
Precautions
Zyrtec is considered a second-generation antihistamine, and Xyzal is a third-generation antihistamine. These medications are classified by how likely they are to reach the brain and cause drowsiness. First-generation antihistamines, such as Benadryl (diphenhydramine), are the most likely to reach the brain and affect the nervous system.
Is there 3ed Gen antihistamine?
Second- and third-generation antihistamine brands
- Zyrtec. Cetirizine is the main active ingredient in Zyrtec. It helps relieve runny nose, sneezing, itchy and watery eyes, and nose or throat itching from hay fever and other upper ...
- Claritin. Loratadine is the main active ingredient in Claritin. ...
- Allegra. Fexofenadine is the main active ingredient in Allegra. ...
What antihistamine is best?
Zyrtec is generally a stronger antihistamine, but it is slightly more likely to make you drowsy than Claritin. Not everyone gets drowsy on it, though. It also works faster than Claritin, in about an hour. Claritin is somewhat weaker and takes longer to kick in (~3 hours), but rarely causes drowsiness and lasts longer.
Is Zyrtec better than Claritin?
Zyrtec contains the both the left- and the right hand turning molecule of cetirizine. It is predominantly the right hand turning enantiomer that is causing the drowsiness, as you call it. And the reason is, is that this molecule breaks through the blood-brain barrier. Thus it gets in the cerebrospinal fluid, giving the sedative effects.
Does Zyrtec Make you Sleepy?

Are there third generation antihistamines?
Second- and third-generation antihistamines Allegra (fexofenadine) is currently the only third-generation antihistamine available without a prescription. Some of the newer antihistamines come in combination with pseudoephedrine, found in Sudafed. Some examples include: Allegra-D, Claritin-D, and Zyrtec-D.
What are 2nd and 3rd generation antihistamines?
While many of the antihistamines still commonly used to treat urticaria are first generation H1 antagonists (e.g., diphenhydramine, hydroxyzine), the more recently developed second-generation agents (e.g., loratadine, cetirizine) and their metabolites—the third-generation antihistamines (e.g., fexofenadine, ...
Which generation antihistamine is best?
The main difference between first-generation and second-generation antihistamines is that the latter do not cause sleepiness and are considered safer because they interact better with other medications.
What are the 3 antihistamines?
OTC antihistamines include: Brompheniramine (Dimetane) Cetirizine (Zyrtec) Chlorpheniramine (Chlor-Trimeton)
What are the top five antihistamines?
Antihistamines, a popular class of allergy medicines, can cause drowsiness....What are the best allergy medicines to take?Benadryl (diphenhydramine)Claritin (loratadine)Allegra (fexofenadine)Zyrtec (cetirizine)Xyzal (levocetirizine)
What is the newest antihistamine?
Xyzal is one of the newer, third-generation antihistamines used to treat allergies. It is available OTC and by prescription. Xyzal is taken by mouth once a day or as needed for allergies. Xyzal is very similar to other non-drowsy allergy medications, such as Zyrtec, Claritin, Allegra, and Clarinex.
What drugs should not be taken with antihistamines?
Avoid taking MAO inhibitors (isocarboxazid, linezolid, metaxalone, methylene blue, moclobemide, phenelzine, procarbazine, rasagiline, safinamide, selegiline, tranylcypromine) during treatment with this medication. Most MAO inhibitors should also not be taken for two weeks before treatment with this medication.
Which is the safest antihistamine?
Loratadine, cetrizine, and fexofenadine all have excellent safety records. Their cardiovascular safety has been demonstrated in drug-interaction studies, elevated-dose studies, and clinical trials. These three antihistamines have also been shown safe in special populations, including pediatric and elderly patients.
What are the side effects of long term use of antihistamines?
These common side effects include sedation, impaired motor function, dizziness, dry mouth and throat, blurred vision, urinary retention and constipation. Antihistamines can worsen urinary retention and narrow angle glaucoma. The antihistamines rarely cause liver injury.
What do antihistamines do to the brain?
First-generation antihistamines like Benadryl not only block the effect of histamine, but as anticholinergics, they also block the effect of acetylcholine, a chemical in your brain that helps send messages between cells. Blocking acetylcholine can cause temporary drowsiness, confusion, and memory loss.
