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Melatonin Therapy

Experts debate whether melatonin is actually a hormone. A common misconception is that the pineal gland is the only source of melatonin production. The pineal gland is not actually an endocrine gland. It is specialized nervous system tissue. Over the course of evolution it has lost the capacity to respond directly to light stimulation. It has developed the function of intermediary in our adaptation to day-night periodicity via neural impulses from the retina. Melatonin is synthesized at multiple sites in the body. It is produced in the intestinal wall lining cells in much greater quantity than in the pineal. It is produced by components of our white blood cell system as well.

After the pineal is removed, melatonin is still produced at other sites. There is no central “releasing factor” for melatonin, as in the case with other hormones. Melatonin is a universal chemical mediator in the plant and animal world. It is not a species-specific molecule.  This debate has fascinating implications for the scientists who study the subject. From a practical point of view melatonin is safe and can be very beneficial for the appropriate person. A reduction in melatonin production or an alteration of the normal circadian pattern of secretion is not an inevitable consequence of aging. Not all people need or will benefit from melatonin supplementation. The need for supplementation, the route of supplementation and the dose needs to be individualized, monitored and adjusted.

Signs and Symptoms of Melatonin deficiency:

• Premature aging; including premature graying
• Sleep disturbance manifested by difficulty falling asleep and a sleep that is light, agitated and easily interrupted
• A poor quality of dreaming
• Anxiety, hyperirritability, hypersensitivity
• Depressed immune function manifested by frequent infections that do not resolve in a reasonable time

Association of Melatonin deficiency and Illness:

• Women with PMS have lower levels of melatonin than age/matched controls
• Patients with coronary artery disease have a significantly lower level of melatonin
• Low levels of melatonin are noted in hypertension and melatonin supplementation has been noted to improve blood pressure in hypertensive patients

Recent advances in the knowledge of psychoneuroimmunology have demonstrated that anticancer immunity is under neuroendocrine control and that melatonin may stimulate IL-2-dependent anticancer activity. Experimental manipulations activating the pineal gland, or the administration of melatonin, reduce the incidence and growth rate of chemically induced murine mammary tumors, while pinealectomy, or situations which cause a reduction of melatonin production usually stimulate mammary carcinogenesis. The direct actions of melatonin on mammary tumors have been suggested because of its ability to inhibit, at physiological doses, the in vitro proliferation of MCF-7 human breast cancer cells. There are studies in the literature suggesting similar benefit for other solid tumors and hematologic malignancies. This does not mean that taking melatonin will prevent cancer or treat cancer. It is preliminary research that is interesting and suggestive. In appropriate patients, with low levels of melatonin, supplementation may be helpful. When dosed correctly it will not be harmful.

Melatonin may be helpful in the management of autoimmune diseases such as Multiple Sclerosis and some forms of arthritis.

Strategies for Increasing Melatonin Levels:

It is always seductive to solve our problems by just taking a pill. There are many strategies for improving pineal function and melatonin levels before resorting to supplementation:

1. Increase your exposure to daytime sunlight especially early morning light. In the winter months consider using full spectrum lighting or sitting in front of a “light box” for 30-90 minutes in the early morning.
2. Sleeping in a dark room will improve melatonin production. Minimize external lighting at night; get rid of all those ‘ever present’ clocks, night-lights and other gadgets that make unnecessary light. Get effective shading on the windows.
3. The temperature at which you sleep will effect melatonin production. Sleeping in environments that are too warm or too cold will impair melatonin production.
4. Certain medications may impair melatonin production.
   • Clonidine an anti-hypertensive medication
   • Beta blockers such as Propranolol and Atenolol
   • Benzodiazepines such as Valium, Ativan and Xanax
   • Neuroleptics such as Haldol disrupt the normal circadian rhythm of melatonin secretion.
   • Corticosteroids such as Prednisone will reduce melatonin levels.
5. Coffee and alcohol ingestion may decrease melatonin secretion and certainly contribute to sleep disturbance.
6. There are many dietary factors that will help pineal function and improve melatonin secretion:
   • Fruits such as bananas
   • Vegetables such as corn and tomatoes
   • Grains such as rice and oats
   • L Carnitine is a nutritional supplement that may be beneficial. I suggest Acetyl L Carnitine because it has the best absorption.
   • 5-HTP is a precursor to melatonin that has many benefits including improving symptoms of Anxiety, Depression, Sleep Disturbance, PMS, Headache
   • Vitamin B3 (Niacin)

Calcium and Magnesium

Melatonin Supplementation:
Episodic treatment may be useful in the following situations:

• Travel related sleep disturbance: take 1-3 mgs at bedtime for 1-3 days as needed to reset the sleep cycle.
• Weekend related sleep disturbance: this is useful for the individual who tends to stay up later on the weekend only to find it difficult to fall asleep on Sunday. Suggested dose is 1-3 mgs on Sunday and possibly Monday night.
• Stress related sleep disturbance

Regular Treatment may be indicated in individuals with the following conditions:

• Chronic health problems that disturb normal sleep patterns
• Chronic health problems for which melatonin therapy may be useful in overall management
• Chronic medication use that impairs melatonin secretion
• Aging individuals with documented deficiency by serum or salivary testing
• Sleep disturbance problems where melatonin may be part of a comprehensive therapeutic program
• Testing blood or salivary levels is in accurate, expensive and not helpful.

Dosing Options:

• Sublingual dosing is faster and the absorption is more reliable. The onset of action is 10-30 minutes and the duration of action is 3-6 hours. The average dose is 0.5-3 mgs.
• Oral dosing is slower in onset and more erratic in absorption. Onset of action is 30-60 minutes and duration of action is 5-8 hours.

Dosing Strategies:

Start low and escalate the dose slowly. Effects that suggest that the dose is excessive for you include excessive sleepiness in the early morning hours, day time sedation, hyperirritability, excessively vivid dreaming. I suggest starting as low as 0.5 mgs each night and escalating the dose by 0.5-1.0 mgs every three to five days. Keep a diary so you can track the effects. When there is a need to reduce the dose do it slowly by 0.5-1.0 mg increments.

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