H1-antagonists with classical structure -> Newer agents -> Ketotifen Fumarate (Zaditen)
Ketotifen Fumarate (Zaditen)
Synthesis
Properties and uses: Ketotifen fumarate is a white to brownish-yellow
crystalline powder, sparingly soluble in water, slightly soluble in methanol
and in acetonitrile. The recommended dose of ketotifen solution is one drop
instilled into each affected eye every 8–12 hr. Most frequently used for
conjuctival infection, and rhinitis. Ketotifen solution should be used with
caution during pregnancy or during nursing. This is an analogue of the
tricyclic H1-receptor antagonist and serotonin receptor antagonist.
It has only minor anticholinergic and antiserotonergic activity. It has been
used in the prophylactic treatment of asthma.
Assay: Dissolve the sample in a mixture of anhydrous acetic acid and
acetic anhydride and titrate against 0.1 M perchloric acid. Determine the end point
potentiometrically.
Dose: Usually, the dose is 1 mg orally two times a day.
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