What is Zopiclone?
Zopiclone (Zimovane & Imovane) is a non benzodiazepine z-drug and hypnotic used to treat insomnia. We all need sleep to rest, repair, and prepare for the stresses and strains of the next day. A person's health, work, and family can suffer when they don't get a good night's sleep.
Approximately 33% of UK residents suffer from insomnia or some other form of sleeping disorder, and it is rapidly becoming a major public health issue. Rather than experiencing the normal sleep cycle, around 13 million people are suffering from the vicious cycle of an overactive brain, which leads to poor sleep, stress, and anxiety.
Chronic insomnia, which leads to chronic sleep deprivation, can be destructive for the sufferer's health and overall well-being.
The main cause of primary insomnia is a lack of melatonin in the brain, which is a hormone that controls sleeping and waking cycles. This results in the brain being disrupted when trying to fall asleep.
CNS drugs like benzodiazepines have been used for many years and are effective in inducing sleep. (Mostly used for short-term treatment of insomnia).
Pharmacological properties of Zopiclone are similar to other sedative hypnotics, derived from the benzodiazepine class.
Central nervous system (CNS) depressants are a diverse group of drugs that reduce brain activity, slowing down responses in the brain and body. In low doses, they can cause relaxation and sleepiness.
Psychiatric disorders are the most common cause of insomnia around the world, and they affect around 12% of all patients.
Zimovane and Imovane are brand names of the active ingredient zopiclone, not benzodiazepines, which are old-school sleeping aids.
This non-benzodiazepine sedative was developed by Rhone-Poulenc in 1986 and has proven to be effective as a sleep aid (hypnotic effect).
Pharmacological action of Zopiclone is due to the ability of the drug to act on GABA receptor.
Zopiclone is used for the short-term management of insomnia, to relieve symptoms of anxiety and to promote sleep.
Effects of Zopiclone in the Brain (Mechanisms of Action)
Sometimes called a "Z drug", it works by relieving anxiety and enhancing the effectiveness of gamma-aminobutyric acid (GABA) in the brain. It reduces the activity of the nervous system by blocking some of the brain's signals.
GABA is an inhibitory neurotransmitter (one that slows down the brain) that has been found to be deficient in insomniacs.
The activity of GABA increases when the Zopiclone molecule binds to GABA receptors in the brain, which leads to a sedative effect. Treatments for insomnia often use GABAergic drugs (hypnotic drugs) such as diazepam to increase activity of GABA receptors in the brain.
Metabolism of Zopiclone
Zopiclone has a high protein binding. This means it will be mainly metabolized by your liver, which is responsible for the majority of drug metabolism.
Cytochrome p450 3A4 is the enzyme which metabolizes Zopiclone into its active metabolite, Imovane.
People with insomnia and other sleeping disorders benefit from this medication because it helps them fall asleep quickly and gives them 8-9 hours of sleep without waking up.
See Our Other Zopiclone Resources
- Who can and cannot take Zopiclone
- How is Zopiclone Effectiveness Compared to Other Drugs?
- How and when to take Zopiclone?
- 7 Things to Avoid while taking Zopiclone
How does Zopiclone Work?
Basically, it works by affecting the way signals are sent to the brain, causing sleepiness. In addition to reducing the time you need to fall asleep, it increases the amount of time you spend sleeping.
There are no adverse effects associated with pharmacologic agent Zopiclone, more so it is safe to use for most people than other medications for insomnia.
Zopiclone abuse may cause dependence on the drug and prolonged withdrawal effects—avoid misuse of zopiclone.
Since your body becomes dependent on Zopiclone, you should taper off the dosage very slowly. This will prevent any withdrawal symptoms (Withdrawal effects can be very uncomfortable).
However, the dependence potential of Zopiclone is considered low. (This means that its withdrawal symptoms are unlikely to be unpleasant and do not last for too long).
Zopiclone can cause rebound insomnia when the drug is abruptly discontinued, so doctors encourage people to taper off the drug.
