CLASSIFICATION OF ANTIHISTAMINES DRUGS - Pharmacareerinsider
April 17, 2025
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CLASSIFICATION OF ANTIHISTAMINES DRUGS

Table of Contents

1. H1-Antagonists with classical structures

According to the chemical features, they are further classified as follows:

a. Ethylene diamine derivatives

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b. Amino alkyl ether analogues

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c. Cyclic basic chain analogues

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d. Mono amino propyl analogues

d. i. Saturated analogues

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d. ii. Unsaturated analogues

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e. Tricyclic ring system or Phenothiazine derivatives

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f. Dibenzocyclo heptane’s

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g. Miscellaneous agents

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h. Newer agents

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II. H1-Antagonists with nonclassical structures

i. Azelastine

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ii. Tazifylline

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iii. Astemizole

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III. Nonsedative H1-antihistamines

Nonsedative antihistamines bind only to peripheral H1-receptors and produce with little or no sedation because of poor CNS penetration and lower affinity for central histaminic activity.

These are divided into two main classes:

1. Piperazine derivatives—Cetirizine

2. Pyridine and piperidine derivatives—Loratadine, Fexofenadine, Terfenadine, Astemizole, Acrivastine

i. Loratadine

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ii. Epinastine

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iii. Rocastine

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iv. Cetirizine

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v. Fexofenadine

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vi. Acrivastine

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IV. Inhibition of histamine release (mast cells stabilizers)

i. Cromolyn sodium

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ii. Nedocromil sodium

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