Close-up of two white pills

The human pineal gland manufactures the original sleep aid, melatonin (derived from serotonin), to put us into sleep. Although the pineal gland and its melatonin do not create our circadian rhythm, they act on it by increasing activity and levels, respectively, from a higher source of instructions, which is of course the brain.

Melatonin—the original hypnotic

The pineal gland is an endocrine gland that secretes melatonin, a hormone, into the blood and, more importantly, the cerebrospinal fluid (CSF). The melatonin in the blood is ten times higher at night than in the daytime blood.

Melatonin begins to be made during an infant’s 3rd to 4th month of age, when sleep patterns begin consolidating at nighttime.

Synthetic melatonin, a sleep-aid, has been shown to affect the circadian rhythm, but before going out to buy it, know that melatonin’s receptor sites become desensitized (less stimulated by melatonin) in larger doses.

Today’s anti-melatonin—laptops, pads, smartphones, and TV

It has been shown that blue light-emitting diodes suppress melatonin. The blue light frequencies of 446 to 477nm from light-emitting devices before bedtime can interfere with circadian rhythms and sleep by delaying their phases.  

Insomnia

Insomnia has three components:

  • Difficulty falling or staying asleep;
  • Occurring even with the right opportunity and circumstances for sleep;
  • Impaired daytime functioning due to this difficulty.

Previously, it was thought that insomnia was due to something else and that treating that something else be it a medical, psychiatric, or pharmaceutical condition, would treat the insomnia. This, however, is incorrect. Insomnia can occur all by itself and can make other conditions worse.

It can either be short-term or chronic. Short-term insomnia is usually an adjustment problem to stress or other factors and lasts less than three months. Chronic insomnia occurs at least three times a week for more than three months. It is associated with taking more than 30 minutes to fall asleep. Up to 10% of people experience chronic insomnia, and it is more likely in older populations.

The problem of insomnia

Besides the obvious problem of impairing daytime performance, insomnia can also provoke chronic self-medicating with over-the-counter (OTC) sleep-aids or alcohol and can cause prescription abuse of sedatives and hypnotics, which can become another significant problem.

How is chronic insomnia diagnosed?

There is no test. The diagnosis of insomnia is done via what is called a clinical diagnosis, a medical conclusion based on symptoms reported by the patient. A simple history that describes the sleep disturbance can differentiate it from other sleep disorders. Furthermore, a physical exam and perhaps blood or urine tests are helpful to catch any associated illnesses of insomnia.

How is insomnia treated?

  • Self-treatment: This is included only to explain the risks of self-treating insomnia. The preferred way of many sufferers of insomnia to undertake self-treatment is with alcohol, which will definitely shorten the time it takes to fall asleep but will interfere with the normal stages of sleep; using alcohol can result in sleep “fragmentation” and/or awakening too early.

  • Behavioral therapy: “Sleep hygiene” is the condition of having proper, healthy sleep patterns. Sleep phases of REM and Non-REM transition during the night, so it is important to establish a healthy quantity of sleep, which is usually eight hours for adults, a longer time for children, and a shorter time in elderly. An adequate duration assures all the phases carry through; as such, the right quantity of sleep assures the right quality of sleep and all of its regenerative properties.

Sleep hygiene can be achieved via the following:

    • Relaxation techniques and/or stimulus restrictions, such as ending domestic discord and limiting the usage of TV, electronic devices, caffeine, bedtime alcohol, smoking;
    • A rigid sleep/wake schedule, which re-establishes and reinforces circadian rhythm;
    • Regular exercise;
    • Bedtime environment adjustment.
  • Pharmacologic therapy:
  • Benzodiazepines These kind of drugs include Ativan, Halcion, and Rozerem. These are melatonin receptor agonists (help melatonin) and, except for Rozerem, are usually controlled prescriptions because they are associated with risks for tolerance and addiction.

  • Non-benzodiazepine hypnotics These kinds of drugs include Zaleplon (Sonata), zolpidem (Ambien), and eszopiclone (Lunesta). These are controlled prescriptions because they are associated with risks for tolerance or abuse; however, the risks of these occurring with this medication is smaller than the risks of tolerance or abuse occurring with the use of benzodiazepines.

  • Melatonin agonists One such agonist is ramelteon (Rozerem). Melatonin agonists, including the one just mentioned, are not associated with abuse, tolerance, or addiction, so they are not a controlled substance like most hypnotics are.

  • Antidepressants Such antidepressants include doxepin (Sinequan) and trazodone (Desyrel).

  • Suvorexant (Belsomra) This is a new class of hypnotics. It has a 12-hour half-life and promotes a normal sleep-wake cycle.

  Since both quantity and quality of sleep are important, the ideal drug for insomnia will have to allow one to fall asleep quickly but also leave the system quickly, so as to allow the subsequent phases of the normal sleep cycle to take place. Short acting medications include the following:

  • Zaleplon (Sonata);
  • Zolpidem (Ambien);
  • Triazolam (Halcion);
  • Lorazepam (Ativan);
  • Ramelteon (Rozerem).

For those with difficulty remaining asleep, the following longer-acting drugs can be indicated:

  • Zolpidem ER (Ambien ER);
  • Eszopiclone (Lunesta);
  • Temazepam (Restoril);
  • Estazolam (ProSom);
  • Doxepin (Sinequan);
  • Suvorexant (Belsomra).

Combined CBT and pharmacologic approach

This gives the best results.

What are treatment approaches to insomnia that should be avoided?

  • Alcohol: This shortens time to fall asleep but interferes with normal stages of sleep.
  • Diphenhydramine: This is sedating antihistamine that leaves a next-day hangover.
  • Antipsychotics: These have not yet been proven to be effective.
  • Barbiturates: These are addictive, and the body can grow a tolerance to them.
  • OTC: Herbal products are not under the scrutiny of the FDA for effectiveness, although melatonin may be helpful (see below).
  • Melatonin: This is safe and possibly helpful if it is used for less than three months.

What are the risks in NOT treating chronic insomnia?

Insomnia overstimulates the metabolism, brain, cardiac activity, and glandular activity. Therefore, there is an increased risk of hypertension and heart attack (myocardial infarction), diabetes, and both depression and anxiety. If it is left untreated, insomnia is likely to recur in half of the patients who experience improvements in their own insomnia over a year or two.

Insomnia’s risks are impaired next-day performance and the likelihood of dependence on hypnotics or other substances. This is contrasted by the risks of not treating it when it is deemed chronic: increased risk of heart disease, diabetes, and an increased metabolism. A healthcare professional is best qualified to assess the risks and benefits for treating insomnia.