Dibenzoxazepinones

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Chapter: Medicinal Chemistry : Tranquillizers

Tranquillizers - Loxapine succinate (Loxapac) - SYNTHESIS AND DRUG PROFILE : Structure, Properties, uses, Synthesis, Assay, Storage, Dosage forms, Dose | Synthesis and Drug Profile


SYNTHESIS AND DRUG PROFILE


Dibenzoxazepinones


a. Loxapine succinate (Loxapac)


Synthesis


Properties and uses: Exist as white to off-white crystalline powder, slightly soluble in water or alcohol. It may give rise to possible anticholinergic and antiadrenergic activity. It must be employed with great caution in such patients who have either a history of glaucoma or urinary retention problems. It has resulted from the expansion of the six-member central ring of phenothiazine followed by isosteric replacement of one or more atoms with oxygen. Because of its seven-member central ring, the conformation of loxapine is more twisted than that of the phenothiazine rings. It is used for symptomatic control of schizophrenia.

Dose: The usual dose is 20–250 mg/day.


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