Eszopiclone

Treatment of Insomnia

Eszopiclone is primarily used to treat insomnia, a condition where a person has difficulty falling asleep or staying asleep. It belongs to a class of medications known as hypnotics or sedatives. These drugs work by slowing activity in the brain to allow for sleep.

How It Is Used

Healthcare providers prescribe eszopiclone to help manage various symptoms of sleep disruption. Its use is generally focused on:

• Falling asleep: Helping individuals who lie awake for long periods before drifting off.
• Staying asleep: Reducing the frequency of waking up during the middle of the night.
• Sleep duration: Increasing the total amount of time spent sleeping to ensure a more restful night.

Unlike some other sleep medications that are only indicated for short-term use (such as 7 to 10 days), eszopiclone has been studied for use over longer periods. A healthcare provider will determine the appropriate length of treatment based on the individual's specific sleep patterns and needs.

How Eszopiclone Works

Eszopiclone belongs to a class of medications known as sedative-hypnotics. It is specifically designed to treat insomnia by affecting certain chemicals in the brain that may be unbalanced in people with sleep difficulties.

Interaction with GABA

The medication works by interacting with gamma-aminobutyric acid (GABA) receptors in the central nervous system. GABA is a neurotransmitter, a chemical messenger that helps regulate brain activity by sending signals that reduce or inhibit nerve excitability.

When eszopiclone binds to these receptors, it enhances the calming effects of GABA. This process results in a sedative effect on the brain, which helps to:

• Reduce the time it takes to fall asleep.
• Decrease the number of times a person wakes up during the night.
• Improve the overall duration of sleep.

While the exact mechanism of action is not fully understood in every detail, it is known to produce its effects by slowing down the nervous system to facilitate rest. Although it works on similar pathways as other sleep aids, it has a distinct chemical structure that classifies it as a non-benzodiazepine hypnotic.

Common Side Effects

Eszopiclone can cause several mild side effects. The most frequently reported is an unpleasant, bitter, or metallic taste in the mouth. Other common side effects include:

• Daytime drowsiness, grogginess, or a feeling of being drugged
• Headache
• Dizziness or lightheadedness
• Dry mouth
• Nausea, vomiting, or heartburn
• Diarrhea or constipation
• Painful menstrual periods
• Decreased sexual desire
• Breast enlargement in males

Serious Side Effects

Some side effects can be severe and require immediate medical attention. These include:

• Complex sleep behaviors: Getting out of bed while not fully awake and performing activities you do not remember, such as sleep-walking, sleep-driving, making phone calls, or preparing and eating food.
• Mental health and mood changes: New or worsening depression, anxiety, agitation, aggressive behavior, hallucinations, or thoughts of hurting yourself.
• Severe allergic reactions: Swelling of the face, lips, tongue, or throat; hives; or difficulty breathing or swallowing.
• Memory loss: Difficulty remembering events that occurred after taking the medication.
• Coordination issues: Severe dizziness or lack of coordination, which may increase the risk of falls, especially in older adults.
• Confusion: Feeling disoriented or having trouble concentrating.

Boxed Warning: Complex Sleep Behaviors

Eszopiclone can cause complex sleep behaviors, which are activities performed while not fully awake. These behaviors may include sleepwalking, sleep-driving, preparing and eating food, making phone calls, or having sexual intercourse. Because these activities can result in serious injuries or death, the medication must be stopped immediately if any such behavior occurs. It should not be used by anyone who has previously experienced complex sleep behaviors after taking certain sleep medicines.

Next-Day Impairment

This medication may cause decreased mental alertness and coordination the morning after it is taken. This risk is higher if a person takes a dose higher than 1 mg or if they do not get a full 7 to 8 hours of sleep. Impairment can occur even if the individual feels fully awake, potentially affecting the ability to drive or operate machinery safely. The FDA has lowered the recommended starting dose to 1 mg to help reduce this risk.

Severe Allergic Reactions

Rare but serious allergic reactions, including anaphylaxis and angioedema, have been reported. Symptoms may include swelling of the tongue, throat, or face, which can cause difficulty breathing. Emergency medical help is necessary if these symptoms occur.

Mental Health and Behavior Changes

Some people taking eszopiclone experience abnormal changes in thinking or behavior. These may include:

• Increased outgoingness or aggressive behavior.
• Confusion or agitation.
• Hallucinations (seeing or hearing things that are not there).
• Worsening of depression or suicidal thoughts.

