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Neuro 4 > Anxiolytics [3] > Flashcards

Anxiolytics [3] Flashcards

1
Q

NTs involved in anxiety

Neuropharmacological targets

A

5HT

GABA

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2
Q

1st line agent for most anxiety disorders

A

Antidepressants (SSRI-SNRIs) → increase 5HT

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3
Q

Benzodiazepine agonist action and when it is good to use for anxiety

A

Indirectly Augment GABA Cl- Channels

  • good in acute and situational anxiety
  • INTENSIFY effect of GABA
  • Non-linear, less steep CNS effects (greater dose req. to reach CNS depressant)
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4
Q

Barbiturate action and when it is good to use for anxiety

A

Indirectly Augment GABA Cl- Channels

  • rarely used for anxiety
  • PROLONG effect of GABA
  • less selective
  • depresses excitatory NT (Glu)
  • IV barb maintain surgical anesthesia ( stage III)
  • LINEAR CNS effects
  • very easy to overdose and abuse
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5
Q 
BDZ vs Barbs
Which has greater margin of safety?
Which has higher therapeutic index?
Which one prolongs effect of GABA?
Binds to gamma subunit of GABA R Ion channel?
A

BDZ (greater dose to achieve CNS depression)
BDZ
Barbs - prolongs in presence of GABA and opens channels directly at higher doses
BDZ

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6
Q

BDZ vs General Anesthetics (GA)

  • maintain stage III surgical anesthesia
  • potentiate GABAa receptor activity
  • Low margin of safety
  • Low potency
  • Inhibition of Excitatory synaptic transmission
A 
GA
Both
GA
GA
GA
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7
Q

Non BDZ

A

“Z drugs”
Eszopiclone
Zaleplon
Zolpidem

  • binds only to GABA Cl- channels with a1
  • makes you sleepy (w/o anxiolytics)
  • reduced potential for dependence

(if you want to relieve anxiety, bind a2-5 - BDZ binds a1, a2-5)

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8
Q

BDZ alone are safe, but combined with what is lethal?

A

Ethanol (can open GABA Cl- channel directly at a nonspecific site)
BDZ open indirectly

Can result in coma (additive effect of CNS depressant)

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9
Q

Admin of flumazenil will reverse the toxicities associated with overdose of____

A

BDZs
(BDZ R antagonist)
- reverses CNS depression

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10
Q

What reverses toxicity of morphine?

A

naloxone blocks binding

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11
Q

a1 GABA receptor Cl- channel subunit

  • agonist
  • location
  • action
  • side effects
A

BDZ + Z drugs

Cortex

Sleep, Anticonvulsants
(no anti-anxiety)

Amnesia, Additive CNS depression

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12
Q

a2-5 GABA receptor Cl- channel subunit

  • agonist
  • location
  • action
  • side effects
A

BDZ

Limbic system, brain stem

Anxiolytics, myorelaxants
- can treat anxiety, convulsions at dose where pt is still awake

Tolerance, Dependence, Addiction

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13
Q

BDZ low dose

A

Anxiolytics (a2-a5)

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14
Q

BDZ high dose

A

anticonvulsant effects

(a1- higher barbs and BDZ inhibit seizure activity in cortical neurons)

Myorelaxants

  • BDZ inhibit spinal cord reflexes
  • usually accompanied with sig CNS depression

Sleep

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15
Q

Drug of choice for status epilepticus

A

diazepam

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16
Q

which is used for anesthesia induction?

- Barbs or BDZ?

A

Barbituates: anesthesia induction (phenobarbitol)

BDZ NOT capable of induction (used as adjuncts)

17
Q

dependence of BDZ

A

psychologic dep
physical dep (chronic use)
withdrawal syndrome

  • Most common adverse rxns are extension of CNS depression
18
Q

BDZ ready to be conjugated +inactivated in 1 step

A

Oxazepam
Lorazepam
Temazepam

conjugation enzymes dont diminish with age

  • dont worry about slow metabolism in old people
  • can reliably eliminate it with age

(look for O or L)

19
Q

BDZ eliminated by CYP450

A

Diazepam

  • most BDZ
  • phase I with subsequent inactivation via conjugation by glucuronidation (phase II)
20
Q

Anterograde Amnesia is common in drugs that

A

enhance GABA neuronal fxn
(→ indirectly depressing glutamate fxn)
- ie: BDZ

Beneficial use in uncomfortable procedure as pt is able to cooperate w/o any memory afterward
eg: colonscopy

21
Q

Midazolam (versed)

A

BDZ

antianxiety - act by potentiating GABAa receptors

22
Q 
Alprazolam
Lorazepam
Diazepam
\_\_\_\_\_\_\_\_\_\_\_
Buspirone
A

Anti -anxiety
BDZs

(Buspirone is a partial 5HT1A partial agonist)

23
Q

Do BDZ result in retrograde or anterograde amnesia?

A

Anterograde amnesia
- enhance GABA neuronal fxn
(→ indirectly depressing glutamate fxn)

24
Q

Do BDZ or SSRIs work better in anxiety?

A

SSRI

- BDZ can be used as an adjunct for acute management while SSRI take effect

25
Q

Difference btwn treating anxiety disorders in:
acute panic attack
Mild-moderate symptoms
Severe symptoms

A

acute: BDZ
mild-mod: SSRI (antidepressant OR CBT)
Severe: SSRI AND CBT

26
Q

Schedules of Barbs vs BDZ

A 
Barbs: sched II
- lower therapeutic index
- higher abuse potential than BDZ
- more likely to result in death by resp. depression
- classic inducers of cytP450
BDZ: sched IV
- hgher a

Neuro 4 (18 decks)

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