Melatonin is a hormone naturally produced by the body to prepare for and induce sleep. This hormone is produced in the brain when it starts getting dark outside. For this reason, melatonin plays a key role in maintaining sleep patterns and regulating other hormones.
Melatonin plays a key role in reproductive function and development, and also has antioxidant properties. Researchers also believe it may be related to aging, as melatonin production levels decrease with age. The most common use of melatonin supplementation is to help normalize irregular sleep patterns.
Melatonin supplementation is increasingly more popular given today’s modern technology. Backlit screens on our computers, televisions, and smartphones are known to interfere with our natural melatonin production, causing an increase in reports of difficulty falling asleep.
Benefits of Melatonin
Melatonin was not discovered until the turn of the 20th century, and its association with various health conditions did not emerge until nearly 1960. Melatonin’s use as a sleep aid began just 20 years ago, around the same time that it was discovered to be an antioxidant. To date, over 400 articles have been published on melatonin.
Insomnia is characterized by a difficulty in falling asleep or staying asleep. People with insomnia may experience fatigue, low energy, difficulty concentrating, mood disturbances, and decreased performance at work or school. When insomnia occurs at least three nights a week for at least 3 months, it is considered chronic. Insomnia is a common disorder in the US. About 15 to 20% of adults have short-term insomnia, and 10% have chronic insomnia.
Melatonin supplementation appears to be highly effective in reducing symptoms of insomnia when taken before sleep. Studies suggest that melatonin may also promote sleep in other situations, such as with jet lag, combating disruptions of the body’s internal “clock”, and augmenting abnormal working hours.
Depression (major depressive disorder or clinical depression) is a common but serious mood disorder. This condition causes severe symptoms that affect how you feel, think, and handle daily activities, such as sleeping, eating, or working. To be diagnosed with depression, symptoms must be present for at least two weeks. About 6.7% of the US adult population is affected by depression in a given year.
If the body’s natural sleep patterns are off, fatigue and depression might result. By regulating sleep and resetting the internal “clock,” melatonin can improve symptoms of depression and increase overall energy levels. Research has shown that melatonin can also reduce mood swings.
Stomach (gastric) ulcers are open sores that develop on the inside lining of your stomach. The most common causes of stomach ulcers are infection with the bacterium Helicobacter pylori (H. pylori) and long-term use of aspirin and certain other painkillers. 15.5 million people were diagnosed with stomach or intestinal ulcers in the US in 2011.
Research studies have demonstrated that melatonin, either alone or with other agents, has a notable protective effect against ulcers caused by either H. pylori or aspirin.
Cognitive Function / Alzheimer’s
Production of melatonin decreases with age. Research has shown that people with more significant symptoms of memory loss also have lower levels of melatonin than expected. Melatonin supplementation may replenish the body’s levels of melatonin and slow age-related cognitive decline.
melatonin and warfarin
It’s not surprising that melatonin has so many vast functions in the body, as hormones are key regulators of the body’s function. Each year there are new, promising research studies being conducted on melatonin’s benefits.
Melatonin may be beneficial in treating endometriosis, which is heavily affected by hormone levels. Research also suggests that melatonin may be useful in lowering blood pressure and improving cholesterol. Melatonin is now being heavily researched for its strong antioxidant effects. It may help strengthen the immune system, improve symptoms of fibromyalgia, aid digestion, reduce eczema outbreaks and possibly even help treat multiple sclerosis. Preliminary studies also suggest that melatonin may help women with PCOS improve fertility.
Common Food Sources
- Extra virgin olive oil
Do I Need A Melatonin Supplement?
Though uncommon, true melatonin deficiency can occur. The most common signs are trouble falling and/or staying asleep, fatigue, and not feeling well rested after a proper amount of sleep.
How Much Melatonin Do I Need?
The benefits of melatonin are not dose-dependent – taking more will not help you fall asleep faster. As of yet, melatonin does not appear to produce any adverse effects at high dosages (known interactions aside – as listed below).
To help encourage sleep, take melatonin roughly 30 minutes before going to bed.
What are the side effects of melatonin?
Side effects of melatonin are uncommon but may include drowsiness, headache, dizziness, or nausea. People taking anti-hypertensive drugs should avoid taking melatonin, and should consult with a physician before supplementing with melatonin. Women that are pregnant or trying to become pregnant should not take melatonin, as its safety has not been thoroughly studied. Though melatonin supplementation does not affect your body’s production of the same hormone, some individuals may become reliant on melatonin supplements with long-term usage.
Are There Any Medications or Supplements I Shouldn’t Take With melatonin?
Melatonin is one of the most thoroughly researched hormones. As such, there are a number of medications and supplements known to interact in some way with melatonin supplements, but they are rarely serious since melatonin is a naturally occurring hormone.
The majority of medications and supplements listed below are precautionary – there is no evidence that melatonin supplements will cause detrimental effects, but given what we know about their mechanisms, it is possible.
