How do antihistamines cause drowsiness. What are non-drowsy alternatives for allergy relief. How to minimize sedation from cold and flu medications. When should you consult an allergist for persistent symptoms.

Understanding Histamine and Its Role in Allergies

Histamine is a crucial chemical produced by the immune system to combat allergens and germs. During allergy flare-ups 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 uncomfortable symptoms.

Interestingly, histamine also plays a vital role in the brain, contributing to wakefulness and alertness. When antihistamines used for respiratory symptoms cross the blood-brain barrier, they can interfere with this function, resulting in drowsiness.

First-Generation vs. Second-Generation Antihistamines

Antihistamines are classified into two main categories: first-generation and second-generation. Understanding the differences between these types can help you make informed decisions about your allergy treatment.

First-Generation Antihistamines

• Examples: Diphenhydramine (Benadryl速)
• More likely to cause drowsiness
• Often used in cold and flu medications for nighttime relief
• Shorter duration of action

Second-Generation Antihistamines

• Examples: Cetirizine (Zyrtec速), Fexofenadine (Allegra速), Loratadine (Claritin速)
• Marketed as “non-sedating” or “less sedating”
• Longer-lasting effects
• Less likely to cross the blood-brain barrier

Why are second-generation antihistamines less likely to cause drowsiness? These newer medications are designed to have a reduced ability to cross the blood-brain barrier, minimizing their impact on brain histamine levels. As a result, they tend to cause less sedation while still effectively treating allergy symptoms.

Strategies to Minimize Drowsiness from Allergy Medications

If you find yourself struggling with drowsiness from allergy medications, consider implementing these strategies to help manage this side effect:

1. Opt for second-generation antihistamines like Allegra, which is generally considered the least sedating option.
2. Take your antihistamine in the evening rather than the morning to allow any drowsy effects to wear off overnight.
3. Explore nasal spray antihistamines, which target nasal passages directly and are less likely to cause systemic drowsiness.
4. Consider using intranasal corticosteroids, which can be effective in reducing the need for antihistamines.
5. Avoid alcohol consumption when taking antihistamines, as it can intensify sedation.

How long does antihistamine-induced drowsiness typically last? The duration of drowsiness can vary depending on the specific medication and individual factors. Some people may experience drowsiness for several hours after taking an antihistamine, while others may feel the effects for up to 24 hours. It’s important to pay attention to how your body reacts and adjust your medication schedule accordingly.

Navigating Cold and Flu Medications

Many people are unaware that cold and flu medications often contain first-generation antihistamines to address symptoms like runny nose and sneezing. These formulations are typically labeled for nighttime use due to their sedating effects.

When using cold and flu medications, keep the following tips in mind:

• Read labels carefully to identify antihistamine ingredients
• Follow dosage instructions precisely
• Avoid combining multi-symptom cold medications with additional antihistamines
• Be cautious of medications containing doxylamine, which can be particularly sedating

Why do cold and flu medications often include more sedating antihistamines? First-generation antihistamines are often more effective at treating cold symptoms and reducing nasal congestion compared to newer, less sedating options. Their drowsiness-inducing properties can also be beneficial for nighttime symptom relief, helping patients get much-needed rest.

The Role of Intranasal Corticosteroids in Allergy Management

Intranasal corticosteroids have emerged as a valuable tool in the management of allergies, offering several advantages over traditional antihistamines:

• Targeted delivery to nasal passages
• Reduced risk of systemic side effects
• Effective at reducing inflammation and allergy symptoms
• Can decrease reliance on antihistamines

How do intranasal corticosteroids work to alleviate allergy symptoms? These medications work by reducing inflammation in the nasal passages, which helps to prevent and relieve allergy symptoms. Unlike antihistamines, which block the effects of histamine after it’s released, corticosteroids help prevent the release of inflammatory substances in the first place.

It’s important to note that intranasal corticosteroids may take a few days to reach their full effectiveness. During this initial period, your healthcare provider may recommend using an antihistamine in conjunction with the corticosteroid spray.

