Zotepine
Zotepine is an atypical antipsychotic drug indicated for acute and chronic schizophrenia. It has been used in Germany since 1990 and Japan since 1982.
Zotepine is not approved for use in the United States, United Kingdom, Australia, Canada or New Zealand.Medical uses
Zotepine's primary use is as a treatment for schizophrenia although clinical trials have been conducted into its efficacy as an antimanic agent in patients with acute bipolar mania. In a 2013 study in a comparison of 15 antipsychotic drugs in effectivity in treating schizophrenic symptoms, zotepine demonstrated medium-strong effectivity. Less effective than clozapine, slightly less effective than olanzapine and risperidone, approximately as effective as paliperidone, and slightly more effective than haloperidol, quetiapine, and aripiprazole.Side effects
; Common
;Unknown frequency
;Rare
Pharmacodynamics
The antipsychotic effect of zotepine is thought to be mediated through antagonist activity at dopamine and serotonin receptors. Zotepine has a high affinity for the D1 and D2 receptors. It also affects the 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors. In addition, its active metabolite, norzotepine, serves as a potent norepinephrine reuptake inhibitor.
| Macromolecule | Ki |
| SERT | 151 |
| NET | 530 |
| DAT | 3621 |
| 5-HT1A | 470.5 |
| 5-HT1B | 59.5 |
| 5-HT1D | 119 |
| 5-HT1E | 700 |
| 5-HT2A | 2.7 |
| 5-HT2C | 2.6 |
| 5-HT3 | 472 |
| 5-HT5A | 29 |
| 5-HT6 | 6 |
| 5-HT7 | 12 |
| α1A | 7 |
| α1B | 5 |
| α2A | 180 |
| α2B | 5.35 |
| α2C | 106 |
| M1 | 18 |
| M2 | 140 |
| M3 | 73 |
| M4 | 77 |
| M5 | 260 |
| D1 | 71 |
| D2 | 25 |
| D2S | 5.4 |
| D2L | 11 |
| D3 | 6.4 |
| D4 | 18 |
| D5 | 248 |
| H1 | 3.21 |
| H2 | 500 |
| H4 | 1977 |
Names
Brand names include Losizopilon, Lodopin, Setous, Zoleptil ; where † indicates a formulation that has been discontinued.
