Zotepine 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.
Medical uses
Zotepine'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. 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
Tachycardia
Hypotension
Orthostatic hypotension
Palpitations
Hyperprolactinaemia
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) Constipation Xerostomia (dry mouth) Blurred vision Hypersalivation (drooling) Mydriasis Anxiety Agitation Rhinitis Sexual dysfunction Dyspnoea Diarrhoea Influenza-like symptoms Cough Vertigo Confusion Dyspepsia Flushing dry skin Arthralgia Myalgia Acne Conjunctivitis Thrombocythaemia
Unknown frequency
QT interval prolongation
Hyperthermia
Hypothermia
Increased serum creatinine
Hyperglycaemia
Hypoglycaemia
Hyperlipidaemia
Thirst
Urinary incontinence
Rare
Angle-closure glaucoma
Agranulocytosis
Neutropaenia
Eosinophilia
Leukocytopenia
Hypoesthesia
Anaemia
Myoclonus
Myasthenia
Alopecia
Thrombocytopaenia
Bradycardia
Epistaxis
Abdominal enlargement
Deep vein thrombosis
Paralytic ileus
Leukopenia
Tardive dyskinesia
Neuroleptic malignant syndrome
Laryngeal edema
Urinary retention
Depression
Ataxia
Amnesia
Seizure (dose-dependent risk) Metabolic syndrome Diabetes mellitus type II Cholestasis Increased liver enzymes Photosensitivity Exanthema Pruritus Hypouricemia Oedema
Pharmacology
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.
Society and culture
Brand names
Brand names include Losizopilon (JP), Lodopin (ID, JP), Setous (JP), Zoleptil (CZ, PT, TR, UK†); where † indicates a formulation that has been discontinued.
See also
Carbinoxamine, diphenhydramine, doxylamine, and orphenadrine—the termination chain is the same Dosulepin Noxiptyline Toll-like receptor 4—investigating probable antagonistic (antiinflammatory) property of several TCA-based molecules