Theoretically, melatonin might increase the effect of anticoagulant or antiplatelet drugs.
There are isolated case reports of minor bleeding and decreased prothrombin activity in people taking melatonin with warfarin. The mechanism, if any, of this interaction is unknown. Taking melatonin orally seems to decrease coagulation activity within one hour of dosing in healthy men.
Some drugs with anticoagulant or antiplatelet effects include aspirin, clopidogrel (Plavix), nonsteroidal anti-inflammatory drugs (NSAIDs) such as diclofenac (Voltaren, Cataflam, others), ibuprofen (Advil, Motrin, others), naproxen (Anaprox, Naprosyn, others), dalteparin (Fragmin), enoxaparin (Lovenox), heparin, warfarin (Coumadin), and others.
Theoretically, melatonin may inhibit the effects of anticonvulsants in some patients.
Some clinical evidence suggests that melatonin may increase the frequency of seizures in certain patients, particularly children who are neurologically disabled.
Some anticonvulsant drugs include phenobarbital, primidone (Mysoline), valproic acid (Depakene), gabapentin (Neurontin), carbamazepine (Tegretol), phenytoin (Dilantin), and others.
Some research suggests that melatonin might impair glucose utilization and increase insulin resistance. However, other research shows that melatonin with zinc acetate actually improves glycemic control and decreases glycated hemoglobin (HbA1c). Other research found that melatonin supplementation does not affect glucose levels.
Until more is known, use melatonin cautiously in combination with antidiabetes drugs.
Some antidiabetes drugs include glimepiride (Amaryl), glyburide (DiaBeta, Glynase PresTab, Micronase), insulin, pioglitazone (Actos), rosiglitazone (Avandia), chlorpropamide (Diabinese), glipizide (Glucotrol), tolbutamide (Orinase), and others.
Theoretically, taking melatonin in combination with antihypertensive drugs might increase the risk of hypertension.
Some clinical evidence suggests that taking melatonin decreases blood pressure in healthy adults. Also, melatonin seems to lower systolic and diastolic blood pressure in individuals with high blood pressure at nighttime or untreated essential hypertension. However, melatonin seems to worsen blood pressure in patients who are taking antihypertensive medications. Also, results from animal research suggest that melatonin reduces the effectiveness of certain antihypertensive drugs, including methoxamine and clonidine.
Some antihypertensive drugs include captopril (Capoten), enalapril (Vasotec), losartan (Cozaar), valsartan (Diovan), diltiazem (Cardizem), Amlodipine (Norvasc), hydrochlorothiazide (HydroDiuril), furosemide (Lasix), methoxamine (Vasoxyl), clonidine (Catapres, Kapvay, Nexiclon), and many others.
Some evidence suggests that caffeine consumption can decrease endogenous melatonin levels, while other evidence suggests that caffeine increases endogenous melatonin levels. When administered in combination with melatonin supplements, caffeine seems to increase melatonin levels. The reason for this discrepancy is not completely clear. Part of the discrepancy may result from the fact that caffeine can inhibit melatonin synthesis as well as inhibit melatonin metabolism.
Melatonin may enhance the efficacy of chemotherapy and reduce its toxicity, at least in advanced cancer patients of poor clinical status. In a clinical study of 250 metastatic solid tumour patients on chemotherapy, the 1-year survival rate and the objective tumour regression rate were significantly higher in patients concomitantly treated with melatonin than in those who received chemotherapy alone. Moreover, the concomitant administration of MLT significantly reduced the frequency of thrombocytopenia, neurotoxicity, cardiotoxicity, stomatitis and asthenia.
Central Nervous System (CNS) Depressants/Sedatives
Theoretically, concomitant use of melatonin with alcohol, benzodiazepines, or other sedative drugs might cause additive sedation.
Contraceptive drugs can increase the levels of endogenous melatonin. Theoretically, these drugs may increase the effects and adverse effects of oral melatonin use.
Fluvoxamine can significantly increase melatonin levels. In some cases, fluvoxamine might increase bioavailability of exogenously administered melatonin by up to 20 times. Some researchers think this might be a beneficial interaction and be potentially useful for cases of refractory insomnia. However, this interaction might also cause unwanted excessive drowsiness and possibly other adverse effects. Fluvoxamine is known to increase endogenous melatonin secretion. It also seems to increase serum levels of exogenously administered melatonin possibly by decreasing melatonin metabolism by inhibiting cytochrome P450 (CYP450) 1A2 and 2C19 or by inhibiting melatonin elimination. This effect has been found in healthy people taking fluvoxamine 50-75 mg and melatonin 5 mg.
Melatonin can decrease the effectiveness of nifedipine GITS in humans. Immediate-release melatonin 5 mg at night in combination with nifedipine GITS 30-60 mg daily increases systolic blood pressure an average of 6.5 mmHg and diastolic by an average of 4.9 mmHg. Concomitant use with melatonin also increases heart rate by 3.9 bpm (6436). The mechanism of this interaction is not known.
