THE BENEFITS OF MELATONIN ARE MORE THAN SLEEP
If you are on any medications be sure to see our long list of drugs which deplete melatonin. This list will be found later in this newsletter.
Melatonin helps regulate other hormones & maintains your body's circadian rhythm. This is the internal 24-hour clock regulating sleep/wake cycles & setting the biorhythm of every cell in your body. It is ubiquitously distributed throughout your body & has multiple other critical functions in all organs, some of which will be discussed here.
Melatonin is a hormone which is secreted by the pineal gland at the base of your brain. Maximum secretion is around 2AM & stops at sunrise. Since melatonin is only secreted while you are sleeping, yet melatonin is needed for sleep, you can see how insomnia begets more insomnia. Normal nighttime production is 5-25 mcg. Secretion of melatonin declines with aging & is thought to be decreased by up to 75% by age 70. This decline is one of the many changes & depletions furthering the aging process.
Our natural melatonin production is dependent upon both adequate light & sufficient dark during certain times of the day. Each day we need at least 30-60 minutes of bright light in the daytime hours & preferably the morning. If you live where the daylight is mostly dim & gloomy such as during the winter in many places, it is best to use full spectrum lighting in your home or workplace when possible. Conversely, absolute darkness is essential for proper melatonin production during your sleep hours. This means no lights from clocks or TVs, other appliances, or through the window from outside etc. If you cannot achieve absolute darkness, use a sleep mask if you are having sleep problems.
Most people only think of melatonin in relation to sleep, but its effects & benefits are far-reaching. One of melatonin’s most important effects on other hormones is to enhance the production of youth promoting growth hormone (GH). The aging process is associated with declining growth hormone. A study showed melatonin administration doubled (GH) production in men. With a decline in growth hormone we start to lose muscle mass, strength, energy, skin tone, hair, hearing, etc. & disease risk increases.
Melatonin has wide-spectrum antioxidant, anti-inflammatory, immune boosting, hypotensive, cell communication enhancing, cancer suppressing, brown fat-activating, and blood-lipid-lowering effects, and thereby protects tissues from a variety of insults. Melatonin is so important to your immune system that depleted levels cause atrophy of the thymus gland, an important part of your immune system.
COMMON SIGNS & SYMPTOMS OF MELATONIN DEFICIENCY INCLUDE:
- Difficulty getting to sleep
- Difficulty falling back to sleep when awaken during the night light sleep with easy waking during the nigh
- Early morning awakening
- Un-refreshing sleep
- Lack of dreaming or poor dream recall
- Family history of insomnia
- Personal or family history of breast cancer
- Personal or family history of prostate cancer
- Prostate enlargement
- Irregular menstrual cycle
- Unusual menstrual flow (light or heavy)
- Poor sleeping prior to menses
- Hypersensitivity to stress
- Neurodegenerative disorders (MS, Parkinson's, Alzheimer's, ALS, etc.)
- Elevated cholesterol
- High blood pressure
- Blood clots
- Heart attack
- Heart arrhythmias
Use this link to test yourself for Melatonin Deficiency by questionaire. There is also a saliva test available to check your melatonin levels. I use the one from Genova Diagnostics.
WHAT SUPPLEMENTS HELP BOOST MELATONIN?
WHAT ELSE CAN INCREASE MELATONIN?
Adequate vitamin B12 promotes a faster release of melatonin. Interestingly marijuana (cannabis) can increase melatonin levels in contrast to the many other drugs which deplete levels. The herb, St. John’s Wort can also increase melatonin.
DRUGS THAT LOWER MELATONIN LEVELS:
Unfortunately, numerous drugs have the side effect of decreasing melatonin, even tranquilizers, sleeping pills & widely used over the counter medications! I suggest you review the following drugs and if you regularly use anything listed be sure to supplement with at least 3 mg of melatonin nightly. Also take the saliva test to check for deficiency.
Acid Blockers: Cimetidine(Tagamet), Esomeprazole (Nexium), Famotidine (Pepcid and Pepcid Complete), Lansoprazole (Prevacid 24HR), Nizatidine (Axid), Omeprazole (Prilosec OTC), Pantoprazole (Protonix), Rabeprazole (Aciphex), Ranitidine (Zantac).
