OTC Products for Insomnia: from Sleepless to Sweet Dreams

The value of a good night’s sleep is often underestimated until one experiences insomnia. Left untreated, insomnia can negatively impact an individual’s health, ability to perform routine tasks, and overall quality of life.

Insomnia is considered one of the most prevalent patient complaints, ranking third after headaches and the common cold.¹ More than 95% of Americans experience an episode of insomnia at some point in their life. Although the condition is more prevalent in females, middleaged and older adults, and patients with medical and psychiatric conditions, it can occur at any age.² Many female patients report sleeping difficulties during menstruation, pregnancy, and menopause, and the frequency of insomnia increases with age.^1-3 Patients with medical conditions such as hypertension, arthritis, heartburn, gastroesophageal reflux disease, depression, diabetes, and cardiovascular disease (CVD) are most likely to report having problems sleeping.² Patients who work various shifts and those with sleep apnea or restless leg syndrome may also be at greater risk for developing insomnia or sleep issues.^2,4

According to the National Institutes of Health, an estimated 30% of the general population reports sleep disruptions and an estimated 10% experience some degree of daytime cognitive impairment consistent with a diagnosis of insomnia.^3,5 Only a small percentage of patients actually discuss their sleep problems with their primary health care provider.^1,2 The Centers for Disease Control and Prevention reports that insomnia may be a risk factor for or increase the incidence of depression as well as other chronic disorders; insufficient sleep is associated with several chronic diseases and conditions, such as diabetes, CVD, sleep apnea, obesity, and depression.^2,6 Individuals with insomnia may experience low energy levels, decreased performance at work or school, difficulty concentrating, and fatigue.^3,7

Pharmacists are in a pivotal position to identify those medical conditions or pharmacologic agents associated with (or that may exacerbate) episodes of insomnia, as well as assist patients in making informed choices regarding the management and treatment of insomnia. Pharmacists can also be instrumental in recommending patients for further medical evaluations when warranted.

Types of Insomnia

Insomnia is generally classified as either primary or secondary.^1-3 Primary insomnia typically lasts for 1 month or longer; does not result directly from another sleep disorder, general medical condition, or psychiatric disorder; and does not result from the use of any pharmacologic agent.^1-3,6,8-10 Secondary insomnia is the most prevalent form, accounting for 8 of every 10 cases.^1,8-10 Secondary insomnia results from another identifiable underlying source, such as certain medical conditions or pharmacologic agents.^8-10 Insomnia can be further categorized based on the duration and severity of the episodes (Online Table 1^1,2,6,8-10).

TABLE 1: TYPES OF INSOMNIA

• Transient: Self-limiting and lasting less than 1 week; often caused by temporary stress, anxiety, or schedule changes

• Acute or short-term: Lasting 1 to 3 weeks; often caused by prolonged stress or anxiety caused by the death of a loved one, financial problems, etc

• Chronic: Lasting more than 3 weeks; often the result of medical conditions, mental disorders, or substance abuse; according to the NIH, the majority of chronic insomnia cases are due to secondary insomnia

Adapted from references 1, 2, 6, 8-10.

Causes of Insomnia

A number of psychological, physical, and environmental factors can cause insomnia (Online Table 2^1-3,8-10). Although the debate continues, results from some clinical studies suggest that there is a possible link between insomnia and the use of laptops, tablets, and mobile phones before bedtime. For example, results from 2 studies published in 2014 concurred that media use before bedtime contributed to an increased incidence of insomnia, and results from a third study showed that routine technology use at bedtime contributed to difficulty in falling asleep.^11-13 Because light exposure can impede melatonin production, results from a 2013 Mayo Clinic study suggest that dimming smartphone, laptop, and tablet brightness settings and holding the device at least 14 inches from the face while using it may decrease its potential to interfere with melatonin and negatively affect sleep.¹⁴

TABLE 2: CAUSES OF INSOMNIA

• Stress, anxiety, or depression
• Alterations in environment, routine, or schedule
• Certain medical conditions (eg, chronic pain conditions, congestive heart failure, hyperthyroidism, gastroesophageal reflux disease, respiratory disorders, psychiatric disorders , nocturia, restless leg syndrome)
• Use of certain pharmacologic agents (eg, anti-depressants, anti-hypertensives, sympathomimetic amines)
• Use of caffeine, nicotine, and alcohol

Adapted from references 1-3, 8-10.

Managing and Treating Insomnia

The effects of insomnia vary from patient to patient and can include irritability, difficulty concentrating, cognitive impairment, extreme fatigue, and anxiety.^1-4 Patients with insomnia may complain of trouble falling asleep or difficulty staying asleep accompanied by episodes of frequent waking. Before recommending any type of treatment, clinicians should evaluate the possible causes and the duration and severity of symptoms of the insomnia to determine the most appropriate treatment approach. The patient’s medical history, current medication profile, and allergy history should be taken into consideration before initiating therapy.

