How do antihistamines cause drowsiness. What are the differences between first-generation and second-generation antihistamines. How can you minimize drowsiness when taking allergy medications. What precautions should you take when using cold and flu medicines containing antihistamines.

Understanding Histamine and Its Role in Allergies and Sleep

Histamine is a crucial chemical produced by the immune system to combat allergens and germs. During allergic reactions or infections like the common cold, histamine production increases, leading to symptoms such as runny nose, coughing, sneezing, and itchy eyes. Antihistamine medications work by blocking the effects of histamine, thereby alleviating these symptoms.

However, histamine also plays a vital role in the brain, contributing to wakefulness. When antihistamines used for respiratory symptoms enter the brain, they can interfere with this function, resulting in drowsiness.

The Dual Nature of Histamine

• Immune system function: Fights allergens and germs
• Brain function: Promotes wakefulness

Can histamine levels affect sleep patterns? Yes, histamine levels can influence sleep-wake cycles. Higher histamine levels in the brain are associated with increased alertness, while lower levels can contribute to drowsiness.

First-Generation vs. Second-Generation Antihistamines: Drowsiness Factors

Antihistamines are classified into two main categories: first-generation and second-generation. The primary difference between these types lies in their likelihood to cause drowsiness and their duration of action.

First-Generation Antihistamines

First-generation antihistamines, such as diphenhydramine (Benadryl速), are more likely to cause drowsiness. This is because they can easily cross the blood-brain barrier and affect histamine in the brain. While this makes them effective for treating allergy symptoms, it also increases the likelihood of sedation.

Second-Generation Antihistamines

Newer, second-generation antihistamines like cetirizine (Zyrtec速), fexofenadine (Allegra速), and loratadine (Claritin速) are often marketed as “non-sedating” options. These medications are less likely to cross the blood-brain barrier, resulting in reduced drowsiness for many users.

Do all second-generation antihistamines have the same level of drowsiness? No, even among second-generation antihistamines, there can be variations in sedating effects. For example, Allegra is generally considered the least sedating option among this group.

Strategies to Minimize Drowsiness from Allergy Medications

While drowsiness is a common side effect of antihistamines, there are several strategies you can employ to minimize its impact on your daily life:

1. Opt for second-generation antihistamines
2. Consider nasal spray antihistamines
3. Use intranasal corticosteroids
4. Take antihistamines in the evening
5. Avoid alcohol consumption

Nasal Spray Antihistamines

Nasal spray antihistamines are less likely to cause drowsiness as they target nasal passages directly, rather than circulating throughout the body via the bloodstream. These are typically available by prescription only.

Intranasal Corticosteroids

Regular use of intranasal corticosteroids can be an effective way to reduce reliance on antihistamines. While they may take a few days to start working, they are generally safe and can provide long-term relief. Some intranasal corticosteroids are available over-the-counter, while others require a prescription.

Is it safe to use antihistamines with intranasal corticosteroids? Yes, it is generally safe to use both medications together, especially during the initial days of corticosteroid treatment. However, always consult with your doctor or pharmacist for personalized advice.

Cold and Flu Medications: Hidden Antihistamines and Drowsiness Risks

Many people are unaware that cold and flu medications often contain first-generation antihistamines, which are more likely to cause drowsiness. These medications are typically better at treating cold symptoms and reducing nasal congestion than newer antihistamines.

Nighttime Use and Labeling

Due to their sedating effects, cold medicines containing antihistamines are usually labeled for nighttime use. It’s crucial to take this labeling seriously, as some formulations may include highly sedating ingredients like doxylamine.

Dosage Considerations

Always check labels carefully for dosage instructions, as these may vary even within the same brand. It’s important to follow recommended dosages and avoid supplementing multi-symptom cold medications with additional single-ingredient antihistamines.

Why should you avoid combining different antihistamine-containing medications? Combining multiple antihistamine products can increase the risk of side effects, including severe drowsiness, without providing additional therapeutic benefits.

