estazolam PROSOM
Class: BenzodiazepineFDA Indications: Short-term Treatment Of Insomnia
Off-Label Use: Catatonia
Prescribing
FDA Schedule IVForms: 1, 2mg tablet
Dose Range: 0.5-2 mg/day
Starting: 1 mg at bedtime; some patients may require 2 mg
Stopping: Abrupt discontinuation should be avoided. Daily dose may be decreased by 0.5 mg q3 days; however, some patients may require a slower reduction.
Precautions
Serious Side Effects: Overdose can result in hypotension, respiratory depression, and comaSide Effects: constipation, dysarthria, sedation/somnolence, dizziness, confusion, disequilibrium, ataxia, lightheadedness, weakness/asthenia, decreased libido, increased appetite, weight gain
Pharmacokinetics
t½: 18 (10-24)° TMAX: 2°Absorption Rate: Fast
Lipid Solubility: Low-moderate
Substrate of: 3A4
Inhibits: ∅ ; Induces: ∅
Active Metabolites: ∅
DDIs
- - CNS depression with combined use of opioids
- - 3A4 inhibitors can ↑ levels; likewise, 3A4 inducers can ↓ levels
Misc
- - Its long t½ makes it helpful for patients with late-insomnia, i.e. early morning awakening, but for the same reason has a liability for producing a hangover effect the morning after
Special Populations
Category X—Human Data Suggest Risk in 1st and 3rd Trimesters
No reports describing the use of estazolam in human pregnancy have been located. The effects of this drug on the fetus should be similar to other benzodiazepines. Maternal use near delivery may potentially cause neonatal motor depression and withdrawal.
0.5-1 mg at bed time. Initiate at lower doses for small elderly or debilitated patients
2019 BEE℞S Recommendation: Avoid. Older adults have increased sensitivity to benzodiazepines and decreased metabolism of long- acting agents; in general, all benzodiazepines increase risk of cognitive impairment, delirium, falls, fractures, and motor vehicle crashes in older adults. May be appropriate for seizure disorders, RBD, benzodiazepine withdrawal, EtOH withdrawal, severe GAD, and periprocedural anesthesia.
No adjustment provided in package insert; use with caution
No adjustment provided in package insert; use with caution