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 are the alternatives to drowsy allergy medicines.

Understanding Antihistamines and Their Effects on the Body

Antihistamines are commonly used medications to treat allergies and cold symptoms. However, many people experience drowsiness as a side effect. To understand why this happens, it’s essential to know how antihistamines work in the body.

Histamine is a chemical produced by the immune system to combat allergens and germs. During allergic reactions or infections like the common cold, histamine becomes more active, leading to symptoms such as runny nose, coughing, sneezing, and itchy eyes. Antihistamines work by blocking the effects of histamine, thereby relieving these symptoms.

Interestingly, histamine also plays a crucial role in the brain, helping us feel awake and alert. When antihistamines used to treat respiratory symptoms enter the brain, they can interfere with this process, resulting in drowsiness.

Why do some antihistamines cause more drowsiness than others?

The drowsiness caused by antihistamines varies depending on the type of medication and individual reactions. First-generation antihistamines, such as diphenhydramine (Benadryl®), are more likely to cause drowsiness because they can easily cross the blood-brain barrier and affect histamine production in the brain. On the other hand, second-generation antihistamines like cetirizine (Zyrtec®), fexofenadine (Allegra®), and loratadine (Claritin®) are designed to be less sedating and have fewer effects on the brain.

Comparing First-Generation and Second-Generation Antihistamines

Understanding the differences between first-generation and second-generation antihistamines can help you make informed decisions about which medication to use for your allergy or cold symptoms.

First-Generation Antihistamines

• Examples: Diphenhydramine (Benadryl®)
• More likely to cause drowsiness
• Shorter duration of action
• Often found in cold and flu medications for nighttime use
• May be more effective at treating cold symptoms and drying up runny noses

Second-Generation Antihistamines

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

It’s important to note that individual reactions to these medications can vary. What works well for one person may cause unwanted side effects in another. Experimenting with different types of antihistamines under the guidance of a healthcare professional can help you find the most effective option with the least side effects.

Strategies to Minimize Drowsiness from Allergy Medications

If you’re concerned about feeling drowsy from your allergy medication, there are several strategies you can employ to minimize this side effect:

1. Take the medication in the evening: By taking your antihistamine before bed, you may be able to sleep through the drowsy effects, which could wear off by morning.
2. Try a second-generation antihistamine: These newer medications are less likely to cause drowsiness. Allegra is generally considered the least sedating among them.
3. Consider nasal spray antihistamines: These target nasal passages directly and are less likely to cause systemic drowsiness.
4. Use intranasal corticosteroids: Regular use of these sprays can effectively reduce the need for antihistamines. Some are available over-the-counter, while others require a prescription.
5. Avoid alcohol: Drinking alcohol while taking antihistamines can increase sedation.
6. Be consistent: Once you find a medication that works for you, stick with it. Check chemical ingredients and dosages before switching brands or generics.

Can you build up a tolerance to the drowsy effects of antihistamines?

While some people may develop a tolerance to the sedating effects of antihistamines over time, this is not guaranteed and can vary from person to person. It’s generally not recommended to rely on building up a tolerance as a strategy to combat drowsiness. Instead, focus on finding the right medication and dosage that works best for your individual needs.

Alternatives to Drowsy Allergy Medicines

For those who find the drowsiness caused by antihistamines to be problematic, there are several alternative approaches to managing allergy symptoms:

• Nasal corticosteroid sprays: These can effectively reduce inflammation and allergy symptoms without causing drowsiness.
• Allergen immunotherapy: This treatment involves gradually exposing your body to small amounts of allergens to build up tolerance over time.
• Natural remedies: Some people find relief from allergy symptoms through methods such as nasal irrigation with saline solution or consuming local honey.
• Environmental controls: Reducing exposure to allergens through measures like using air purifiers, keeping windows closed during high pollen days, and regularly cleaning bedding can help manage symptoms.

It’s important to consult with a board-certified allergist if your allergy symptoms persist for more than two weeks or are not adequately controlled with over-the-counter medications. They can provide a full diagnosis and offer personalized treatment options.

