Classification of Antihistamines

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Chapter: Medicinal Chemistry : Antihistamines

1. H1-Antagonists with classical structures II. H1-Antagonists with nonclassical structures III. Nonsedative H1-antihistamines IV. Inhibition of histamine release (mast cells stabilizers)


CLASSIFICATION

 

1. H1-Antagonists with classical structures

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

a.            Ethylene diamine derivatives

b.           Amino alkyl ether analogues

c.            Cyclic basic chain analogues

d.           Mono amino propyl analogues

e.            Tricyclic ring system or Phenothiazine derivaties

f.Dibenzocyclo heptenes

g.           Miscellaneous agents

h.           Newer agents

 

a. Ethylene diamine derivatives


 

b. Amino alkyl ethers


 

c. Cyclic basic chain analogues or piperazine derivatives


 

d. Mono amino propyl analogues

 

d. i. Saturated analogues


 

d. ii. Unsaturated analogues


 

e. Tricyclic ring systems or phenothiazine derivatives


 

f. Dibenzocyclo heptenes


 

g. Miscellaneous


 

h. Newer agents


 

II. H1-Antagonists with nonclassical structures

 

i. Azelastine


ii. Tazifylline


iii. Astemizole


 

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


ii. Epinastine


iii. Rocastine


iv. Cetirizine


v. Fexofenadine


vi. Acrivastine


 

IV. Inhibition of histamine release (mast cells stabilizers)

 

i. Cromolyn sodium


ii. Nedocromil sodium



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