Personalized Approaches to Allergy and Cold Symptom Management

Individual responses to antihistamines can vary significantly. What works well for one person may cause excessive drowsiness in another. Therefore, it’s essential to adopt a personalized approach to managing allergy and cold symptoms.

Finding the Right Medication

Experiment with different types of antihistamines to find the one that effectively relieves your symptoms without causing unacceptable levels of drowsiness. Once you find a medication that works well for you, stick with it. Be sure to check chemical ingredients and dosages before switching brands or generics.

Consulting a Healthcare Professional

If your allergy symptoms persist for more than two weeks or are not adequately controlled with over-the-counter medications, it’s advisable to consult a board-certified allergist. They can provide a comprehensive diagnosis and offer alternative treatment options if antihistamines are causing problematic side effects.

When should you consider allergen immunotherapy? Allergen immunotherapy may be recommended if you experience frequent or severe allergy symptoms, or if medications are not providing sufficient relief. This treatment can help reduce your sensitivity to specific allergens over time.

Beyond Medication: Holistic Approaches to Allergy Management

While antihistamines and other medications can provide relief from allergy symptoms, a holistic approach to allergy management can lead to better long-term outcomes. This involves understanding your specific allergens and taking steps to prevent or reduce exposure.

Allergen Identification

Working with an allergist to identify your specific allergens through tests such as skin prick tests or blood tests can provide valuable information for managing your allergies effectively.

Environmental Control Measures

Implementing strategies to reduce allergen exposure in your home and daily environment can significantly decrease your reliance on medications. This may include:

• Using air purifiers with HEPA filters
• Regularly washing bedding in hot water
• Keeping windows closed during high pollen days
• Using dust mite-proof covers on mattresses and pillows
• Controlling humidity levels to prevent mold growth

How can you monitor local pollen levels? Many weather apps and websites provide daily pollen forecasts. Checking these regularly can help you plan outdoor activities and take preventive measures on high pollen days.

Emerging Treatments and Future Directions in Allergy Management

The field of allergy treatment is continually evolving, with researchers exploring new approaches to manage symptoms more effectively while minimizing side effects like drowsiness.

Biologics for Severe Allergies

For individuals with severe allergies or asthma, biologic medications that target specific components of the allergic response are becoming increasingly available. These treatments can provide relief without the systemic side effects often associated with traditional antihistamines.

Nasal Filters and Barrier Devices

Innovative nasal filters and barrier devices are being developed to physically block allergens from entering the nasal passages. These non-pharmacological approaches may offer an alternative for those who experience significant drowsiness with antihistamines.

Personalized Medicine Approaches

Advances in genetic testing and biomarker identification may lead to more personalized treatment strategies in the future. This could allow healthcare providers to predict which medications will be most effective and least likely to cause side effects for individual patients.

Will allergy treatments become more personalized in the future? As our understanding of the genetic and molecular basis of allergies improves, it’s likely that treatment approaches will become increasingly tailored to individual patients, potentially leading to more effective symptom management with fewer side effects.

Lifestyle Considerations for Managing Allergy Symptoms and Medication Side Effects

Effectively managing allergy symptoms while minimizing the impact of medication side effects often requires a multifaceted approach that includes lifestyle modifications.

Sleep Hygiene

Maintaining good sleep hygiene can help counteract the drowsiness sometimes associated with antihistamine use. This includes:

• Establishing a consistent sleep schedule
• Creating a relaxing bedtime routine
• Ensuring your bedroom is dark, quiet, and cool
• Limiting screen time before bed

Dietary Considerations

Certain foods and dietary habits may influence allergy symptoms and medication effectiveness:

• Staying hydrated to thin mucus secretions
• Consuming foods rich in vitamin C and quercetin, which may have natural antihistamine properties
• Limiting alcohol and caffeine, especially when taking antihistamines

Exercise and Physical Activity

Regular exercise can help boost overall health and may even help alleviate some allergy symptoms. However, it’s important to consider timing and location:

• Exercise indoors on high pollen days
• Shower and change clothes after outdoor activities
• Consider wearing a mask during outdoor exercise in allergy season

Can exercise help reduce allergy symptoms? While exercise itself doesn’t cure allergies, it can help improve overall health and may reduce the severity of some allergy symptoms. Additionally, the endorphins released during exercise can help counteract feelings of fatigue or drowsiness.

