BZ1 receptors of alpha 1

17
Q

BZD antagonists

A

flumazenil, overdose treatment

18
Q

Inverse BZD agonists

A

B carbolines

19
Q

Ligands acting at “other” non-orthosteric sites

A

BZDs: Increase frequency of channel opening

Barbiturates: Increase duration of channel opening, and direct effects on GABAa

Alcohol: Enhances actions of GABA and GABAa receptor

GABA channel blockers: picrotoxin

Etomidate and Propofol: B2 and B3 subunit containing receptors

Neurosteroids for treating depression

20
Q

Structure activity relationships of benzodiazepines

A
  1. Position alkylation