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Anxiolytics
Lambert's Anxiolytic lecture
7
Medical
Graduate
11/20/2011

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Term
Busiprone
Definition

- Partial 5-HT1A agonist

- Effective as monotherapy or with SSRIs

- Slower onset than BZDs, faster than ADs

- Hepatic metabolism

- No psychomotor impairment

- Well tolerated, non-sedative, no abuse potential

Term
List of Benzo's
Definition
Anxiety:
  • Diazepam
  • Chlordiazapoxide
  • Alprazolam
  • Clorazepate
Insomnia:
  • Triazolam
  • Estazolam
  • Temazepam
Short acting:
  • Midazolam
  • Lorazepam
Term
Benzo's for treatment of anxiety
Definition
  • 2nd or 1st line therapy
  • Rapid onset of action, effective in acute panic
  • Lipophilic, hepatic metabolism, active metabolites
  • Rebound anxiety upon cessation 
  • Ineffective by themselves against comorbid depression
  • High therapeutic index bu HIGH potential for interactions
  • Potentially fatal w/ other CNS depressants
  • Adverse effects include sedation, ataxia & amnesia
Term
Benzo's for treatment of insomnia
Definition
  • not subtype-selective
  • decrease REM and SWS, increase stage 2 NREM
  • REM sleep rebound after discontinuation
  • Motor impairmnet, amnesia, residual sedation
  • Therapy limited to 4 weeks
  • Risk dependency & tolerance
Term
Flumazenil
Definition
  • BZD binding site antagonist
  • IV only
  • For reversal of therapeutic effect of BZD overdose
Term
"Z" Drugs
Definition

Zolpidem - Ambien

Zaleplon - short T1/2; can be given up to 4 hours before waking

Eszopiclone - Lunesta; only drug approved for chronic use

 

- α1 selective

- Lack BZD structure but act at BZD site

- First-line therapy

- Minimal disruption of sleep architecture

- no REM sleep rebound

- Can cause motor impairment, amnesia and residual sedation

Term
Ramelteon
Definition
  • MT1 agonist
  • no effect on GABA
  • no rebound
  • no tolerance or dependence
  • not a controlled substance
  • circadian desynchrony
  • short duration of action
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