Navigating Seasonal Changes and Allergy Medication Adjustments

Allergy symptoms and medication needs often fluctuate with seasonal changes. Understanding these patterns can help you manage your symptoms more effectively throughout the year.

Anticipating Seasonal Allergies

Different allergens tend to peak at various times of the year:

• Spring: Tree pollen
• Summer: Grass pollen
• Fall: Weed pollen and mold spores
• Winter: Indoor allergens (dust mites, pet dander)

Proactive Medication Management

Consider starting allergy medications before your typical symptom onset. This proactive approach can help prevent symptoms from becoming severe and may reduce the need for higher doses of antihistamines.

Adjusting Treatment Plans

Work with your healthcare provider to develop a flexible treatment plan that can be adjusted based on seasonal changes and symptom severity. This may involve switching between different types of antihistamines or incorporating other treatments as needed.

Should you take allergy medications year-round or only during peak allergy seasons? The answer depends on your specific allergy profile and symptom patterns. Some individuals may benefit from year-round treatment, while others may only need medication during specific seasons. Consult with an allergist to determine the best approach for your situation.

Educating Others: Workplace and School Considerations

Managing allergy symptoms and medication side effects can be challenging in professional and educational settings. Educating those around you about your condition and needs can help create a more supportive environment.

Workplace Accommodations

Consider discussing your allergy management needs with your employer or HR department. Potential accommodations might include:

• Flexibility in scheduling to accommodate medication timing
• Adjustments to the work environment to reduce allergen exposure
• Permission to use air purifiers or other allergy management devices

School and Academic Settings

For students, it’s important to communicate with teachers, school nurses, and administrators about allergy management needs. This may involve:

• Developing an allergy action plan
• Ensuring access to necessary medications during school hours
• Educating classmates about allergy awareness and prevention

Travel Considerations

When traveling for work or leisure, planning ahead can help manage allergy symptoms effectively:

• Research pollen levels and common allergens at your destination
• Pack necessary medications and consider bringing extras
• Communicate any special needs to travel companions or hosts

How can you effectively communicate your allergy needs in new environments? Be clear and specific about your allergy triggers, symptoms, and medication requirements. Providing written information or an allergy action plan can be helpful in ensuring others understand and can support your needs.

When Allergy or Cold Medication Makes You Drowsy

Tips for Staying Alert

By Purvi Parikh, MD

In treating allergies or a cold with antihistamines, you may experience drowsiness, a common side effect of the medication.

How does this happen? Histamine is a chemical produced by the immune system to fight off allergens and germs. When there is a threat of allergies or infection (such as the common cold), histamine is even more active. In its search-and-destroy process, it can cause allergy or cold symptoms such as runny nose, coughing, sneezing and itch eyes. Antihistamine medications relieve these symptoms by blocking the unwanted effects of histamine.

Unrelated to the immune system, histamine is also produced in the brain, where it plays an important part in feeling awake. Antihistamines used to treat respiratory symptoms can get into the brain and interrupt this work, making you feel drowsy.

What can you do about drowsiness from allergy medicines?

Some antihistamines are less likely to cause drowsiness than others. Reactions vary considerably from one person to another. What relieves your symptoms without making you sleepy may be different from what works for someone else.

When you find one that works for you, stick with it – check chemical ingredients and dosages before changing brands or generics. On the other hand, if one doesn’t work for you, try another type.

Does diphenhydramine (Benadryl®) make you sleepy? First-generation antihistamines such as diphenhydramine (Benadryl®) usually cause drowsiness because they are less likely to affect the histamine produced in the brain or have other unwanted effects in the brain. Currently, there is no non-drowsy Benadryl® on the market.