Decoding Cold and Flu Medication Labels

Many people may not realize that cold and flu medications often contain antihistamines, particularly first-generation types that are more likely to cause drowsiness. These are included because they are often effective at treating cold symptoms and drying up runny noses.

How can you identify drowsy ingredients in cold and flu medications?

To avoid unexpected drowsiness, it’s crucial to read medication labels carefully. Look for the following:

• Ingredients like diphenhydramine or doxylamine, which are known to cause drowsiness
• Labels indicating “nighttime” or “PM” use
• Warnings about drowsiness or advice against operating heavy machinery

Remember that dosages may vary even within brands, so always check the label and take only as recommended. Avoid supplementing a multi-symptom cold medication with another single-ingredient antihistamine, as this can increase the risk of side effects.

The Importance of Proper Allergy Diagnosis and Management

While managing the side effects of allergy medications is important, it’s equally crucial to understand the root cause of your allergy symptoms. Proper diagnosis and management can lead to more effective treatment and potentially reduce the need for medications that cause drowsiness.

What are the benefits of seeing an allergist?

Consulting with a board-certified allergist can provide several advantages:

• Accurate diagnosis of specific allergens triggering your symptoms
• Personalized treatment plans tailored to your individual needs
• Access to advanced treatment options like immunotherapy
• Guidance on environmental control measures to reduce allergen exposure
• Monitoring of treatment effectiveness and adjustment as needed

An allergist can help you develop a comprehensive approach to managing your allergies, which may include a combination of medications, lifestyle changes, and other therapies to provide relief while minimizing side effects like drowsiness.

Navigating Seasonal Allergies and Medication Use

Seasonal allergies can present unique challenges when it comes to managing symptoms and medication use. The severity of symptoms may fluctuate throughout the year, requiring adjustments to your treatment approach.

How can you effectively manage seasonal allergies while minimizing drowsiness?

Consider the following strategies:

1. Start medications before allergy season begins: This can help prevent symptoms from becoming severe.
2. Monitor pollen counts: Adjust your medication use and outdoor activities based on forecasted pollen levels.
3. Use a combination of treatments: Pairing a non-drowsy antihistamine with a nasal corticosteroid spray can provide comprehensive relief.
4. Consider allergy shots: For severe seasonal allergies, immunotherapy may provide long-term relief without the need for daily medications.
5. Practice good hygiene: Shower after spending time outdoors to remove pollen from your skin and hair.

By taking a proactive approach to seasonal allergy management, you can often achieve better symptom control while minimizing the need for medications that cause drowsiness.

The Future of Allergy Treatments: Emerging Options and Research

As our understanding of allergies and immune responses continues to grow, new treatment options are being developed that may provide relief without the side effect of drowsiness.

What are some promising new developments in allergy treatment?

Several areas of research show potential for improving allergy management:

• Biologics: These targeted therapies work by blocking specific components of the allergic response.
• Sublingual immunotherapy: This form of immunotherapy involves placing small amounts of allergen under the tongue, potentially offering a more convenient alternative to allergy shots.
• Nasal filters: These devices can physically block allergens from entering the nasal passages.
• Gene therapy: Research is exploring ways to modify the immune response at a genetic level.
• Probiotics: Some studies suggest that certain probiotics may help modulate the immune system and reduce allergic responses.

While many of these treatments are still in development or early stages of use, they represent exciting possibilities for future allergy management without the drawback of drowsiness.

As we continue to explore new frontiers in allergy treatment, it’s important to work closely with healthcare professionals to find the most effective and least disruptive management strategies for your individual needs. By staying informed about new developments and maintaining open communication with your allergist, you can navigate the challenges of allergy symptoms and medication side effects more effectively.

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.

Allegra vs. Zyrtec: How Do They Differ?

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Introduction

Sneezing, runny nose, and itchy, watery eyes. This can only mean one thing: allergy season.

Seasonal allergies are typically caused by your body’s reaction to pollen, a substance produced by trees and other plants. When these allergies strike, your body combats them by creating the symptoms you so despise. When these occur, you may consider using an over-the-counter (OTC) medication to ease your symptoms.

