| Clinical data | |
|---|---|
| Trade names | Dislep, Sulpepta, others |
| Other names | L-Sulpiride; S-(–)-Sulpiride; RV-12309 |
| Routes of administration | Oral |
| ATC code | |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| IUPHAR/BPS | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C15H23N3O4S |
| Molar mass | 341.43 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
| (verify) | |
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.1234 It is taken by mouth.
It is a selective antagonist of the dopamine D2 receptor and an agonist of the serotonin 5-HT4 receptor.45 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:31
- Psychosis
- Negative symptoms of schizophrenia
- Major depressive disorder
- Anxiety disorders
- Dysthymia
- Vertigo
- Nausea and vomiting
- Gastroparesis
- Dyspepsia
- Irritable bowel syndrome
- Premature ejaculation67
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.
References
References
- "Levosulpiride". AdisInsight. 24 October 2021. Retrieved 22 October 2024.
- "Levosulpiride (International database)". Drugs.com. 6 October 2024. Retrieved 22 October 2024.
- Mucci A, Nolfe G, Maj M (February 1995). "Levosulpiride: a review of its clinical use in psychiatry". Pharmacol Res. 31 (2): 95–101. doi:10.1016/1043-6618(95)80053-0. PMID 7596960.
- Rossi F, Forgione A (February 1995). "Pharmacotoxicological aspects of levosulpiride". Pharmacol Res. 31 (2): 81–94. doi:10.1016/1043-6618(95)80052-2. PMID 7596959.
- Tonini M, De Giorgio R, Spelta V, Bassotti G, Di Nucci A, Anselmi L, Balestra B, De Ponti F (April 2003). "5-HT4 receptors contribute to the motor stimulating effect of levosulpiride in the guinea-pig gastrointestinal tract". Dig Liver Dis. 35 (4): 244–250. doi:10.1016/s1590-8658(03)00061-6. PMID 12801035.
- Arshad A, Irfan M, Inam M, Hussain NH, Ismail SB (2022). "Levosulpiride for Premature Ejaculation: A Systematic Review and Meta-Analysis". Am J Men's Health. 16 (5) 15579883221124832. doi:10.1177/15579883221124832. PMC 9515538. PMID 36154321.
- Greco E, Polonio-Balbi P, Speranza JC (August 2002). "Levosulpiride: a new solution for premature ejaculation?". Int J Impot Res. 14 (4): 308–309. doi:10.1038/sj.ijir.3900901. PMID 12152121.
- Poluzzi E, Raschi E, Koci A, Moretti U, Spina E, Behr ER, et al. (June 2013). "Antipsychotics and torsadogenic risk: signals emerging from the US FDA Adverse Event Reporting System database". Drug Safety. 36 (6): 467–79. doi:10.1007/s40264-013-0032-z. PMC 3664739. PMID 23553446.
- "Levosulpiride drug information". DrugsUpdate India.
- Naskar S, Nath K (January 2007). "Rapid onset resistant dystonia with low dose of Levosulpiride". British Journal of Psychiatry. 190 (1): 81. doi:10.1192/bjp.190.1.81a.