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From the Townsend Letter
February / March 2019

New Whys and Ways to Sleep Better,
Especially After 40

by Dr. Devaki Lindsey Berkson
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BDNF EssentialsNatural Ways to Help You Sleep
Before taking any sleep aids, even over-the-counter or natural, it's best to work with a practitioner that understands your personal physiology and medical history. Sometimes relentless insomnia occurs due to a hidden disease. For example, excess calcium blood levels from primary hyperparathyroidism (a benign tumor on a parathyroid gland) can adversely affect the brain and manifest as insomnia. Sleep apnea, trouble breathing during sleep, can cause insomnia. Chronic hidden infections can cause insomnia.
Once disease is ruled out, natural sleep aids can be very helpful for midlife sleep issues. Some of these natural sleep aids bind to the same places in the brain as prescription sleep meds (sleep hypnotics) and may lose their effectiveness over time, just like those drugs do. Thus, it's good to have lots of sleep-promoting tools, especially ones that work by mechanisms that do not lose their effectiveness, such as hormones, nutrients, and lifestyle improvements.

  • Hormone Hacking. A healthy brain produces progesterone right inside the brain.30 This is because progesterone is a brain-protective hormone in both men and women. Progesterone is also one of Nature's chief sleep protectors.
    o Progesterone binds to the GABA31 receptors in the brain and calms the brain to help it turn off and promote restorative sleep.
    o Progesterone regulates a member of the neurotrophin family, brain-derived neurotrophic factor, which keeps your brain healthy. A healthier brain turns off easier at night as well as being more protected from neurodegeneration.32
    o As we age, both genders' brains produce less progesterone, and this contributes to poorer sleep. Progesterone therapy usually improves it. In fact, perimenopausal insomnia is often a woman's body "screaming" for additional progesterone.33 But sometimes males need some progesterone replacement, too.
    o Oral progesterone is a better tool to improve sleep, most of the time, than topical. This is because progesterone's major sleep-promoting metabolite, pregnenolone, is only produced if progesterone is taken orally. When swallowed, progesterone goes from the gut into the liver (called the first hepatic pass) where liver cells morph the progesterone into sleep-promoting pregnenolone. This progesterone metabolite acts very similarly to Valium™,34 but without the adverse and potentially dangerous side effects.35
    o Progesterone reduces "brain on fire" or excessive inflammation in the brain. In this way, progesterone also fights depression and possibly small vessel ischemic brain disease.36
    o If men are recommended progesterone, it's usually prescribed in much lower dosages than women and can be given orally from 30 to 50 mg, or sometimes is prescribed in facial creams (Key Pharmacy in Federal Way, WA, has been making a male hormone face cream for many years).
    o Sometimes men and women need other hormones. Estrogen therapy in ladies or T replacement in gents can help achieve deeper and healthier sleep.
  • Less caffeine. Too much caffeine is a commonly overlooked problem in too many insomniacs. This is because there is a lot of individuality in the "caffeine sensitivity" effect on sleep.37 Some persons can drink espresso all day long and right before bed, and still sleep like a baby. Other people may be extremely sensitive to caffeine (usually due to how genetics affects the speed at which they rinse caffeine out of their bodies). These people may become insomniacs from just one caffeinated beverage a day, sometimes even in the morning. Many caffeine-sensitive folks find that not consuming caffeine after 3 PM does the trick. But sometimes any caffeine may be too much for you. We don't appreciate that what we sip, can sap sleep.
    o Make sure you aren't suffering sleep issues because you are hitting Starbucks too often for your physiology. Also, as crazy as it seems, caffeine can promote sleep apnea, even in kids.38 There is a lot of caffeine in many sodas.
    o There are gender differences, too. Women are typically more sensitive to caffeine than gents. Women metabolize caffeine much more slowly than men.39 This is why many men can down a cup of coffee right before bed, while if a woman did this, she would spend the night staring at the ceiling.
  • Melatonin. Melatonin is secreted by the brain's pineal gland in response to cycles of light and darkness. Melatonin regulates your ability to stay "in sync" with light and dark, in sync with Mother Earth. Melatonin is thus often helpful for traveling across time zones, to keep you in sync with new light and dark cycles. When you are more in sync with light and dark, you are tired at night and sleep deeply, and are more awake and energized during the day. When melatonin production or metabolism is dysregulated, this gets reversed; you can't sleep at night and are tired throughout the day. You're out of sync with Nature's light and dark cycles
    o Natural melatonin secretion is dysregulated by light at night, depression, shift work, seasonal affective disorder, and as you read above, excessive caffeine intake over a long period of time.
    o Melatonin is a major antioxidant and protector of estrogen, keeping it from acting less as a cancer-causing molecule in both men and women. Melatonin, in combination with omega-3 fatty acids, especially does its estrogen and cancer fighting actions while you sleep, if your levels of melatonin are high and healthy enough (PS Meridian 24-hr hormone test assesses melatonin levels. Excessively high melatonin levels can suggest health issues such as cancers. This test has helped me ID cancers on several patients.)
    o The usual dose is 0.5–3.0 mg, taken one-half hour before bedtime. (I have found it works best as a non-time-released tablet chewed and held under the tongue for 30 seconds)
    o For some recent cancer patients, the dosage can go up to 20 mg, but this must be done in conjunction with an in-the-know doctor.
    o Melatonin can safely be used with aromatase inhibitors40 and estrogen blockers, as it has been shown to reduce some of their adverse side effects.
    o Melatonin itself acts as a natural aromatase inhibitor and also limits cancer growth by additional helpful mechanisms other than aromatase blocking. Melatonin is one of the cancer patient's best friends.
