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Zotepine
Systematic (IUPAC) name
2-[(8-​chlorodibenzo(b,f)​thiepin-​10-​yl)oxy]-​ N,N-​dimethylethanamine
Identifiers
CAS number 26615-21-4
ATC code N05AX11
PubChem 5736
DrugBank none
Chemical data
Formula C 18H18ClNOS 
Mol. mass 331.86
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status Unscheduled, Rx Only. (not approved in the U.S.)
Routes Oral

Zotepine (Nipolept, Losizopilon, Lodopin, Setous) is an atypical antipsychotic indicated for acute and chronic schizophrenia. It has been used in Germany since 1990 and Japan since 1982.

Contents

Pharmacology

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, it acts as a norepinephrine reuptake inhibitor, likely contributing to its efficacy against the negative symptoms of schizophrenia.

Dosing

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.

Side effects

The most common side effect of zotepine is weight gain. This weight gain side effect compares badly to the older typical antipsychotics. Somnolence is the second most common side effect. Constipation, asthenia, dry mouth, and akathisia are also reported. As with all antipsychotics, there is a risk of tardive dyskinesia, a potentially incurable neurologic disorder, with prolonged use of zotepine.

The likelihood of side effects are as follows:

  • Weight gain: Medium to high
  • Hyperprolactinemia: High
  • Sexual problems: High
  • Sedation: High
  • Extrapyramindal: Low
  • Hypotension: Medium
  • Hyperglycemia: Low

References








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