Helping you with your sweet dreams: Lunesta fights off insomnia

Since time immemorial people have tried to understand sleep and the factors that influence it. From herbal potions to teas, different cultures have come up with natural concoctions that could delay or hasten the onset of sleep. In today’s world, almost no one is happy with the amount of rest they get. On the one hand, there are those, who have to drink more than 5 cups of coffee per day to remain functional and productive. On the other hand, there are those, who can only dream about falling asleep throughout the day and night. Which situation is better? Is it better to become sleepy early in the evening and fall asleep immediately as soon as you hit the hay? Or is it better to remain alert throughout the day and wait for a couple of hours past bedtime for sweet sleep? It is debatable since each thinks the grass is greener on the other side. However, it is understandable that these two problems share a strong association.

Once you do not get enough restorative sleep, you are bound to feel drowsy throughout the day. If you doze off multiple times a day, it is harder for you to fall asleep at night. People, who have to wait for more than a couple of hours per day to go to sleep, may have a case of insomnia. Doctors and experts classify it as a sleeping disorder that involves the inability to fall asleep, even when a person has enough time to do so. The affected feel stressed, fatigued, easily agitated, irritable and easily distracted throughout the day. For some, the cases are sporadic, and the causes vary from anxiety to change of daytime routines. Others, who have chronic insomnia, experience disturbed sleep for about three times a week. Chronic cases have various underlying causes including shift work, clinical disorders, mental or psychiatric disorders and unhealthy sleeping habits. These usually last for longer durations and command medical attention. More importantly, cases of sleeplessness can be comorbid. In such cases, it is difficult to pinpoint the exact cause-effect relationship.

Combating sleepless nights with Lunesta

Over 30% of the general population complains of sleep disturbances. Millions of people have insomnia. It prompts the question – is there a cure for the disorder? Understandably, it is impossible for a person to carry on daily work without sleeping soundly for weeks and, sometimes, months. Modern pharmacology and biochemical engineering have made it possible to design drugs that can help people with sleep onset. Lunesta is one such popular medication that doctors have been prescribing for more than a decade for treating symptomatic insomnia. Adults taking Lunesta have reported an improvement in their sleep quality, daytime productivity and onset time. It is a common drug for treating insomnia that affects the elderly population.

However, just like any other sleeping aid, there should be several indications and contraindications of the drug. Medicines work by intervening or decreasing one or multiple biochemical pathways in our body. That makes it necessary for every one of us to learn all that we can about the sleeping medication we are about to take to improve our rest quality. You must always ask yourself – “the new medicine can help me fall asleep faster, but at what cost?” So here we are, exploring all critical aspects of the medicine and its effect on our system, in the short term and long term.

What is Lunesta?

Lunesta is the brand name of the hypnotic agent Eszopiclone. It is a non-benzodiazepine hypnotic that medical practitioners and sleep experts have been using for almost a decade to treat chronic sleeplessness in patients. It is a stereoisomer of zopiclone. It belongs to the cyclopyrrolone class of sedatives. While it is readily available in the USA, it is not available in the EU due to its pharmacological similarity to zopiclone. As of May 15, 2014, the USFDA lowered the beginning dose of the drug to 1 milligram from 2 milligrams. It was after extensive study of the drug half-life showed that the consumers were unable to cope with the daily daytime activities after 8 hours of undisturbed rest. Since it works by interacting with the GABA receptors in the brain, it can impair all activities that require full alertness (driving and operating heavy machinery) and decision making.

What are the specific uses of Eszopiclone?

Zopiclone and its stereoisomer are highly active hypnotic agents that stimulate sleep. When the main complaint is the inability to fall asleep, patients often find relief from taking Eszopiclone for a brief period. The drug trial studies were controversial due to small sample (test group) size. The placebo response was questionable due to the low variance. Nonetheless, Lunesta has gained popularity over the years, but doctors do not recommend it for the long-term treatment of chronic insomnia in the elderly.