Allegra and Zyrtec are two commonly used allergy drugs. Both are available in prescription forms as well, but this article only covers the OTC versions. Here’s a side-by-side comparison to help you decide if one of them is right for you.

The main active ingredient in Allegra is fexofenadine. The main active ingredient in Zyrtec is cetirizine. Both of these drugs are antihistamines.

Antihistamines work by blocking a substance called histamine in your body. Histamine is known for causing allergy symptoms. Blocking it helps prevent symptoms of seasonal allergies or hay fever.

Allegra and Zyrtec are available OTC in many forms. The table below details the forms. For specific dosage information on either drug, read the product package carefully or talk to your doctor or pharmacist.

Allegra and Zyrtec may cause mild side effects that tend to go away as your body gets used to the drug. Most of these don’t call for medical attention. But tell your doctor if any side effects are especially bothersome or don’t go away. Call your doctor or seek medical attention if you experience serious side effects.

The tables below list examples of side effects of Allegra and Zyrtec. Both Allegra and Zyrtec can cause similar side effects. The main difference is that Zyrtec is more likely to cause drowsiness than Allegra.

Drug interactions

If you’re taking other drugs, you should talk to your doctor before using Allegra or Zyrtec. Either one can affect the way the other medications work in your body. These interactions can increase or decrease the effect of the other medications, or of Allegra or Zyrtec. Interactions may also increase your risk of side effects from any drug you’re taking.

Zyrtec may interact with drugs such as theophylline.

Allegra may interact with drugs such as:

• ketoconazole
• erythromycin
• rifampin
• antacids

If you’re taking antacids such as Maalox or Mylanta, take Allegra a few hours before or after you take the antacid. These antacids contain aluminum and magnesium, which can prevent your body from absorbing enough Allegra. This can make Allegra less effective. By taking your antacid at a different time from when you take Allegra, you can reduce this interaction.

Conditions of concern

Allegra and Zyrtec may also not be safe for people with certain health issues. For example, you should talk to your doctor about how safe it is to use Allegra or Zyrtec if you have kidney disease.

If you have liver disease, you should also talk to your doctor before using Zyrtec.

Other warnings

Fruit juices such as grapefruit juice, orange juice, and apple juice can decrease the amount of Allegra that your body absorbs. This can make the drug less effective.

To avoid this interaction, wait at least 4 hours after drinking fruit juice before taking Allegra. Or, you can wait 2 hours after taking Allegra to drink fruit juice. Make sure you take Allegra tablets with water, not juice.

You should also avoid taking Zyrtec and Allegra with alcohol. Combining the drugs with alcohol can cause excessive drowsiness.

Allegra and Zyrtec treat the same symptoms and come in similar forms, but these drugs have a few key differences between them:

• You need to pay attention to what you drink with Allegra because fruit juices can affect how well it works.
• Zyrtec is more likely to cause drowsiness than Allegra.
• The effects of Zyrtec may last a few hours longer than the effects of Allegra.

Your doctor or pharmacist can tell you more about Allegra and Zyrtec and which drug may be right for you. They can also give you advice on taking the drugs safely.

Shop for Allegra.

Shop for Zyrtec.

Allegra and Zyrtec are common over-the-counter drugs used to treat allergy symptoms. Both drugs are safe and effective, but studies show Zyrtec’s effects may last longer than Allegra’s. Zyrtec is more likely to cause drowsiness. Drinking fruit juices can make Allegra less effective.

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. The effect of the drug lasts for 24 hours, so it is taken only once a day. ⁵
In addition, with seasonal allergic rhinitis and chronic urticaria, it is reasonable to prescribe Allegra. It is approved for use in children over 12 years of age and, like Zodak®, is taken only once a day. ⁶
As a conclusion – a small reminder.
For allergies:
– Always consult an experienced allergist;
– Do not be lazy to study this issue yourself. This will allow you to ask the right questions at the doctor’s appointment and understand the essence of the treatment prescribed for your child.