Naltrexone is a medication approved by the U.S. Food and Drug Administration (FDA) to manage Alcohol Use Disorder (AUD) and Opioid Use Disorder (OUD). It functions as an opioid receptor antagonist, meaning it blocks the effects of both external opioids and the body’s own naturally produced opioids. The primary goal is to reduce cravings and prevent the euphoric effects of these substances, thereby supporting long-term recovery. While its benefits in addiction treatment are well-established, Naltrexone can interfere with normal sleep patterns. Insomnia, characterized by difficulty falling or staying asleep, is a documented and common side effect experienced by many patients beginning this treatment.
Insomnia as a Recognized Side Effect
Sleep disturbance is a frequently reported adverse effect in the clinical data for Naltrexone. The prescribing information for the oral formulation lists “difficulty sleeping” among the common side effects. In clinical trials for opioid addiction, difficulty sleeping was reported at an incidence rate exceeding 10% of participants, making it one of the more prevalent non-gastrointestinal complaints. In studies involving opioid-free individuals being treated for alcohol use disorder, insomnia was reported by approximately 3% of patients. A broader analysis comparing Naltrexone to a placebo confirmed a statistically significant increase in reports of both insomnia and somnolence (drowsiness) in the group receiving the active medication. The severity of these sleep changes can vary widely.
How Naltrexone Affects Sleep Regulation
The mechanism by which Naltrexone disrupts sleep is directly tied to its fundamental action as an opioid antagonist. Naltrexone works by competitively binding to and blocking the mu-opioid receptors in the central nervous system (CNS). These receptors are not solely involved in pain and pleasure pathways, but are also deeply integrated into the body’s natural sleep-wake cycle regulation.
The endogenous opioid system, which uses the body’s own endorphins and enkephalins, plays a role in modulating sleep architecture. Activation of mu-opioid receptors tends to promote sedation and can influence the duration and structure of various sleep stages. Specifically, opioids are known to suppress the activity of certain brain regions that control wakefulness, facilitating the transition into sleep.
When Naltrexone blocks these receptors, it effectively prevents the calming and sedative influence of the endogenous opioids on the CNS. This blockade can lead to a state of central nervous system activation or dysregulation. The resulting imbalance manifests as an increased difficulty in initiating sleep or maintaining a continuous sleep state throughout the night. The overall effect is a reduction in the total time spent sleeping and a decrease in the restorative quality of that sleep.
Strategies for Managing Sleep Disturbances
Addressing Naltrexone-induced insomnia often begins with optimizing non-pharmacological interventions, collectively known as sleep hygiene practices. Maintaining a consistent sleep schedule by going to bed and waking up at the same time every day, even on weekends, helps to reinforce the body’s natural circadian rhythm. Limiting exposure to stimulating blue light from electronic screens for at least an hour before bedtime is also beneficial, as this light can suppress the production of the sleep hormone melatonin.
Patients should also evaluate the timing of their medication. For individuals taking the oral form of Naltrexone, which has a relatively short half-life, taking the dose earlier in the day may minimize its concentration in the bloodstream during the night. Shifting the administration time to the morning can allow the peak effects of the medication to pass before the patient attempts to sleep. This adjustment should only be made following a discussion with the prescribing healthcare provider.
If non-drug methods are insufficient, Cognitive Behavioral Therapy for Insomnia (CBT-I) is often recommended as an effective, long-term solution. This structured program addresses the thoughts and behaviors that prevent restful sleep, which may be beneficial for managing medication-related sleep problems. Patients experiencing persistent or severe insomnia should always consult their provider before making any changes to their dosage or seeking additional sleep aids. The provider can assess the situation and determine if a temporary sleep medication or a change in the Naltrexone treatment plan is appropriate.

