Drug Detail:Eszopiclone (Eszopiclone [ e-zop-i-klone ])
Drug Class: Miscellaneous anxiolytics, sedatives and hypnotics
1. How it works
- Eszopiclone may be used to help people get to, and stay, asleep.
- Experts aren't exactly sure how eszopiclone works but believe it has an effect on GABA receptors within the brain. This causes the release of natural chemicals associated with sleep.
- Eszopiclone belongs to the class of medicines known as sedatives (also called hypnotics).
2. Upsides
- May be used to treat insomnia. It reduces the time it takes for people to get to sleep and also increases the time they sleep for.
- Unrelated to benzodiazepines; however, it does appear to share some pharmacological properties with benzodiazepines.
- Decreases the amount of time it takes to fall asleep and helps people stay asleep.
- The recommended starting dose is 1mg. The dosage of 2mg should not be exceeded in elderly or frail patients, those with severe liver disease, or taking potent CYP3A4 inhibitors. The lowest effective dose should be used.
- Available in three strengths: 1mg, 2mg, and 3mg.
- Best taken without food because research has shown high-fat meals can result in slower absorption and reduce the effect of eszopiclone.
- Can be taken immediately before bedtime because it works quickly.
- Generic eszopiclone is available.
3. Downsides
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- A headache is the most common side effect reported. Other less common effects include a dry mouth, nausea, infection, dizziness, memory impairment, hallucinations, or impaired coordination.
- Causes drowsiness but this is the intended effect. Side effects can be more pronounced if eszopiclone is taken with alcohol or other sedating medicines.
- Sometimes, sedatives such as eszopiclone have been associated with abnormal thinking, behavior changes, or decreased inhibition (eg, extreme behaviors that are out of character).
- Do not drive or perform hazardous tasks after taking eszopiclone. Be aware that eszopiclone's sedating effects may persist until the next day - avoid driving and other unsafe tasks until you feel fully awake. The risk is higher if less than a full night's sleep remains when the person takes eszopiclone.
- May not be suitable for some people including those already taking medications that cause sedation, women who are pregnant, with a history of substance or alcohol abuse, or with a history of liver, lung, or breathing problems.
- Sleep disturbances may be a sign of other underlying problems such as depression or anxiety and all people requesting sleeping tablets should undergo a thorough evaluation for other comorbid conditions.
- May interact with some medicines including lorazepam, rifampin, antifungals, HIV drugs, antibiotics, sedating antihistamines, antidepressants, and opioid pain medications. Alcohol should not be drunk on the same evening that eszopiclone is taken.
- Elderly or frail people may be more sensitive to eszopiclone's effects. Taking a sedative, such as eszopiclone, increases the risk of falls.
- Has the potential to be abused. Extended or over-use may lead to dependence and tolerance. Rapid dose decrease or an abrupt discontinuation may cause withdrawal symptoms such as anxiety, abnormal dreams, nausea, and an upset stomach.
- Rarely, angioedema or anaphylactic reactions have been reported in people taking their first or subsequent doses of eszopiclone. If a severe reaction occurs, do not attempt to retreat with eszopiclone.
- Only available in tablet form.
- The safety of eszopiclone in children has not been established.
- Is a Schedule IV controlled substance which means it is considered to have a low potential for abuse relative to substances in Schedule III.
- Not recommended during pregnancy unless the benefits outweigh the risks. It is not known if eszopiclone is excreted into breastmilk.
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
4. Tips
- Always take the lowest effective dose. 1mg is generally recommended as a starting dose. Dosage may be increased to 2mg or 3mg (maximum of 2mg in elderly people, those with liver disease or taking certain medications) but be aware this increases the risk of next-day impairment of driving and other activities that require alertness. Higher dosages also increase the risk of dependence and addiction.
- Do not take with or immediately after a meal. Take immediately before bed as eszopiclone works very quickly. This will help decrease the risk of falling and other side effects.
- Do not drive after taking eszopiclone. You may still feel the effects of eszopiclone after you wake up in the morning, so do not drive or perform unsafe tasks until you are fully awake. The risk is greater with the 3mg dose.
- Do not take eszopiclone if you have drunk alcohol that evening. Do not drink any alcohol after taking eszopiclone.
- Do not take more than the recommended dose or take for longer than prescribed without checking with your doctor.
- Be aware that some people have performed certain activities such as sleep-driving, making and eating food, telephone conversations, and having sex while they were not fully awake after taking eszopiclone. Talk to your doctor if such an event happens to you.
- Eszopiclone can be addictive and you can become dependant on it if you take too much for too long. If your sleep does not improve within 7 to 10 days or worsens, talk with your doctor.
- Do not take eszopiclone if you have to get up earlier than seven to eight hours after going to bed. Do not take eszopiclone after midnight if you plan to awaken before 9 am.
- Talk to your doctor about the possibility of an underlying reason for your insomnia, such as anxiety or depression. Tell your doctor immediately if you experience any worsening of mood symptoms such as depression or suicidal thoughts.
- Talk to your doctor if you experience any unusual side effects such as abnormal thinking or behavioral changes or allergic reactions.
- Do not use eszopiclone at the same time as other sedatives. Talk to your doctor or pharmacist before taking any other medications, including those brought over the counter, with eszopiclone.
- Do not take eszopiclone if you are pregnant unless you have talked through the risks to your unborn baby with your doctor. It is not known if eszopiclone is excreted into breastmilk.
5. Response and effectiveness
- The peak effects of eszopiclone are reached within approximately one hour after oral administration.
- Effects of eszopiclone may be reduced if taken with a high-fat or heavy meal; therefore, it is best taken away from food.
- Research in people with transient and chronic insomnia has shown eszopiclone significantly decreased sleep latency (time to get to sleep) and improved measures of sleep maintenance (duration of sleep) compared to a placebo (an inactive medication).
6. Interactions
Medicines that interact with eszopiclone may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with eszopiclone. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Common medications that may interact with eszopiclone include:
- anti-anxiety medications, such as diazepam and oxazepam
- anticonvulsants such as valproate
- antidepressants, such as amitriptyline, imipramine, nortriptyline
- antihistamines that cause sedation, such as diphenhydramine
- azelastine
- barbiturates
- buprenorphine
- chlormethiazole
- duloxetine
- medications that induce or inhibit CYP3A4, such as carbamazepine, phenytoin, clarithromycin, itraconazole, ritonavir, rifampicin, or verapamil
- monoamine oxidase inhibitors, such as selegiline, isocarboxazid, or phenelzine
- opioid analgesics such as codeine, oxycodone, and morphine
- oral contraceptives
- melatonin
- muscle relaxants such as cyclobenzaprine
- probenecid
- scopolamine
- some medications used to treat mental illness, such as clozapine and thioridazine
- theophylline
- other medications that cause sedation, such as zolpidem.
Alcohol may worsen the side effects of eszopiclone such as drowsiness and dizziness.
A dosage adjustment may be necessary if eszopiclone is combined with other CNS depressants.
Note that this list is not all-inclusive and includes only common medications that may interact with eszopiclone. You should refer to the prescribing information for eszopiclone for a complete list of interactions.