Can you use two types of antihistamine?
Do not take 2 antihistamines together unless recommended by your doctor.
Which antihistamine is best for skin itching?
A nonprescription oral antihistamine, such as loratadine (Alavert, Claritin, others), cetirizine (Zyrtec Allergy, others) or diphenhydramine (Benadryl Allergy, others), may help relieve itching. Consider whether you might prefer a type that doesn't cause drowsiness.
What is 2nd generation antihistamine?
Second-generation antihistamines are a type of antihistamines that are used for treating allergies and itching. They work by binding to the histamine receptors in the brain and spinal cord and blocking the release of histamine.
What is the difference between 1st generation and 2nd generation antihistamines?
First-generation antihistamines block both histaminic and muscarinic receptors as well as passing the blood-brain barrier. Second-generation antihistamines mainly block histaminic receptors but do not or only minimally cross the blood-brain barrier.
What are the two types of antihistamines?
They're usually divided into 2 main groups: antihistamines that make you feel sleepy – such as chlorphenamine (Piriton), cinnarizine, diphenhydramine, hydroxyzine and promethazine. non-drowsy antihistamines that are less likely to make you feel sleepy – such as acrivastine, cetirizine, fexofenadine and loratadine.
What is the difference between H1 and H2 antihistamines?
H1 receptor antagonists are typically utilized to suppress the body's histamine-mediated effects in anaphylactoid or anaphylactic reactions. H2 antagonists are competitive antagonists at the parietal cell H2 receptor and are typically used to suppress gastric acid secretion.
What Are Antihistamines Used for?
Antihistamines are very good at relieving symptoms of an allergic reaction, such as: 1. edema (swelling) 2. inflammation (redness) 3. itch 4. rash...
What Are The Differences Between Antihistamines?
Antihistamines can be classified into two main categories: 1. first-generation antihistamines 2. second-generation antihistamines.First-generation...
What Are The Side Effects of Antihistamines?
Side effects of first-generation antihistamines may include: 1. abdominal pain 2. blurred or double vision 3. constipation 4. dry eyes 5. a dry mou...
Which antihistamines cross the blood-brain barrier?
First-generation oral antihistamines, including diphenhydramine (Benadryl) and chlorpheniramine (Chlor-Trimeton), easily cross the blood-brain barrier and affect H1 receptors in the central nervous system (CNS). H1receptors in the CNS help regulate the body’s sleep-wake cycle.
What is the purpose of antihistamines?
Antihistamines refer to a type of medication that treats allergy symptoms, motion sickness, and some cold and flu symptoms. Antihistamines block H1 histamine receptors.
What are the symptoms of an allergic reaction?
When a person has an allergic reaction, they may experience symptoms such as nasal congestion, sneezing, and itchy skin. Antihistamines can help ease these symptoms.
What are the substances that trigger allergic reactions?
Allergens are substances that trigger allergic reactions, and they include anything from pet dander and pollen to specific proteins found in foods. When an allergen enters a person’s body or touches their skin, cells in the immune system release histamines, which bind to specific receptors located on cells found throughout the body.
How old do you have to be to take antihistamines?
These antihistamines are safe for adults and children over 12 years old to use.
Do antihistamines have sedative properties?
Second- and third-generation antihistamines do not have sedative properties. According to an article in the journal National Institute of Diabetes and Digestive and Kidney Diseases, second- and third-generation antihistamines are less likely. Trusted Source.
Can you take antihistamines for rhinitis?
A person may take antihistamines to treat allergic rhinitis. A person experiences an allergic reaction when they come into contact with a harmless substance that their body interprets as an invading pathogen. Allergens are substances that trigger allergic reactions, and they include anything from pet dander and pollen to specific proteins found in ...
What are the reactions of first generation antihistamines?
colds. flu. food allergies. hay fever. hives ( urticaria) hypersensitivity reactions to drugs. insect bites. stings. First generation antihistamines (see explanation below) also act in the brain and spinal cord, and on other receptors.
What are the two main categories of antihistamines?
Antihistamines can be classified into two main categories: second-generation antihistamines. First-generation antihistamines were developed more than seventy years ago and are still in widespread use today. They act on histamine receptors in the brain and spinal cord and in the rest of the body (called the periphery).
What are antihistamines used for?
