Introduction:

Insomnia is a problem that plagues a majority of the adult US population.  Insomnia results from a variety of clinical situations, resulting from metabolic disorders, physical or physiatric problems as well as from primary neuropychiatric pathology.  Oddly, a tremendous number of individuals choose to treat themselves, using non-prescription techniques, due to the ineffectiveness of traditional medicine. According to the National Health Interview Survey analysis, over 1.6 million civilian, noninstitutionalized adult US citizens use complimentry and alternative medicine to treat insomnia. (1).

Sleep deprivation, if allowed to persist will result in clinical depression, in as little as 3 days.(2)  If that depression is allowed to persist for 6 weeks, the problem can result in permanent biochemical changes in the brain.

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Diagnosis:

 

Research has demonstrated that the average adult requires at least 7, if not as much as 10 to 10.5 hours of un-interrupted sleep per night. Sleep deprivation implies external or environmental causes to the lack of sleep, such as a crying baby, schedule and shift work changes, environmental noises such as sirens, music, and traffic. Insomnia, however refers to the internal or physiologic manifestation of inadequate sleep.

Insomnia can be divided into 3 main types:

  1. Early insomnia-difficulty in falling asleep
  2. Mid-insomnia- wakening in the middle of the night with difficulty in returning to sleep
  3. Late insomnia- awakening before the desired time, again, with difficulty in returning to sleep.

The different types of insomnia have different causes, and treatment does, in fact, differ.

Treatment:

Non-prescription medications can be used effectively to restore a more normal sleep pattern.  Of the many choices, the most commonly used agents include:

  1. melatonin
  2. 5-HTP (5- hydroxy tryptophan)
  3. L-Theanine

A derivative of glutamic acid, theanine is classified as a non-protein amino acid. Theanine is one of the few nutrients able to cross the blood-brain-barrier with relative ease.  Upon entering the brain, theanine stimulates the striatum, hypothalamus, and hippocampus. These specialized areas of the brain are responsible for the release of the aforementioned mood-enhancing agents, such as serotonin and dopamine. [1, 2] An increased output of these neurotransmitters is associated with relaxation and stress relief. Theanine has been shown in various animal studies to counteract the stimulation affect of ingested caffeine, while increasing the output of GABA in the brain. [3] There is speculation that theanine actually blocks the glutamate (NMDA) binding site in the brain.

Theanine also acts as an antagonist to caffeine

    1. Chamomile
    2. Valerian root

Choice of agent and dosage is dependent on individual gender, age, and ‘co-morbidity.’  That is, different disease states influence the absorption of many medications, thereby resulting in higher, or lower, individual need.

  1. Early insomnia can be treated with, or without the careful use of prescription medications combined with nutraceutical agents. For centuries, alcohol and opiates have been used to induce sleep. Unfortunately, the sleep will typically persist for only 2-4 hours before awakening. The net effect is amelioration of early insomnia and inducement of mid-insomnia.
  2. Early insomnia can be treated with a variety of sopophorics, including the benzodiazepines, but there are other, newer agents that can be prescribed. The newer non-benzodiazepines are less likely to cause tolerance and rebound problems.
  3. Early insomnia can be treated with non-prescription agents, the most effective of which are 5-HTP, L-theanine and melatonin.  There are a variety of herbal products that contain these chemicals, but quality control issues are such that inconsistent results can be expected.  If used individually, or if used in pharmaceutical grade preparations, much more consistent results are obtainable.
  4. Mid-insomnia generally results from low or inadequate secretion of cortisol from the adrenal glands.
  5. Mid-insomnia can be treated with longer acting benzodiazepines, which will result an appearance of restorative sleep, either due to the amnestic nature of these medications or due to the sedative nature when given at higher doses. In either situation, sleep has not been adequately restored.
  6. Mid-insomnia commonly occurs in patients who take pain-medicines or alcohol, during the evening hours.
  7. Mid-insomnia can be treated with the co-administration of hydrocortisone, by mouth, and the administration of DHEA combined with Pregnenolone. Some patients respond to a number of ‘proprietary’ animal-derived glandular products. In any event, cortisone or hydrocortisone should only be administered after obtaining base-line, morning cortisol levels. If the morning cortisol levels are below 7.0 micrograms/dl.
  1. Late-insomnia is a common consequence of chronic stress states, and depression.
  2. Late-insomnia can occur in patients who suffer from back and hip problems. Very often these persons have difficulty finding a ‘comfortable’ sleep position, and awaken when pressure is put on a particular joint, bursa or nerve. In the very early morning hours, body temperature is the lowest, and muscles stiffen. Often the clinical picture, in these patients  is that of mixed mid and late insomnia.
  3. Late-insomnia can be treated with the use of magnesium chelate, melatonin, malic acid, and long-acting anti-inflammatory agents, taken at bed time. Evening use of muscle relaxants can be beneficial, including low-dose Baclofen, combined with low dosages of a long-acting benzodiazepine.  Evening use of opiates should be minimized or eliminiated, and evening or night-time use of alcohol should be avoided.

