Zopiclone

This is one of the most prescribed medications for insomnia in the UK, as well as on a global scale. Its popularity exponentially grew because it was a much better, and safer solution compared to other drugs in this category, such as benzodiazepines.

Although zopiclone acts similarly to drugs such as Valium, it provides patients with targeted sleep benefits that can be felt right after their first dose. This medication improves rest onset, improves the quality of slumber, and the total resting time in diagnosed adults. However, these benefits do come with drawbacks and precautions that people have to be aware of.

This article will highlight all of the necessary information about zopiclone online, including how it works to the strict dosage guidelines that have to be followed.

Zopiclone PharmacologicalStructure and Profile

This medication is a non-benzodiazepine hypnotic, which is otherwise known as a z-drug. Collectively, this group of treatments are the preferred solution for conditions like insomnia in the UK. Zopiclone was actually the first Cyclopyrrolone that was created, meaning that it is chemically different from benzodiazepines, but acts through the same channels.

Much like benzodiazepines, this treatment also contains two mirror-image enantiomers, namely the r- and s-enantiomers. Zopiclone attaches to the same benzodiazepine site located on GABA-A receptors, but it has a slightly different binding orientation, which focuses its impact directly on the main sleeping subunit. This α1 subunit, when stimulated, is primarily responsible for the hypnotic and sedative effects being felt.

Once this medication is absorbed, it finds its way to GABA-A receptors. This is when it acts as a positive allosteric modulator in this region, which makes GABA signalling more efficient. As a result, more chloride ions flow into nerve endings and brain cells, which makes them less excitable and overall brain activity starts to slow down.

By focusing these effects on the α1 subunit, patients will be able to drift off much more easily at night. Even though it mainly targets sedation, zopiclone also has a mild effect on other channels, these subunits help with muscle relaxation and anti-anxiety responses, which then further enhance this experience.

Metabolism and Pharmacokinetics

Zopiclone is mostly metabolised in the liver through CYP3A4 enzymes, as well as CYP2E1 enzymes in minor amounts. This drug has a high lipid solubility, which means that it dissolves in fats and crosses the blood-brain barrier more easily, leading to the rapid effects being felt.

Liver, or hepatic, enzymes break down this medication, and then the remaining metabolites are flushed out by the kidneys. The body processes this treatment efficiently because only 5% leaves the body in the form of urine. This breakdown process heavily influences how long the medication lasts, and the tapering-off period from the peak effects to lingering traces of the drug.

The peak plasma concentration will happen in the first 1-2 hours after ingesting this medication, where the effects will be the strongest. The half-life of zopiclone is roughly 5 hours, which means that half of the medication is eliminated. The total active window of this treatment is 6-8 hours, meaning that there is a much lower chance of the sedative effects lingering into the following morning.

ComparingSedative Hypnotics

This table compares zopiclone online to other similar z-drugs that are popular in the UK. Zolpidem has the shortest onset, and the effects are very short-lived. Eszopiclone, which is a derivative, has the longest active window and a similar activation time.

This highlights that zopiclone is the most balanced medication in this class, giving people fast sedative results, with a duration that is ideal for a good night's rest. This medication's impact wears off before the patient wakes up, which ensures that they feel rested, without feeling drowsy in the morning.

This said, there are many off-label/secondary uses for this medication that are becoming more common in the UK. These all revolve around the condition of insomnia itself, but they are accompanied by various triggers. These include anxiety, stress, or situational insomnia. Although it is far rarer, some doctors administer zopiclone before a medical procedure for sedation.

Short-Term Insomnia Treatment Efficacy

This medication has been researched extensively, and the outcomes are overwhelmingly positive all around. A notable UK study posted on the NIH highlighted that in middle-aged patients, zopiclone proved to be a tolerable and effective treatment for insomnia.