Doctors have been using a large percentage of hypnotic drugs like Eszopiclone to treat insomnia among the elderly population. This drug is not typical for the treatment of sleep deprivation in the young adults or the middle-aged. Most importantly, sleep experts should never prescribe this medicine for children at any cost. Besides the unwarranted side effects in the youth, the drug has not shown impressive improvements among them. In case, it is the drug of choice due to unavailability of other medications; the doctor should begin therapy at the lowest possible dose. That will minimize the side effects if any.

Research on long-term management of insomnia without the use of benzodiazepines and non-benzodiazepines, including Eszopiclone shows promise. That discourages long-term use and abuse of the drug due to increased chances of cognitive impairment, impaired motor coordination, and daytime sedation. The indications of long-term use and its relationship with effectiveness are not yet clear. There are several controversies about the effects of Eszopiclone on patient’s mental health. However, there has not been enough precise study to outline a strong relationship between Lunesta intake and the genesis of a psychological disorder. Several studies prove a strong bond between the medication and exacerbation of depressive symptoms in adults.

Amidst a lot of controversies, Lunesta has become one of the shining stars among the 3-Z drugs. Millions are regularly using it to get the rest and restoration they deserve. Every day, Eszopiclone, in different forms, is saving millions from collapsing due to fatigue, stress, and anxiety. Nonetheless, that is not reason enough to ignore the potential side effects of this medicine. So keep reading to find out the truth about the activity, efficacy, contraindications, and risks of taking Lunesta for treating insomnia.

What are the side effects of this non-benzodiazepine hypnotic drug?

Hypersensitivity to Eszopiclone is not uncommon, and it is undoubtedly a contraindication you should remember. Almost all sedatives and hypnotics in the market have some form of side-effect, whether it is in short-term or long-term usage. The recommended dosage and use of this medication depend on existing health conditions.

Here are a few instances that call for a reconsideration of Eszopiclone prescription –

1. Slow metabolism rate: people with a slower than average metabolism rate will find it difficult to eliminate the drug from their system within 8 hours. They are likely to suffer from a daytime impairment.
2. Liver problems: liver enzymes help with metabolizing the drug. People with liver function impairment will experience a longer half-life of the drug.

Here are a few side effects of the drug people may experience –

• Headache
• Peripheral edema
• Abnormal thinking
• Dryness of mouth
• Excessive thirst
• Rashes
• Alteration of sleep patterns
• Dizziness
• Drowsiness
• Chest pain
• Confusion
• Agitation
• Frequent and painful urination
• Amnesia

There are several contraindications of long-term usage of Eszopiclone that include –

• Stomach cramp
• Anxiety, nervousness, mood swings and irritability
• Vomiting and nausea
• Sleep activities (sleep talking, sleepwalking and sleep driving)
• Impaired concentration

Medication like Lunesta and Ambien are ideal for short-term treatment of insomnia. During the initial phases of trial and research, the experts tested them for long-term curative therapy. However, that does not make these hypnotics suitable for regular, extended period of use.

Can Eszopiclone cause dependence?

The Control Substances Act classifies Lunesta as a schedule IV-controlled substance. The regular use of benzodiazepines and non-benzodiazepine hypnotics can lead to psychological and physiological dependence among the consumers. As the dose of the drug increases, so does the chance of dependence. The duration of use contributes directly to the probability of addiction and dependence.

Research shows that the history of dependence is prominent among patients with a history of alcohol use and drug abuse. Additionally, most people develop a tolerance towards these hypnotic drugs, and that leads them to opt for successively higher doses. In fact, several people may develop a tolerance towards non-benzodiazepines in less than two months.

Individuals with a history of benzodiazepine abuse, use Lunesta for its hallucinogenic effects. Research on the addiction and abuse of this compound shows the high potential for the same. An individual addicted to it may do the following –

1. Continue the prescription long after the expiry of the prescription.
2. Forge prescriptions to acquire the medicine from pharmacies.

• Opt for higher doses due to the quick tolerance buildup.

1. Consume it with alcohol and other hypnotics to increase its effects.
2. Resist falling asleep to experience the hallucinations.

There have been cases of people taking Lunesta at 6 mg and 12 mg doses regularly, which produce effects similar to 20 mg of diazepam. Experts have also noted the coincidence of such high doses with chronic anxiety, amnesia, sedation, and hallucinations.

Can people overdose on Lunesta?

