OTCs Today

Daniel L. Krinsky, BS, MS, RPh, FAPhA

Welcome to 2022! As we continue to navigate stressful and uncertain times, an issue such as insomnia—normally a fairly common complaint— will become even more prevalent. Nearly 60% of medications used for insomnia are nonprescription sleep aids—primarily antihistamines, which are associated with adverse effects in older adults. The combination of the frequent misuse of hypnotics and availability of nonprescription agents makes insomnia a disorder of significant concern.

Counseling counting sheep

Treatment goals are to improve your patient’s presenting symptoms, quality of life, and functioning while minimizing adverse effects. Nonpharmacologic options should be first-line recommendations. These include using a bed only for sleeping or intimacy, establishing a routine sleep pattern, engaging in relaxing activities before bedtime, and avoiding use of electronic devices (particularly smartphones, television, and tablets) around bedtime. Other suggestions include

• Make the bedroom comfortable for sleeping
• Avoid temperature extremes, noise, and light
• Avoid eating within 2 hours of bedtime
• Avoid using caffeine, alcohol, or nicotine for at least 4 to 6 hours before bedtime

OTC assistance

Diphenhydramine is the only product deemed safe and effective for self-administration as sleep support, per the most recent FDA final monograph on nonprescription sleep aids. Its primary indication is symptomatic management of transient and short-term sleep difficulty, particularly in individuals who complain of occasional problems falling asleep. The usual dosage is 50 mg nightly (the maximum daily dose), while some individuals benefit from a 25 mg dosage.

Doses should be taken 30 to 60 minutes before desired sleep onset. Maximum sedation occurs between 3 and 6 hours after a dose. Tolerance often develops within days of repeated use, so it’s best that patients skip a night after 2 to 3 nights to determine if insomnia is relieved. Patients should not take the medication longer than 10 days because of the potential for tolerance development to the sleep-inducing effects, but not necessarily to its adverse effects.

The primary adverse effects are anticholinergic and include dry mouth and throat, constipation, blurred vision, urinary retention, and tinnitus. Morning grogginess or excessive sedation are also possible. Contraindications include prostatic hyperplasia, difficulty urinating, angle-closure glaucoma, cardiovascular disease such as angina or arrhythmias, and dementia. A paradoxical effect of excitation occurs more often in children, older patients, and patients with neurocognitive disorders. Symptoms include nervousness, restlessness, agitation, tremors, insomnia, delirium, and in rare cases seizures.

Refer patients who are pregnant or breastfeeding for further evaluation. Behavioral interventions and good sleep hygiene are first-line treatment options for insomnia in children and adolescents. Treatment of insomnia in older adults consists of behavioral therapy and pharmacotherapy with approved agents. The Beers criteria recommend avoiding use of anticholinergic drugs; refer patients in this age group to their primary care provider for further evaluation.

Control of the sleep-wake cycle

Melatonin, a popular “natural” option to manage insomnia, is a hormone produced by the pineal gland. The dietary supplement form of melatonin is used primarily for insomnia, prevention of jet lag, and sleep issues related to shift work. This hormone regulates sleep and circadian rhythms and its release is induced by darkness and suppressed by light, especially blue light emitted by phone and computer screens. Exogenous administration stimulates sleep regulation mechanisms.

Melatonin usually does not cause “sleepiness,” although some morning drowsiness can occur as an adverse effect; rather, it may make attempts to sleep more successful. For insomnia, 0.3 mg to 5 mg is taken orally 30 to 60 minutes prior to bedtime. The dosage for occasional insomnia is unclear; supraphysiologic concentrations are produced by a 0.3 mg dose, and higher doses may not be more effective. Rare adverse effects include nausea and vomiting, headache, irritability, dysthymia and worsening of depressive symptoms, and morning grogginess. Any use in children in or around the age of puberty should be discussed first with a primary care provider. Pregnant and lactating women should not use melatonin.

Only a small percentage of patients with symptoms of insomnia actually consult their health care provider. Attempt to engage your patients interested in a sleep aid to determine the best options for an optimal outcome. ■