Ahmedabad
(Head Office)Address : 506, 3rd EYE THREE (III), Opp. Induben Khakhrawala, Girish Cold Drink Cross Road, CG Road, Navrangpura, Ahmedabad, 380009.
Mobile : 8469231587 / 9586028957
Telephone : 079-40098991
E-mail: dics.upsc@gmail.com
Antihistamines
Context: Currently, there is extensive research underway on H3 and H4 receptors, specifically to mitigate the effects of neurological and immunological disorders, respectively, using specialized drugs.
About:
• Antihistamines are medications used to treat allergi creactions and related symptoms.
• They work by blocking the action of histamine, a chemical released by the immune system during allergic responses.
• Histamine binds to specific receptors in the body, particularly H1 receptors.
• Binding of histamine to these receptors leads to symptoms such as sneezing, itching, runny nose, and watery eyes.
• By blocking histamine receptors, antihistamines help alleviate these allergic symptoms.
• Antihistamines are commonly used to manage allergies, hay fever (allergic rhinitis), hives (urticaria), and allergic conditions
Receptors:
• Histamine Receptors: Histamine mediates its effects through different types of receptors known as H1, H2,H3, and H4 receptors.
• H1 Receptors:
o Found in the inner surface of blood and lymphatic vessels, neurons, and smooth muscle cells.
o Blocking H1 receptors with antihistamines alleviates symptoms of minor allergies such as sneezing,itching, and hives.
• H2 Receptors:
o Located in certain cells of the gastric glands.
o Stimulate the release of gastric acid for digestion.
o H2 antihistamines reduce gastric acid secretion and treat conditions like peptic ulcers and gastroesophageal reflux disease (GERD).
• H3 Receptors:
o Found in cells in the central nervous system.
o Regulate the release of neurotransmitters such as dopamine and serotonin.
o Ongoing research aims to develop drugs that modulate neurotransmitter release via H3 receptors,potentially treating neurological disorders like Alzheimer\'s disease and attention deficit hyperactivity disorder (ADHD).
• H4 Receptors:
o Located on cells involved in the body\'s inflammatory response, including immune cells.
o Regulate inflammation, including allergic reactions.
o Ongoing research seeks to develop drugs targeting H4 receptors to alleviate symptoms of various immunological disorders.
Mechanism of Action | Classification |
---|---|
Histamine Receptors: | |
Histamine acts on specific receptors, mainly H1 (involved in allergic reactions) and H2 (involved in gastric acid secretion) | |
Antagonistic Action: | |
Antihistamines block H1 receptors to prevent allergic responses | |
Classification | |
First-Generation Antihistamines | Second-Generation Antihistamines |
Older antihistamines that readily cross the blood-brain barrier, causing sedation. | Newer antihistamines designed to have reduced sedative effects due to limited penetration of the blood-brain barrier. |
Common First-Generation Antihistamines: | Common Second-Generation Antihistamines: |
Diphenhydramine (Benadryl): Used for allergies, itching, and insomnia. | Cetirizine (Zyrtec): Used for allergies, hay fever, and hives |
Chlorpheniramine (Chlor-Trimeton): Used for allergies, hay fever, and the common cold. | Loratadine (Claritin): Used for allergies and allergic rhinitis. |
Hydroxyzine (Atarax, Vistaril): Used for itching, anxiety, and nausea. | Fexofenadine (Allegra): Used for allergies and chronic idiopathic urticaria. |
Indications | Side Effects | Dosage Forms |
---|---|---|
Allergic Rhinitis: | First-Generation: Sedation, drowsiness, dry mouth, blurred vision, constipation, urinary retention, confusion. | Oral Tablets/Capsules: Most antihistamines are available in oral forms. |
Relief of sneezing, itching, rhinorrhea, and nasal congestion. | Second-Generation: Less sedation compared to first-generation; may cause drowsiness in some individuals, headache, and dry mouth. | Liquid Formulations: Available for pediatric patients or those who have difficulty swallowing pills |
Topical Preparations: Some antihistamines are available in creams or ointments for skin conditions like itching and urticaria. | ||
Allergic Conjunctivitis: | Nasal Sprays: Certain antihistamines are formulated as nasal sprays for allergic rhinitis | |
Alleviation of itching and redness of the eyes. | ||
Urticaria (Hives): | ||
Treatment of itching and rash associated with hives. | ||
Anaphylaxis | ||
Adjunctive therapy in severe allergic reactions. | ||
Motion Sickness: | ||
Some antihistamines have antiemetic effects and can be used to prevent motion sickness. |
Address : 506, 3rd EYE THREE (III), Opp. Induben Khakhrawala, Girish Cold Drink Cross Road, CG Road, Navrangpura, Ahmedabad, 380009.
Mobile : 8469231587 / 9586028957
Telephone : 079-40098991
E-mail: dics.upsc@gmail.com
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