13
Melatonin
Think of melatonin as nightfall in a pill. Melatonin is your sleep hormone, and it plays a pivotal role in both sleep and immune function. You make this hormone naturally; it is secreted by your pineal gland, which functions as your body’s master clock. When night falls and it gets dark outside, melatonin leaks out of your pineal gland, your brain becomes flooded with the potent sleep hormone GABA (gamma-aminobutyric acid), and voila! You drift off to la-la land. Melatonin is thought to amplify the effects of GABA. When the sun rises, all the melatonin scurries away and you wake up. Even though it’s not quite that simple, I think you get the gist.
Night-shift workers have to overcome the urge to sleep at nightfall and must reverse their sleep cycles. Many of them rely on melatonin supplements to help. When you take supplements of this hormone, you might say that you’re taking nature’s sleeping pill. Since melatonin helps you sleep, it gives your mind a mini vacation. This goes a long way in rejuvenating your body, healing your damaged cells, and refreshing your spirit for the next day.
Melatonin actually sets the biological rhythm of every cell in your body. It supports your immune system while you sleep by producing immune-boosting and anticancer substances that prevent infection and reduce signs of aging. Healthy adults usually secrete about 5 to 25 mcg of melatonin during the night, which is about 80 times less than is in the widely available 2 mg over-the-counter tablets. It doesn’t take much. The problem is that when we get older, our melatonin level—like everything else—begins to decline.
This is why as you age you begin to awaken earlier and earlier. This is also why your 80-year-old mother-in-law phones you at 6:00 a.m. to remind you that she will be arriving for dinner at 5:00! (Sheesh, go back to sleep like the rest of the world, would ya?) Melatonin is secreted only while you sleep, so the minute you open the fridge for that 2:00 a.m. ice cream binge, your melatonin production screeches to a halt. Melatonin is suppressed during daylight hours. This is one of the ways it helps with our natural sleep/wake cycle and biological rhythm. I recommend using a flashlight (instead of bright lights) for that 4:00 a.m. potty break, too, so your melatonin level doesn’t drop so drastically, making it more difficult to go back to sleep. People with insomnia have lower levels of melatonin than good sleepers. And obviously teenagers have high levels of melatonin; my teens never crawled out of bed before noon.
Melatonin’s most important role is to enhance production of youthful growth hormones. The antiaging benefits of this hormone occur with natural secretion, as well as with dietary supplementation. On the surface, this makes sense, right? Without adequate melatonin, you suffer from sleep deprivation, and everyone knows how bad that is for the body. But it goes much deeper than that.
Melatonin’s ability to increase natural growth hormones in the body has been examined in several studies, and in one particular study, published in Clinical Endocrinology in 1993, melatonin administration produced an approximate twofold increase in levels of growth hormone in men. This makes sense to me; we all know that as we age, levels of melatonin and growth hormone decline, almost in sync with one another. Perhaps the reason is in part because the melatonin is responsible for the growth hormone release. And both of these hormones are known to scavenge free radicals, thereby protecting our cells and organs from damage and dysfunction.
Why is this such a big deal? Because when your growth hormone declines, you start to lose muscle mass, strength, energy, passion, skin tone, hair, hearing, and so forth. Your risk of disease increases too. As years go by, your age starts to show. So maintaining an adequate level of melatonin may help you maintain some youthfulness.
In other words, just because your kids think you are over the hill doesn’t mean that you can’t take melatonin supplements and cheat Father Time a little.
Now, if you’re a young person who happens to take a drug mugger, melatonin depletion occurs—the same kind of depletion that aging people experience. Stress and all-nighters also make you run low on melatonin. Melatonin deficiency actually poses a bigger problem than missing a good night’s sleep. This important hormone has anticancer properties because it is a very good antioxidant. Melatonin is especially important for protecting the DNA inside our cells against dangerous chemicals called peroxynitrites, which damage the cells’ energy powerhouses (mitochondria) and kill cells. This will shock you, so I hope you’re sitting down. Peroxynitrites are formed in the body from nitrites. Certain foods, namely cured meats, are high in these nitrites, which are added to protect their pink color. Cured meats have, in fact, been implicated in most neurological disorders, including Parkinson’s disease, as well as chronic obstructive pulmonary disease, cancer, and diabetes. So if you like hot dogs, salami, and bologna, you are probably producing lots more peroxynitrites than you want to, and I’d recommend antioxidants for you (as well as a change in diet!). Can melatonin repair bologna damage? No, but melatonin does play a strong neuroprotective role in the body and suppresses the formation of dangerous peroxynitrites.