Non-drowsy allergy medicines do exist. Newer, second-generation antihistamines such as cetirizine (Zyrtec®), fexofenadine (Allegra®) and loratadine (Claritin®) – marketed as “nonsedating” – usually cause less drowsiness. An added benefit is that second-generation antihistamines last longer than Benadryl. Allegra is generally the least sedating.

Nasal spray antihistamines are also somewhat less likely to make you sleepy, since they target nasal passages directly rather than sending medicine throughout your body in the bloodstream. These are available only by prescription.

Regular use of an intranasal corticosteroid is not only safe but also an effective way to reduce use of antihistamines. They take a few days to start working, so you need to be patient. Ask your doctor or pharmacist about using an antihistamine with an intranasal corticosteroid the first few days. Some intranasal corticosteroids are available over-the-counter, while others are available as prescription medication.

To avoid daytime drowsiness, take an antihistamine in the evening rather than in the morning. It may help you sleep, with drowsy effects wearing off by the next morning. Be aware that drowsiness can last longer than you might expect – and that some antihistamines can cause vivid dreams.

Don’t drink alcohol when taking antihistamines, as it will increase the sedation.

What about antihistamines in cold and flu medications?

What many people may not know is that cold and flu medicines marketed to treat runny nose and sneezing usually include first-generation antihistamines – the more sedating types. That’s because they are often better at treating cold symptoms and drying up runny nose than the newer types.

Because of their sedating effect, cold medicines with antihistamines are labeled for nighttime use. Take this labeling seriously, as some include medications like doxylamine that are more sedating than others. Check labels for dosages as well, as these may vary, even within brands.

More is not better – read labels carefully and take only as recommended. Don’t supplement a multi-symptom cold medication with another single-ingredient antihistamine.

Be smart, be aware of allergy medication side effects

Smart use of allergy medications – knowing how they treat symptoms of an allergic reaction, being aware of potential unwanted side effects and, most important, monitoring their effect on you and your health – is just one step toward controlling allergy and cold symptoms. Even more important: knowing what you are allergic to and taking steps to prevent or reduce exposure.

If your allergy symptoms tend to last longer than two weeks or are not adequately controlled with over-the-counter medications, schedule an appointment with a board-certified allergist for a full diagnosis.

Antihistamines and intranasal corticosteroids are intended for symptom relief. If antihistamines or intranasal corticosteroids are causing side effects such as drowsiness or other problems, there are other treatment options your doctor can offer for relief from allergic reactions. These options include allergen immunotherapy and non-drowsy allergy medicines like second-generation antihistamines or nasal sprays.

Reviewed by:
Dennis Williams, PharmD, is an Associate Professor at the University of North Carolina Eshelman School of Pharmacy. He practices at UNC Medical Center with the pulmonary medicine medical service. He has served as a member of the National Asthma Education Program Coordinating Committee and the National Asthma Educator Certification Board. He serves on Allergy & Asthma Network’s Board of Directors.

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Get tips for managing indoor and outdoor allergies

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What and how to treat allergies?

With various allergic symptoms – runny nose, conjunctivitis, urticaria, etc. – we, of course, resort to the help of antihistamines. But at the same time, we rarely think about their features: for example, to which generation this or that remedy belongs, what side effects it has. And it should.

Determining the diagnosis

Let’s start with what is currently known two generations of antihistamines . The first antihistamines began to be used in the 40-50s of the last century. These drugs initially had a number of serious side effects, which, however, did not prevent them from “gaining popularity” – the work on their creation was even awarded the Nobel Prize! ²
Meanwhile, medicine was advancing. In the 1980s, 2nd generation antihistamines appeared. They acted faster, more efficiently and were deprived of a number of side effects. But, nevertheless, many representatives of first-generation antihistamines continue to be widely used, and this despite the fact that reports of undesirable consequences of their use appeared almost 60 years ago! ¹
To this day, we continue to treat allergies with outdated remedies. Out of ignorance or “out of habit” – it doesn’t matter! Agree, if there are more modern and safe drugs, it is unreasonable to use their less successful predecessors, which can harm the health of you and your children.
Still in doubt? Let’s talk in more detail about the dangers of first-generation antihistamines, what advantages second-generation drugs have over them, and which of their representatives should be remembered.