Analgesics: Aspirin (Bayer, Bufferin), Ibuprofen (Advil, Motrin), Naproxen (Aleve, Naprosyn), Oxycodone (Oxycontin), Hydrocodone-containing drugs (Vicodin, Lortab)
Antacids: Aluminum and magnesium hydroxide (Maalox, Mylanta), Aluminum carbonate gel (Basaljel), Calcium carbonate (Tums, Titralac, Rolaids), Magnesium hydroxide (Phillips’ Milk of Magnesia), Sodium bicarbonate (Alka-Seltzer, bakinf soda)
Antianxiety Medications: Alprazolam (Xanax), Clonazepam (Klonopin), Diazepam (Valium), Lorazepam (Ativan), Triazolam (halcion)
Antidepressants, SSSIs: Fluoxetine (Prozac), Paroxetine (Paxil), Sertraline (Zoloft)
Antidepressants, Tricyclic: Desipramine (Norpramin, increases levels of melatonin)
Antihistamines: Hydroxyzine (Atarax, Vistaril)
Anti-Inflammatory Drugs: (NSAIDs), Celecoxib (Celebrex), Diclofenac (Voltaren), etodolac (Lodine), Ibuprofen (Advil, Motrin), Indomethacin (Indocin), Ketoprofen (Orudis), Naproxen (Aleve, Anaprox, Naprosyn), Sulindac (Clinoril)
Antipsychotics: Chlorpromazine (Thorazine), Fluphenazine (Prolixin), Haloperidol (Haldol), Thioridazine (Mellaril)
Blood Thinners: Warfarin (Coumadin) (Melatonin may potentiate the effect of this blood thinner, and too much blood-thinning increases the risk of bruising or bleeding)
Blood Pressure Drugs:
1. Adrenergic receptor agonist: Methoxamine (Vasoxyl)
2. Beta-blockers: Atenolol (Tenormin), Bisoprolol (Cardicor, Zebeta, Ziac), Carvedilol (Coreg), Metoprolol (Lopressor and Toprol XL), Nadolol (Corgard), Propranolol (Inderal), Sotalol (Betapace)
3. Calcium channel blockers: Amlodipine (Norvasc), Diltiazem (Cardizem), Felodipine (Plendil), Nifedipine (Procardia) This combination is not recommended. Melatonin may reduce effectiveness of the drug, Nisoldipine (Sulfar), Verapamil (Calan, Isoptin)
4. Centrally acting alpha-agonist hypotensive agents: Clonidine (Catapres)
Cancer Drugs: Tamoxifen (Nolvadex) The combination of melatonin with this breast cancer drug may enhance the effect.
Corticosteroids (all of them): Betamethasone (Diprolene, Luxiq), Cortisone (Cortone Acetate), Dexamethasone (Decadron), Fluocinolone (Synalar topical),Halobetasol (Ultravate topical), Mometasone (Elocon), Methylprednisolone (Medrol), Prednisolone (Pediapred and Orapred liquid), Triamcinolone(Aristocort)
Inhaled corticosteroids: Budesonide (Rhinocort], Flunisolide (Nasacort, Nasalide, Nasarel), Fluticasone (Flonase), Fluticasone and Salmeterol (Advair)
Inhibitory Hormones/Somatostatins: Octreotide (Sandostatin)
MAO Inhibitors: Phenelzine (Nardil), Tranylcypromine (Parnate), and others increase melatonin levels.
Sleep Medications: Eszopiclone (Lunesta), temazepam (Restoril), Zaleplon (Sonata) and others, Zolpidem (Ambien)
Miscellaneous: ALCOHOL, CAFFEINE & NICOTINE, Any drug that reduces niacin, B1, B6, calcium, or magnesium because these nutrients are needed to make melatonin. Hypochlorhydria because you need stomach acid to convert proteins in your food into key amino acids, which ultimately form melatonin.
MELATONIN & SLEEP
If you have tried melatonin for sleep & it has not worked or you feel hung over, you are likely taking too large a dose. Stop for a few days & resume at a dose of ½ to 1 mg sublingually at bedtime & once again if your sleep is disturbed in the night. Melatonin has a half life of about 4 hours so half is gone in that time.
For more about sleeping difficulties see my previous newsletters on the subject:
We have known for years about the connection between melatonin & sleep patterns, but scientific studies have shown it may be beneficial in assisting with the treatment of many other conditions.
These conditions have been widely published. If you go to the National Library of Medicine the Pub med web site, there are 18, 645 entries with melatonin as the search term. You can cross reference melatonin with other words to drill down on specific disorders, etc.
