From the Guidelines
Zolpidem (Ambien) is a nonbenzodiazepine benzodiazepine receptor agonist (BZRA) used for the treatment of insomnia.
Key Characteristics
- It is one of the four nonbenzodiazepine BZRAs, which include zolpidem, zaleplon, eszopiclone, and zopiclone 1.
- Zolpidem improves sleep efficiency, sleep onset latency, sleep quality, total sleep time, and wake after sleep onset compared with placebo 1.
Important Considerations
- The benefits of zolpidem seem to outweigh potential harms, but it can cause serious injuries due to sleep behaviors such as sleepwalking, sleep driving, and other activities while not fully awake 1.
- To minimize adverse events, zolpidem should be administered at the lowest effective dose and for the shortest possible duration, and patients should be counseled on potential risks 1.
- Zolpidem is preferred over benzodiazepines and trazodone for the treatment of chronic insomnia disorder due to their widely known harms and adverse effects 1.
From the Research
Overview of Zolpidem (Ambien) Tablet
- Zolpidem is an imidazopyridine, a nonbenzodiazepine hypnotic agent that acts at the benzodiazepine omega 1-receptor subtype in the brain 2, 3
- It is used for the short-term treatment of insomnia, improving sleep in patients with insomnia by reducing sleep latency and prolonging the duration of sleep 2, 4
Pharmacokinetics and Pharmacodynamics
- Zolpidem has a rapid onset of action and a short elimination half-life, with peak plasma concentration occurring in 0.75 to 2.6 hours postdose 3
- The terminal elimination half-life of zolpidem is approximately 1.5 to 3.2 hours, with total clearance of 0.24 to 0.27 ml/min/kg 3
- Zolpidem is approximately 92% bound to plasma proteins, with an absolute bioavailability of about 70% 3
Therapeutic Uses and Forms
- Zolpidem is available in immediate-release (IR) and extended-release (ER) formulations, as well as sublingual tablets and an oral spray form 5
- The extended-release formulation is indicated for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance 6
- Zolpidem-IR reduces sleep latency at recommended doses of 5mg and 10mg in elderly and non-elderly patients, respectively, while zolpidem-ER improves sleep maintenance in elderly and non-elderly patients, respectively 5
Safety and Tolerability
- Zolpidem has a favorable tolerability profile, with a low propensity to cause clinical residual effects, withdrawal, dependence, or tolerance 4
- Adverse effects are predominantly CNS and gastrointestinal in nature, with altered pharmacokinetics leading to an increase in dose-proportionate adverse effects in the elderly and in patients with renal dysfunction 2