There were multiple improvements that the participants saw. Overall, this medication significantly reduced the time to fall asleep, along with fewer instances of patients waking up at random points during the night. The participants also reported that they had better resting patterns and slept for longer durations with zopiclone.

All of this was achieved without any major disruptions to the patients' sleep architecture. Researchers noted that the second stage of slumber was extended. This is a crucial phase of rest in terms of memory consolidation and general bodily repairs. The REM cycle itself was marginally delayed; however, zopiclone did not reduce the total amount of REM stages throughout the night.

Efficacy Studies: Older Adults

While other medications can pose potential risks in the older generation, zopiclone is actually very suitable for this age group. Insomnia is a common condition in those aged 65 and older, and in fact, it affects more than 50% of elderly adults in the UK.

This medication is much safer compared to its predecessors, which are known to cause next-day tiredness and have a higher risk of unwanted side effects. On top of this, Wiley Library states that this treatment did not affect short-term memory, and adverse reactions were infrequently reported. There was little evidence of any withdrawal symptoms in elderly patients who used zopiclone correctly.

Even if these patients suffer from other health complications that contribute to insomnia, this treatment still works as intended. However, older patients must visit a doctor to receive the right dosage strength because this age group is generally more sensitive to medications in general.

Administration and Application Guidelines

For most patients who access zopiclone online in the UK, they will be able to manage their condition with the standard 7.5mg dose. Older patients, along with those with hepatic impairments, may have to start on a lower dose and only increase it if it is necessary.

Regardless of the zopiclone dosage strength, all patients should take their dose right before they plan on going to bed. This timing is essential as it will ensure that people sleep for a full 7-8 hours, and the medication does not cause a hangover effect.

The tablets should only be swallowed whole with water, and if patients eat close to their dosing time, the sedative effects may take longer to set in. For the best results, people should take their zopiclone treatment on an empty stomach.

Selection Criteria

UK doctors will only prescribe this medication to patients who meet the requirements for insomnia. This includes those who struggle with their resting patterns most nights of the week, and it starts interfering with moods or daily life overall. It is also important that these patients exhaust any other non-drug or natural approaches before starting a new treatment.

The ideal subjects for this medication include:

• Patients who routinely struggle with slumber and have a confirmed diagnosis
• Those who do not see improvements when adjusting their bedtime routine
• Individuals who are not currently struggling with substance abuse
• People who have relatively stable mental health

Moreover, zopiclone is not suitable for patients who have breathing issues, myasthenia gravis, or complex behaviours like sleep apnoea. Pregnant women or breastfeeding individuals should also steer clear of this drug.

Dependence is another vulnerability for some people, especially if they have dealt with substance abuse in the past. This risk also increases if patients take this medication after their prescribed treatment duration ends.

Zopiclone is designed as a short-term solution, and UK doctors, along with medical professionals around the world, will only prescribe it for 2-4 weeks at the maximum. If patients stick to this medication term, and take their personal dosage once a day, the odds of further health complications occurring become minimal.

Common and Serious Side Effects

New users who access zopiclone online can sometimes experience side effects in the beginning stages of the treatment. The most reported symptoms include a dry mouth, headaches, tiredness, and memory mishaps. Another reaction that affects up to 40% of patients is a bitter taste in the mouth that can linger for hours on end.

More serious side effects can also occur in some cases. Respiratory depression or failure can happen if this medication is mixed with other sedatives or alcohol. Abnormal night-time behaviours like sleepwalking are also possible, along with allergic reactions in the form of swelling or rashes.

Excessive tiredness is another potential risk. This is often accompanied by cognitive impairments and poor decision-making. If patients are struggling with this rare symptom, it is essential that they avoid driving or using heavy machinery until their bodies adjust to zopiclone.

Dependence and Misuse

Despite this drug having a lesser impact than benzodiazepines as a whole, there is still a risk of dependence, and it can become habit-forming. UK Addiction Treatment Centres outlines that some people can develop a tolerance to their zopiclone dosage, which leads to them taking more to achieve the same effects.