Antihistamines are very good at relieving symptoms of an allergic reaction, such as:
What receptors do antihistamines work on?
They act on histamine receptors in the brain and spinal cord and in the rest of the body (called the periphery). They also act on muscarinic, alpha-adrenergic, and serotonin receptors. This means that first-generation antihistamines are more likely to cause side effects such as sedation, dry mouth, dizziness, low blood pressure, ...
What is the purpose of antihistamines?
Antihistamines are a class of agents that block histamine release from histamine-1 receptors and are mostly used to treat allergies or cold and flu symptoms , although some first-generation antihistamines may also be used for other conditions.
Where are histamine receptors located?
Histamine-1 receptors are located in the airways, blood vessels and gastrointestinal tract (stomach and esophagus). Stimulation of these receptors can lead to conditions such as a skin rash or inflammation, a narrowing of the airways (bronchoconstriction), hay fever, or motion sickness. Histamine-1 receptors are also found in ...
Do second generation antihistamines cause drowsiness?
Most second-generation antihistamines do not cause drowsiness, although some (such as cetirizine and fexofenadine), may be more likely to do so at higher dosages.
What is the name of the first generation of antihistamines?
Phenothiazines are first-generation antihistamines that include only one active substance: promethazine. Under the trade name of Fenergal or Frinova, these antihistamines are often used, thanks to the induction of dryness of the mucous membranes, for the treatment of nasal congestion both in children and adults.
What are the effects of antihistamines?
That is, they are capable of crossing the blood-brain barrier and causing adverse effects such as sleep, sedation, drowsiness, increased appetite, dry mouth, constipation, urine retention, blurred vision and, although this may have therapeutic effects, dry mucous membranes. (can relieve nasal congestion) and inhibition of vomiting and dizziness.
What is histamine in the body?
But what exactly is histamine? Histamine is a molecule that, in addition to acting as a neurotransmitter (modulates the activity of the nervous system by influencing neuronal synapses), functions as a hormone. And it is in this role as a hormone that, when histamine is released into the bloodstream by immune cells, it moves to the place where the foreign substance is present and initiates the inflammatory response.
What is the best antihistamine for sleep?
Ethanolamines are first generation antihistamines that stand out for being one of those that produce the most drowsiness. It is an organic chemical compound that is both a primary amine and a primary alcohol. The most famous commercial brands that use these active ingredients are Biodramina, Benadryl, Soñodor, Cinfamar, Dormidina and Tavegil. As we can see, they use what is a side effect (sleep) as the basis of their administration.
How does the body fight allergies?
Our body believes that it is fighting a danger and tries to eliminate that allergen from the body, which it achieves by stimulating the synthesis of histamine, the chemical substance that, as we see, is behind the typical symptoms of allergies.
What is an allergy?
An allergy is an excessive hypersensitivity reaction of our body to exposure to a substance called an allergen. , which does not have to be harmful and does not arouse reactions in non-allergic people. But the immune system of someone with allergies considers that particle as dangerous and, therefore, acts to eliminate it.
How many people are allergic to something?
And, in fact, it is estimated that, in less than a decade, 1 in 2 people in the world will be allergic to something.
Why are there 2nd and 3rd generation antihistamines?
The newer second-generation and third-generation OTC oral antihistamines were developed to target their action on more specific receptors. This helps decrease side effects, including drowsiness. Also, these drugs work longer in your body so you need fewer doses.
Which OTC antihistamines are the oldest?
First-generation OTC oral antihistamines, including diphenhydramine and chlorpheniramine, are the oldest group. They are sedating, which means they’re likely to make you drowsy after you use them. They also don’t last as long in your system, so they require more frequent dosing than the newer generations.
What is the best medicine for a runny nose?
Benadryl. The first-generation antihistamine diphenhydramine is the main active ingredient in Benadryl. Benadryl helps relieve runny nose, sneezing, itchy or watery eyes, and nose or throat itching. These symptoms may be due to hay fever, other upper respiratory allergies, or the common cold.
What is the main ingredient in chlor trimeton?
Chlorpheniramine is the main active ingredient in Chlor-Trimeton. It helps relieve runny nose, sneezing, itchy or watery eyes, and nose and throat itching from hay fever. It also helps relieve other respiratory allergies.
