Medications for Falling Asleep
For patients with difficulty falling asleep, short-intermediate acting benzodiazepine receptor agonists (BzRAs) or ramelteon are recommended as first-line pharmacological treatments. 1
First-Line Pharmacological Options
- Zolpidem (10mg, 5mg in elderly) is effective for both sleep onset and sleep maintenance insomnia 1
- Zaleplon (10mg) is specifically recommended for sleep onset insomnia 1
- Eszopiclone (2-3mg) is effective for both sleep onset and sleep maintenance insomnia 1
- Ramelteon (8mg) is recommended specifically for sleep onset insomnia and works on melatonin receptors without risk of tolerance 1, 2
Second-Line Options
- Temazepam (15mg) can be used for both sleep onset and sleep maintenance insomnia when first-line agents are ineffective 1
- Doxepin (3-6mg) is suggested primarily for sleep maintenance insomnia 1
- Suvorexant (orexin receptor antagonist) is recommended for sleep maintenance issues 1, 2
Treatment Algorithm
- Begin with cognitive behavioral therapy for insomnia (CBT-I) as the initial treatment for all adults with chronic insomnia due to its superior long-term efficacy and minimal risk of adverse effects 1, 2
- If medication is necessary, start with short/intermediate-acting BzRAs (zolpidem, zaleplon, eszopiclone) or ramelteon 1
- For sleep onset difficulty specifically, consider zaleplon, ramelteon, or zolpidem 1
- If first-line agents fail, try alternative BzRAs or consider sedating antidepressants for patients with comorbid depression/anxiety 1
Special Considerations for Older Adults
- Lower doses should be used in elderly patients (e.g., zolpidem 5mg instead of 10mg) 1, 3
- Benzodiazepines should be avoided when possible in older adults due to increased risk of falls, cognitive impairment, and dependence 4, 3
- Ramelteon has a minimal adverse effect profile, making it a valuable first-line option for older adults 3
Medications to Avoid
- Over-the-counter antihistamines (e.g., diphenhydramine) are not recommended due to lack of efficacy data and safety concerns 1, 3
- Trazodone is not recommended for sleep onset insomnia 1
- Tiagabine (anticonvulsant) is not recommended for sleep onset or maintenance insomnia 1
- Herbal supplements (e.g., valerian) and melatonin have insufficient evidence of efficacy 1
- Older hypnotics including barbiturates and chloral hydrate are not recommended 1
Important Clinical Considerations
- Short-term hypnotic treatment should be supplemented with behavioral and cognitive therapies 1, 5
- Use medications for the shortest duration possible at the lowest effective dose 5, 6
- Monitor patients regularly to assess effectiveness and side effects 1
- Long-term use of benzodiazepines and non-benzodiazepine hypnotics can lead to tolerance and diminished efficacy 2, 7
- Sleep hygiene education (regular exercise, daytime bright light exposure, comfortable sleep environment, avoiding heavy meals/alcohol/nicotine near bedtime) should be part of any insomnia treatment plan 4
Common Pitfalls to Avoid
- Using sedating agents without considering their specific effects on sleep onset versus maintenance 1
- Failing to consider drug interactions and contraindications 1
- Continuing pharmacotherapy long-term without periodic reassessment 1, 2
- Abrupt discontinuation of benzodiazepines or z-drugs, which can precipitate withdrawal symptoms 2
- Focusing solely on pharmacological approaches without addressing behavioral components 2, 5