Studies show that women with low levels of this sleep hormone tend to have higher rates of breast cancer. According to some recent and well-designed trials, bringing in a melatonin supplement might halt the growth of breast cancer cells. One of these studies was published in the International Journal of Cancer in January 2006. Scientists found that melatonin acted like a weak aromatase inhibitor similar to a type of drug (Femara, Arimidex, Aromasin, or Evista) used to prevent or treat early breast cancer. Aromatase inhibitors act by controlling and slowing down the production of estrogen. Less estrogen equals slower tumor growth. Simply put, melatonin acted as a weak but effective antiestrogen.
One study was conducted at Harvard, where scientists evaluated 147 women with invasive breast cancer and 291 without cancer. Melatonin was measured using morning urine samples. What they found is incredibly important to women. Basically, women who had the highest levels of melatonin had the lowest risk of cancer! Has your physician told you about this?
And this is also amazing: A meta-analysis that pooled data from 10 studies was conducted by scientists at McMaster University in Canada. The researchers examined data from studies on people who had solid tumors and looked at their survival rate after 1 year. They found that melatonin reduced the risk of death, regardless of the type of cancer, and there were no reported serious adverse effects.
All this doesn’t surprise me, because melatonin regulates your hormones and seeks to balance them. I happen to think that what’s good for Betty is also good for Bob in this case! Supplements that help with breast cancer can also help with prostate cancer because these cancers are often driven by the estrogen hormone. The prostate actually contains melatonin receptors, so melatonin is needed for a healthy prostate.
Back in 1998 a German study found that men with prostate cancer showed extremely low melatonin levels and therefore altered circadian rhythms, causing poor sleep. Circadian rhythm is the scientific name given to your internal body clock, which includes all the biological processes that regulate a 24-hour cycle. Both plants and animals have their own circadian rhythms. In people, this normal biorhythm can be disrupted by events like chronic illness, stress, grief, and traveling across time zones, just to name a few. There have, in fact, been many studies on laboratory animals showing that melatonin in varying doses could shrink the prostate and lower prostate weight. Melatonin has a place in the prevention and management of prostate tumors, not just mammary ones. I believe that melatonin may improve survival for some men, especially when the hormone is combined with other anticancer compounds or treatments.
Some of the best cancer-protective substances include medicinal mushrooms, antioxidants, B vitamins, minerals, and a diet rich in fresh organic herbs, vegetables, and fruits. I know you try hard to protect your precious cells from negative environmental and dietary influences. There is more on the subject of hormones as they relate to cancer in my new Breast Cancer Protection e-book available on my Web site. You should also read the section in this book beginning on page 11 regarding menopause to find out what nutrients you need if you are taking a prescribed hormone drug.
Finally, it’s worth mentioning that melatonin can be helpful in dealing with the discomforts of jet lag. Jet lag doesn’t rank up there with the serious conditions just discussed, but many people fly internationally, and crossing six time zones, for example, is no picnic. It’s hard for your body to adjust to the new hours of daylight and nightfall, which makes it difficult to conduct business meetings, give a lecture, or simply enjoy a vacation. Your body doesn’t know whether to sleep or stay awake, because all of a sudden you’re in bright daylight in a hustling, bustling city when your body thinks it’s 4:00 a.m. and you are sleepy. Fortunately, melatonin is universally accepted as a safe remedy.
Simply take 2 to 5 mg at nighttime in the time zone you have arrived in. If you are still on the plane when nighttime occurs in the location to which you are headed, take the first dose while still in the air. How many nights should you take it? Divide the number of time zones you’ve crossed by half. For example, if you’ve crossed six time zones, take the melatonin each night for 3 nights. If the opposite occurs, that is, you land in broad daylight but it’s 4:00 a.m. where you came from, I would skip the melatonin. Just check in at your hotel, take a catnap, and then wake up with the rest of the country, find a nice café, and get yourself a large mocha latte! The whole idea is to minimize the confusion in your body and quickly adapt to the time zone you’re in.
