Non BZD Anxiolytics and Non-BZD hypnotics Flashcards
What are the non BZD anxiolytics
Barbiturates
Buspirone
SSRIs
SNRIs - venlafaxine, duloxetine
ie this topic is about the barbiturates and buspirone
List the barbiturates, shortest to longest acting
Thiopental - ultra short, onset 1 min action 5-10 minutes
Amobarbital - mid acting 6-8 hours
Pentobarbital
Phenobarbital - from 4 hours thru 2 days.
Primadone
- prodrug that generates phenobarbital
Phenobarbitral indications
1st line for seizures in neonates. Not much else
Can be used to stop seizures or SE, but second line to Diazepam Lorazepam
Phenobarbital side effectss
Significant cardiac and respiratory depression
Significant CNS depression, Coma.
Very risky in elderly. POtentially lethal CNS and cardiorespiratory suppression.
Long duration and ‘hangover’ effect for a couple days after use.
Tolderance, dependance, and addiction
Potent CYP INDUCER. increases warfarin, statin metabolism, decreasing concentration.
Primadone indications
1st line for essential tremor along with a beta blocker
2nd line antiseizure prophylaxis
Thiopental indications
Induction anesthetic. Not 1st line
Reduction of Intracranial pressure, constrictor of CNS vessels.
Busipirone mechanism and indication
PARTIAL AGONIST of 5HT1A
slow onset anxiolytic, used for GAD.
often used with bridging therapy of short term benzos for a few weeks, then Busipirone continued alone.
What antidepressants are used as anxiolytics?
SNRIs: venlafaxine duloxetine
SSRIs: Fluoxetine, Sertraline, Citalopram, Escitalopram.
NRIs: Reboxetine in some countries for panic disorder.
What are the non-benzo hypnotics?
The Z’s, the Melatonins, and Suvorexant.
The Z’s
Zolpidem
Zaleplon (Zales, dream of diamonds)
Eszopiclone
What are the melatonin agonists
Ramelteon
Tasimelteon
What is Suvorexant
Orexin receptor ANTAGONIST.
Half life of the Z’s
Zaleplon duration 1 hour, least hangover effect. good at promoting sleep but not maintaining it.
Zolpidem 3 hours
Esopiclone ~6 hours. best at maintenance but also hangover.
Note: ELDERLY patients have DRASTICALLY increased half life for these drugs, and should be careful using them. sedation, falls,
abs. contraindication for use with other depressants.
How do the Z’s act?
Bind specifically to the BZ1 receptor, alpha subunit of the BZ receptor.
Only have sedative/hypnotic effects and not anxiolytic.
Side effects of Suvoerexant
Strange dreams
CNS depression
Suicidal thoughts
Upper resp tract infections.
Side effects of the melatonin agonists
Not really any.
Best ones for elderly patients.
Also the only hypnotic of these drugs that don’t alter REM or sleep architecture.
mild fatigue.