The primary goals of treatment for insomnia are to improve quality of sleep and daytime impairments.^1,2 Patients with transient or short-term insomnia typically can resolve the condition by incorporating better bedtime habits, also known as sleep hygiene measures, with or without nonprescription sleep aids.¹

An estimated 9% of the adult population in the United States uses some type of nonprescription insomnia medication to manage their insomnia. In addition, an estimated 5% of older adults, many of whom have restless leg syndrome or obstructive sleep apnea, report using a nonprescription sleep aid several times a week.¹

Currently available nonprescription products marketed for insomnia are indicated for the treatment of transient and short-term insomnia (Online Table 3).¹ One popular formulation is single-entity antihistamine products containing diphenhydramine or doxylamine; these are available in a variety of dosage forms, including flavored liquids, tablets, rapid melt tabs, and capsules. Another available formulation is antihistamine and analgesic products in combination for individuals whose insomnia is the result of uncontrolled pain.¹ Both diphenhydramine and doxylamine are ethanolamine antihistamines and are thought to affect sleep through their affinity for blocking histamine¹ and muscarinic receptors.^1,15

TABLE 3: EXAMPLES OF NONPRESCRIPTION PRODUCTS MARKETED FOR INSOMNIA

Active ingredient: diphenhydramine

• Maximum Strength Tranquil (25 mg)
• Nytol QuickCaps (25 mg)
• Sominex Maximum Strength Formula (50 mg)
• Sominex Original Formula (25 mg)
• Unisom Liquid (50 mg)
• Unisom SleepGels (50 mg)
• Unisom Sleep Quick Melts (25 mg)
• Tylenol Simply Sleep (25 mg)
• ZzzQuil LiquiCaps (25 mg)
• ZzzQuil Liquid (50 mg per 30 mL)

Active ingredient: doxylamine succinate

• Unisom SleepTabs (25 mg)

Antihistamine—analgesic combination products

• Advil PM (ibuprofen 200 mg/diphenhydramine citrate 38 mg)
• Bayer PM (aspirin 500 mg/diphenhydramine citrate 38.3 mg)
• Excedrin PM (acetaminophen 500 mg/diphenhydramine citrate 38 mg)
• Goody’s PM (acetaminophen 500 mg/diphenhydramine citrate 38 mg)
• Legatrin PM (acetaminophen 500 mg/diphenhydramine HCl 50 mg)
• Tylenol PM Simply Sleep (acetaminophen 500 mg/diphenyhydramine HCl 25 mg)
• Unisom PM Pain SleepCaps (acetaminophen 325 mg/diphenhydramine HCl 50 mg)

Melatonin-containing products

• MidNite (1.5 mg)
• Natrol Melatonin (5 mg)
• Nature Made Melatonin (3 mg)
• Nature Made Sleep (3 mg)
• Nature’s Bounty Melatonin Super Strength (5 mg)
• Schiff Melatonin Plus (3 mg)
• Sundown Melatonin (3 mg)
• Twinlab Melatonin (3 mg)

Products containing valerian root

• NatureMade Valerian Capsules (400 mg)
• Nature’s Bounty Valerian Root (450 mg)
• Nature’s Way Valerian Root (530 mg)
• Sundown Naturals Valerian Root (530 mg)

Other herbal combination products

• Alluna Sleep
• Boiron Quietude
• Hyland’s 4 Kids Calm ‘n Restful
• Hyland’s Calms
• Hyland's Insomnia
• NatraBio Insomnia Relief
• Nature Made Sleep Natural Sleep Aid
• Rapid Sleep PM
• Schiff Knock-Out
• Sleep MD Tablets

The majority of nonprescription sleep aids contain diphenhydramine and should be taken 30 to 60 minutes before bedtime, and only as needed. The typical dose is 50 mg, but some patients may benefit from only 25 mg.¹ Patients should be advised to take no more than 50 mg nightly for no longer than 7 to 10 days, unless otherwise directed by their physician.^1,15 In addition, a variety of alternative complementary products are available that include melatonin, valerian, and kava.^1,15

During counseling, pharmacists should encourage patients to discuss their sleep issues with their primary health care provider, especially if the insomnia shows no signs of improvement or worsens. Before recommending any nonprescription sleep aids, pharmacists should always screen for potential drug interactions or contraindications. Moreover, patients should be reminded that nonprescription sleep aids are indicated for short-term use only.1 In addition, pharmacists should ascertain whether the patient is an appropriate candidate for the use of these nonprescription sleep aids and ensure that patients thoroughly understand the proper use of these products and the their potential adverse effects, such as morning grogginess, dry mouth, constipation, and blurred vision.¹ Patients should be advised to adhere to the recommended dosing guidelines and to avoid the use of alcohol when taking these products. They should be cautioned to avoid performing tasks such as driving or operating machinery until their response to these products is known.^1,15

Nonprescription sleep aids are contraindicated in patients with prostatic hyperplasia and difficulty urinating, as well as in those with glaucoma, emphysema, and chronic bronchitis.^1,15 Patients with CVD, such as angina, may be more susceptible to anticholinergic adverse effects of these products and should not use them.1 Individuals with insomnia who are younger than 12 years, older than 65 years, or pregnant or breast-feeding, or have preexisting medical conditions should consult their primary health care provider prior to using any of these products.^1,15 Patients should also be advised not to take any other sleep aid products or any other products that may contain antihistamines, including topical antihistamine products, while taking these sleep aids.^1,15 In addition, pharmacists can suggest nonpharmacologic measures (Online Table 4^1,15-18) that may aid in getting a good night’s sleep and recommend resources that can offer further insight into insomnia (Online Table 5). Finally, pharmacists should always refer patients with chronic insomnia for further medical evaluation when warranted and recommend talking to their primary health care provider about a sleep study, as well as the various prescription sleep aids that are available.

