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What are the negative effects of doxylamine?

4 min read

Doxylamine, a common over-the-counter sleep aid often sold under the brand name Unisom, is a first-generation antihistamine widely used for short-term insomnia. However, its sedative properties and anticholinergic effects mean that understanding what are the negative effects of doxylamine is crucial for safe use.

Quick Summary

Doxylamine can cause next-day drowsiness, dry mouth, blurred vision, and constipation due to its anticholinergic properties. Serious risks include increased falls in older adults, cognitive impairment with long-term use, and severe overdose symptoms.

Key Points

  • Lingering Drowsiness: The most common negative effect is next-day drowsiness or a 'hangover effect' due to doxylamine's long half-life.

  • Anticholinergic Issues: Doxylamine can cause dry mouth, blurred vision, constipation, and difficulty urinating by blocking acetylcholine.

  • Increased Risk for Older Adults: Individuals over 65 have a higher risk of confusion, memory problems, and falls due to reduced clearance of the drug.

  • Dangerous Drug Interactions: Combining doxylamine with alcohol, opioids, or other CNS depressants can lead to severe sedation and slowed breathing.

  • Overdose Potential: High doses can result in serious complications like hallucinations, seizures, and rhabdomyolysis.

  • Not for Long-Term Use: Tolerance can develop, and chronic use is associated with cognitive decline and dependence.

In This Article

Common Side Effects of Doxylamine

Doxylamine is a first-generation antihistamine, and its most frequent negative effects are directly related to its sedative and anticholinergic properties. While many users tolerate the medication well for short-term use, these effects are important to be aware of.

Sedation and CNS Depression

  • Daytime Drowsiness: The most common effect is lingering drowsiness the morning after use, often referred to as a "hangover effect". Because doxylamine has a relatively long half-life of around 10 hours, it can stay in the system longer, particularly in older adults.
  • Dizziness and Impaired Coordination: Dizziness and a lack of coordination are common, especially when standing up or changing positions, which can increase the risk of falls. This effect can be more pronounced in older individuals.
  • Confusion: Mild confusion can occur, and it is more prevalent among older adults who are more sensitive to the drug's effects.

Anticholinergic Effects

The anticholinergic actions of doxylamine can affect various bodily functions, leading to several uncomfortable side effects. These include:

  • Dry mouth, nose, and throat (Xerostomia): A very common complaint, as the medication reduces secretions.
  • Constipation: By slowing intestinal movement, doxylamine can lead to constipation.
  • Blurred Vision: Blocking the chemical acetylcholine can cause temporary blurred vision that typically resolves once the drug's effects wear off.
  • Difficulty Urinating: Doxylamine can cause urinary retention or difficulty passing urine, a particular concern for men with an enlarged prostate.

Serious Risks and Considerations

While generally safe for short-term use, doxylamine carries more significant risks, especially in certain populations or when misused. These more severe negative effects warrant careful consideration.

Risks in Older Adults

Because older adults clear the medication from their bodies more slowly, they face a higher risk of side effects. Doxylamine is included in the Beers Criteria, a list of potentially inappropriate medications for people aged 65 and older. The risks include:

  • Increased Fall Risk: The combined effects of dizziness, confusion, and impaired coordination significantly increase the likelihood of falls and related injuries.
  • Cognitive Decline: Long-term or cumulative use of anticholinergic drugs like doxylamine is associated with a higher risk of cognitive impairment and dementia in older people.

Drug Interactions and Alcohol

Combining doxylamine with other substances can lead to severe central nervous system (CNS) depression and other dangerous effects. It is vital to consult a healthcare provider about all medications being taken.

  • CNS Depressants: Taking doxylamine with alcohol, opioids, muscle relaxants, other sleep medications, or benzodiazepines can dramatically increase drowsiness and lead to life-threatening slowed breathing.
  • MAO Inhibitors: Monoamine oxidase inhibitors (MAOIs) should not be used with doxylamine, as the combination can prolong and intensify anticholinergic effects.
  • Other Antihistamines: As many nighttime cold and allergy products contain antihistamines, combining them with a doxylamine sleep aid can lead to an overdose and excessive side effects.

Overdose Symptoms

An overdose of doxylamine can be serious and potentially fatal, with symptoms that include:

  • Severe drowsiness, confusion, or hallucinations.
  • Dilated pupils.
  • Fast or irregular heartbeat (tachycardia).
  • Seizures.
  • Rhabdomyolysis (breakdown of muscle tissue).

Long-Term Use and Rebound Insomnia

Doxylamine is not intended for long-term use, and reliance on the medication can lead to other issues. With repeated use, tolerance can develop, meaning the drug becomes less effective over time. Discontinuing the medication can sometimes lead to rebound insomnia, where sleep problems become temporarily worse than they were before treatment. To avoid dependency, doxylamine should be used for no longer than two weeks at a time.

Doxylamine vs. Diphenhydramine: A Comparison of Side Effects

As another popular over-the-counter sleep aid, diphenhydramine (Benadryl) offers a useful comparison for understanding doxylamine's profile.

Feature Doxylamine (Unisom SleepTabs) Diphenhydramine (Benadryl, ZzzQuil)
Primary Use Short-term sleep aid Allergies, cold symptoms, sleep aid
Half-Life Longer (10-12 hours) Shorter (4-8 hours)
Next-Day Drowsiness More likely due to longer half-life Less likely due to shorter half-life
Sedation Level Generally considered more sedating Strong sedative effect
Anticholinergic Effects Prominent (dry mouth, constipation, etc.) Prominent (dry mouth, constipation, etc.)
Primary Risk for Elderly Increased risk of confusion, falls Increased risk of confusion, falls

Conclusion

While doxylamine is an effective short-term sleep aid for some, it is not without significant negative effects, especially when used improperly or for extended periods. Common side effects like next-day drowsiness, dry mouth, and constipation are frequent and can be troublesome. More serious risks exist, particularly for older adults, who are vulnerable to cognitive side effects and an increased risk of falls. The potential for dangerous drug interactions with other CNS depressants and the risk of overdose highlight the importance of careful use and consulting a healthcare professional. For those with chronic sleep issues, a non-pharmacological approach or a different, less risky treatment may be more appropriate and safer in the long run.

For more detailed guidance on medication safety and usage, consider consulting the National Institutes of Health (NIH) website.

Frequently Asked Questions

The most common side effect is next-day drowsiness or a "hangover effect". Doxylamine's long half-life means its sedative effects can last into the next morning, potentially affecting alertness and coordination.

Yes, doxylamine has anticholinergic effects that can cause a variety of side effects, including dry mouth and constipation.

No, doxylamine is generally not recommended for adults over 65. It has a higher risk of causing confusion, dizziness, memory issues, and falls in this population due to slower clearance of the drug.

No, you should avoid drinking alcohol while taking doxylamine. Both are CNS depressants, and combining them can lead to dangerously excessive drowsiness and impaired coordination.

A doxylamine overdose can cause serious symptoms like severe drowsiness, confusion, hallucinations, a rapid or irregular heartbeat, seizures, and rhabdomyolysis. It can be fatal and requires immediate medical attention.

No, doxylamine is not recommended for long-term use. The body can build up a tolerance, making it less effective, and chronic use in older adults has been linked to a higher risk of cognitive decline.

Yes, doxylamine interacts with numerous other medications. You should avoid combining it with other sleep aids, other antihistamines, opioids, benzodiazepines, and MAO inhibitors due to the risk of severe sedation and other adverse effects.

References

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Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.