[3] Zotepine's primary use is as a treatment for schizophrenia[4] although clinical trials have been conducted (with positive results) into its efficacy as an antimanic agent in patients with acute bipolar mania.

[8] The antipsychotic effect of zotepine is thought to be mediated through antagonist activity at dopamine and serotonin receptors.

[10] In addition, its active metabolite, norzotepine, serves as a potent norepinephrine reuptake inhibitor.

Cyclization of this compound in the presence of polyphosphoric acid forms the dibenzothiepin ring system of the drug.

The enol ether, zotepine, is produced when this is treated with the chloroethyl amine and potassium carbonate in methyl isobutyl ketone as solvent.