Common Trade Names: Lunesta
Other Names: [(7S)-6-(5-chloropyridin-2-yl)-5-oxo-7H-pyrrolo[3,4-b]pyrazin-7-yl] 4-methylpiperazine-1-carboxylate
Eszopiclone is a sedative-hypnotic medication that is indicated for the treatment of insomnia among adults. It is a Schedule IV controlled substance and is associated with a significant abuse potential especially when taken in high doses. This can quickly result in the development of substance use disorder which must be treated at a qualified rehabilitative care center. Learn more about eszopiclone below.
A Brief History of Eszopiclone
Eszopiclone is a short-acting nonbenzodiazepine sedative-hypnotic agent. The drug has received the approval of the US Food and Drug Administration in 2004. In 2005, eszopiclone was introduced to the market under the brand name Lunesta. While eszopiclone was available in Europe in the past, it was ruled to be too similar to zopiclone, and was subsequently removed from circulation in 2009.
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How Does Eszopiclone Work in the Human Body?
The mechanism of action of eszopiclone as a hypnotic is believed to be related to its activity at the gamma-aminobutyric (GABA) receptor complexes close to benzodiazepine receptors within the central nervous system (CNS). Eszopiclone is a pyrrolopyrazine derivative of the cyclopyrrolone class. While it exerts the same effects as benzodiazepines, its chemical structure is different from benzodiazepines, barbiturates, and other hypnotic drugs.
The only indication for eszopiclone is for the treatment of insomnia, a sleep disorder that manifests as trouble falling asleep or staying asleep. Its only absolute contraindication is known hypersensitivity or allergic reaction to it or any of its components.
How Is Eszopiclone Taken or Administered?
Eszopiclone is available in 1mg, 2mg, and 3mg tablets. The recommended initial dose of eszopiclone is 1mg to be taken immediately before bedtime and at least seven hours before the planned time of awakening. The dose can be increased gradually to a maximum of 3mg. Sleep laboratory studies have shown that taking eszopiclone at bedtime decreases sleep latency, which is the time between being fully awake and falling asleep.
If insomnia persists after 10 days of eszopiclone use, presence of co-morbid diseases must be evaluated. Failure of insomnia to improve may indicate a primary medical or psychiatric disorder.
For people with a history of depression, the dose of eszopiclone must be kept to a minimum because it can worsen suicidal ideation and to avoid intentional overdose. If eszopiclone is to be discontinued, it should be done slowly over a period of several weeks to prevent withdrawal symptoms.
The maximum daily dose of eszopiclone must not exceed 2mg in the following patients:
- Geriatric or ill patients
- Patients with severe hepatic impairment
- Patients taking CYP3A4 inhibitors such as clarithromycin, erythromycin, ketoconazole, and verapamil
Clinical data among adults have demonstrated that blood levels of eszopiclone remain high enough the following morning (and up to 11 hours after administration). As such, it is not recommended to engage in activities requiring mental alertness, memory, and body coordination, such as driving a vehicle, during this time.
What Are the Immediate and Long-Term Effects of Eszopiclone Use?
The following are the most common adverse reactions seen in eszopiclone:
- Dry mouth
- Respiratory and viral infections
While it is uncertain whether eszopiclone is excreted in human milk, animal studies have demonstrated that eszopiclone may cause fetal harm. Thus, physicians must prescribe eszopiclone with caution to pregnant patients. Pediatric use of eszopiclone is also not well-studied, but limited evidence shows that eszopiclone can cause dizziness, hallucinations, and suicidal ideation among younger patients.
Eszopiclone can also cause rare yet serious side effects, including:
- Abnormalities in thoughts and behavior
- Aggressive behavior
- Excessively depressed mood
- Suicidal ideation
- Memory loss
- Severe allergic reactions that may present as swelling of the throat or tongue or difficulty in breathing
Most sedative-hypnotic medications, such as eszopiclone, are also associated with risky behaviors such as sleep-driving. Sleep-driving, or driving while being half-asleep after taking a sedative-hypnotic, may occur even at therapeutic doses. However, it has been found that taking eszopiclone in supratherapeutic doses or concomitant administration of eszopiclone with alcohol and other CNS depressants can increase the risk of these behaviors. Discontinuation of eszopiclone must be strongly considered if patients report sleep-driving episodes.
