Insomnia Flashcards
Daridorexant
Orexin A & B Antagonist
Onset and Maintenance
Lower in mod hepatic, avoid in severe hepatic
Empty stomach
CI: Narcolepsy
Major 3A4 substrate
Diphenhydramine
Competes with histamine at H1 receptors
Latency and total sleep time
Not recommended
Residual sedation
Rapid tolerance - do not use longer than 10 days
Anticholinergic ADRs
Doxepin
Selective H1 Antagonist
Maintenance
Good for those with substance abuse concerns
Lower in hepatic
Should not take within 3 hours of eating
Doxylamine
Competes with histamine at H1 receptors
Not recommended
Residual sedation
Anticholinergic effects
Rapid tolerance - do not use longer than 10 days
Estazolam
Modulation of GABA-A receptor
Not frequently used d/t long half-life
Eszopiclone
Modulation of GABA-A receptor
Onset and Maintenance
Improvement seen in pts with depression &/or anxiety
Bitter taste
Empty stomach
Lower in hepatic
Major 3A4 substrate
Flurazepam
Modulation of GABA-A receptor
Not frequently used d/t long half-life
Lemborexant
Orexin A & B Antagonist
Onset and Maintenance
Residual drowsiness
Lower in moderate hepatic, avoid in severe hepatic
CI: Narcolepsy
Major 3A4 substrate
Quazepam
Modulation of GABA-A receptor
Not frequently used d/t long half-life
Ramelteon
MT1 & MT2 Agonist
Onset
Good for patients with substance abuse concerns
Safe option for pts with OSA/COPD
Avoid in severe hepatic
Empty stomach (high-fat meal)
Substrate: 1A2, 2C9, 3A4
Suvorexant
Orexin A & B Antagonist
Onset and Maintenance
Residual drowsiness
Safe in OSA/COPD
Avoid in severe hepatic
Empty stomach
CI: Narcolepsy
Major 3A4 substrate
Temazepam
Modulation of GABA-A receptor
Onset and Maintenance
Inexpensive
Triazolam
Modulation of GABA-A receptor
Onset
“Speech disorder”
Empty stomach
Zaleplon
Modulation of GABA-A receptor
Onset
Lower in mild-mod hepatic, avoid in severe hepatic
Empty stomach
Limit use to 30 days
Major 3A4 substrate
Zolpidem
Modulation of GABA-A receptor
Onset and Maintenance
Improvements seen in pts with depression &/or anxiety
SL&ER formulations
Lower in mild-mod hepatic, avoid in severe hepatic
Empty stomach
Major 3A4 substrate