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a drug that neutralizes or counteracts the effects of another drug
a muscle that relaxes while another contracts; "when bending the elbow the triceps are the antagonist"
a monoamine neurotransmitter found in the brain and essential for the normal functioning of the central nervous system; as a drug (trade names Dopastat and Intropin) it is used to treat shock and hypotension (同)Dopastat, Intropin

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/02/01 13:34:39」(JST)

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A dopamine antagonist (antidopaminergic) is a type of drug which blocks dopamine receptors by receptor antagonism. Most antipsychotics are dopamine antagonists, and as such they have found use in treating schizophrenia, bipolar disorder, and stimulant psychosis. Several other dopamine antagonists are antiemetics used in the treatment of nausea and vomiting.

Uses and examples

Clozapine, a second generation antipsychotic

Dopamine receptor antagonists are used for some diseases such as schizophrenia, bipolar disorder, nausea and vomiting. It can also control the symptoms of hypersexuality and increased orgasmic activity.

Antidopaminergics such as haloperidol can be an antidote for poisoning with cocaine, amphetamines and dopamine agonists such as bromocriptine and/or ropinirole.

Agents such as atypical antipsychotics (coupled with serotonin antagonist effects): paliperidone, clozapine, risperidone, olanzapine, quetiapine, and ziprasidone
Used as antiemetics: metoclopramide, droperidol, domperidone
Used as tricyclic antidepressants: amoxapine, clomipramine, trimipramine
Choline can antagonize dopamine directly or interfere with receptor function
Melatonin suppresses dopamine activity^[1] as part of normal circadian rhythm functions, although pathological imbalances have been implicated in Parkinson's disease^[2]

Side effects

They may include one or more of the following and last indefinitely even after cessation of the dopamine antagonist, especially after long-term or high-dosage use:

Dysphoria and depression
Extrapyramidal symptoms, including:
- Akathisia
- Parkinsonism due to effects on the nigrostriatal pathway
- Tardive dyskinesia (long-term use)
Galactorrhea due to removal of dopamine-mediated inhibition (D2 receptor antagonism) on the lactotrophic cells in the anterior pituitary preventing the release of prolactin.
Hyperprolactinaemia due to effects on the tuberoinfundibular pathway
Increased appetite
Irritability and aggression
Low libido, sexual dysfunction and impotence due to blockage of the pleasure center (dopaminergic pathways)
Menstrual disorder
Metabolic changes with increased risk of obesity and diabetes mellitus type 2
Neuroleptic Induced Deficit Syndrome (long-term use)
Paranoia (rare)^{[citation needed]}
Sedation or psychomotor agitation
Symptoms similar to ADHD
Symptoms similar to narcolepsy

Examples

Examples of Dopamine antagonists include:^[3]

acepromazine
amisulpride
amoxapine
asenapine
azaperone
benperidol
bromopride
butaclamol
clomipramine (mild)
chlorpromazine
chlorprothixene
clopenthixol
domperidone
droperidol
eticlopride
flupenthixol
fluphenazine
fluspirilene
haloperidol
hydroxyzine
iodobenzamide
loxapine
mesoridazine
levomepromazine
metoclopramide
nafadotride
nemonapride
olanzapine
paliperidone
penfluridol
perazine
perphenazine
pimozide
prochlorperazine
promazine
quetiapine
raclopride
remoxipride
risperidone
spiperone
spiroxatrine
stepholidine
sulpiride
sultopride
tetrahydropalmatine
thiethylperazine
thioridazine
thiothixene
tiapride
trifluoperazine
trifluperidol
triflupromazine
ziprasidone

References

^ Zisapel, N (2001). "Melatonin-dopamine interactions: from basic neurochemistry to a clinical setting". Cellular and Molecular Neurobiology 21 (6): 605–16. PMID 12043836.
^ Willis, GL (2008). "Parkinson's disease as a neuroendocrine disorder of circadian function: dopamine-melatonin imbalance and the visual system in the genesis and progression of the degenerative process". Reviews in the Neurosciences 19 (4–5): 245–316. PMID 19145986.
^ MeSH list of agents 82018492

External links

Dopamine antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)

This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it.

This drug article relating to the gastrointestinal system is a stub. You can help Wikipedia by expanding it.

UpToDate Contents

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1. 制吐剤の特性 characteristics of antiemetic drugs
2. 遅発性ジスキネジア：病因および疫学 tardive dyskinesia etiology and epidemiology
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5. 悪性腫瘍関連胃不全麻痺：病態生理およびマネージメント malignancy associated gastroparesis pathophysiology and management

English Journal

Role of dopamine neurotransmission in the long-term effects of repeated social defeat on the conditioned rewarding effects of cocaine.