SOME MELATONIN RESEARCH
The below is only a small fraction of the research just to give an idea of the variety of benefits.
- Anti-Aging: A team at laboratoire Arago in Banyuls sur Mer (CNRS / Université Pierre et Marie Curie) has found that a treatment based on melatonin can delay the first signs of aging in a small mammal. In studies conducted with mice, administering melatonin in dosages of 10 mcg/ml of water increased their lifespan by 20% and the older mice began taking on traits of the younger mice.
- Stress: Chronic stress depletes melatonin. Chronic stress causes the production of too much cortisol which lowers melatonin. Conversely, adequate melatonin can be stress protective by keeping down the hyper production of cortisol (the stress hormone). Since melatonin can help control excess cortisol production those with low adrenal function & low cortisol need to be careful about taking too much melatonin. It can make them even more tired. In summary, too little or too much melatonin will impair stress tolerance.
- Migraine Headaches: A recent study conducted by Randall Neustaedter OMD showed that melatonin is an effective treatment for migraine headaches. Study participants had a history of 2 to 8 migraines per month. Melatonin not only resulted in fewer headaches, but also less side effects and less daytime sleepiness than the antidepressant used in the study.
- Amyotrophic lateral sclerosis (ALS), or Lou Gehrig's disease: A new study conducted by researchers at the University of Pittsburgh, School of Medicine showed that melatonin injections delay amyotrophic lateral sclerosis (ALS), disease symptom onset & death in mice. "Our experiments show for the first time that a lack of melatonin and melatonin receptor 1, or MT1, is associated with the progression of ALS," said Robert Friedlander, M.D., UPMC Endowed Professor of Neurosurgery and Neurobiology and chair, Department of Neurological Surgery, Pitt School of Medicine.
- Alzheimer's disease: A study carried out by a group of researchers from the Barcelona Biomedical Research Institute (IIBB), showed daily voluntary exercise and daily intake of melatonin, had a synergistic effect against brain deterioration in the mice with three mutations of Alzheimer's disease. "After six months, the state of the mice undergoing treatment was closer to that of the mice with no mutations than to their own initial pathological state. From this we can say that the disease has significantly regressed"
- Parkinson’s: A study published in the Behavioral and Brain Functions journal found that patients suffering from Parkinson`s disease were deficient in circulating levels of melatonin. The study concluded that providing supplemental melatonin dramatically lowered the degree of oxidative stress on neural mitochondria and was protective against related free radical damage. These results were more pronounced for patients in the earliest stages of disease.
- Protection Against Brain Injury & Inflammation in the Central Nervous System: Swiss neurologists showed that mice treated for 30 days with melatonin beginning 24 hours after an experimentally induced stroke had improved survival of brain cells and better recovery of injured cells than the injured mice not given melatonin. These changes were associated with long-lasting improvement of motor and coordination deficits (both common after human strokes)
- Inflammation: Earlier this year, researchers in New Zealand reported that, in addition to its anti-inflammatory properties, melatonin can promote a healthy immune response early in the process of wound healing, improving the quality of wound healing and scar formation. Studies like this are revealing much about melatonin’s ability to modulate the inflammatory process, not only in the important area of wound healing, but in other forms of tissue injury that occur throughout the body.
- Tinnitus Symptoms: Jay Piccirillo, MD, et al, Washington University School of Medicine, St. Louis, MO. conducted a study which suggests melatonin may be a safe treatment for patients with idiopathic tinnitus, especially those with sleep disturbance due to tinnitus.
- Cancer: Melatonin suppresses proliferation of a wide range of cancers & also help trigger self destruction of cancer cells. Melatonin can improve the effectiveness & decrease the toxicity of chemotherapy. Melatonin confers particular protection against sex hormone related cancers such as ovarian, breast, prostate & testicular cancers.
The world health organization has designated night shift work as a possible cancer provoking risk. Reduced melatonin production has been proposed to be a factor in the increased cancer rates in night workers.
A meta analysis of 10 studies released in the Journal of Pineal Research indicated melatonin is able to decrease the risk of many cancer lines by up to thirty four percent. A review of clinical studies involving 643 cancer patients using melatonin revealed a reduced incidence of death.
Melatonin is a powerful & versatile antioxidant which can scavenge the most dangerous free radicals such as hydroxyl, oxygen & nitrous oxide, & peroxynitrite free radicals. These free radicals can attack DNA to result in genetic deletious, & can attack proteins & cell membranes. These attacks by free radicals dramatically increase the risk of many cancers. Researchers have discovered there are melatonin receptors in the prostate gland. Studies show men with prostate cancer had lower melatonin levels.