Drug Muggers of Melatonin
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)
Aluminum hydroxide (Amphojel, AlternaGEL)
Calcium carbonate (Tums, Titralac, Rolaids)
Magnesium hydroxide (Phillips’ Milk of Magnesia)
Sodium bicarbonate (Alka-Seltzer, baking soda)
Antianxiety Medications
Alprazolam (Xanax)
Clonazepam (Klonopin)
Diazepam (Valium)
Lorazepam (Ativan)
Triazolam (Halcion)
Antidepressants, Tricyclic
Desipramine (Norpramin, for example, is not a drug mugger, but it increases levels of melatonin.)
Antihistamine
Hydroxyzine (Atarax, Vistaril)
Antipsychotics
Chlorpromazine (Thorazine)
Fluphenazine (Prolixin)
Haloperidol (Haldol)
Thioridazine (Mellaril)
Blood Thinner
Warfarin (Coumadin) (Not a drug mugger; melatonin may potentiate the effect of this blood thinner, and too much blood-thinning increases the risk of bleeding.)
Blood Pressure Drugs
Adrenergic receptor agonist:
Methoxamine (Vasoxyl)
Beta-blockers:
Atenolol (Tenormin)
Bisoprolol (Cardicor, Zebeta, Ziac)
Carvedilol (Coreg)
Metoprolol (Lopressor and Toprol XL)
Nadolol (Corgard)
Propranolol (Inderal)
Sotalol (Betapace)
Calcium channel blockers:
Amlodipine (Norvasc)
Diltiazem (Cardizem)
Felodipine (Plendil)
Nifedipine (Procardia) This combination is not recommended. (Melatonin may reduce effectiveness of the drug.)
Nisoldipine (Sular)
Verapamil (Calan, Isoptin)
Centrally acting alpha-agonist hypotensive agents:
Clonidine (Catapres)
Cancer Drugs
Tamoxifen (Nolvadex) (Not a drug mugger, but the combination of melatonin with this breast cancer drug may enhance the effect.)
Inhibitory Hormones/Somatostatins
Octreotide (Sandostatin)
MAO Inhibitors
Phenelzine (Nardil)
Tranylcypromine (Parnate) and others increase melatonin levels.
Selective Serotonin Reuptake
Inhibitors (SSRIs)
Fluoxetine (Prozac)
Fluticasone (Flonase)
Fluvoxamine (Luvox) (Not a drug mugger; it increases melatonin levels.)
Sleep Medications
Eszopiclone (Lunesta)
Temazepam (Restoril)
Zaleplon (Sonata) and others
Zolpidem (Ambien)
MISC:
Alcohol
Any drug mugger of niacin, B1, B6, calcium, or magnesium because you need those nutrients to make melatonin.
Caffeine
Hypochlorhydria (because you need stomach acid to convert proteins in your food into key amino acids, which ultimately form melatonin)
Marijuana (Cannabis) (can increase levels of melatonin)
Niacin muggers
Nicotine (tobacco)
St. John’s wort (can increase melatonin levels)
Smoking cessation patches, lozenges, or gum
Sunlight, lamps, fluorescent light
Vitamin B6 muggers
Protection from Psychiatric Medications
Psychiatric medications can cause a dreadful and usually irreversible side effect called tardive dyskinesia. It is usually seen with drugs that treat schizophrenia, but also sometimes with others. This side effect causes a person to perform involuntary, purposeless movements, such as tongue rolling, lip smacking, and grimacing, or wild movements of the arms and legs. One study suggests that melatonin supplements can reduce symptoms. This treatment is worth discussing with your doctor.
Melatonin: Put This on Your Plate
Oats, corn, rice, ginger, tomatoes, banana, barley, cherries, spirulina, seaweed, soybeans, chicken liver, pumpkin seeds, turkey, chicken, almonds, peanuts, brewer’s yeast, and dairy products
An Absurdly Inexpensive Way to Feel Better
For general health: For insomnia, 0.5–1 mg at bedtime (may increase to 2 or 3 mg if no effect after 1 month)
Drug mugger dose: 1–3 mg at bedtime (ask your physician if 4 or 5 mg is okay if no effect after 1 month)
For cluster headaches: 6 mg at bedtime
For cancer or autoimmune disorders: Doctors suggest 5–20 mg per night (I am not recommending that you take it unless your doctor approves it. You can have your melatonin level assessed through urine or saliva testing)
Dose for jet lag: 2–5 mg at nighttime in your new location
Just So You Know
This is one of those rare instances when I prefer a synthetic brand to a natural one. Synthetic melatonin is better than natural melatonin because the natural type is extracted from cows’ brains and some people are sensitive to proteins and potential viruses from the animals. Synthetic is cleaner in this case. That’s what I take when I need it for jet lag.