General Precautions

Eszopiclone should not be taken with alcohol or other medications that cause drowsiness, as this increases the risk of severe sedation and respiratory issues. It is generally not recommended for individuals with severe liver disease. Stopping the medication abruptly after long-term use may lead to withdrawal symptoms such as anxiety, nausea, or stomach cramps. The medication should only be taken immediately before going to bed.

Pregnancy

The safety of eszopiclone during pregnancy has not been fully established due to a lack of comprehensive studies in humans. It is generally advised that the medication be used during pregnancy only if the potential benefits to the parent outweigh the potential risks to the fetus. If you are pregnant or planning to become pregnant, it is important to discuss your treatment options with a healthcare professional.

Breastfeeding

It is currently unknown if eszopiclone is excreted in human breast milk. Because many drugs can pass into breast milk and potentially affect a nursing infant, caution is recommended. Healthcare providers suggest monitoring the infant for symptoms such as excessive sedation or difficulty feeding if the medication is used while breastfeeding. Decisions regarding the use of this medication while nursing should be made in consultation with a doctor.

Important Considerations

• Inform your healthcare provider if you are pregnant, planning to become pregnant, or breastfeeding before starting this medication.
• If you become pregnant while taking eszopiclone, contact your doctor to discuss whether to continue the treatment.
• The risks and benefits of alternative treatments for insomnia may be considered during pregnancy or lactation.

Dosage Forms

Eszopiclone is supplied as a film-coated tablet for oral administration. It is designed to be taken once daily, immediately before bedtime, when a full night of sleep is possible.

Available Strengths

This medication is available in the following strengths:

• 1 milligram (mg)
• 2 milligrams (mg)
• 3 milligrams (mg)

The appropriate strength is determined by a healthcare provider based on the patient's age, medical condition, and response to treatment. Lower strengths are often used initially to reduce the risk of impaired alertness the following morning.

FDA Approval and Indications

Eszopiclone was approved by the U.S. Food and Drug Administration (FDA) for the treatment of insomnia. It is indicated for use in adults who have difficulty falling asleep or staying asleep. Unlike some earlier sleep medications, it is not restricted to short-term use, though patients are typically re-evaluated periodically.

Boxed Warning

The FDA requires a Boxed Warning for eszopiclone because the medication can cause complex sleep behaviors. These are activities that occur while the patient is not fully awake and of which they may have no memory. These behaviors can lead to serious injuries or death and include:

• Sleepwalking
• Sleep driving
• Cooking or eating food
• Making phone calls
• Engaging in sexual activity

The FDA advises that healthcare providers should not prescribe eszopiclone to patients who have previously experienced complex sleep behaviors after taking sleep medications. Treatment must be stopped immediately if these behaviors occur.

Safety Communications and Dosage Adjustments

In 2014, the FDA issued a safety communication warning that eszopiclone can cause next-day impairment of driving and other activities that require full alertness. Because the drug can remain in the system at high enough levels to impair function the following morning, the FDA lowered the recommended starting dose from 2 mg to 1 mg for both men and women. Patients are cautioned that they may still feel impaired the next day even if they feel fully awake.

Regulatory Classification

Eszopiclone is classified by the Drug Enforcement Administration (DEA) as a Schedule IV controlled substance. This designation means the drug has a recognized medical use but also carries a potential for misuse, physical or psychological dependence, and diversion.

Treatment of Insomnia

Eszopiclone is primarily prescribed to manage insomnia, a condition characterized by difficulty falling asleep, frequent nighttime awakenings, or waking up too early. It belongs to a class of medications known as non-benzodiazepine sedative-hypnotics. It works by slowing activity in the brain to facilitate sleep.

Sleep Benefits

This medication is used to improve various aspects of the sleep cycle. Clinical evidence indicates that eszopiclone can help with:

• Sleep Latency: Reducing the amount of time it takes to fall asleep after getting into bed.
• Sleep Maintenance: Decreasing the number of times a person wakes up during the night.
• Total Sleep Time: Increasing the overall duration of sleep to improve restfulness.

Usage for Sleep

Eszopiclone should be taken immediately before going to bed. It is essential that users have at least 7 to 8 hours available for sleep before they need to be active again. If a person takes the medication and wakes up before 7 to 8 hours have passed, they may experience memory problems or difficulty performing tasks that require alertness, such as driving. Additionally, taking the medication with or immediately after a high-fat or heavy meal may slow its absorption, causing it to take longer to work.