Pharm 4 Anxiolytics Flashcards
Goal of anxiety Tx
Anxiolytics w/o sedation
Tx of choice for long term anxiety
SSRI
Benzodiazepines v Barbiturates
Benzo much safer
Benzo doesn’t induce liver enzymes
Benzo MOA
Binds GABA (Cl-) channel, allosteric modulation increase GABA binding affinity
5 subunit channel leads to many different drugs
Anxiolytic subunits
A2,3 (amygdala)
Sedative subunits
A1,5 (attention, arousal)
Benzo metabolism
Liver conjugation- no grapefruit juice, erythromycin
Benzo use for medical procedures
Amnesia adjuvant, NOT anesthetic
Benzo overdose Tx
Flumazenil (antagonist)
Z drug with shortest half life
Zaleplon (sonata)
Z drug with possible residual morning effects
Zolpidem (ambien)
Z drug for long term use
Eszopiclone (lunesta)
Barbiturate MOA
Low dose - facilitate GABA binding
High dose - directly open channel
Barbiturate anesthesia adjunct
Thiopental
Barbiturate for anticonvulsion
Phenobarbital (less sedation)
Melatonin agonist
Ramelteon
Ramelteon MOA
Melatonin receptors, NOT GABA
Ramelteon indication
Sleep onset insomnia
Orexin drug
Antagonist - orexin promotes wakefulness
Antihistamine SE
Daytime sleepiness
Trazadone
Promote sleep at low doses
Antidepressant at high doses