Is doxylamine succinate (Doxylamine) okay to take for sleep?

From the Guidelines

Doxylamine succinate should not be used as a long-term solution for sleep problems due to its potential for tolerance and antimuscarinic adverse effects, and its use should be limited to short-term, occasional treatment of insomnia symptoms in healthy adults. According to the 2019 U.S. Department of Veterans Affairs and U.S. Department of Defense clinical practice guidelines 1, antihistamines like doxylamine succinate are not recommended for the treatment of chronic insomnia disorder due to their adverse effect profile and limited benefit. The guidelines advise against the use of antihistamines and antipsychotics for treatment of chronic insomnia disorder, citing the antimuscarinic adverse effect profile of antihistamines and the lack of systematic evidence supporting their efficacy.

Some key points to consider when using doxylamine succinate for sleep include:

• It should only be used occasionally for temporary sleep problems, not as a long-term solution
• Side effects may include morning drowsiness, dry mouth, dizziness, and constipation
• Doxylamine isn't recommended for people with certain medical conditions like glaucoma, enlarged prostate, asthma, or COPD
• It can also interact with other medications, particularly other sedatives or CNS depressants
• If sleep problems persist beyond 2 weeks of occasional use, it's essential to consult a healthcare provider as this could indicate an underlying condition requiring different treatment.

The American College of Physicians guideline on the management of chronic insomnia disorder in adults 1 also highlights the importance of using a shared decision-making approach when considering pharmacological therapy for insomnia, taking into account the benefits, harms, and costs of treatment. However, this guideline does not specifically address the use of doxylamine succinate for sleep.

In terms of alternative treatments, cognitive behavioral therapy for insomnia (CBT-I) is a recommended first-line treatment for chronic insomnia disorder, with moderate-quality evidence showing its effectiveness in improving sleep outcomes 1. Developing good sleep habits is also preferable to medication for managing chronic sleep issues.

From the FDA Drug Label

Warnings Do not use • in children under 12 years of age • with any other product containing doxylamine • unless you have time for a full night’s sleep

Ask a doctor before use if you have • a breathing problem such as emphyoma or chronic bronchitis • glaucoma • trouble urinating due to an enlarged prostate gland

Ask a doctor or pharmacist before use if you are taking • a sedative or any other sleep-aid • tranquilizers • any other antihistamines • any other drugs

When using this product • avoid alcoholic beverages • do not drive a motor vehicle or operate machinery • take only at bedtime

Stop use and ask a doctor if • sleeplessness persists continuously for more than two weeks. Insomnia may be a symptom of serious underlying medical illness.

Directions • adults and children 12 years of age and over: take one tablet 30 minutes before going to bed; take once daily or as directed by a doctor

Doxylamine succinate is okay to take for sleep in adults and children 12 years of age and over, as directed, with certain precautions:

• Take only at bedtime
• Avoid alcoholic beverages
• Do not drive a motor vehicle or operate machinery
• Use only if you have time for a full night's sleep
• Ask a doctor before use if you have certain medical conditions or are taking other medications 2 2

From the Research

Doxylamine Succinate for Sleep

• Doxylamine succinate is used in the short-term management of insomnia due to its sedative effects 3, 4.
• Evidence for the use of antihistamines to treat insomnia is generally lacking, but doxylamine is effective for up to four weeks 5.
• Doxylamine succinate 25 mg tablets exhibited similar oral bioavailability of doxylamine in the fasting state and in the fed state, indicating that food intake does not affect the kinetics of doxylamine in healthy subjects 4.

Pharmacokinetics and Safety

• The pharmacokinetics of doxylamine are dose-proportional over the therapeutic dose range of 12.5-25 mg in healthy volunteers 3.
• Doxylamine hydrogen succinate was safe and well tolerated, with the most common adverse event being somnolence 3, 4.
• The nasal spray formulation of doxylamine did not increase doxylamine absorption or systemic bioavailability compared to the oral tablet 6.

Clinical Use

• Doxylamine may be appropriate for treating insomnia in the last third of the night, particularly for maintenance insomnia 7.
• Better information to pharmacists on the prescription of doxylamine as an anti-H1 hypnotic would be beneficial to patients 7.
• Doxylamine is commonly proposed by pharmacists as a sleeping pill that does not require a prescription, but its use should be guided by pharmacokinetic and pharmacodynamic principles 7.