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.
|Dopamine receptor antagonist
|Use||Schizophrenia, bipolar disorder, nausea and vomiting, etc.|
|Biological target||Dopamine receptors|
Uses and examplesEdit
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.
- 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 as part of normal circadian rhythm functions, although pathological imbalances have been implicated in Parkinson's disease
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:
- 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)
- Sedation or psychomotor agitation
- Symptoms similar to ADHD
- Symptoms similar to narcolepsy
Examples of Dopamine antagonists include:
- clomipramine (mild)
- 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. doi:10.1515/revneuro.2008.19.4-5.245. PMID 19145986.
- MeSH list of agents 82018492