Anti Histamine ( anti Allergy) ; Definition, Types, Pharmacokinetic and Side effects



Anti Histamine


Antihistamines are a class of drugs that work by blocking the effects of histamine, a chemical that is released by the body during an allergic reaction. Antihistamines are most commonly used by people who have allergic reactions to pollen and other allergens. They are also used to treat a variety of other conditions such as stomach problems, colds, anxiety and more.


 What are Allergy ?

Allergies are your body’s reaction to a foreign protein. Usually, these proteins (allergens) are harmless. However, if you have an allergy to a particular protein, your body’s defense system (immune system) overreacts to its presence in your body. In the case of an allergy, substances that are usually harmless and don’t bother some people, such as dust or animal dander, do bother you! Your body views these substances as “foreign,” which then triggers an overreaction by your body’s defense system that includes the release of histamine. 

What is Histamine ?

Histamine is an organic compound which is involved in local immune responses and also acts as a neurotransmitter. It is also involved in the inflammatory response and is a mediator of pruritus. Histamine is produced by basophils and is found in tissues that are connected nearby. The permeability of white blood cells is increased by histamine and this allows the pathogens to get engaged with the infected tissues.

Commonest substances causing Allergies ?


  • Food.
  • Dust.
  • Pollen.
  • Pet dander, saliva or urine.
  • Mold.
  • Insect bites and stings.
  • Latex.
  • Certain medication/ Drugs.
Allergic symptoms ;
  • Congestion 
  • coughing.
  • Wheezing, shortness of breath.
  • nausea and vomiting.
  • Itchy skin, hives and other skin rashes.
  • A running or blocked nose, or sneezing.
  • tiredness.
  • Insomnia.
  • Itchy, red, watering eyes.
Classification of Anti Histamine ;

It is divided into 2 major subtypes
  • H-1 receptor antagonists or H-1 blockers
  • H-2 receptor antagonists or H-2 blockers
H1-antihistamines function by binding to the H1 receptor of histamine in mast cells, smooth muscles, endothelial cells in the body and in the brain tuberomammillary nucleus. Antihistamines targeting the H1-receptor of histamine are useful in treating allergic reactions in the nose (itching, runny nose, and sneezing). And it also helps treat insomnia, motion sickness or dizziness caused by complications in the inner ear.
H1- antihistamines has two generations ;

  • First generation Antihistamines;
 First generation Antihistamines began to be approved in the United States in the 1930s and are still prescribed today.
  1. H₁ antagonists, also called H₁ blockers, are a class of medications that block the action of histamine at the H₁ receptor, helping to relieve from allergic reaction.
  2. They work on histamine receptor in the brain and spinal cord along with other types of receptors.
  •  Second generation Antihistamines,
Second-generation antihistamines were approved by the FDA and first came to market in the 1980s. 
  1. Generally do not cause the sedation and drying seen in first-generation antihistamines
  2. Do not cross the blood-brain barrier as readily as First Generation compounds
  3. Lipophobicity
  4. Large molecular size
  5. Electrostatic charge


H2-antihistamines bind to histamines H2 receptors in the upper gastrointestinal tract, mainly in the stomach. Antihistamines targeting the H2-receptor of histamine are helpful in treating gastric acid symptoms (e.g., peptic ulcers and acid reflux).

H3-antihistamine is a classification of medicines used to suppress the activity of histamine in the H3 receptor. H3 receptors are usually present in the brain. 

H4-antihistamines block the activation of the H4 receptors.



Some common antihistamines ;

First-generation antihistamines: diphenhydramine (Benadryl), chlorpheniramine (Chlor-Trimeton), loratadine (Claritin), cetirizine (Zyrtec)

Second-generation antihistamines: fexofenadine (Allegra), loratadine (Claritin), desloratadine (Clarinex), cetirizine (Zyrtec)



What other medical condition Antihistamines treat ?

