Lecture 37 - Anxiolytics and Hypnotics Flashcards
3 anxiolyitcs; order and clinical uses
First line – SSRIs
Second line - Buspar
Acute setting - benzos
SSRIs
the bad
takes a few weeks to get benefits
HA, Fatigue, sexual dysfucntion
Buspar
mechanism
the bad
the good
5ht1a agonist
Good: few side effects; no reactions wtih ETOH
no sedation, or addiction potential
The bad: takes time for benefits;
Benzos –
clinical use
mechanism (receptor, subtype, subunit)
the bad
acute anxiety
Increases open potential of GABA-a receptor (chloride channel)
alpha 2 subunit -anxiety mediation
the bad – abuse potential; bad to mix with ETOH;
Dizaepam – active metabolites
addiction
withdrawal
what is narcolepsy –
Mutation in Hypocretin Receptor 2
Humans – loss of lateral hypothalamic neurons (autoimmune) to produce hypocretin
what are the Z drugs?
some side effects?
AmbienCR (zolpidem CR) Lunesta (eszopiclone) Sonata (zaleplon)
night walking, night eating; but minor compared to
what drugs are used to treat insomina
Benzos
Z drugs –AmbienCR (zolpidem CR) Lunesta (eszopiclone) Sonata (zaleplon)
Trazadone
Benadryl
Melatonin
mechanism for sedation of these drugs (receptor, subtype, subunit)
GABA-a
alpha 1 subunit
Some benefits of in regards to hypnosis of Z drugs over benzos
Benzos – slower rise to hypnotic effect; reboind insomina when taken off the drug
SE: ataxia;
Z –
rapid rise hypnotic effect; no rebound insomina
fewer side effects
metabolism of benzos?
oxidation/Glucuronidation in the Liver
slows with age
subunity for anxiolytics
subunit for sedation
alpha 2 of gaba-a
alpha 1 of gaba-a
what drug do you give for a BZD OD?
Flumenzanil