TABLE 4: NONPHARMACOLOGIC MEASURES TO MANAGE INSOMNIA

• Ensure that the sleeping environment is conducive to sleep by minimizing both light and noise and regulating room temperature to a comfortable temperature.

• If possible, establish a bedtime ritual by going to bed at the same time each day. When possible, avoid napping during the day. Try to keep a consistent schedule.

• Avoid eating a heavy meal within 2 hours of bedtime. If hungry, eat a light snack.

• Practice relaxation techniques prior to retiring for the evening.

• Avoid the use of any caffeine, nicotine, or alcohol at least 4 to 6 hours before bedtime.

• Do not exercise regularly within 2 to 4 hours of bedtime.

• If unable to fall asleep after 20 minutes, get out of bed until tired.

Adapted from references 1, 15-18.

TABLE 5: RESOURCES REGARDING INSOMNIA

For more information on insomnia, please visit the following websites:

• National Center on Sleep Disorders Research: www.nhlbi.nih.gov/sleep

• American Sleep Association: www.sleepassociation.org

• National Sleep Foundation: www.sleepfoundation.org

• American Academy of Sleep Medicine: www.aasmnet.org/resources/factsheets/insomnia.pdf

Ms. Terrie is a clinical pharmacy writer based in Haymarket, Virginia.

References

1. Kirkwood C, Melton S. Insomnia. In Krinsky D. Berardi R, Ferreri S, et al, eds. Handbook of Nonprescription Drugs. 17th ed. Washington, DC: American Pharmacists Association; 2012.

2. Chawla J, Park Ya, Passaro EA, et al. Insomnia. Medscape website. http://emedicine.medscape.com/article/1187829-overview#aw2aab6b2b2. Accessed January 23, 2015.

3. Insomnia. National Sleep Foundation website. http://sleepfoundation.org/sleep-disorders-problems/insomnia. Accessed January 23, 2015.

4. Insomnia: overview and facts. American Academy of Sleep Medicine website. www.sleepeducation.com/essentials-in-sleep/insomnia. Accessed January 23, 2015.

5. Insomnia - symptoms and causes. American Academy of Sleep Medicine website. www.sleepeducation.com/essentials-in-sleep/insomnia/symptoms-causes. Accessed January 23, 2015.

6. Insomnia. American Academy of Sleep Medicine website. www.aasmnet.org/resources/factsheets/insomnia.pdf. Accessed January 23, 2015.

7. Sleep and sleep disorders. enters for Disease Control and Prevention website. www.cdc.gov/sleep/. Accessed January 23, 2015.

8. What are different types of insomnia? National Sleep Foundation website. http://sleepfoundation.org/sleep-news/what-are-different-types-insomnia. Accessed January 23, 2015.

9. What is insomnia? What causes insomnia? Medical News Today website. www.medicalnewstoday.com/articles/9155.php. Accessed January 23, 2015.

10. About insomnia. American Sleep Association website. www.sleepassociation.org/patients-general-public/insomnia/insomnia/. Accessed January 10, 2015.

11. Fossum I, Nordnes LT, Storemark SS, Bjorvatn B, Pallesen S. The association between use of electronic media in bed before going to sleep and insomnia symptoms, daytime sleepiness, morningness, and chronotype. Behav Sleep Med. 2014;12(5):343-57.

12. Arora T, Broglia A, Thomas GN, Taheri S. Associations between specific technologies and adolescent sleep quantity, sleep quality, and parasomnias. Sleep Med. 2014;15(2):240-247.

13. Brunborg GS, Mentzoni RA, Molde H, et al. The relationship between media use in the bedroom, sleep habits and symptoms of insomnia. J Sleep Res. 2011;20(4):569-575.

14. Mayo Clinic. Are smartphones disrupting your sleep? Science Daily website. www.sciencedaily.com/releases/2013/06/130603163610.htm. Accessed January 23, 2015.

15. Diphenhydramine. Medscape website. http://reference.medscape.com/drug/benadryl-nytol-diphenhydramine-343392. Accessed January 10, 2015.

16. Thorpy M. Sleep hygiene. National Sleep Foundation website. http://sleepfoundation.org/ask-the-expert/sleep-hygiene. Accessed January 10, 2015.

17. Sleep hygiene tips. Centers for Disease Control and Prevention website. www.cdc.gov/sleep/about_sleep/sleep_hygiene.htm. Accessed January 10, 2015.

18. Healthy sleep habits. American Academy of Sleep Medicine website. www.sleepeducation.com/essentials-in-sleep/healthy-sleep-habits. Accessed January 23, 2015.