What are the side effects of antihistamines?
Some of the more common side effects of first-generation antihistamines can include: drowsiness. dry mouth, nose, and throat. headache. Some side effects that are not as common include: dizziness. nausea.
What is the substance that causes allergies?
When you have an allergic reaction, your body releases a substance called histamine. Histamine causes allergy symptoms when it binds to receptors on certain cells in your body. Antihistamines work by decreasing the effects of histamine at certain cell receptors.
Can Claritin cause allergic reactions?
Serious side effects of Claritin can include allergic reactions. Symptoms can include:
Why does it matter if an antihistamine is first or second generation?
That matters because there is a fundamental difference in side effects between the generations. First-gen antihistamines are well-known for producing drowsiness. Newer generations have solved this problem while still retaining their effectiveness. So higher marks for next-gen antihistamines.
What is the purpose of antihistamines?
Antihistamines are chemical compounds that provide relief from allergy, cold and flu symptoms.
Why do antihistamines make you drowsy?
In a nutshell, drowsiness occurs when the antihistamines cross the blood-brain barrier ( 17) which regulates the movement of microscopic compounds and cells between blood vessels and the brain.
Why do people take antihistamines?
The primary reason people use antihistamines is to help them deal with their allergy symptoms. And they (the antihistamines) do a generally outstanding job of it. Whether you have a runny nose, watery eyes, sneezing, or nasal swelling, antihistamines can and do help. Antihistamines can help you get to sleep.
How long does it take for antihistamines to work?
A: In most cases, oral antihistamines take about 30 minutes to produce noticeable relief. But it depends, in part, on your metabolism as well. A person with a faster metabolism might start seeing relief in 15 or 20 minutes. Antihistamine nasal sprays tend to get to work faster.
What is zyrtec used for?
Zyrtec is an all-purpose second-generation antihistamine that tackles cold and flu symptoms as well as it handles your allergy symptoms. It can also address hives and a multitude of upper respiratory allergies.
What is the best sleep gel for allergies?
Unisom SleepGels use the first-generation antihistamine diphenhydramine to alleviate your allergy symptoms. At the same time, they help you get the sleep you need. Just take one SleepGel right before bed.
Which generation of antihistamines are the least likely to make you feel tired?
Second generation are less likely to reach the brain or be sedating, and third-generation antihistamines are the least likely. However, they all still have the potential to make you feel tired.
Which antihistamines are most likely to cause drowsiness?
These medications are classified by how likely they are to reach the brain and cause drowsiness. First-generation antihistamines, such as Benadryl (diphenhydramine), are the most likely to reach the brain and affect the nervous system. They’re also more likely to result in drowsiness and sedation.
What is the difference between Xyzal and Zyrtec?
The difference between Xyzal and Zyrtec. Xyzal ( levocetirizine) and Zyrtec ( cetirizine) are both antihistamines. Xyzal is produced by Sanofi, and Zyrtec is produced by a division of Johnson & Johnson. They’re both marketed as providing relief from the symptoms of allergies.
How do antihistamines stop allergies?
Antihistamines stop these allergy symptoms by reducing or blocking the action of histamines.
Does Sanofi sell Xyzal?
Sanofi promotes Xyzal as a mirror image of Zyrtec, without the part of the drug that causes drowsiness. Both are available over-the-counter (OTC) without prescriptions.
Is Xyzal the same as Zyrtec?
Both Xyzal and Zyrtec are effective over-the-counter allergy relief drugs with a very similar chemical makeup. Both are likely to make you less drowsy than alternatives such as Benadryl. Ask your doctor for a recommendation about which one might best address your allergy symptoms.
History and effects of antihistamines
Antihistamines are used to treat diseases and conditions accompanied by the release of histamine, in particular, allergic pathologies. Today, two generations of antihistamines are widely used; they have significant differences in both pharmacological properties and indications.
First-Generation Antihistamines
First-generation H1- antagonists (tab.I) are often referred to sedatives. They have been widely used in clinical practice for decades: the first available drugs of this group were developed in the 40s of the 20th century.
Second-Generation Antihistamines
The drugs of this class (tab.I), unlike their predecessors, selectively act on H1-receptors and therefore practically do not have sedative and atropine-like effects. However, some drugs in this group are cardiotoxic.