Seizure Threshold Lowering Drugs
Theoretically, taking melatonin with drugs that also lower the seizure threshold might increase the risk of seizure activity.
Some clinical evidence suggests that melatonin may increase the frequency of seizures in certain patients, particularly children who are neurologically disabled.
Some drugs that lower the seizure threshold include anesthetics (propofol, others), antiarrhythmics (mexiletine), antibiotics (amphotericin, penicillin, cephalosporins, imipenem), antidepressants (bupropion, others), antihistamines (cyproheptadine, others), immunosuppressants (cyclosporine), narcotics (fentanyl, others), stimulants (methylphenidate), theophylline, and others.
Verapamil (Calan, Covera, Isoptin, Verelan)
Concomitant use can increase melatonin excretion.
Three cases of increased prothrombin time have been reported for patients aged 48 to 72 years who took melatonin orally in combination with warfarin. However, three cases of decreased prothrombin time have also been reported for patients aged 51 to 84 years who took melatonin orally in combination with warfarin.
Until more is known, use melatonin cautiously in patients taking warfarin. Theoretically, melatonin may potentiate the effects of warfarin and increase the risk of bleeding.
Anticoagulant and Antiplatelet Herbs and Supplements
Theoretically, melatonin might increase the effect of herbs that have antiplatelet/anticoagulant constituents and might theoretically increase the risk of bleeding in some people. Taking melatonin orally seems to decrease coagulation activity in healthy men.
These herbs include angelica, clove, danshen, garlic, ginger, ginkgo, Panax ginseng, red clover, willow, and others.
Some evidence suggests that caffeine consumption can decrease endogenous melatonin levels, while other evidence suggests that caffeine increases melatonin levels (human research). When administered in combination with melatonin supplements, caffeine seems to increase melatonin levels. The reason for this discrepancy is not completely clear. By functioning as an adenosine receptor antagonist, caffeine might indirectly inhibit the synthesis of melatonin.
Conversely, because melatonin and caffeine are both metabolized by cytochrome P450 1A2 (CYP1A2) enzyme, concomitant use of melatonin and caffeine might reduce the metabolism of melatonin, resulting in higher serum levels.
Theoretically, concomitant use of echinacea and melatonin may have a negative effect on innate immune function. Preliminary animal research suggests that taking echinacea in combination with melatonin inhibits the formation of functional granulocytes in the spleen and bone marrow.
Herbs and Supplements with Hypotensive Effects
Theoretically, combining melatonin with other herbs and supplements with hypotensive effects might increase the risk of hypotension in some individuals.
Some clinical evidence suggests that taking melatonin decreases blood pressure in healthy adults. Also, melatonin seems to lower systolic and diastolic blood pressure in individuals with high blood pressure at nighttime or untreated essential hypertension.
Some of these herbs and supplements include andrographis, casein peptides, cat’s claw, coenzyme Q-10, fish oil, L-arginine, lycium, stinging nettle, theanine, and others.
Herbs and Supplements with Sedative Properties
Melatonin has shown to have sedative effects in humans. Theoretically, concomitant use with herbs that have sedative properties might enhance therapeutic and adverse effects.
Some of these supplements include 5-HTP, calamus, California poppy, catnip, hops, Jamaican dogwood, kava, St. John’s Wort, skullcap, valerian, yerba mansa, and others.
Seizure Threshold-Lowering Herbs and Supplements
Some clinical evidence suggests that melatonin may increase the frequency of seizures in certain patients, particularly children who are neurologically disabled. Theoretically, patients taking supplements that also lower the seizure threshold might be at greater risk.
Some of these supplements include butanediol (BD), cedar leaf, Chinese club moss, EDTA, folic acid, gamma butyrolactone (GBL), gamma hydroxybutyrate (GHB), glutamine, huperzine A, hydrazine sulfate, hyssop oil, juniper, L-carnitine, rosemary, sage, wormwood, and others.
St. John’s Wort
Some clinical evidence suggests that taking St. John’s Wort increases levels of 6-sulphatoxymelatonin, the primary urinary metabolite of melatonin, in depressed individuals.
Preliminary clinical evidence suggests that taking vitamin B12 reduces plasma levels of endogenous melatonin.
Theoretically, concomitant use of vitex agnus-castus and melatonin might enhance therapeutic and adverse effects of melatonin.
Preliminary evidence suggests that taking vitex agnus-castus 120-480 mg daily for 2 weeks significantly increases melatonin levels in healthy males.
Should you be supplementing with melatonin?
Individuals with melatonin deficiencies and those that have trouble falling or staying asleep are most likely to benefit from melatonin supplementation.
As previously mentioned, if you have a depressive disorder, stomach ulcers, or are concerned about mental/cognitive function, there is strong evidence to suggest that melatonin supplementation could be beneficial.
Interested in learning whether melatonin is right for you? Take the Vitality DNA test today to learn the optimal diet, exercise, and supplementation for your DNA and lifestyle.