The use of prescription agents is often limited by insurance-coverage and expense.  Further, many of the prescription agents have secondary effects or side-effects that might not be so desirable, such as amnesia, memory impairment, lethargy, confusion, decrease in libido, changes in hormone levels, particularly cortisol and testosterone.

This is not necessarily the case with the ‘naturally occurring’ substances, such as 5-HTP, melatonin and L-Theanine.

  1. 5-HTP not only helps with sleep, but it is also useful in the treatment of depression and anxiety-disorders.
  2. Melatonin not only helps with induction of sleep, but it is a modulator of the immune system and it may be protective with certain cancers. It has shown to be a useful adjunt in the treatment of osteoporosis, auto-immune disorders, chronic pain & Fibromyalgia. In patients that use pain medications on a daily basis, melatonin may be the only medication that restores a normal sleep pattern.  Dosages of melatonin are greater in women than in men, and dosages are greater in opiate users than in non-opiate users.
  3. L-Theanine not only helps with induction of sleep, but it is a very useful anti-oxidant that is cyto-protective of the liver, and L-Theanine is useful in treating anxiety states.

 

Summary

 

Insomnia is a symptom, not a disease state.  Treatment is entirely dependent upon the disease state that is causing the insomnia.

To that end, a thorough hormonal evaluation should be considered in order to properly determine or detect those factors that have resulted in the sleep disorder.

Sequential or follow-up studies must be performed to refine the therapeutic intervention.

After a somewhat lengthy recovery period, whereby adequate sleep has been restored, the use of these sleep medications can be tapered downward. The period of recovery is variable, and it is generally longer in patients that are older.  It may be a matter of 3-4 weeks in adolescents, but this period could be 6 months to a year, or more in the elderly.  In patients where the underlying endocrinopathy is chronic, it may be necessary to anticipate an indefinite treatment period.

L-theanine
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5-HTP
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Melatonin 5 mg
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References

Theanine references:

  1. 1. Yokogoshi H, Kobayashi M, Mochizuki M, Terashima T. “Effect of theanine, r-glutamylethylamide, on brain monoamines and striatal dopamine release in conscious rats.  “Neurochem Res. 1998 May;23(5):667-73.
  1. 2. Yokogoshi H, Terashima T. “Effect of theanine, r-glutamylethylamide, on brain monoamines, striatal dopamine release and some kinds of behavior in rats.” Nutrition. 2000 Sep;16(9):776-7.
  1. 3. Kamath AB, Wang L, Das H, Li L, Reinhold VN, Bukowski JF. “Antigens in tea-beverage prime human Vgamma 2Vdelta 2 T cells in vitro and in vivo for memory and nonmemory antibacterial cytokine responses.” Proc Natl Acad Sci U S A. 2003 May 13;100(10):6009-14. Epub 2003 Apr 28.

1. Pearson NJ, Johnson LL, and Nahin RL: Insomnia, trouble sleeping, and complementary and alternative medicine: Analysis of the 2002 national health interview survey data.Arch Intern Med. 2006 ;166(16):1775-82.

2. Banks S, & Dinges DF: Behavioral and physiological consequences of sleep restriction.Clin Sleep Med. 2007 Aug 15;3(5):519-28.

Lamarche LJ, De Koninck J. Sleep disturbance in adults with post-traumatic stress disorder: a review.J Clin Psychiatry. 2007 Aug;68(8):1257-70.


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David S Klein

Stages of Life Medical Institute

1917 Boothe Circle

Longwood, FL 32750