Levosulpiride
Dopamine antagonist medication
From Wikipedia, the free encyclopedia
Levosulpiride, sold under the brand names Dislep and Sulpepta among others, is a dopamine antagonist medication which is used in the treatment of psychotic disorders like schizophrenia, major depressive disorder, nausea and vomiting, and gastroparesis.[1][2][3][4] It is taken by mouth.
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| Trade names | Dislep, Sulpepta, others |
| Other names | L-Sulpiride; S-(–)-Sulpiride; RV-12309 |
| Routes of administration | Oral |
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| Formula | C15H23N3O4S |
| Molar mass | 341.43 g·mol−1 |
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It is a selective antagonist of the dopamine D2 receptor and an agonist of the serotonin 5-HT4 receptor.[4][5] Chemically, it is a benzamide and the (S)-(−)-enantiomer of sulpiride.[4]
Levosulpiride is marketed widely throughout the world, including in Europe, South Korea, Latin America, India, and Pakistan.[2] It is not available in the United States or the United Kingdom.[2]
Medical uses
Levosulpiride is used in the treatment of:[3][1]
- Psychosis
- Negative symptoms of schizophrenia
- Major depressive disorder
- Anxiety disorders
- Dysthymia
- Vertigo
- Nausea and vomiting
- Gastroparesis
- Dyspepsia
- Irritable bowel syndrome
- Premature ejaculation[6][7]
Levosulpiride is not currently licensed for treatment of premature ejaculation in the United Kingdom or other European countries.[8]
Side effects
Side effects of levosulpiride include amenorrhea, gynecomastia, galactorrhea, changes in libido, and neuroleptic malignant syndrome.[9] In the United States, as of 2013 only one case of adverse reaction to levosulpiride had been recorded on the FDA Adverse Event Reporting System Database.[8] A case of rapid-onset resistant dystonia caused by low-dose levosulpiride was reported in India.[10]
Pharmacology
Pharmacodynamics
Levosulpiride is a selective dopamine D2 receptor antagonist.[4] The drug has also been found to act as a moderate agonist of the serotonin 5-HT4 receptor.[5] It is said to have antipsychotic, antidepressant, antiemetic, and gastroprokinetic effects.[4]
Chemistry
Levosulpiride is a substituted benzamide derivative.[4] It is the levorotatory enantiomer of sulpiride.[4] Other benzamide derivatives include amisulpride, metoclopramide, tiapride, sultopride, and veralipride, among others.