zaleplon SONATA
Class: Nonbenzodiazepine/PyrazolopyrimidineFDA Indications: Short-term Treatment Of Insomnia
Off-Label Use: NONE
Prescribing
FDA Schedule IVForms: 5, 10mg capsule
Dose Range: 5-20 mg/day
Starting: Start at 5 mg QHS for elderly, 10 mg QHS otherwise. High-fat/heavy meal can ↑ absorption and delay TMAX by ~2°
Stopping: Taper to avoid rebound insomnia
Precautions
Contraindications: None, other than patients with known hypersensitivity to zaleplonSerious Side Effects: "complex" behaviors i.e., somnambulism, sleep related eating and sleep-driving
Side Effects: sedation/somnolence, dizziness, amnesia, headache
Pharmacodynamics
1° MOA: GABAAR α1 subunit agonistTarget: GABAA α1
Pharmacokinetics
t½: 1 (1-1.5)° TMAX: 1°Absorption Rate: Rapid
Substrate of: Aldehyde oxidase; 3A4
Inhibits: ∅ ; Induces: ∅
Active Metabolites: ∅
DDIs
- - caution with other CNS-depressants
- - 3A4 inhibitors can ↑ levels
Misc
- - shortest t½ amongst ALL hypnotic agents ∴ good choice for early insomnia, but not helpful for sleep maintenance
- - ~4° duration of action, ∴ ∅ next-day sedation even when taken in the middle of the night
- - preserves normal sleep architecture
- - preferential binding of GABAAR α1 subunits > α2/α3 subunits → sedation > anxiolysis
Special Populations
Category C—∅ studies of zaleplon in pregnant women ∴ not recommended for use during pregnancy
RID 1.5%; Probably safe. Levels in milk averaged 14 ug/liter
Start at 5mg qhs
2019 BEE℞S Recommendation: Avoid. Nonbenzodiazepine benzodiazepine receptor agonist hypnotics (ie, Z drugs) have adverse events similar to those of benzodiazepines in older adults (eg, delirium, falls, fractures); increased emergency room visits/ hospitalizations; motor vehicle crashes; minimal improvement in sleep latency and duration.
No dosage adjustment necessary
Cut dose in half in hepatic insufficiency
Thank you for using psychopharmacopeia.com!