H-1 antihistamines treat:

  • Allergic rhinitis/hay fever.
  • Allergic conjunctivitis.
  • Hives and other skin rashes.
  • Colds.
  • Food allergies.
  • Hypersensitivity to certain drugs.
  • Insect bites and stings.

First-generation H-1 antihistamines also treat:

  • Insomnia.
  • Motion sickness.
  • Anxiety.

H-2 antihistamines treat:

  • Heartburn.
  • Gastroesophageal reflux disease (GERD).
  • Duodenal and gastric ulcers.
  • Zollinger-Ellison syndrome.

Other conditions antihistamines treat include:

  • Anorexia.
  • Headaches.
  • Anaphylaxis.
  • Vertigo.
  • Parkinson’s disease (to decrease stiffness and tremors).
  • Some types of bone pain.

Your healthcare provider may prescribe antihistamines for even other conditions.

What are the Side Effects ;

First Generation ;

  • Drowsiness.
  • Dry mouth, dry eyes.
  • Blurred or double vision.
  • Dizziness and headache.
  • Low blood pressure.
  • Mucous thickening in the airways.
  • Rapid heart rate.
  • Difficulty urinating and constipation.
Second Generation ;
  • Headache.
  • Cough.
  • Tiredness.
  • Sore throat.
  • Abdominal pain or discomfort
  • Nausea or vomiting.
H2 Antihistamines ;
  • Drowsiness.
  • Joint or muscle pain.
  • Headache.
  • Confusion in the elderly.
  • Dizziness.
  • Breast swelling and tenderness.

Can antihistamine be taken in pregnancy ?

If you are pregnant and need to take an antihistamine, your doctor will likely recommend an older, over-the-counter medication, such as diphenhydramine (Benadryl) or chlorpheniramine (Chlor-Trimeton). These medications have been studied extensively in pregnant women and have been found to be safe and effective. Newer antihistamines, such as loratadine (Claritin) and cetirizine (Zyrtec) may also be safe. 

one of the most common decongestants, pseudoephedrine, has been linked to a small risk of abdominal wall birth defects. Do not use pseudoephedrine during the first 3 months of pregnancy.

It is important to talk to your doctor before taking any medication, especially if you are pregnant or breastfeeding. Your doctor can help you choose the safest and most effective antihistamine for your needs.

Conclusion ;

Antihistamines are a safe and effective way to treat the symptoms of allergies. They are available over-the-counter and by prescription. When choosing an antihistamine, it is important to consider the type of allergy, the severity of the symptoms, and the potential side effects.

Here are some additional tips for taking antihistamines:

  • Start with a low dose and increase it as needed.
  • Take the antihistamine at least 30 minutes before exposure to the allergen.
  • Avoid driving or operating machinery until you know how the antihistamine affects you.
Talk to your doctor if you have any concerns about taking antihistamines.

Frequently Asked Questions – FAQs

Q1

What is the best antihistamine to take?

Antihistamines such as Claritin and Zyrtec are widely used over-the-counter. Doctors consider them to be safe and efficient allergy therapies. Both are antihistamines of the second generation. These antihistamines are less sedating than first-generation antihistamines.

Q2

Are antihistamines anti-inflammatory?

Antihistamines have lately been discovered to have anti-inflammatory effects that go beyond simple histamine receptor inhibition. New research, for example, reveals that these medications decrease the expression of cell adhesion molecules.

Q3

How quickly does antihistamine work?

Antihistamine medications usually start working within 30 minutes of taking them and are most effective within 1-2 hours of taking them. Antihistamines are more effective when taken on a regular basis as a preventative measure, rather than merely when symptoms appear.

Q4

What fruits are high in histamine?

Strawberries, bananas, pineapple, and pears are examples of citrus fruits. Eggplant, avocado, tomatoes, olives, and beans are examples of vegetables. Cheese, yoghurt, and processed cheese are examples of dairy products.

Q5

Does drinking water reduce histamine?

More than 95 percent of excess histamines are removed from the body through the urine, therefore water does help with histamine clearance. Drinking enough water keeps histamine levels safe and healthy, allowing your body to digest them efficiently.

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