Insomnia Treatment (Sleep Aids and Stimulants)

Treating insomnia may include various sleep aids and stimulants.

Insomnia is difficulty falling or staying asleep, the absence of restful sleep, or poor quality of sleep. Insomnia is a symptom and not a disease.

The most common causes of insomnia include:

• Medications
• Psychological conditions (for example, depression, anxiety)
• Environmental changes (travel, jet lag, or altitude changes)
• Stressful events or a stressful lifestyle

Insomnia can also be caused by poor sleeping habits such as excessive daytime naps or caffeine consumption and poor sleep hygiene.

The American Academy of Sleep Medicine estimates that 30% of adults have some symptoms of insomnia, 10% have insomnia symptoms so severe they cause consequences such as daytime sleepiness, and less than 10% have chronic insomnia.

Insomnia may be classified by how long the symptoms are present.

• Transient insomnia usually is due to situational changes such as travel, extreme climate changes, and stressful events. It lasts for less than a week or until the stressful event is resolved.
• Short-term insomnia usually is due to ongoing stressful lifestyles or events, medication side effects, or medical conditions and lasts for one to three weeks.
• Chronic insomnia (long-term insomnia) often results from depression, digestive problems, sleep disorders, or substance abuse and continues for more than three weeks.

Transient insomnia may progress to short-term insomnia, and without adequate treatment, short-term insomnia may become chronic insomnia.

Some of the medications and substances that can contribute to insomnia include:

• Caffeine and coffee
• Tobacco
• Alcohol
• Decongestants (for example, pseudoephedrine)
• Diuretics (for example, furosemide [Lasix], hydrochlorothiazide [Dyazide]) especially if taken in the evening or at bedtime
• Antidepressants (for example, bupropion [Wellbutrin, Wellbutrin SR, Wellbutrin XL, Zyban], fluoxetine [Prozac])
• Appetite suppressants (for example, sibutramine [Meridia], phentermine [Fastin])
• Amphetamines

• Benzodiazepines (for example, diazepam [Valium], chlordiazepoxide [Librium], lorazepam [Ativan])
• Alcohol
• Antihistamines
• Amphetamines
• Cocaine
• Marijuana
• Other addicting drugs

Insomnia can also result from poor sleep-related habits (poor sleep hygiene).

There are several ways insomnia may be treated without the use of medication. These include behavioral modification and the use of natural herbal remedies.

When a person consults a doctor about insomnia, they may be asked to keep a sleep log for several weeks to monitor sleep habits. The treatment options for short-term or chronic insomnia include not only medications but often sleep habits and behavioral modifications for optimal long-term results.

Evaluating sleep habits is important in the management of insomnia. Treatment of underlying sleep disorders and in some instances, changing sleep habits may correct the problem without the need for medications.

Good sleep habits (also referred to as good sleep hygiene) should include the following:

• Regular sleep times
• A comfortable bed and quiet room at a comfortable, temperature
• A darkened room
• Regular exercise, but not close to bedtime or late in the evening
• A bedroom that is not used for work, watching television, or other activities not related to sleep other than sex
• Avoid stimulants (for example, caffeine, or tobacco), alcohol, and large meals close to bedtime (avoid 2-4 hours before bedtime if possible)
• Many people watch television before falling asleep. TV can be a very stimulating medium and needs to be closely evaluated if it adds to a person's insomnia.
• Relaxation techniques such as breathing exercises or yoga
• No naps during the day
• Try drinking warm milk before bed. It is high in the amino acid tryptophan, which helps induce sleep.

Melatonin (for example, Melatonex) is the only hormone available in OTC for insomnia. Melatonin is a hormone produced by the pineal gland that helps regulate the body's clock or sleep-wake cycle. The secretion of melatonin is increased by darkness and decreased by light. The exact mechanism of how melatonin induces sleep has not been determined. Melatonin also decreases mental alertness and body temperature.

Melatonin is sold as a dietary supplement and is, therefore, not regulated by the FDA. It is commonly used for jet lag, insomnia, and sleep disturbances related to working night shifts. Some limited evidence suggests melatonin may be useful for treating sleep disturbances.

In 2005, MIT analyzed 17 peer-reviewed studies using melatonin. The analysis showed that melatonin was effective in helping people fall asleep at doses of 0.3 milligrams (mg). In some preparations, the dosage of melatonin is significantly higher and these larger doses have shown to be less effective after only a few days of use. If possible, patients may want to stay with the same formulation or brand if it is effective for them.

If a person would like to try melatonin tablets, consult a doctor first.