Montagud-Romero S1, Reguilon MD1, Roger-Sanchez C1, Pascual M2, Aguilar MA1, Guerri C2, Miñarro J1, Rodríguez-Arias M3.
Progress in neuro-psychopharmacology & biological psychiatry.Prog Neuropsychopharmacol Biol Psychiatry.2016 Nov 3;71:144-54. doi: 10.1016/j.pnpbp.2016.07.008. Epub 2016 Jul 28.
Numerous studies report that social defeat stress alters dopamine (DA) neurotransmission in several areas of the brain. Alterations of the mesolimbic dopaminergic pathway are believed to be responsible for the increased vulnerability to drug use observed as a result of social stress. In the present
PMID 27476156

Reproductive steroid receptors and actions in the locus coeruleus of male macaques: Part of an aggression circuit?

Bethea CL1, Belikova Y2, Phu K2, Mammerella G2.
Progress in neuro-psychopharmacology & biological psychiatry.Prog Neuropsychopharmacol Biol Psychiatry.2016 Nov 3;71:210-22. doi: 10.1016/j.pnpbp.2016.04.002. Epub 2016 Apr 12.
This study was initiated to determine whether the noradrenergic (NE) neurons of the locus coeruleus (LC) could mediate the stimulatory action of androgens on serotonin-related gene expression in male macaques. These experiments follow our observations that serotonin neurons lack androgen receptors (
PMID 27083854

Signaling in dopamine D2 receptor-oxytocin receptor heterocomplexes and its relevance for the anxiolytic effects of dopamine and oxytocin interactions in the amygdala of the rat.

de la Mora MP1, Pérez-Carrera D2, Crespo-Ramírez M3, Tarakanov A4, Fuxe K5, Borroto-Escuela DO6.
Biochimica et biophysica acta.Biochim Biophys Acta.2016 Nov;1862(11):2075-2085. doi: 10.1016/j.bbadis.2016.07.004. Epub 2016 Jul 15.
Dopamine D2 receptor (D2R)-oxytocin receptor (OTR) interactions exist within heterocomplexes with facilitatory effects on D2R recognition and Gi/o coupling. In this work the hypothesis is tested using cotransfected HEK293 cells whether allosteric reciprocal D2R-OTR interactions can enhance signaling
PMID 27425032

Japanese Journal

Antidepressant-Like Effects of Sanggenon G, Isolated from the Root Bark of Morus alba, in Rats: Involvement of the Serotonergic System

Biological and Pharmaceutical Bulletin 38(11), 1772-1778, 2015
NAID 130005106373

先端巨大症の治療戦略

脳神経外科ジャーナル 24(8), 521-527, 2015
NAID 130005094985

Antidepressant-like effects of sanggenon G, isolated from the root bark of Morus alba, in rats: involvement of the serotonergic system

Biological and Pharmaceutical Bulletin advpub(0), 2015
NAID 130005094019

Related Pictures

★リンクテーブル★

リンク元	「ドパミン拮抗薬」
拡張検索	「serotonm-dopamine antagonist」「serotonin-dopamine antagonist」

「ドパミン拮抗薬」

Dopamine receptor antagonist; Dopaminergic blockers
	Drug class
	Skeletal structor formula of Haloperidol, a typical antipsychotic
Class identifiers
Use	Schizophrenia, bipolar disorder, nausea and vomiting, etc.
ATC code	N05A
Biological target	Dopamine receptors
External links
MeSH	D012559

　　[★]

英: dopamine antagonist、dopaminergic antagonist, dopamine receptor antagonist
同: ドパミン受容体拮抗薬、ドパミン受容体遮断薬、ドパミン拮抗薬、ドパミン遮断薬、抗ドパミン薬 antidopaminergic agent

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ドパミン受容体遮断薬 : 約 12,400 件
ドパミン受容体拮抗薬 : 約 17,900 件
ドパミン遮断薬 : 約 15,500 件
ドパミン拮抗薬 : 約 19,100 件

「serotonm-dopamine antagonist」

　　[★] セロトニン・ドパミン拮抗薬 SDA

「serotonin-dopamine antagonist」

　　[★] セロトニン・ドパミン拮抗薬

[1] Zisapel, N (2001). "Melatonin-dopamine interactions: from basic neurochemistry to a clinical setting". Cellular and Molecular Neurobiology 21 (6): 605–16. PMID 12043836.

[2] Willis, GL (2008). "Parkinson's disease as a neuroendocrine disorder of circadian function: dopamine-melatonin imbalance and the visual system in the genesis and progression of the degenerative process". Reviews in the Neurosciences 19 (4–5): 245–316. PMID 19145986.

[3] MeSH list of agents 82018492

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案内

dopamine antagonist