Ultimately, this sets people down the road of misuse, as their bodies need this extra quantity to function properly. Psychological dependence is a common outcome of this decision, as many people become anxious or worried if they do not take this medication.

The highest risk factors to be aware of include:

• Taking zopiclone for longer than 4 weeks
• Having a history of addiction
• Personality traits that align with dependence
• Using higher dosages than what was advised

Managing Withdrawal

Withdrawal symptoms are a frequent outcome if patients stop their zopiclone treatment abruptly after using it regularly. These symptoms can occur anywhere between 24-48 hours after stopping, and in some cases, they can last for weeks. The intensity and longevity of these symptoms depend on the dosage strength that was taken, along with how long the patient was using it for.

The most common withdrawal symptoms are nausea, vomiting, tremors, anxiety, excessive sweating, and insomnia rebounding. In difficult situations, seizures can occur, but this is mostly linked to patients who have taken zopiclone for long periods.

This is why doctors recommend a gradual tapering-off period close to when the treatment plan ends. Typically, patients should cut their dose by 25% each week, but some may need to follow through with this more slowly.

Public Health Concerns and Non-Medical Usage

The improper use of this medication has become a concern across the UK, especially since people can now find zopiclone online. This is often tied to mixing this treatment with other medications and substances, and taking it recreationally for long periods. This medication is a Class C controlled drug, meaning that it can only be prescribed by a doctor due to the risks of addiction.

Almost 635,000 adults use zopiclone without a prescription, and these nonmedical applications have unsettled many medical professionals across the country. Not only does it increase the risk of future health problems, but this trend highlights that there is not enough awareness around this medication.

This stresses the importance of strict medical interventions, and better access to zopiclone rehabilitation services to combat this widespread issue.

Signs of Non-Medical Usage

Many reputable studies across the UK have revealed that roughly 1.2% of people use zopiclone recreationally, which translates to the 635,000 figure mentioned above. Shockingly, these numbers are closely associated with other illicit drug usage, with some known heroin addicts also using this medication irresponsibly.

Part of this problem is the fact that zopiclone can be acquired much more easily than before. These nonmedical uses are often driven by getting this treatment through illegal UK internet pharmacies, or even through family and friends.

Some of the most telling signs that someone is using this drug include:

• Using this medicine outside of bedtime schedules
• Combining it with alcohol or other substances
• Consistently increasing the dose without medical approval
• Becoming secretive or defensive around the topic of this medication

Associated Dangers and Impact Socially

Unfortunately, zopiclone carries a greater risk of dependence than other z-drugs, such as zaleplon or zolpidem. If it is not used correctly, it can have a negative impact on daily life, and it poses a huge health risk for the individual, along with disrupting their social life.

Withdrawal symptoms, physical dependence, and cognitive impairment are some of the potential end results of misusing this medication. Overdosing is another concern that is common with mixing medications, which compounds on taking zopiclone in larger doses and for an extended period.

The social impact can be equally devastating. Relationships can become strained, and jobs can be harder to maintain or excel in. A complete retreat from social circles as a whole is a potential risk that these people face.

Recommendations and Prevention Strategies

The UK public health system has had to take drastic measures to reduce and prevent the irresponsible use of this medication, along with other z-drugs as well. This can include revised prescription management systems, patient education programmes and better monitoring of long-term applications.

These strategies can also include doctors and pharmacists going through dedicated training sessions that focus on dependence and misuse cues. Moreover, zopiclone online purchases should also have tighter regulations. Investigations into supply chains and surveying repeat purchases can assist in identifying the patients who need help.

These developments and improvements in these systems will ensure that zopiclone is well-understood, and UK-based prevention or rehabilitation measures can continue to be effective.

Reviewed by:

Dr. Ashish Dhyani, PhD, MSc, BMLT

Scientific Researcher & Medical Content Specialist