Diagnosis established

“Search and neutralize” ²
Imagine: an allergen enters the body, an allergic reaction begins, during which histamine is released. By binding to receptors, this substance causes swelling, redness of the skin, bronchospasm, difficulty in nasal breathing, so it is very important to block its action, stop the inflammatory reaction.
Histamine receptors are found in blood vessels, smooth muscles, the heart, tissues of the central nervous system, epithelium, and also in the brain. ⁷ In order to relieve allergy symptoms, it is enough to act on peripheral receptors. However, first-generation antihistamines also block receptors in the brain, resulting in a number of side effects:
– They act on the central nervous system, and therefore cause sedation – drowsiness, inhibition of reactions .
– Their action is not stable and durable, which makes it necessary to use high doses several times a day (up to 4-6 times) of these drugs. ( And this despite the fact that the therapeutic concentration is reached only after 2 hours! ³ ) As a result, when using these drugs, there is a possibility of a whole range of side effects: drowsiness, dizziness, lethargy, impaired coordination, inability to concentrate.
– They do not have selectivity (“targeting” action on histamine receptors), they also block other types of receptors, which can cause tachycardia, dryness of the nasopharynx and oral cavity, urinary retention, constipation, and visual impairment. The condition of bronchial asthma may even be aggravated (sputum viscosity increases) and cardiac arrhythmia may occur as a result of toxic effects on the heart. ¹
– May be addictive, and with prolonged (more than 7-10 days) use, the therapeutic activity of the drug decreases.
It is clear that in diseases such as bronchial asthma, chronic urticaria and perennial allergic rhinitis, requiring long-term use of antihistamines, the use of first-generation drugs is highly undesirable. ²
Mistakes we make ¹
Perhaps the biggest mistake of using 1st generation drugs is that many mothers give these drugs to babies before bed at night, hoping that the sedative effect will contribute to a deeper sleep of the child.
In the course of recent studies of the effect of 1st generation antihistamines on the functioning of the brain, it was proved that they cause unnatural sleep, disrupt the course of sleep phases! ¹ The onset of REM sleep (necessary for memory formation and brain development) is delayed, its duration is reduced. The use of first-generation antihistamines often leads to daytime sleepiness, reduced daytime activity, and impaired brain function, which is especially dangerous when they are used in children.

It has also been proven that 1st generation drugs contribute to a significant decrease in the ability of schoolchildren to learn, impaired concentration and memory.
With the regular use of such funds, cognitive functions (the ability of the brain to perceive and process information) are seriously affected, and therefore there is a threat to the full intellectual development of the child.

A special study was conducted in the UK with 1,834 teenage students taking exams. Among the students were those who suffered from allergic rhinitis. They were divided into two groups – those who were not treated with anything, and those who took first-generation antihistamines. For the former, the probability of “failing” the exam was 40%, for the latter – 70%. ¹
In general, it becomes clear why many developed countries are raising the issue of limiting the use of first-generation antihistamines without a prescription. ²
So, if you see one of the following substances on the package or in the instructions, know that you have a 1st generation antihistamine in your hands: Diphenhydramine, chloropyramine, promethazine, dimethindene, clemastine, mebhydrolin, etc. . ²

New generation chooses… ^2.3
What kind of allergy medications do we, modern people, need? Well, of course, those that:
– act quickly and efficiently;
– in therapeutic doses, they practically do not have a sedative effect;
– work even at a high concentration of histamine in the blood, without harming the body;
– suitable for the treatment of most allergic diseases, including chronic forms;
– practically do not affect the ability of children to learn and concentrate;
– contribute to improving the quality of life against the background of the current allergic disease.
It is these qualities that second-generation antihistamines have. These drugs include cetirizine (Zodak®), levocetirizine (Zodak Express®), and fexofenadine (Allegra).
These drugs can also be taken by children. Zodak® in the form of drops can be used in children from 6 months. ⁴ A Zodak® and Zodak Express® tablets are approved for use from 6 years of age.