A spectrum of pharmacological treatments for insomnia
Pharmacological treatment for insomnia is typically considered a second-line option after non-drug approaches, like cognitive behavioral therapy for insomnia (CBT-I), have been explored. However, when medication is necessary, several classes of drugs can be effective. A healthcare provider tailors the choice of medication based on the patient's specific symptoms (e.g., difficulty falling asleep versus staying asleep), treatment goals, and overall health status. Below is an overview of the main types of drugs used to combat sleep problems.
Non-benzodiazepine hypnotics (Z-drugs)
Z-drugs, including zolpidem (Ambien), zaleplon (Sonata), and eszopiclone (Lunesta), are frequently used for insomnia. They work by affecting GABA-A receptors in the brain to produce a sedative effect. Zolpidem helps with both falling and staying asleep but has been linked to next-day impairment and complex sleep behaviors. Zaleplon is best for those who struggle only with falling asleep due to its short duration. Eszopiclone is approved for longer use but can cause an unpleasant taste and next-day grogginess.
Orexin receptor antagonists
This newer class of medication blocks orexin neurotransmitters that promote wakefulness. Examples include suvorexant (Belsomra), lemborexant (Dayvigo), and daridorexant (Quviviq). They are used for both difficulty falling and staying asleep. While classified as controlled substances, they are thought to have a lower potential for abuse than older sedatives.
Melatonin receptor agonists
These drugs mimic melatonin to regulate the sleep-wake cycle. Ramelteon (Rozerem) is the only FDA-approved prescription option and is used for difficulty falling asleep. It is not a controlled substance, making it suitable for patients with a history of substance abuse. Over-the-counter melatonin is also available but is not FDA-regulated and its effectiveness for general insomnia is less proven than for circadian rhythm issues.
Sedating antidepressants and antihistamines
Some medications with sedative effects are used off-label for insomnia, particularly when associated with other conditions like depression. Low-dose doxepin (Silenor), an antidepressant, is approved for maintaining sleep. Trazodone is also used off-label, but evidence for its effectiveness primarily for insomnia is limited. Over-the-counter antihistamines like diphenhydramine block histamine to cause drowsiness. However, their effectiveness diminishes over time, and they can cause next-day effects and potentially increase dementia risk in older adults.
Older treatments: Benzodiazepines and barbiturates
Benzodiazepines (e.g., temazepam, triazolam) are older sedatives generally used only for very short periods due to high risks of dependence, abuse, and side effects like impaired memory and coordination. Barbiturates are now rarely used for insomnia because of the high risk of overdose and dependence.
Comparison of insomnia medication classes
| Medication Class | Mechanism | Typical Use | Major Side Effects/Risks |
|---|---|---|---|
| Z-drugs | Modulate GABA-A receptors | Short-term; some for longer use | Next-day impairment, complex sleep behaviors, dependence |
| Orexin Antagonists | Block wakefulness-promoting orexin receptors | Short or long-term | Headache, somnolence, abnormal dreams |
| Melatonin Agonists | Mimic melatonin, regulating circadian rhythm | Long-term (ramelteon) | Dizziness, headache, fatigue; generally well-tolerated |
| Benzodiazepines | Enhance GABA inhibition | Very short-term only | Dependence, rebound insomnia, cognitive impairment, falls |
| Sedating Antidepressants | Varies (e.g., histamine antagonism) | Off-label; specific sleep issues | Daytime sleepiness, anticholinergic effects |
| Over-the-Counter Antihistamines | Block histamine receptors | Occasional, short-term | Next-day drowsiness, confusion, dry mouth, long-term dementia risk |
The crucial role of non-pharmacological therapies
Non-drug treatments like Cognitive Behavioral Therapy for Insomnia (CBT-I) are widely recommended as a first step before medication. CBT-I addresses the thoughts and behaviors contributing to poor sleep through techniques like sleep hygiene education, stimulus control, sleep restriction, and relaxation. Combining medication with CBT-I can lead to better and more lasting results, often allowing for medication to be eventually discontinued.
Conclusion
Addressing the question "what is the drug used for insomnia?" reveals a range of pharmacological options, including Z-drugs, orexin antagonists, melatonin agonists, and other sedating medications. Each class has distinct properties, benefits, and potential risks, such as dependence and side effects. Due to these risks, medical guidance is essential for selecting the most appropriate treatment. Integrating medication with non-pharmacological methods like CBT-I often provides the most effective long-term solution for managing insomnia.
{Link: Clinical Practice Guideline for the Pharmacologic Treatment of Chronic Insomnia in Adults https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5664/}
Important considerations before starting medication for insomnia
Before starting any medication for insomnia, it is crucial to consult your doctor to discuss your symptoms, health conditions, and current medications. Non-medication options like CBT-I should be considered first due to their effectiveness and fewer side effects compared to medication. Understanding potential side effects like next-day drowsiness and dizziness is important. Be aware of dependence risks associated with certain medications like benzodiazepines and Z-drugs. Mixing sleep aids with alcohol is dangerous and should be avoided. Use OTC sleep aids cautiously, especially in older adults, due to potential risks like cognitive issues. Many sleep medications are for short-term use, and a discontinuation plan should be made with your doctor.