Physical dependance of the drug Zopiclone is rare and if occurs, it gets reversed when the drug treatment is stopped.
Zopiclone Benefits—Consumer Information
Insomnia and poor sleep are relatively common and usually don't last long. Continuous sleep deprivation can, however, have negative effects such as mood changes, lack of motivation, irritability, and fatigue. As the ability to concentrate will be reduced, drowsiness during the day may hurt your social life and occupation.
When you take the pharmacologic agent zopiclone, you can get the rest your body needs, reducing or eliminating the negative effects of lack of sleep.
Are there Side Effects?
Just like after any other drug interactions with the body, it may cause some mild effects.
Some people experience dizziness or drowsiness during treatment and for a short time after it is stopped. You may feel tired, chilled, risk of falls, shivery or hot. You may have muscle stiffness or cramps. Some people will have an upset stomach and diarrhea.
Do not drive (impairs driving ability), operate machinery or engage in other potentially dangerous activities until you know how Zopiclone affect you.
Rebound effects are not common with Zopiclone, but they can occur. This is the case when a patient no longer has a drug at the time of waking and withdrawal occurs. Drug abusers experience this often.
How do I take Zopiclone?
Take the tablet whole with a glass of water. It should not be crushed, broken, or chewed. Meals can be taken with or without the tablet.
Take the missed dose only if you can still get 7-8 uninterrupted hours of sleep if you forget to take it before bed. It is best not to take a dose if this is not possible. Next night, you may take the dose of zopiclone as usual.
Forgetful doses should not be made up with double doses.
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An effective dose will help you sleep without waking up. However, this is only the case if you take Zopiclone as prescribed.
What is the dosage for Zopiclone Tablets?
Zopiclone 3.75mg / 7.5mg
Zopiclone is available in two strengths: 3.75mg and 7.5mg. Healthcare professionals will determine which strength is suitable for you based on the severity of your condition.
Before going to bed, take one tablet. To prevent your body from becoming dependent on the drug, you may only need to take a tablet twice a week.
Patients who suffer from temporary insomnia, as well as those who suffer from longer-term insomnia, can benefit from the use of Zopiclone. As well as helping you sleep (improving sleep), Zopiclone can also be prescribed under the brand name Zimovane.
Diazepam is another popular sleeping medication. Diazepam (Valium) is prescribed for insomnia caused by anxiety.
Depending on the doctor's recommendation, Zopiclone and Zimovane can be used in adults for up to four weeks. It is usually recommended that you take Zopiclone for no longer than 4 weeks, as prolonged use may result in it not working as well as it once did, and you may become dependent on it.
Elderly patients are advised to start with a lower dose (3.75 mg) and titrate upwards slowly.
Please stick to the recommended dose for better results, or else can cause, increased risk of overdose – people can build up a tolerance to CNS depressants and end up taking more than the recommended amount.
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It is usually recommended that you take one 7.5mg tablet just before going to bed. It takes about an hour to work. If you are over 65 years old or have kidney or liver problems, a lower dose of 3.75mg may be recommended. In these cases, lowering the dose reduces the risk of excessive sleepiness.
Abuse of zopiclone can lead to symptoms such as chest pain, heart palpitations, nightmares, amnesia, abdominal pain, constipation, sinusitis, sore throat, dry mouth, lethargy, back pain, flu-like symptoms, dizziness, and depression.
Zopiclone may interact with any of the following:
- An alcoholic beverage.
- Anxiety medications (e.g., alprazolam, clonazepam, lorazepam)
- Medications that prevent seizures, such as phenytoin, valproic acid, carbamazepine, and gabapentin.
Typically, you shouldn’t use zopiclone more than seven to ten days at a time. It is not advisable to stop taking this medication suddenly if you have been taking it regularly for a long time.
Instead of using zopiclone every night, use it only two or three nights per week to reduce the risk of dependence. Use zopiclone only if you cannot fall asleep using sleep hygiene techniques first, and then zopiclone if you can’t.