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Melatonin-time-release: 7 things you should know

Medically reviewed by Carmen Fookes, BPharm. Last updated on June 29, 2021.

1. How it works

  • Melatonin-time-release is a supplement that may be used to aid sleep and help decrease jet lag. It is also reported to have a range of other actions in the body.
  • Melatonin is a natural hormone produced mainly by the pineal gland that our body secretes in response to darkness to help maintain our sleep-wake cycle. Environmental light inhibits the secretion of melatonin and darkness stimulates the secretion of melatonin. Secretion of melatonin in humans starts around 9 pm and peaks between 2 and 4 am; with the duration of melatonin production varying from season to season.
  • Natural melatonin is synthesized from the amino acid tryptophan and released into the blood and cerebrospinal fluid where it works by acting on receptors in the brain and other areas of the body. Most melatonin that is available as a supplement is a synthetic version of naturally occurring melatonin.
  • Melatonin-time-release taken as a supplement mimics the effects of naturally occurring melatonin. It may be called a hormone, a supplement, a miscellaneous hypnotic, or a nutraceutical.

2. Upsides

  • Melatonin-time-release is classed as a supplement which means it is available without a prescription from pharmacies, nutrition stores, and other retail outlets.
  • Melatonin may be used to treat jet lag, sleep disorders in the blind, shift-work sleep disorders, and general insomnia. It is an antioxidant and is purported to have numerous other properties (such as boosting the immune system, treating headaches, easing the symptoms of fibromyalgia). Short-acting melatonin may be more effective for some indications than melatonin-time-release.
  • Melatonin-time-release is marketed as improving sleep duration and may help people who awaken too early.
  • Occasional short-term use appears safe.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

  • Dizziness, drowsiness, bed-wetting, headache, nausea, and excessive daytime sedation are the most common side effects.
  • Melatonin-time-release may cause drowsiness that persists and may affect a person's ability to drive or operate machinery the next day.
  • Not FDA approved.
  • May not be suitable for some people including those with epilepsy or autoimmune diseases, or taking warfarin. Caffeine and fluvoxamine may elevate plasma concentrations of melatonin-time-release. Melatonin-time-release may decrease plasma concentrations of nifedipine.
  • If melatonin-time-release is not taken at the right time of day it may cause drowsiness and delay adaption to local time.
  • Some melatonin supplements use naturally occurring melatonin derived from animal pineal tissue. Their use is to be discouraged because of the risk of contamination or viral transmission.
  • High doses of melatonin may affect ovulation, making it difficult for a woman to get pregnant.
  • Melatonin may not work for everyone.
  • Should not be given to children without medical advice.
  • Dosages over 5mg appear no more effective than lower dosages and are associated with more side effects such as headache, next-day dizziness, or vivid dreams. Side effects may be worse in older adults.
  • Should not be used by women who are pregnant and medical advice should be sought before using it while breastfeeding.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. For a complete list of all side effects, see product information.

4. Bottom Line

Supplemental melatonin-time-release is an extended-release tablet that may be taken to improve sleep duration. Short-acting melatonin appears more effective for managing the effects of jet lag.

5. Tips

  • Use the lowest dose of melatonin-time-release when starting this product.
  • Do not crush break or chew the extended-release tablet. Swallow whole.
  • Melatonin-time-release may take up to an hour to be effective. Take half to one hour before going to bed at your destination (10 pm to midnight). For jet lag, one dose is usually taken each night for four nights.
  • If melatonin-time-release appears ineffective, take short-acting melatonin. Do not take melatonin-time-release and short-acting melatonin together.
  • Buy melatonin-time-release from a reputable brand with good quality control measures.
  • Do not drive or operate machinery if you feel sleepy with melatonin-time-release the next day or within 4 hours of taking it.
  • For sleep disorders, melatonin 5mg should be taken three to four hours before a defined, set, bedtime. Controlled-release melatonin may be better for maintaining sleep.
  • Buy melatonin from a reputable brand with good quality control measures.
  • Caffeine (contained in coffee and cola) may increase the effects of melatonin, causing increased or prolonged sedation.
  • Talk to your doctor if you experience any unusual reactions after taking melatonin.
  • Melatonin-time-release should only be used short-term unless a doctor has advised you to take it long-term.
  • Do not take melatonin-time-release if you are pregnant and do not use it if you are breastfeeding unless on a doctor's advice.

6. Response and effectiveness

  • Drowsiness may be experienced within an hour of taking melatonin-time-release and generally persists for several hours.
  • Plasma levels of melatonin return to normal within 24 hours of a single dose of melatonin-time-release.

7. Interactions

Medicines that interact with melatonin-time-release may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with melatonin-time-release. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Common medications that may interact with melatonin-time-release include:

  • echinacea
  • fluvoxamine
  • hormones, such as estrogens or hydroxyprogesterone
  • hydroxyprogesterone
  • ifosfamide
  • medications that also cause sedation, such as alprazolam, clobazam, diazepam, midazolam, temazepam, zaleplon, or zolpidem
  • PARP inhibitors, such as olaparib
  • some quinolone antibiotics, such as moxifloxacin
  • warfarin.

Note that this list is not all-inclusive and includes only common medications that may interact with melatonin-time-release. You should refer to the prescribing information for melatonin-time-release for a complete list of interactions.

References

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use melatonin-time-release only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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