Zotepine (brand names: Losizopilon (JP), Lodopin (ID, JP), Setous (JP), Zoleptil (CZ, PT, TR, UK†); where † indicates a formulation that has been discontinued) is an atypical antipsychotic drug indicated for acute and chronic schizophrenia. It has been used in Germany since 1990 (although it has been discontinued in Germany) and Japan since 1982.
Zotepine is not approved for use in the United States, United Kingdom, Australia, Canada or New Zealand.
- Description 1
- Taxonomy 2
- Distribution 3
- References 4
- External links 5
Medical UsesZotepine's primary use is as a treatment for schizophrenia although clinical trials have been conducted (with positive results) into its efficacy as an antimanic agent in patients with acute bipolar mania.
- Orthostatic hypotension
- Weight gain (produces a similar degree of weight gain to that seen with clozapine and olanzapine treatment)
Somnolence (2nd highest effect size for causing sedation out of fifteen antipsychotics compared in a recent meta-analysis)
- Extrapyramidal side effects [EPSE] (2nd largest odds ratio for causing EPSE out of fifteen antipsychotics compared in a recent meta-analysis, second only to haloperidol)
- Xerostomia (dry mouth)
- Blurred vision
- Hypersalivation (drooling)
- Sexual dysfunction
- Influenza-like symptoms
- Flushing dry skin
- Unknown Frequency
- Angle-closure glaucoma
- Abdominal enlargement
- Deep vein thrombosis
- Paralytic ileus
- Tardive dyskinesia
- Neuroleptic malignant syndrome
- Laryngeal edema
- Urinary retention
- Seizure (dose-dependent risk)
- Metabolic syndrome
- Diabetes mellitus type II
- Increased liver enzymes
PharmacologyThe 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 (Receptor or transporter protein)||Ki [nM]|
The most common dosage used is 150 mg daily. It is suggested that zotepine therapy starts at 75 mg to 150 mg divided into three daily doses. Some people may need to have their dosage increased to 300 mg.
- , abstract (in French and English)
- http://www.nyrdtc.nhs.uk/docs/nde/Zotepine.pdf -
- LOSIZOPILON SUGAR-COATED TABLETS & FINE GRANULES (PDF)
- ロドピン（ゾテピン） 1982年 精神神経学雑誌