- Gastrointestinal Tract Protection: Melatonin is directly involved in preventing tumor initiation, promotion, and progression in a variety of cancers of the gastrointestinal tract including colorectal cancer, cholangiocarcinoma, hepatocarcinoma, and pancreatic carcinoma.
European researchers have also shown that melatonin protects against damage to both the stomach and the pancreas and accelerates healing of chronic gastric ulcers by stimulating blood flow. See gastroesophageal protection and ulcer healing.
It may protect the pancreas against pancreatitis & attenuate pancreatic tissue changes.
Further research from Europe has revealed that melatonin reduces symptoms in patients with another painful condition called “functional dyspepsia,” or “sour stomach. In a placebo-controlled trial, gastroenterologists treated 60 patients who had functional dyspepsia with either melatonin 5 mg or placebo, once every evening for 12 weeks. Fifty seven percent of the melatonin-treated group showed complete resolution of symptoms and 30% had partial improvement, while 93% of placebo recipients reported no change at all.
- Melatonin protects the liver from non-alcoholic liver disease.
- Breast Cancer: Women with low melatonin levels have a higher rate of breast cancer. In fact, melatonin acts as a weak aromatase inhibitor similar to the drugs: Evista, Femara, Arimidex & Aromasin. In A Harvard study of 147 women with invasive breast cancer & 291 women without, those with the highest melatonin levels had the lowest risk of breast cancer. Some Studies related to breast cancer and melatonin.
- Anxiety: Melatonin enhances the production in the brain of the calming neuro inhibitor GABA
- Type 2 Diabetes: Melatonin is important for proper glucose metabolism. Researchers at Brigham and Women's Hospital noted "Loss-of-function mutations in the melatonin receptor are associated with insulin resistance and type 2 diabetes. Additionally, in a cross-sectional analysis of persons without diabetes, lower nocturnal melatonin secretion was associated with increased insulin resistance."
- Weight Gain & Heart Disease Associated with Obesity: New research conducted by University of Granada has demonstrated melatonin has the ability to control the metabolic functions that determine fat accumulation, obesity and lipid levels. The researchers believe this is the first proof that melatonin can act as a critical hormonal agent in the fight against cardiovascular disease and lipid dysfunction.
- Jet Lag: Melatonin helps to decrease or eliminate jet lag if you take 3-6 mg at 10 PM nightly before traveling. Then once embarking & on route, take your dose at what is 10 PM at your destination, then use at 10 PM for first three nights after arrival.
Low melatonin levels are found in those with Seasonal Affective Disorder. Reversed levels are found in those who are bipolar. They have low levels at night & high levels in the morning, the reverse of what it should be. Schizophrenics tend to have low melatonin. Is this caused by their medications or does it have other implications? Those who suicide in the night have lower levels of melatonin than those dying in the night from other causes. This should be no surprise because low trytophan levels are associated with a higher incidence of suicide & tryptophan is a precursor to melatonin. Low melatonin levels are also found in those with breast & prostate cancer, those with decreased blood flow in the heart, those with Alzheimers & other dementias.
WHAT FOODS CONTAIN MELATONIN?
The best food source of melatonin is tart (sour) cherries, but this is not a commonly eaten food. Tart (sour) cherries, especially the Montmorency variety, have been scientifically proven to have the largest concentration of melatonin – such a significant amount that it is actually enough to produce positive results in the body according to Dr. Reiter who conducted research on tart cherries.
Oats, corn, rice, ginger, tomatoes, banana, barley, spirulina, seaweed, soybeans, chicken liver, pumpkin seeds, turkey, chicken, almonds, peanuts, walnuts, brewer’s yeast, and dairy products are other food sources of melatonin.
This information is important if you are looking for natural ways to improve the quality of your sleep and to add a powerful antioxidant to your diet but are unwilling to experiment with synthetic forms of melatonin.
SAFETY OF MELATONIN
Melatonin is safe but should be avoided in women trying to conceive because it may hinder ovulation.
Side effects can be next day grogginess, irritability, vivid dreams/ or nightmares & decreased body temperature. In these cases adjust the dose downward.
Toxicity has not been seen in doses as high as 200 mg/kg of body weight in mice which would be the equivalent of 14,000mg in a 150 lb. person.
For further information about Melatonin, I recommend the following books: