Zotepine

Zotepine

Systematic (IUPAC) name
2-[(8-​chlorodibenzo(b,f)​thiepin-​10-​yl)oxy]-​N,N-​dimethylethanamine
Clinical data
AHFS/Drugs.com	International Drug Names
Pregnancy cat.	?
Legal status	Unscheduled, Rx Only. (not approved in the U.S.)
Routes	Oral
Identifiers
CAS number	26615-21-4 N
ATC code	N05AX11
PubChem	CID 5736
IUPHAR ligand	103
DrugBank	none
ChemSpider	5534 Y
UNII	U29O83JAZW Y
KEGG	D01321 Y
ChEBI	CHEBI:32316 Y
ChEMBL	CHEMBL285802 Y
Chemical data
Formula	C18H18ClNOS
Mol. mass	331.86
SMILES Clc2cc1C(/OCCN(C)C)=C\c3c(Sc1cc2)cccc3
InChI InChI=1S/C18H18ClNOS/c1-20(2)9-10-21-16-11-13-5-3-4-6-17(13)22-18-8-7-14(19)12-15(16)18/h3-8,11-12H,9-10H2,1-2H3 Y Key:HDOZVRUNCMBHFH-UHFFFAOYSA-N Y
N (what is this?)  (verify)

Zotepine (Nipolept, Losizopilon, Lodopin, Setous) 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.

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-HT_2A, 5-HT_2C, 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

50 mg Lodopin® pills

References

• http://www.priory.com/focus11.htm
• 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