It is possible to overdose on non-benzodiazepines like Lunesta. According to the US Prescribing Information, people have overdosed on up to 90 times the prescribed dose of the medication but have made a full recovery after medical intervention. As per the reports from the same authorities in 2014, the fatalities in case of Lunesta overdose are common with coincidental alcohol abuse only.

The overdoses are not always intentional. Since people develop tolerance to this medication fast, it is common for them to try out higher doses. It can lead to accidental overdose. Timely detection and medical attention can prevent physiological damage. Activated charcoal and gastric leverage are standard procedures for the treatment of an overdose in adults. Doctors often treat an overdose with Flumazenil.

Overdose symptoms can vary from mild to severe, depending upon the quantity of intake. From unnecessary confusion and grogginess, it can escalate to loss of consciousness and short-term amnesia. Severe overdoses can lead to slowed breathing, a sharp drop in blood pressure and insufficient supply of oxygen to the brain and other vital organs. Without proper medical attention, Lunesta overdose can lead to brain damage, coma, respiratory damage and even death.

As of last year, there were over 600 isolated cases of Eszopiclone. Most of these cases were attempted suicide. However, the percentage of fatalities was significantly low due to the treatability of Lunesta overdose.

How does Lunesta interact with other drugs and substances?

When individuals take Eszopiclone along with other sedatives, antipsychotics, opioid, and antidepressants the risk of central nervous system depression (CNS depression) increases significantly. It also interacts with anti-histamines or allergy medications.

Several medications that suppress the secretion of the CYP3A4 enzyme from the liver can cause high chances of CNS depression. The inhibiting medications include ketoconazole, clarithromycin, itraconazole, ritonavir, and nelfinavir.

Alcohol and opioid have additive effects on Lunesta. Cough relievers like codeine and hydrocodone can increase the impact of it as well. Marijuana, sleep-inducing drugs like alprazolam and lorazepam, and muscle relaxants can interact with Eszopiclone.

Is Lunesta the best medication for insomnia?

Finding medication to treat insomnia or sleep deprivation is not tricky at all. In fact, it is a bit too easy to come across a considerable variation of drug types that can reduce sleep latency. Most doctors prescribe a generic version of Ambien, Lunesta or Sonata. If you are currently under treatment for insomnia, you are likely taking Zolpidem, Eszopiclone or Zaleplon. These are the three most popular and well-researched z-drugs in the market. These are all non-benzodiazepines that can induce sleep by producing a hypnotic effect. They have lower dependency levels as compared to benzodiazepines.

The dilemma lies in the condition or environment of the sleep studies. There is extensive documentation on the actions, interactions and side effects of popular sedatives like Ambien or sonata or Lunesta, but the companies have conducted the trials inside sleep laboratories, which are akin to luxury motels. The conditions of experimentation and tests are different from real life, where a person might have to awake multiple times per night to adjust temperature and humidity. These laboratories are unfamiliar, so they are likely to exacerbate cases of anxiety that compels higher doses of any hypnotic.

Real life data will vary considerably from the lab data. Here’s a brief glimpse of the kind of data the researchers have collected from the real world –

1. People between the age of 35 and 54 years stated that Sonata and Ambien worked equally well.
2. Participants above the age of 55 years found Lunesta worked best for them.

• The participants also stated that Lunesta had the least side effect among the three z-drugs.

This study involved 414 respondents. It revealed that Lunesta gets an average of 55% of the score and Ambient works for 67% of the time. That leaves a lot of people awake, and craving rest at night. Even with regular medication, people find it difficult to fall asleep. Several studies in Japan showed that at doses of 2 mg or higher, Eszopiclone is more effective than Zolpidem. The effect was wholly dose-dependent, and the advantage of it vanishes once the amount is lower than 1 mg. The same study also reported a higher incidence of morning drowsiness, confusion and lower levels of alertness in people taking the higher quantity.

It is difficult to say which drug is the best since there are several factors one has to consider during a comprehensive comparison. Therefore, for some people, Lunesta might be the best option due to its short-term effectiveness and high power by reducing sleep-onset latency.

Who should be using Lunesta?