• Dosing: There is no established dose or time of administration. Individuals should follow the product labeling for dosing and administration.
• Pregnancy and lactation: The use of melatonin during pregnancy or lactation has not been studied adequately. Based on experience with other agents and the possibility of unknown risks to the fetus, melatonin should be avoided during pregnancy while breastfeeding. Consult your doctor before you use melatonin if you are pregnant or breastfeeding.
• Children: The use of melatonin in children may be effective, particularly in children with disturbed sleep due to autism spectrum disorders. However, it should not be used as a first-choice treatment in children. Consult your pediatrician before giving your child melatonin for sleep.
• Drug interactions: Although melatonin is sold as a dietary supplement, it should be thought of as a drug. It has side effects and may have drug interactions that have not been identified. The level of melatonin that the body produces is increased by certain drugs, such as selective serotonin reuptake inhibitor antidepressants or SRRIs (for example, fluoxetine [Prozac], sertraline [Zoloft], paroxetine [Paxil]) and monoamine oxidase inhibitors (for example, tranylcypromine [Parnate], phenelzine [Nardil]). The interaction between these antidepressants and melatonin used as a sleeping aid has not been assessed.
• Side effects: The most common adverse effect of melatonin is drowsiness. Therefore, tasks that require alertness (for example, driving) should be avoided for four to five hours after taking melatonin. Melatonin also may cause itching, abnormal heartbeats, and headaches. Melatonin appears to be safe when used short term (less than three months). The long-term side effects of melatonin are unknown.
  • Melatonin is either derived from animal sources or synthesized in a laboratory. Melatonin obtained from animal sources has a higher likelihood of contamination, which can cause allergic reactions and viral transmission, than synthetic melatonin.
  • Melatonin may stimulate the immune system. People with severe allergies or other disorders that may be caused by an overactive immune system (for example, systemic lupus erythematosus, or rheumatoid arthritis) should avoid using melatonin.
• Other herbal products: Natural herbal supplements such as valerian, chamomile, kava kava, and others have been touted as remedies for insomnia; however, the safety or effectiveness of these products has not been documented. Consult your doctor before taking any herbal supplements to treat insomnia.

Self-treatment of insomnia with over-the-counter (OTC) drugs is advisable only for transient or short-term insomnia. OTC sleep aids should only be used for a short period in conjunction with changes in sleeping habits. Chronic use of these drugs may result in dependence on them. This creates a situation in which sleep is not possible unless the drug is used. Chronic insomnia should be evaluated by a physician.

Diphenhydramine (for example, Sominex, Nytol) and doxylamine (for example, Unisom) are antihistamines currently marketed as OTC sleep aids. Diphenhydramine is the only agent considered to be safe and effective by the Food and Drug Administration. Other uses for diphenhydramine include allergies, motion sickness, and cough suppression. Scientists believe that diphenhydramine and doxylamine cause sedation by blocking the action of histamine in the brain, but the exact mechanism of action is not known.

If insomnia is associated with pain, there are numerous products containing a combination of an antihistamine and pain reliever. These combination products should not be used if pain is not present because the added pain reliever is not necessary.

• Pregnancy and lactation: The effects of diphenhydramine and doxylamine on the fetus have not been evaluated adequately. Diphenhydramine is classified as a pregnancy "category B" drug and is routinely safely used during pregnancy. Although the likelihood of an adverse effect on the fetus is low, sleeping agents probably should be avoided during pregnancy. Both agents may decrease lactation (production of milk). Additionally, these drugs are secreted into the breast milk, which could affect the newborn. Nursing mothers should avoid both drugs. Consult a physician if you are pregnant and have insomnia.
• Children: Children less than 12 years of age should not use doxylamine because its use in this age group has not been assessed.
• Elderly: The sedative effects of these drugs may interact with other potentially sedating medications. Consult a doctor before using these drugs.
• Drug interactions: Diphenhydramine and doxylamine add to the sedative effects of alcohol and other medications that cause drowsiness.
• Side effects: Drowsiness is the most frequent side effect of both diphenhydramine and doxylamine. These agents should not be used in situations where mental alertness is required (for example, driving). Diphenhydramine and doxylamine also cause constipation, dry mouth, and difficulty urinating. Both drugs may worsen the symptoms of glaucoma, asthma, heart problems, and prostate gland enlargement. People with these conditions should not use OTC sleep aids without consulting a physician.
  • Both drugs may paradoxically cause excitation, resulting in nervousness and insomnia. This occurs most often in children and the elderly.

There are numerous prescription medication options a doctor may prescribe if a person is suffering from short-term or chronic insomnia. Most are not recommended for long-term use.

Medication to treat insomnia includes several classes of drugs.

• Short-acting sedative-hypnotics (non-benzodiazepines) - these medications slow activity in the brain to allow sleep.
  • zolpidem (Ambien, ZolpiMist)
    • Intermezzo was approved by the FDA in 2011. It is a form of zolpidem, taken sublingually (dissolved under the tongue) and in smaller doses than Ambien.
  • zaleplon (Sonata)
  • eszopiclone (Lunesta)

In 2007, the FDA issued a warning regarding sedative-hypnotic drugs and their risks, which "...include severe allergic reactions and complex sleep-related behaviors, which may include sleep driving. Sleep driving is defined as driving while not fully awake after ingestion of a sedative-hypnotic product, with no memory of the event." The recommended dosing has recently changed and is different based on gender and other factors. You should ask your doctor and pharmacist about appropriate levels and warnings.

