Benzisoxazoles

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Chapter: Medicinal Chemistry : Tranquillizers

Benzisoxazoles - Risperidone (Respidon, Sizodon, Rispid) - SYNTHESIS AND DRUG PROFILE : Structure, Properties, uses, Synthesis, Assay, Storage, Dosage forms, Dose


SYNTHESIS AND DRUG PROFILE


Benzisoxazoles


a. Risperidone (Respidon, Sizodon, Rispid)


Synthesis


Properties and uses: It is a white or almost white powder, dissolves in dilute acid solutions, insoluble in water, freely soluble in methylene chloride, sparingly soluble in ethanol. It is a typical antipsychotic and neuroleptic. Its adverse effects include nasal congestion, orthostastic hypotension, insomnia, and possible EPS. Causes more EPS than other atypical agents. May cause weight gain and an increased tendency for glucose intolerance. Risperidone has structural features of hybrid molecules between butyrophenone and trazodone. It is a typical antipsychotic, effective against the negative symptoms of schizophrenia.

Assay: Dissolve the sample in 70 ml of a mixture of 1 volume of anhydrous acetic acid and 7 volumes of methyl ethyl ketone and titrate with 0.1 M perchloric acid. Determine the end point potentiometrically.

Storage: It should be stored in well-closed airtight containers and protected from light.

Dose: For Schizophrena: Adult: Initially, 2 mg daily, may increase to 4 mg daily on the second day, adjusted further in increments or decrements of 1–2 mg daily at weekly intervals. Doses may be given in 1–2 divided doses. Maintenance: 4–6 mg daily. Maximum: 16 mg/day. For elderly: Initially, 0.5 mg two times a day gradually increased in increments of 0.5 mg twice a day. Maintenance: 1–2 mg twice a day.



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