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Neuro III > Anxiolytics > Flashcards

Anxiolytics Flashcards

1
Q

Phenytoin is metabolized by what CYP enzyme?

It induces what CYP enzyme?

A

metabolized - CYP2C9/10

induces - CYP3A4

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2
Q

Which statins are not metabolized by CYP enzymes?

A

pravastatin - none

rosuvastatin (CYP2C <10% ; CYP2C19 minor)

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3
Q

What is the level of response, airway, & CV support from minimal sedation?

What type of drugs is an example of minimal sedation?

A

Anxiolytics

  • Response: responds normally to verbal commands
  • Airway: maintained
  • CV support: not needed
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4
Q

Describe the pathways involved in axiety and how diazepam works to relieve this anxiety.

A
  • basolateral amygdala complex (BLA) receives negative emotional signals from the thalamus
    • activates central nucleus (CeA) via excitatory projections
    • inhibits CeA via inhibitory GABAergic interneurons
  • CeA (a2-containing GABAA) receptors
    • outputs to brainstem & hypothalamus
    • Diazepam inhibits these outputs, which reduces the manifestations of anxiety
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5
Q

hypnotic effects are mediated by what subunit?

A

a1 containing GABAAR

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6
Q

anxiolytic effects are mediated by what subunit?

A

a2 and a3 subunit containing GABAAR

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7
Q

Most benzos bind to waht subunit containing GABAAR?

What about Z-drugs?

A
  • Benzo - a(1,2,3,5)
  • Z-drugs - a1
    • much more selective
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8
Q

Effects of Benzodiasepines?

AE?

A
  • Effect
    • reduce anxiety (limbic)
    • promote sleep (VPLO)
    • Induce muscle relaxation (supraspinal motor area)
    • anti-convulsive (AED)
  • AE
    • decreased motor skills & confusion
    • anterograde amnesia (hipocampus & cortical area)
    • cardiovascular
    • respiratory
    • tolerance
    • sedation
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9
Q

Describe the cardiovascular & respiratry effects of benzodiazepines

A
  • cardiovascular
    • oral administration - very little
    • IV can produce hypotension & cardiac arrest
  • respiratory effects
    • oral administration - very little
      • clinicaly significant only when combined with other CNS depressants
      • can be a proble in pt. with resp disorders
        • COPD, OSA
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10
Q

What are the benzodiazepines?

A
  • alprazolam
  • chlordiazepoxide
  • diazepam
  • lorazepam
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11
Q

What is the order of treatment for generalized anxiety disorder?

A
  1. supportive / cognitive behavioral / biofeedback / relaxation training
  2. pharmacology
    1. SSRI or SNRI or buspirone - delayed onset action (form long-term management)
    2. benzodiasepines - immediate, stabilization for severe anxiety
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12
Q

Which benzodiazepines are most commonly used for anxiety?

A

alprazolam

lorazepam

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13
Q

What is the major mechanism of action for benzodiasepines?

A

potentiate the actions of the inhibitory neurotransmitter, GABA, in the CNS

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14
Q

What are the CNS effects of GABA?

A
  • GABA
    • induces inhibitory post-synaptic potentials
    • hyperpolarize the membrane
    • prevent hte axon from reachign threshold for firing
    • reduce the synaptic potential produced by excitatory amino acids
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15
Q

Synapses on what part of neuron are often excitatory?

What about inhibitory?

A
  • Dendritic synapses - often excitatory
  • Cell body synapses - often inhibitory
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16
Q

What are the binding sites on GABAA Receptors?

A
  • GABA binding site
    • opened via binding of an agonist
  • Benzodiasepine binding site
    • activation GABAA R with
      • a1 subunit underlie hypnotic effects
      • a2 subunit underlie anxiolytic effects
  • Barbiturate binding site
  • Ethanol binding site
  • Anesthetic binding site
17
Q

What is the difference in how barbiturates & benzodiazepines impact the GABA Cl- channel?

A

benzo - increase frequency of opening

barb - increase duration of opening

18
Q

What is the BZ antagonist?

A

flumazenil

competitive antagonist of benzodiazepines

19
Q

What are the indications for flumazenil?

A
  • reverse sedative effect of benzodiazepines after anesthesia
  • reverse benzodiazepine overdose
  • NOT effective in reversing the effects of other CNS depresants
  • May precipitate withdrawl

short half life compared to some BZ - may need repetitive doses

20
Q

What are the toxic signs of benzodiazepines?

A
  • drowsiness
  • ataxia
  • difficulty with speech (dysarthria)
  • decreased reflexes (areflexia)
21
Q

Tolerance develops to what effects of benzodiazepines?

A
  • Tolerance
    • anticonvulsant effects
  • Little / no tolerance
    • andiolytic effects
    • hypnotic effects
  • cross tolerance with other CNS depressant drugs
22
Q

BZ are what schedule drug?

A

schedule IV

23
Q

What are the withdrawl symptoms seen with BZ?

A
  • general anxiety or symptom recurrence
  • autonimic-like symptoms
    • tachycardia, trembling, abdominal issues, systolic hyperension, sweating
  • flu-like symptoms
    • muscle aches, malaise
  • sensory disturbances
  • seizures & delirium - after long-term, high-dose usage
24
Q

Benzodiazepines are contraindicated with what other drugs?

A
  • sedative hypnotics
    • barbiturates
    • other hypnotics
    • general anesthetics
    • ethanol
    • antihistamines
    • anticholinergics
  • opiates
25
Q

Benzodiazepines are what category with relationto pregnancy?

This means what?

A

D or X

CI - pregnancy, labor & delivery, breast feeding

26
Q

cimetidine has what effect on benzodiazepines?

A

inhibits drug metabolism (CYP3A4)

27
Q

What long acting BZ participate in both phase 1 & phase 2 metabolism?

A
  • chlorazepate
  • chlordiazepoxide
  • diazepam
  • flurazepam
28
Q

What short acting BZ participate in both phase 1 & phase 2 metabolism?

A

alprazolam

midazolam

troazolam

29
Q

What short acting BZ participate in only phase 2 metabolism?

A

lorazepam

oxazepam

temazepam

30
Q

What type of metabolism occurs in phase 1? Phase 2?

What patients experience a decrase in phase 1 elimination?

A
  • Phase 1 -
    • oxidation
    • reduction
    • hydrolysis
  • Phase 2
    • conjugation pathway

decreased phase 1 reactions for drug elimination can occur in patients with liver disease & in geriatric patients

31
Q

What BZ would you use in a patient with liver dysfunction?

A

lorazepam

(oxazepam, temazepam)

32
Q

Other than BZ, what drug is used to treat anxiety?

A

buspirone

33
Q

What are the indications to prescripbe buspirone?

MOA?

AE

Time until effectiveness?

A
  • Buspirone
  • Indication
    • generalized anxiety disorder
    • no effective for other types of aniety disorders
  • MOA
    • partial agonist at the 5-HT1A receptor
  • AE
    • dizziness & lightheadedness
    • tachycardia, palpitations
    • nervousness or restlessness
    • GI distress
    • tingling or prickling sensation
  • takes 1-2 weeks to produce antianxiety effect
34
Q

What are the advantages of using buspirone over BZ to treat anxiety?

A

little sedation or euphoric effect

no rebound anxiety or withdrawl symptoms

doens’t potentiate the effects of other CNS depressants

35
Q

What drugs are used for people who have a fear of public performance?

A
  • non-selective beta blocker
    • propranolol (B1 & 2)
  • if has COPD or Asthma
    • metoprolol (B1 selective)

Neuro III (14 decks)

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