Doctors recommend using Lunesta when they require a rapidly acting hypnotic. It is not a permanent solution to your sleep problems. Here are a few situations where your sleep therapist or physician is likely to prescribe Lunesta –

1. You are staying up until late every night (challenges with sleep onset)
2. You have trouble getting proper uninterrupted sleep.

• You frequently wake up early in the morning, and you cannot go back to sleep.

In all three cases, one common result is excessive daytime sleepiness and chronic fatigue from not getting enough rest at night.

Who should not be using this sedative?

Like all medicines, Lunesta can cause allergic reactions in few. If you are allergic to Eszopiclone or any other component in it, you should not be taking Lunesta. It is not suitable for everyone. If you have one or more of the following conditions, you should speak with your doctor immediately before starting therapy –

1. You have a history of mental illness, depression or recurring self-destructive or suicidal thoughts.
2. You have experienced liver disease.

• You have a history of alcohol abuse or drug abuse or any other addiction.

1. You are pregnant. It is a Category C drug, and its effects on the unborn baby are unknown.
2. You are breastfeeding. It effects of Lunesta on lactation and the quality of breast milk is unknown.

You should always disclose information about other pain medication, vitamin or antidepressants you are taking. It can interact with a plethora of other drugs and compounds.

What is Lunesta’s mechanism of action?

Sleep is a result of complication actions and interactions in our body. The brain is the most complex organ and interjecting its sleep mechanism is never easy. A few medications like Lunesta can improve the quality and duration of sleep but understanding the biochemical reaction of the same is of paramount importance to judge its efficacy and risks.

Eszopiclone works as an agonist for the GABA receptor in the brain. It binds to the GABA molecules and prevents their direct binding to the receptors. As a result, the availability of these molecules increases and this results in the onset of sleep. It is quite similar to many anti-anxiety medicines that work by adjusting the interactions of the GABA molecules and their receptors in the brain.

Lunesta is a very fast acting drug. Therefore, you should take it only when you are ready to go to bed. Unless you have 7 to 8 hours in hand to sleep at a stretch, you should not be taking the medication. Scientists and doctors don’t yet know the complete mechanism of action of Eszopiclone, but they recommend a dosage below 2 mg for adults. It is safe to say that this drug treats symptomatic insomnia and it does not address the underlying issues (psychological and physiological) that cause it.

What should you do in case you have missed a recommended dose of Lunesta?

You should always take it immediately before you go to bed. Taking it after the heavy meal or excessively fatty food can reduce its affectivity. If you miss a dose or if you realize late at night that you have forgotten to take the recommended dosage, do not consume the missed Lunesta dose unless you have 7 to 8 hours to sleep it off. It is imperative that you do not take an extra amount of the medication to make up for the missed dose.

Is it possible to stop taking Eszopiclone?

Since Lunesta and other brands of Eszopiclone are highly addictive, it is critical not to take them for an extended period. Although it is safer than contemporary non-benzodiazepine sedatives, it can pose a severe threat of addiction and abuse. As per the 2013 report from CDC, 4% of US adults over the age of 20 years abuse prescription pills on a daily basis. Sudden withdrawal from the medication can elicit the following symptoms –

1. Increased anxiety and irritability
2. Abdominal cramps, upset stomach, nausea, and vomiting.
3. Dizziness, confusion, trouble sleeping and mood swings.
4. Tremors and hypersensitivity of skin.
5. Depression, suicidal thoughts, self-destructiveness and trouble concentrating.
6. Sweating, headaches, fatigue, and neurosis.

The symptoms can vary from person to person, and the intensity can depend on the extent of abuse. It is possible to wean off the medication by speaking with your doctor and consulting a psychologist. They usually recommend gradually lowering the dose of Eszopiclone till you are not dependent on it anymore.

What is the effect of Eszopiclone on mental health?

According to the Substance Abuse and Mental Health Services Administration, there are around 8 million adults in the USA, who suffer from co-occurring substance abuse and mental health disorders. If you have a long history of psychological challenges, you should talk at length with your doctor and psychiatrist before starting Lunesta.