• Orexin receptor antagonists – suvorexant (Belsomra): This is a newer classification of insomnia medication working on orexin receptors in the lateral hypothalamus in the brain.  The drug acts by decreasing activity in the wake centers of the brain and helping patients transition to sleep.  This is in contrast to traditional insomnia medications which attempt to increase activity in the sleep centers of the brain. The medication is generally thought to be safe and well tolerated but some side effects may occur.
• Melatonin receptor agonists help patients who have difficulty falling asleep and it works similarly to melatonin
  • ramelteon (Rozerem): Ramelteon is a medication taken by mouth 30 minutes before bedtime. Ramelteon should not be taken if the patient will not be able to sleep for at least 7-8 hours. Insomnia usually improves in 7-10 days.
  • One of the advantages of ramelteon over other prescription sleep medications is the lack of dependence on the medication.
• Benzodiazepines (tranquilizers) - this class of medication is used to slow down the central nervous system, causing drowsiness. These medications have a high risk of dependence with chronic usage.
  • flurazepam (Dalmane)
  • temazepam (Restoril)
  • estazolam (ProSom)
• Tricyclic antidepressants: Tricyclic antidepressants are medications that work by increasing the amounts of certain natural substances in the brain that are needed for mental balance.
  • doxepin (Silenor): In 2010, this sleep medicine was approved for use in people who have trouble staying asleep. Silenor may help with sleep maintenance by blocking histamine receptors.

If your doctor recommends prescription sleep medications:

• Follow all prescribing instructions given by your physician.
• Tell your doctor about any other medications or supplements you take as many can have adverse interactions with sleep medications.
• Tell your doctor about any pre-existing medical conditions.
• Note any possible negative side effects (changes in your body, and even your emotions)
• Do not use the medications nightly unless instructed to do so by a doctor. This can lead to dependence.
• Avoid drinking alcohol or taking other non-prescription drugs while using sleep medication.
• Never drive a car or operate machinery after taking a sleeping pill.

People with insomnia often suffer from fatigue as a result of sleep deprivation. Stimulant products are frequently used in an attempt to offset fatigue and other unpleasant side effects that can accompany a lack of sleep. (These products are also used by people who need to stay awake for longer periods than is normal for them, such as for school examinations or long-distance driving.) However, the use of stimulant products can also cause insomnia, leading to a counterproductive effort to deal with sleep deprivation.

Caffeine (for example, NoDoz and Caffedrine) is the sole active ingredient in most non-prescription stimulants. It is the only drug approved by the FDA for this purpose. Caffeine is used to improve alertness and for staying awake. Caffeine is a powerful stimulant, but tolerance (the need to use increasing amounts) can be developed. Caffeine also is present in medications for menstrual cramps, headaches, and colds. Additionally, caffeine is found in coffee, tea, soft drinks, and chocolate.

Caffeine increases alertness by stimulating the nerves in the brain and spinal cord. It decreases muscle fatigue by stimulating muscle contraction. Caffeine also increases the heart rate and the force of contraction of the heart. The effect of caffeine varies among individuals and some people are only affected minimally.

• Pregnancy and lactation: Studies have shown that moderate caffeine intake does not cause low birth weights, miscarriages, or premature births. However, there are reports of birth problems in women who consume more than 300 milligrams per day of caffeine. Daily caffeine intake should probably be limited to less than 300 milligrams during pregnancy.
  • Caffeine passes into breast milk. The concentration of caffeine in breast milk is approximately 1% of the amount in the mother's blood. A lack of sleep and irritation may occur in breastfed infants whose mothers consume more than 600 milligrams of caffeine per day. No adverse effects have been noted in breastfed infants whose mothers consume between 200-336 milligrams per day of caffeine. A mother can limit the amount of caffeine her infant receives by limiting the amount of her caffeine intake and ingesting the caffeine after nursing.
• Children: Caffeine is not recommended for children less than 12 years of age.
• Elderly: Older persons may be more sensitive to the effects of caffeine, and it may increase the excretion of calcium from the body. In limited amounts, it is generally considered safe.
• Drug interactions: Cimetidine (Tagamet), norfloxacin Noroxin, ciprofloxacin (Cipro), and the estrogens in oral contraceptives block the breakdown and elimination of caffeine from the body. The use of caffeine with these drugs could lead to increased levels of caffeine in the body and, therefore, a higher likelihood of side effects.
  • Caffeine decreases the absorption of iron tablets. Iron should be administered 1 hour before or 2 hours after the consumption of caffeine.
  • Caffeine decreases the effects of sedatives, and sedatives decrease the restlessness, alertness, and arousal caused by caffeine.
• Adverse effects: The most common adverse effects of caffeine are insomnia, nervousness, excitement, headaches, vomiting, diarrhea, and stomach pain. Caffeine also causes abnormal heartbeats and increases heart rate.
  • Dependence can occur from the regular use of caffeine. If caffeine intake is stopped suddenly, a withdrawal reaction that consists of fatigue, headaches, anxiety, vomiting, and restlessness may occur. Symptoms of withdrawal start 12-24 hours after the last consumption of caffeine and may last for a week.