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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/11/13 09:43:23」(JST)

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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

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English Journal

Atypical antipsychotic drugs, schizophrenia, and metabolic syndrome in non-euro-american societies.

Bou Khalil R.SourcePsychiatric Hospital of the Cross, Jalledib, Lebanon; and Saint Joseph University, Beirut, Lebanon.
Clinical neuropharmacology.Clin Neuropharmacol.2012 May;35(3):141-7.
OBJECTIVE: There has been an increase in the European and North American schizophrenia literature discussing the high prevalence of metabolic syndrome induced by atypical antipsychotic agents. The aim of this article was to review available data on metabolic syndrome induced by atypical antipsychoti
PMID 22592510

Hyperhidrosis under combination of zotepine and haloperidol alleviated by aripiprazole.

Huang WL, Chang LR.
Psychiatry and clinical neurosciences.Psychiatry Clin Neurosci.2012 Apr;66(3):245. doi: 10.1111/j.1440-1819.2012.02328.x.
PMID 22443252

Japanese Journal

Interaction of zotepine and chlorprothixene with URAT1-mediated urate transport

痛風と核酸代謝 39(2), 147-153, 2015
NAID 130005114177

zotepine, chlorprothixeneによる尿酸降下作用の解析

痛風と核酸代謝 39(1), 76, 2015
NAID 130005089259

Improvement in QTc prolongation induced by zotepine following a switch to perospirone

Psychiatry Clin Neurosci 66, 244, 2012
NAID 50008238203

「ゾテピン」

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
ATC code	N05AX11
PubChem	CID 5736
IUPHAR ligand	103
DrugBank	none
ChemSpider	5534
UNII	U29O83JAZW
KEGG	D01321
ChEBI	CHEBI:32316
ChEMBL	CHEMBL285802
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 ; Key:HDOZVRUNCMBHFH-UHFFFAOYSA-N ;
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英: zotepine
商: セトウス、メジャピン、ロシゾピロン、ロドピン
関: 抗精神病薬

統合失調症治療薬

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zotepine