Insomnia Flashcards
Antihistamines
Less effective than benzos
Tolerance develops quickly
Daytime drowsys and anticholinergic side effects
H1 Receptor antagonists
Diphenhydramine
Benadryl IND: Sleep aid MOA: H1A BOX: n/a CON: n/a ADR: Anticholinergic
Doxylamine
IND: Sleep aid MOA: H1A BOX: n/a CON: n/a ADR: Anticholinergic
Non-Benzos
Preferred agent for insomnia
Different than benzos but still act on the GABA receptor Cl channel
Potential for tolerance, dependence, and abuse.
CONTROLLED SUBSTANCES
Zolpidem
Ambien
IND: Insomnia, short term
MOA: GABA receptor agonist. Does not reduce time spent in REM, little to no rebound.
BOX: Complex sleep behaviors; sleep walking, driving, or other activities. Has resulted in death
CON:
ADR: HA, drowsy, dizzy
Zaleplon
IND: Insomnia, short term MOA: Binds to omega-1 receptor on alpha subunit of the GABA-A (same as Ambien for BIlly). Good for sleep induction, not great for sleep maintenance BOX: Complex sleep behaviors CON: ADR: HA
Eszopiclone
IND: Insomnia, long term MOA: GABA receptor agonist. Reduced onset of action with high-fat or large meal BOX: Complex sleep behaviors CON: ADR: HA, dysgeusia
Benzodiazepines
MOA: Agonists on post-synaptic GABA neuron in the CNS; results in less excitable state and stabilization
CONTROLLED SUBSTANCES
BOX: Use with opioids; profound sedation/respiratory depression, coma, and death. Only prescribe to pts with no viable alternatives. Limit duration/quantity
Abuse, misuse, addiction
Dependence and LIFE-THREATENING WITHDRAWAL RXNS
Temazepam
IND: Insomnia MOA: Benzo BOX: Benzo CON: Pregnancy ADR: Drowsy and hangover effect. Anxiety/confusion
Triazolam
IND: Insomnia MOA: Benzo BOX: Benzo CON: Use with CYP inhibitors ADR: Drowsy
Estazolam
IND: Insomnia MOA: Benzo BOX: Benzo CON: Use with Itraconazole or Ketoconazole. Pregnancy ADR:
Ramelteon
IND: Insomnia
MOA: Melatonin receptor agonist in the hypothalamus. MT1: Induces sleepiness. MT2: Sleep-wake cycle
BOX: n/a
CON: Hx of angioedema with previous Ramelteon. Use with Fluvoxamine
ADR: Droswy
Suvorexant
IND: Insomnia MOA: Orexin receptor antagonist. Controlled Substance BOX: n/a CON: Narcolepsy ADR: Narcolepsy
Valerian Root
Herbal supplement from Valeriana
400-600mg/day
No adverse effects. Thought to work on GABA receptors
Non-pharmacologic Treatments
1st line for all insomnia