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Melatonin is a natural hormone produced by the body. Synthetic melatonin is used as a medicine to help the body adjust the internal clock. It is used by people who suffer from jet lag, to adjust the sleep pattern as a result of work schedule changes, and to help blind people establish a day and night cycle. Melatonin can also help those who are suffering with insomnia.
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Circadin Melatonin Sleep
Circadin Melatonin Sleep is used for short-term treatment of primary insomnia in people aged 55 years and older. Primary insomnia means that there is no identified cause, including mental, medical or environmental.
For Circadin Melatonin Sleep to work, it has an active ingredient called melatonin. Melatonin belongs to a natural group of hormones produced by the body that helps control the daily sleep-wake cycles.
Circadin is available as Circadin tablets; white to off-white, round biconvex tablets. Each of the Circadin tablets contains 2mg of melatonin.
The Circadin tablets are packed in PVC/PVDC opaque blister strips with aluminium foil backing. The pack consists of one blister strip containing 7, 20 or 21 tablets, or two blister strips containing 15 tablets each (30 tablets)
Circadin Dose – How to Use
Circadin Dose – How to Use should always be taken exactly as your doctor or pharmacist has told you. If you are unsure about any of the instructions check with your doctor or pharmacist for further clarification.
The recommended Circadin dose – how to use is one tablet per day, taken orally, after food, one to two hours before bedtime. This dose can be continued for up to thirteen weeks. The tablet should be swallowed whole and should not be crushed or cut in half.
Circadin 4mg or 2mg
The difference between Circadin 4mg or 2mg doesn’t exist. Circadin 4mg isn’t an available dose and has never existed. The only dose of Circadin available is 2mg.
If you are still unsure about Circadin 4mg or 2mg, please check with your doctor or pharmacist for further explanation.
What Is Melatonin Circadin 2mg Used For? Circadin Jet Lag
A question we are often asked is ‘What is Melatonin Circadin 2mg Used for?’
One of circadin primary uses is using it as treatment for insomnia. It can help you fall asleep and also stay asleep, rather than waking early.
However, Circadin Jet Lag can be used to relieve the effects of jet lag. As long as it’s used with good judgement, Circadin Jet Lag can help regulate the human circadian rhythm by working as a darkness signal. Using it can depend on where a person is traveling; traveling eastward it can be taken en route, 30 minutes prior to the target bedtime at the destination; it does not need to be taken for westward travel.
For more information about what is melatonin circadin 2mg used for, click here.
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Melatonin Modified Release – Melatonin UK Tablets
Melatonin Modified Release is a formulation that helps treat sleep disorders such as insomnia. The melatonin UK tablets are usually the brand called Circadin 2mg.
The melatonin modified release tablets contain the natural hormone called Melatonin. Produced by the pineal gland in the brain, it can help you fall asleep, however just melatonin alone won’t knock you out. It simply lets your body know that it’s night time and it’s time to fall asleep.
Melatonin UK Tablets can also provide other benefits such as anti-oxidants, support eye health, stomach ulcer treatment, heart burn and ease tinnitus symptoms.
By using Melatonin Modified Release it also helps bind receptors in the body, allowing you to relax. Such receptors in the brain can help reduce nerve activity and in the eyes it can help reduce dopamine levels, a hormone that helps you stay awake.
“I’ve tried numerous prescription sleep aids. I’m on 50 mg of Adderall throughout the day so I definitely have trouble winding down at night. Ambien and similar prescription medicines only made the insomnia problem worse, buy adding hallucinations to the mix. A friend recommended I try Melatonin. It’s fairly inexpensive, and if I take 3 about 30 minutes before bed I have a full night’s sleep and feel rested in the morning. No weird side effects, like I experienced with the prescriptions I’ve tried. Works much better than Unisom or Tylenol PM. I suggest it to everyone I know having sleeping issues.”
Like all medicines, this medicine can cause side effects, although not everybody gets them.
If you experience any of the following serious side effects, stop taking the
medicine and contact your doctor immediately:
Uncommon: (may affect up to 1 in 100 people)
– Chest pain
Rare: (may affect up to 1 in 1000 people)
– Loss of consciousness or fainting
– Severe chest pain due to angina
– Feeling your heartbeat
– Visual impairment
– Blurred vision
– Vertigo (a feeling of dizziness or
– Presence of red blood cells in the
– Reduced number of white blood
cells in the blood
– Reduced blood platelets, which
increases risk of bleeding or
If you experience any of the following non-serious side effects contact your
doctor and/or seek medical advice:
For a full list of side effects please see patient information leaflet.