Overdose of eszopiclone is life-threatening and may manifest as exaggeration of the signs and symptoms observed in therapeutic doses or those mentioned above. It can also lead to a range of adverse effects related to impaired consciousness that may progress to coma and death.
Signs of Eszopiclone Use Disorder
Eszopiclone is a Schedule IV controlled substance under the Controlled Substances Act of the Drug Enforcement Agency. Clinical trials have demonstrated the abuse potential of eszopiclone especially in supratherapeutic doses and among patients with a history of substance abuse.
The Diagnostic and Statistical Manual of Mental Disorders – 5th Edition (DSM-5) Criteria for Substance Use Disorders (SUD) has listed 11 major pathologic behavioral patterns associated with eszopiclone use disorder, which can be grouped into four categories:
- Impaired control
- Social impairment
- Risky use
- Pharmacological indicators (tolerance and withdrawal)
The 11 criteria necessary for the clinical diagnosis of eszopiclone use disorder are as follows:
- Taking eszopiclone in supratherapeutic amounts or for a longer time than was medically prescribed
- Not managing to cut down on or stop eszopiclone use despite many attempts
- Spending a lot of time trying to get, use or recover from eszopiclone
- Feeling intense urges to use eszopiclone
- Eszopiclone use causes major problems in family and work obligations, such as absenteeism or poor work or school performance
- Eszopiclone use causes problems in interpersonal relationships
- Missing important social and recreational activities because of eszopiclone use
- Continued use of eszopiclone during high-risk activities such as while operating a heavy machinery or driving a vehicle
- Continued use of eszopiclone even if it worsens existing medical conditions or gives rise to new ones
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- Requiring higher doses of eszopiclone in order to achieve the desired effects (tolerance)
- Developing withdrawal symptoms after abrupt discontinuation of eszopiclone use (withdrawal)
Rehab and Treatment for Eszopiclone Use Disorder
Schedule IV controlled substances like eszopiclone are associated with a high risk for abuse and misuse that can lead to drug addiction. It is for this reason that Schedule IV medications are available only by prescription. In addition, unpublished data have shown that supratherapeutic doses of eszopiclone produce euphoric, habit-forming effects similar to benzodiazepines in benzodiazepine-dependent individuals. It was concluded that patients who have a history of substance abuse and are taking eszopiclone are at a greater risk for developing eszopiclone addiction. Thus, they must be under active surveillance during eszopiclone therapy.
Just like other substance use disorders, addiction to eszopiclone is highly treatable if caught early. Prompt recognition of the signs and symptoms indicating eszopiclone use disorder allows for early institution of therapy and positively impacts the patient’s recovery process.
In most cases, rehab and treatment for eszopiclone addiction begins with a process called detoxification, or detox. Detox refers to the elimination of toxic substances from the body to reverse drug dependence using medical and non-medical strategies.
Medical detox involves the use of pharmacological interventions to help flush out the accumulation of eszopiclone in the body. The general approach is gradual discontinuation of eszopiclone over a period of several weeks. Abrupt cessation of eszopiclone use is not recommended under any circumstance as this can lead to the development of life-threatening withdrawal symptoms. Drug replacement therapy can also be instituted. In drug replacement therapy, eszopiclone will be replaced with an alternative drug with the same efficacy but with a much lower abuse potential.
On the other hand, non-medical detox makes use of behavioral and psychosocial interventions to support the medical detox process. The goal of non-medical detox is to reduce relapse episodes by helping patients identify their relapse triggers and coming up with ways to cope with them in a healthy way. These programs also aim to provide emotional support to patients as they undergo the rehab process. Non-medical interventions include counselling, psychotherapy, and group therapy.
It is important to note that for any rehab program to be effective, it must be tailor-fit to the needs of the patient. A comprehensive patient evaluation consisting of complete history taking, physical examination, and laboratory workups must be undertaken before initiating any intervention. Moreover, clinical response must regularly be assessed to ensure that the rehab programs are still working for the patient. Modifications to or termination of any part of the rehab program may be done at any point during the treatment if deemed necessary.
Depending on several factors, rehab programs may be taken in an outpatient or an inpatient setting. Generally, outpatient therapy may be more appropriate for patients with only mild withdrawal symptoms or those who can guarantee compliance to treatment. In contrast, inpatient therapy should be strongly considered for patients with extreme addiction, patients with a history of non-compliance to therapy, and those with severe withdrawal symptoms.
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