Antihistamines are a class of drugs designed to counteract the effects of histamine, a natural compound released by the body in response to allergens. Histamine plays a central role in allergic reactions and is responsible for various symptoms such as itching, sneezing, runny nose, and watery eyes. Antihistamines block histamine receptors, thereby preventing or alleviating these allergy symptoms. They are classified into two main generations:
1. First Generation Antihistamines
– Examples: Diphenhydramine, Chlorpheniramine, and Promethazine.
– Characteristics: These drugs often cause sedation and drowsiness because they can cross the blood-brain barrier, leading to central nervous system effects.
– Clinical Uses: Commonly used for allergy symptoms, motion sickness, insomnia, and as sedatives.
– Adverse Effects: Drowsiness, dry mouth, blurred vision, constipation, and urinary retention.
2. Second Generation Antihistamines
– Examples: Loratadine, Cetirizine, Fexofenadine, and Desloratadine.
– Characteristics: These drugs are less likely to cause sedation because they have limited penetration into the central nervous system.
  – Clinical Uses:They primarily use them for allergy symptoms and prefer them for long-term management due to their lower sedative effects.
– Adverse Effects: Generally well-tolerated, with minimal sedation; some reports of headache and gastrointestinal symptoms.
Clinical Uses of Antihistamines
1. Allergic Rhinitis and Conjunctivitis:
– Antihistamines are commonly used to relieve symptoms such as sneezing, itching, and a runny nose associated with allergies.
2. Urticaria (Hives) and Angioedema:
– Antihistamines can help alleviate the itching and swelling associated with hives and angioedema.
3. Motion Sickness:
– Some first-generation antihistamines have antiemetic effects and are used to prevent motion sickness.
4. Insomnia:
– Due to their sedative effects, first-generation antihistamines are sometimes used to treat insomnia.
5. Allergic Reactions:
– Antihistamines can be part of the treatment for severe allergic reactions (anaphylaxis), although they are not the primary intervention.
Adverse Effects of Antihistamines
1. Sedation:
– First-generation antihistamines can cause drowsiness and impair cognitive function.
2. Anticholinergic Effects:
– Dry mouth, blurred vision, constipation, and urinary retention can occur, especially with first-generation antihistamines.
3. Cardiac Effects:
– Some antihistamines may prolong the QT interval and should be used cautiously in patients with pre-existing heart conditions.
4. Interaction with Other Medications:
– Antihistamines may interact with other medications, leading to additive sedative effects or interactions with drugs metabolized by the same enzymes.
5. Potential for Overuse:
– Chronic use of some antihistamines, particularly those with sedative effects, can lead to tolerance and dependence.
Antihistamines are crucial in managing allergic conditions and related symptoms. The choice between first and second-generation antihistamines depends on the desired effects and the balance between efficacy and side effects. Careful consideration of individual patient characteristics and potential drug interactions is essential in prescribing antihistamines.