Case studies of the effect of Eszopiclone on patients with schizophrenia show that it is a safe drug that is suitable for the treatment of insomnia. That was a result of a double-blind, randomized study that does not show any effect of this compound on the cognition of the subjects. In fact, there is not much evidence to outline the relationship between Lunesta and insomnia in schizophrenic patients.

There are instances of Eszopiclone making cases of depression worse. People with mental health disorders including recurring bouts of depression, and anxiety can experience deteriorating symptoms during treatment. Studies show that they can find themselves thinking about suicide or self-harm during this period. People also experience abnormal thoughts and exhibit increased agitation while taking this drug. Additionally, there can be unusual behavior changes. The mental health implication of Lunesta is quite expansive, and you need to understand the cost of getting uninterrupted sleep.

How should you take this sleeping medication?

You should follow the advice of your sleep expert or general physician closely. Always take it before you head to bed with a glass of water. Most modern sleep medications come in the form of extended-release tablets that you should not break in half or bite through or grind.  The recommended dose for adults is between 1 mg and 3 mg. You should take the pill(s) at one go. The total dose should never exceed 3 mg as per the updated recommendations.

The medication can lose its activity and effectiveness if you do not store it in the right conditions. Find a cabinet or storage drawer that is between 59-degrees to 86-degrees Fahrenheit in temperature. Do not keep it in a humid place or an area that receives direct sunlight. Never consume Lunesta if it has crossed the date of expiration.

Taking this medication after a heavy dinner can delay its action by slowing its dispersal and absorption. The mechanism of this drug is still unknown, but research has seen that consuming a high-fat diet for taking Eszopiclone can cause delayed effects.

You should never take this medication in the afternoon. If you are recovering from a recent change in shift or suffering from jetlag, always speak with your sleep expert to understand the implications of this medication on your physical and psychological health.

What is the most critical information you should know about Lunesta?

Lunesta has been around for almost a decade, but the presence of multiple opinions and controversies make it necessary for you to know a few facts about the medication before consuming it.

• Eszopiclone uses several inactive ingredients, and you can get severe allergic reactions to any of them. It uses lactose, microcrystalline cellulose, polyethylene glycol and hypromellose. If you have known allergies to any of the compounds, you should speak with your doctor before taking the pills.
• It works fast, and you should never take this medication on your way home from the office or while operating machinery at home before bedtime. Always pop it when you know you have 7 to 8 hours in hand to sleep it off.
• There have been cases where people have taken the medication and then engaged in walking, holding phone conversations, eating and even driving, but without the memory of it.
• Without proper time to sleep it off, you can experience dizziness, drowsiness, lethargy, cognition impairment and short-term memory problems on the very next day. These are severe challenges in case you have to drive far for work, or you have to handle heavy machinery during work hours.
• Drinking alcohol is very risky while you are taking Lunesta. In can increase the activity of the medication and it contributes to increased side effects. Taking it with other opioid and muscle relaxants can create an unpleasant hallucinogenic effect that can add to dependence and addiction.
• Prolonged usage often builds tolerance in adults and people are more likely to increase the dose without consulting their physicians to experience better sleep. That poses threats of overdosing as well as dependence on everyone.
• You should never stop taking the medication suddenly, especially if you were taking a higher dose. Weaning off is the better option since sudden cessation can lead to intense withdrawal symptoms, similar to the kind opioid withdrawal causes.
• People suffering from lung problems including bronchitis, bronchial pneumonia, and chronic obstructive pulmonary disease (COPD) and asthma should refrain from taking Eszopiclone.
• In case, the symptoms of insomnia do not go away with 7 to 10 days of constant Lunesta use; you should talk to your doctor. Sometimes, when the medication does not work, it can elicit adverse effects like increased sleep onset delays, or more extended bouts of insomnia can result from drug interactions.
• Never share this medication with a friend or family member, who might have symptoms similar to yours. It is a drug of abuse, and it is against the law to share Eszopiclone with others. Always keep this medication out of the reach of children and teenagers.

You must always remember that medications belonging to the category of benzodiazepine and non-benzodiazepine hypnotics can be highly addictive. Almost all of them have side effects. If there are other ways to overcome your sleeping disorder you should always try them before resorting to Eszopiclone. Lunesta is not the one-stop solution for all sleep deprivation problems, and you should not treat it as one.