Anxiolytics Flashcards
Diazepam (Valium) Increasing Dose Effects
Sedation –> Hypnosis –> Anestheia
GABA-a1 receptor
Hypnotic/Anti-Convulsant Effects
GABA-a2 receptor
Anxiolytic effects
No specific drug for only these receptors yet… Good potential
GABA-a5 receptor
Mediates tolerance and dependency
Anxiolytic Treatment
- SSRI’s
- Benzo’s
- Buspirone
Anxiolytic Benzo’s
Diazepam (Valium) Alprazolam (Xanax) Chlordiazepoxide Clorazepate Clonazepam
Short Acting Benzodiazepenes
ATOM: Alprazolam Triazolam Oxazepam Midazolam
Not metabolized by the liver
Oxazepam, Tenazepam, Lorazepam
Outside The Liver
Benzo’s MOA
Bind to allosteric site and increase the action of GABA
Increase the frequency of opening of the Chloride Channel via the GABA-A receptor
Hypnotic Benzo’s
Triazolam
Estazolam
Tenazepam
Limit use to 4 weeks - risk of dependency and tolerance
Increase Stage 2 NREM sleep
Lest restful
Procedural Sedation Benzo’s
Midazolam (Versed)
Lorazepam (Ativan)
Reversal Agent for Benzo Overdose
Flumazenil - IV only
Buspirone
Partial 5HT1A agonist
Effective as mono therapy or with SSRIs
Slower onset
Rarely used
No sedation, addiction, or tolerance. NO WITHDRAWAL
No interaction with alcohol
Anti-Convulsants
Gabapentin, Pregabablin
Hydroxyzine
H1 Antagonist
Separation Anxiety
D-Cycloserine
Used for exposure therapy
Non-Benzo Hypnotics
ZZZ - A1 receptor selective
Zolpidem - short acting
Zaleplon - short acting. Good for people with only intermittent sleep problems
esZopiclone - Lunesta, long term use
First line Hypnotics
Ramelteon
MT1 and MT2 melatonin receptor agonists
Suvorexant
Dural Orexin receptor ANTAGONIST
TX: Insomia
Triazolam
Estazolam
Tenazepam
Hypnotic Benzo’s
Limit use to 4 weeks - risk of dependency and tolerance
Increase Stage 2 NREM sleep
Lest restful
Alprazolam
Triazolam
Oxazepam
Midazolam
Short Acting Benzodiazepenes
ATOM
Higher addictive potential
Diazepam Chlordiazepoxide Alprazolam Clorazepate Clonazepam
Anxiolytic Benzo’s
Diazepam = Valium Alprazolam = Xanax
Midazolam
Lorazepam
Procedural Sedation Benzo’s
Midazolam = Versed Lorazepam = Ativan - Treatment for alcohol withdrawal
OCD
TX: Clomipramine (TCA)
but* SSRI if breastfeeding
Triazolam
Hypnotic Benzo
Estazolam
Hypnotic Benzo
Tenazepam
Hypnotic Benzo