Melatonin is not for everyone, though. Women who are trying to conceive a baby may want to give it a pass, as this hormone may hinder the ovulation process.
You may be getting too much melatonin if you have trouble rolling out of bed and fully waking up—sort of like a morning hangover. Excessive melatonin will also cause wild and crazy dreams that frighten you, increased daytime agitation, sweating, and heart palpitations. It might also suppress the level of estrogen or progesterone.
Some people have adrenal exhaustion (low levels of the hormone cortisol). As a result, they are constantly fatigued, feel faint when standing up, or have trouble coping with little annoyances. Taking melatonin in these cases can be harmful because it can further reduce cortisol levels. You can measure your hormone levels and get a good baseline level with a simple saliva test from ZRT Laboratory (www.zrtlab.com) or urine tests offered by Genova Diagnostics.
Install a Nutrient Security System
As a result of an age-related decline of melatonin, most older people respond to melatonin in a positive way because it increases their youthful growth hormones. One big benefit of melatonin is that it helps you fall asleep faster and stay asleep a little longer. If you could see the complex metabolic pathway on which melatonin is made, you would know that protein is important to that process. Most people get enough protein in their diets, unless they are vegetarian. If you are vegetarian or if you suspect that you don’t get enough protein, consider protein supplements like whey, hemp, or rice protein and make yourself a shake every morning. See Chapter 10 on glutathione for more about these supplements. This is even more important: The B vitamins play an important role in the production of melatonin in the human body, particularly B3 (niacin) and B6 (pyridoxine). If you take a B complex supplement during the day and take your melatonin supplement at night, you can rest easy because you’ve installed the tightest security system possible. This is a good time to tell you that melatonin increases non-REM sleep, which can lead to vivid, bizarre, or frightening dreams. So one potential problem is that you just might create too tight a system by producing a little too much melatonin. If this happens to you, reduce your dosage of melatonin or stop taking it altogether for a few weeks. It’s okay with me if you want to continue with your protein shakes and B complex, though.
What’s in My Cupboard?
Melatonin (Sublingual) by Source Naturals: These 1 mg melatonin tablets are formulated to allow for a gradual release of the active ingredient over an approximate 6-hour period. This provides the body with more even absorption of melatonin through the night. Contact information: www.sourcenaturals.com.
Melatonin 500 mcg by Life Extension: This is a pure product containing a very small but physiologically appropriate dose of melatonin. It is free of all allergens and preservatives. You take it 30 to 60 minutes before bedtime. This company also makes a 3 mg lozenge, which you dissolve in your mouth at bedtime.
Melatonin Forte with L-Theanine by Vitaline: This is a natural sleep aid that combines melatonin with the amino acid theanine, the relaxing chemical found in green tea. Each tablet delivers 3 mg melatonin and 40 mg theanine.
Melatonin 3 mg by Nature’s Bounty: Affordable and easy to find, each tablet delivers 3 mg melatonin.
Melatonin 3 by GNC: Each tablet delivers 3 mg melatonin plus vitamin B6 to help it work faster. It is free of all allergens, gluten, and artificial chemicals.
Melatonin 3 mg by KAL: This 100 percent pure vegetarian form of melatonin offers a 2- to 4-hour sustained-release action. This brand is easy to find at health food stores nationwide.
Melatonin Caps by Twinlab: This easy-to-find supplement contains 3 mg melatonin delivered to the body over the course of a few hours. It’s an easy-to-swallow capsule, and just as with all Twinlab formulas, quality control is assured.
Melatonin by Source Naturals: This company produces three strengths, 1 mg, 2 mg, and 3 mg, and they are timed-release formulas, so they should have a longer action in the body. This product is sold at health food stores.
Melatonin 1 mg Liquid by Natrol: This comes with a dropper so you can gauge your dosage and adjust it up or down as needed. You take it 20 minutes before bedtime and combine it with water or juice. The product is naturally sweetened with raspberry and vanilla flavors.