When to Consult an Allergist

While over-the-counter medications can provide relief for many allergy sufferers, there are situations where professional medical advice is warranted. Consider scheduling an appointment with a board-certified allergist if:

• Your allergy symptoms persist for more than two weeks
• Over-the-counter medications fail to provide adequate symptom control
• You experience significant side effects from allergy medications
• You’re unsure of your specific allergen triggers

What can an allergist offer beyond over-the-counter solutions? A board-certified allergist can provide a comprehensive evaluation of your allergies, including allergy testing to identify specific triggers. They can also offer advanced treatment options such as allergen immunotherapy, which aims to reduce your overall sensitivity to allergens over time. Additionally, allergists can prescribe medications that may not be available over the counter and provide personalized strategies for managing your allergies effectively.

Alternative Treatments for Allergy Relief

For individuals who find antihistamines problematic due to drowsiness or other side effects, there are alternative treatment options to explore:

• Allergen immunotherapy (allergy shots or sublingual tablets)
• Leukotriene receptor antagonists
• Nasal saline irrigation
• Environmental control measures to reduce allergen exposure
• Natural remedies such as butterbur or quercetin (consult with a healthcare provider before use)

How does allergen immunotherapy work to provide long-term allergy relief? Immunotherapy involves exposing the body to gradually increasing amounts of specific allergens over time. This process helps the immune system build tolerance to these allergens, reducing the severity of allergic reactions and potentially eliminating the need for daily medications in some cases. Immunotherapy can be administered through regular injections (allergy shots) or daily sublingual tablets, depending on the specific allergens and patient preferences.

The Importance of Proper Allergy Management

Effective allergy management goes beyond simply treating symptoms as they arise. A comprehensive approach to allergy care includes:

1. Identifying and avoiding allergen triggers
2. Developing a personalized treatment plan with a healthcare provider
3. Consistently using prescribed or recommended medications
4. Monitoring symptoms and adjusting treatment as needed
5. Considering long-term solutions like immunotherapy when appropriate

Why is a proactive approach to allergy management crucial? By taking a proactive stance in managing your allergies, you can significantly improve your quality of life. This approach can help prevent severe allergy symptoms from developing, reduce the need for rescue medications, and minimize the impact of allergies on your daily activities and overall well-being.

Understanding the mechanisms behind antihistamine-induced drowsiness and exploring alternative treatment options can empower you to make informed decisions about your allergy care. Remember that everyone’s experience with allergies and medications is unique, so it may take some trial and error to find the most effective treatment plan for your individual needs. Don’t hesitate to consult with healthcare professionals to ensure you’re receiving the most appropriate and up-to-date care for your allergy symptoms.

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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Product Information

• Adults and children 12 years of age and over:
• Take one 180 mg tablet with water once a day; do not take more than 1 tablet in 24 hours.
• Children under 12 years of age: do not use.
• Adults 65 years of age and older: ask a doctor.
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Do not use if you have ever had an allergic reaction to this product or any of its ingredients.

Ask a doctor before use if you have kidney disease. Your doctor should determine if you need a different dose.

When using this product:

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If pregnant or breastfeeding, ask a health professional before use.

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For 30 count or larger count sizes:

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Ingredients

Active Ingredients

Fexofenadine HCl 180 mg (in each tablet)

An antihistamine that works to relieve allergy symptoms of sneezing, runny nose, itchy/watery eyes, and itchy nose or throat due to hay fever or other upper respiratory allergies.

Purpose: Antihistamine

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• You may be able to use your HSA or FSA tax-preferred savings account to purchase certain OTC products, including Allegra^®. The passage of the CARES Act by Congress includes provisions to restore OTC eligibility under tax-preferred HSA and FSA accounts. Plan details vary, so save your receipt and check with your benefits or health provider for eligibility.

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Get tips for managing indoor and outdoor allergies

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Allergy season is different for everyone. That’s because different kinds of outdoor allergens — or irritants — get distributed into the air year-round.

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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.