Dibenzodiazepines

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Chapter: Medicinal Chemistry : Tranquillizers

Dibenzodiazepines - Clozapine (Lozapin, Sizopin, Clopaz) - SYNTHESIS AND DRUG PROFILE : Structure, Properties, uses, Synthesis, Assay, Storage, Dosage forms, Dose


SYNTHESIS AND DRUG PROFILE


Dibenzodiazepines


a. Clozapine (Lozapin, Sizopin, Clopaz)


Synthesis


Properties and uses: It is a yellow crystalline powder, dissolves in dilute acetic acid, insoluble in water, freely soluble in methylene chloride, and soluble in alcohol. It has more affinity for D1 and less for D2 dopamine receptors. It may have its unique profile due to the blockade of D1 receptors and M1 muscarinic activity. It has high potentially fatal agranulocytosis. Other adverse side effects include drowsiness, dizziness, and doserelated seizures. It is effective in individuals suffering from disorganization. For example, loose associations, inappropriate affect, incoherence, and reduction in rational thought processes.

Assay: Dissolve the sample in anhydrous acetic acid and titrate with 0.1 M perchloric acid. Determine the end point potentiometrically.

Dose: For Schizophrenia: Adult: 12.5 mg 1–2 times on day 1 followed by 25 mg 1–2 times on day 2 increased gradually in increments of 25–50 mg up to a daily dose of 300 mg with 14–21 days. Subsequent increments of 50–100 mg may be made 1–2 times weekly. Usual dose is 200–450 mg/day. Maximum: 900 mg/day. Elderly: Initially, 12.5 mg on day 1 increased subsequently by increments of 25 mg. For psychosis in parkinsonism: Adult: Initially, 12.5 mg once daily at night, increased in steps of 12.5 mg up to two times each week, not >50 mg/day at the end of the second week. Usual dose: 25–37.5 mg daily. Maximum of 100 mg daily.


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