Chapter 19- Anxiolytics Flashcards

1
Q

Why do we need other anxiolytics?

A
  • similarites to alcohol and barbiurates without high misuse potential
  • higher efficacy
  • minimal potential for overdose
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2
Q

How many benzo types have been synthesized, and how many are used clinically?

A
  • > 3000 synthesized
  • 3 dozen used clinically
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3
Q

What is the most popular benzo?

A

Diazepam (Valium)

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4
Q

What is the most commonly prescribed benzo?

A

alprazolam (xanax)

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5
Q

Uses for benzos

A
  • sedative/hypnotic effects similar to barbiturates
  • effective anticonvulsants
  • muscle relaxants
  • reduce aggressive tendencies
  • decrease anxiety
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5
Q

other benzos

A
  • chlordiazepoxide (librium)
  • oxaepam (serax)
  • clorazepate (tranzene)
  • Lorzaepam (ativan)
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6
Q

Why are benzos better than barbiturates?

A
  • more specific than barbiturates and smiliar compounds
  • high therapeutic window
  • works on he limbic system
  • not effective as general anesthetics
  • complex array of pharmacology
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6
Q

How often do benzos work?

A
  • 70-80% of patients
  • less likely in individuals with chronic dissatisfaction, insecurit, and/or characer disorders (ex. antisocial personality)
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7
Q

Barbituates and benzos mechanisms of action

A
  • increase function of the GABA system
  • Positive allosteric modulator (PAM) of the GABA-A receptor (increases agonist affinity and/or efficacy)
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8
Q

What are GABA-A receptors?

A

the major inhibitory receptors in the brain

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9
Q

GABA-A receptor structure

A
  • heteromeric ligand-gated ion channels
  • 2a’s 2 b’s 1 accessory
  • similar in structure to nicotinic acetylcholine receptors
  • permeable to chloride ions (negatively charged)
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10
Q

What do Barbs and BZa increase? how?

A
  • increase chloride currents by binding to allosteric sites
  • this hyperpolarizes neurons
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11
Q

Where do barbiturates bind?

A

between a and B subunits

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12
Q

Where do benzos bind?

A
  • between a and y subunits
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13
Q

What do BZs act on regarding reinforcement?

A
  • they act to suppress the negative reinforcement (stress) network
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14
Q

GABA-A Receptor Ligands: GABA

A
  • function: main activator
  • agonist: GABA, Muscimol
  • antagonist: Bicuculline
15
Q

GABA-A Receptor Ligands: Benzos

A
  • function: allosteric modulator
  • agonist: diazepam, Ro15-4513 (inverse agonist)
  • antagonist: flumazenil
16
Q

GABA-A receptor ligands: Barbituarate

A
  • function: allosteric modulator
  • agonist: phenobarbital
17
Q

GABA-A receptor ligands: neuroactive steroids

A
  • allosteric modulator
  • agonist: progesterone, pregnanolone, allopregnanolone