  • Magnesium-rich foods and supple-mentation. Magnesium is Nature's Valium. It relaxes the body and mind. Magnesium deficiency is linked to causing insomnia.41 It's easy to become deficient in magnesium. Magnesium is deficient in the Standard American Diet (often referred to as SAD). This diet is typically low in green vegetables. Magnesium "lives" inside the center of the chlorophyll molecule that gives veggies their green color. In essence, magnesium is "captured sunlight." Sufficient magnesium inside your red blood cells, where magnesium does most of its magic, makes you feel relaxed and calm, like lying outside under the sun.
    o However, healthy magnesium levels are not easy to maintain inside red blood cells, no matter how normal blood (serum) levels appear.
    o Why? Magnesium is constantly "rinsed out" of the body during times of chronic or severe stress. And today, who's not stressed?
    o To make magnesium matters even more confusing, many magnesium supplements don't contain the "elemental" levels that the label says will be in there, which are necessary for keeping your red blood levels healthy.
    o Thus, there are a lot of magnesium insufficiencies and misunderstandings.
    o Magnesium supplementation before bed may help you sleep more soundly. Sometimes taking taurine42 helps keep magnesium more anchored inside the red blood cell and less at risk of being rinsed out. You could refer to taurine as a "magnesium-sparing nutrient" (coined by Berkson).
  • GABA. Gamma-Aminobutyric acid, or γ-aminobutyric acid, or GABA, is the chief "inhibitory" neurotransmitter that "quiets" down the central nervous system. Some people do well taking 500 mg of GABA one half hour before bed. Some require more. But it's not easy for GABA to pass the blood brain barrier, whereas the progesterone metabolite does and also signals GABA receptors.
  • CBD oil. Cannabidiol (CBD) is a major "non-intoxicating" component of cannabis and possesses anti-epileptic, anxiolytic, anti-hyperalgesic and sleep-promoting properties. CBD signals GABAA receptors. It works in both capsule or drop form, but the dose varies greatly depending on the individual and the cause of insomnia. The CBD signals the cannabinoid system, which relaxes the central nervous system and by the way, overlaps with oxytocin signals.43
  • Magnolia bark. This herb is especially helpful for sleep, if the cause of insomnia is due to elevated nighttime levels of the stress hormone cortisol. This herb lowers both stress hormones (cortisol and adrenaline) and keeps these lower all night to allow you to sleep.
    o Magnolia bark reduces the time it takes you to fall asleep and increases the amount of time you spend in both REM sleep and non-REM sleep.
    o Magnolia acts like an "herbal magnesium." It reduces anxiety. For some people, magnolia bark can be as effective as diazepam (valium) without the risks of dependency or adverse side effects. The typical dosage is 250-500 mg taken with dinner and also before bed.44 Severe insomniacs may need much more at the beginning but can taper down after sleep improves for at least two weeks.
  • Moon Drops. This is a pleasant vanilla-flavored homeopathic that works for a lot of my patients when slowly dissolved in the mouth half an hour before bed. It comes in such a cool-designed small box, tastes delicious, and works so well that it's a real go-to natural sleep aid, if your progesterone replacement is not doing the trick or you want to try to fix your issues sans hormones.
  • L-Theanine. This amino acid increases the levels of the three neurotransmitter musketeers – GABA, serotonin, and dopamine – calming neurotransmitters that "live" inside the brain and regulate emotions, mood, concentration, alertness, energy, and sleep.
    o L-theanine promotes healthier daytime emotions and nighttime sleep, helps with menopause- and andropause-related mood swings, difficulty concentrating, and it even helps some people regulate portion control.
    o If you're a caffeine junkie, L-theanine may even help counteract the anti-sleep effects of caffeine.45
  • 5–HTP. 5-HTP (5–hydroxytryptophan) increases serotonin, which is then converted to melatonin. 5-HTP is, thus, a melatonin-booster. Start at 100 mg, three times per day. Gradually increase to 200 mg, three times per day. Some cases of IBS (irritable bowel syndrome) are worsened by excessive levels of serotonin so don't take this without working with a smart doc, especially if you have gut issues.
  • Herbal helpers.
    o Valerian. (Valeriana officinalis) in capsule form – the liquid has a bitter taste though some of my patients think the liquid works better/faster –  at 150–300 mg standardized to 0.8% valerenic acid. Take one hour before pulling the covers up. Dormeasan ® drops are an organic valerian and hop tincture mixture that doesn't have a severe bitter taste. The dosage is 30 drops half an hour before bed. Putting the drops in a half cup of your favorite nighttime tea is a effective sleep-promoting routine.
    o Traditional Chinese medicines. One is called Suan Zao Ren.46 The formal name is Semen Ziziphi spinosae. It is the dried ripe seed of the sour jujube or spiny date. It has been used for hundreds of years in China to treat insomnia as well as reducing severe sleep disruptive dreams.47 This herb is especially helpful for patients trying to take low dose naltrexone (a super immune booster) but who begin having overwhelming dreams or insomnia as an adverse side-effect. Dosage varies depending on the product.
    o Another standard Chinese formula is called Gui Pi Tang.48 Again, dosage varies depending on the product.
    o Pueraria mirifica. An herb49 from Thailand used for hundreds of years to promote sleep by helping your body's natural estrogen reduce hot flashes or nasty sensations of dysphoria. Boron is a mineral that also helps bodies utilize estrogen in both ladies and gents.50 Estrogen is produced in six places inside a healthy brain and promotes sleep in both genders, although males, of course, have less estrogen than females. Sometimes I recommend the herb and boron together.
    o Pregnancy insomnia: Lettuce Seed (Lactuca sativa L. seeds) has been shown, in a human pregnancy study, to promote better sleep in insomniacs and found safe to take during pregnancy.51 The dose is one 1000 mg capsule of lettuce seed a half-hour before bed.

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