What is Circadin®?
Circadin® 2 mg is a prolonged release formulation of highest grade of pure melatonin (the prolonged release mechanism of Circadin® is due to a polymer matrix), indicated for primary insomnia characterized by poor quality of sleep in patients who are aged 55 or over1. The melatonin in Circadin® is a synthetic molecule, 100% equal to the human melatonin molecule (N-acetyl-5-methoxytryptamine) .
How does melatonin help me to sleep?
Melatonin is a natural hormone released in the body during the evening and night, signaling ‘darkness’, associated with sleepiness and the sleep-wake cycle. Thereby melatonin facilitates the feeling of sleepiness and the ability to induce and maintain sleep.
Melatonin is a naturally occurring neuro-hormone mainly released from the pineal gland in the head in the evening and during the night1 2 3. Melatonin signals ‘darkness’, is associated with feeling sleepy, and regulates the sleep-wake cycle1 2 3 4.
Individual levels of melatonin vary, but it has been found that otherwise healthy people suffering from insomnia often have lower levels of melatonin than people without insomnia, and that melatonin therapy ameliorates the symptoms of insomnia5. Circadin® is prolonged-release melatonin, which adds exogenous melatonin to the endogenous melatonin throughout the night, thereby facilitating the feeling of sleepiness, the ability to fall asleep, and improving sleep quality and daytime functioning1.
How does Circadin® work compared to other melatonin formulations?
Circadin® is a prolonged-release formulation of melatonin, which circumvents the fast clearance of the hormone by releasing the melatonin over an extended period of time12, thereby mimicking physiological patterns of melatonin secretion. Administration of exogenous melatonin does not affect the endogenous secretion of melatonin14. Other melatonin formulations are immediate-release – meaning that they are rapidly absorbed and metabolised with an elimination half-life of ~60 minutes15. Following oral administration of immediate-release melatonin, peak plasma levels that are 5-10 fold higher than those of Circadin®, are reached after ~50 minutes15, rapidly falling off again due to the first-pass hepatic metabolism. Immediate-release melatonin is quickly cleared from the circulation. The differences in the effects of fast vs slow release formulations is best exemplified by their effects on the blood pressure rhythm. Whereas Circadin improves blood pressure control in nocturnal hypertension fast release formulations are not efficacious16. Despite common beliefs, the effect of Circadin® on sleep latency is no less than that of fast release melatonin because the brain is very sensitive to low doses of melatonin in the beginning of the night17 11.
In a study that was performed in the UK in order to assess the efficacy and safety of melatonin in treating patients with REM sleep behaviour disorder it was found out that Circadin® is more effective than standard melatonin preparations (Freeman A, Muza R, Leschziner G, et al. Sustained Release and Standard Preparation Melatonin for the Treatment of REM Sleep Behavioural Disorder. Sleep 2011; 34: A197-A198).
What are the most important benefits to patients?
Circadin® provides good quality natural sleep for patients, while offering an effective and safe treatment for their sleep problems, unlike old common sedative treatments.
Untreated insomnia may lead to various health problems6 7. Market research has shown that many people suffering from insomnia are reluctant to take sleep medications due to fear of dependency and side effects. Therefore, many patients, although suffering with the consequences of insomnia, e.g., fatigue, low daytime performance and even anxiety and depression, do not seek medical consultation but use various over-the-counter (OTC) and herbal remedies, and even alcohol, with limited efficacy at best9 10.
Circadin® decreases time getting to sleep, improves Quality of Sleep, Quality of Life and next-day alertness, while maintaining a very good safety profile5, with no evidence of dependence.
When is it recommended to take Circadin® before bedtime? Circadin® and food intake?
The recommendation according to SPC (Summary of Product Characteristics) is as follows:
“The recommended dose is 2 mg once daily, 1-2 hours before bedtime and after food”1.
In the PK studies a meal was served 1/2 an hour before drug administration – the meal was not big and contained fat. The patients were instructed to have a light meal before (30 minutes) they take Circadin®. If Circadin® is ingested on an empty stomach it will have a somewhat faster release.
How quickly will Circadin® make me fall asleep?
Circadin® should not be considered a traditional ‘hypnotic’ as it is not a CNS depressant and does not work on the same receptors, causing much less side effects, and improving the sleep quality over time 60 . In line with this, Circadin® should not be taken ‘as needed’, but in a course of 3-13 weeks1.
Will Circadin® work on the first night?
