Unsaturated analogues

Triprolidine (Actidil)

Introduction

Triprolidine is a widely utilized antihistamine known for its effectiveness in alleviating symptoms associated with allergic reactions. Functioning as an H1 receptor antagonist. Primarily used in treating allergic rhinitis, hay fever, and cold symptoms, triprolidine is commonly administered orally in tablet or syrup form.

Structure

Synthesis

Mechanism of action

Triprolidine is an H1 receptor antagonist, meaning it blocks the effects of histamine at H1 receptors.
By inhibiting histamine action, it helps alleviate symptoms related to allergic reactions.

Properties and uses: 

Triprolidine hydrochloride is a white crystalline powder, practically insoluble in ether and soluble in water and ethanol. The activity is mainly connected to the geometric isomer in which the pyrrolidino-methyl group is trans to the 2-pyridyl group. Pharmacological studies confirm the high activity of triprolidine and the superiority of (E) over corresponding (Z) isomers as H1-antagonists.

Assay: 

Dissolve the sample in a mixture of anhydrous acetic acid and acetic anhydride and titrate against 0.1 M perchloric acid using crystal violet solution as an indicator.

Dose: 

The usual dose is 5–7.5 mg per day.

Dosage forms: 

Triprolidine HCl tablets I.P., Triprolidine tablets B.P.

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