Onset of sleepiness occurs about 1–2 hours after taking Circadin®1, due to the sleep-promoting effect of melatonin. As Circadin® efficacy is measured as improvement in quality, rahter than quantity of sleep, this improvement has not been measured on a day-to-day basis, but a baseline, and again after 3 weeks and then up to 6 months11. This is similar to other disease areas, e.g., depression and hypertension, where full treatment effect is expected after days or weeks, as the body adjusts to the treatment. It is, therefore, recommended to take Circadin® at the same time every night, continuously for 21 days50. Benefit may be greater with continuous use of up to 3 months.
It is important to realise that, while historically, the treatment of insomnia has involved achieving a rapid CNS suppressant effect by using CNS depressants such as BZDs or ‘z’-drugs, Circadin® represents a new paradigm in the treatment of insomnia, in which treatment of insomnia with poor Quality of Sleep must be approached with the same expectations of gradual improvement as many other diseases, and not a quick ‘knock out’ effect.
How is Circadin® metabolised and how long does it stay in the body?
Circadin®‘s prolonged-release formulation releases melatonin gradually over 8-10 hours, providing a terminal (apparent) half-life of 3.5–4 hours12. The released melatonin is rapidly metabolised by the liver (half-life 40–50 minutes)12 1. The principal metabolite is 6-sulphatoxy-melatonin (6-SMT), which is inactive and accounts for ~80% of the dose excreted in the urine1. Excretion of the metabolites is completed within 12 hours after ingestion12.
Does the use of Circadin® make the body less able to manufacture its own melatonin; i.e., does the natural melatonin system ‘switch off’ and, if so, does it switch back on again when Circadin® treatment is stopped?
Should melatonin levels be measured prior to treatment with Circadin®?
The age-related decline in melatonin production, that is proposed to contribute to poor sleep quality, is well-documented21. Additionally, it has been demonstrated that elderly insomnia sufferers exhibit lower melatonin levels than elderly people without insomnia5. However, the inter-individual variations in ‘normal’ levels of melatonin are large. Therefore, measurement of melatonin is not considered relevant in clinical practice. Age is a good surrogate marker of melatonin deficiency in the primary insomnia patient population22.
I am perfectly satisfied with my benzodiazepine treatment, why should I change to Circadin®?
BZDs have been associated with rebound insomnia, dependence, and neuropsychiatric reactions such as hostility and depression. Also, although effective in getting patients to sleep, these hypnotics further disrupt sleep architecture and structure – primarily by reducing ‘deep sleep’ (NREM stages 3 and 4) as well as REM stages of sleep36 37, a phenomenon that may impair memory consolidation.
Circadin® is safe and is not associated with any of these adverse effects. Furthermore, Circadin® shortens sleep latency to the same extent as most of the ‘z’-drugs but, in addition and unlike BZDs and ‘z’-drugs, Circadin® improves the restorative value of sleep which translates into improved quality of sleep, daytime functioning, and quality of life34 29 31 30.
If a physician wants to switch a patient from Benzodiazepines (BZD) and ‘z’-drugs to Circadin®, what should be the prescribing regimen?
Discontinuation of BZD should be gradual and well controlled because of the risk of withdrawal symptoms and rebound insomnia 60 61 . Circadin® is indicated as monotherapy for the short-term treatment of primary insomnia characterized by poor quality of sleep in patients who are aged 55 or over.
If the physician wishes to switch a patient from BZD / ‘z’-drugs to Circadin®, a reduction in BZD / ‘z’-drugs should be gradual59. It is recommended to reduce the BZD / ‘z’-drugs dose to 50% in the first few weeks while initiating Circadin® co-administration and then to 25% for another several weeks. The dose adjustments and duration of the switching have to be according to medical consultation and under medical supervision.
According to Circadin® SmPC, there can be a pharmacodynamic interaction between BZD / ‘z’-drugs and Circadin® by which Circadin® augments the hypnotic effects of the BZD / ‘z’-drugs1. This is the reason why the dose of BZD / ‘z’-drugs should be reduced to 50% of the usual dose in the first weeks of initiation of Circadin® co-administration while maintaining good sleep.
Why does Circadin® smell?
Circadin® has a distinctive smell which is due to the natural excipient used in the prolonged-release formulation.
Are there any new trials on the horizon?
Neurim is now conducting a Phase III clinical study with Circadin-Ped for the treatment of sleep problems in children with Pervasive Developmental Disorders (PDD) and neurogenetic diseases.