Chemistry:Levosulpiride

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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.

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]

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

  1. ↑ 1.0 1.1 "Levosulpiride". 24 October 2021. https://adisinsight.springer.com/drugs/800003554. 
  2. ↑ 2.0 2.1 2.2 "Levosulpiride (International database)". 6 October 2024. https://www.drugs.com/international/levosulpiride.html. 
  3. ↑ 3.0 3.1 "Levosulpiride: a review of its clinical use in psychiatry". Pharmacol Res 31 (2): 95–101. February 1995. doi:10.1016/1043-6618(95)80053-0. PMID 7596960. 
  4. ↑ 4.0 4.1 4.2 4.3 4.4 4.5 4.6 "Pharmacotoxicological aspects of levosulpiride". Pharmacol Res 31 (2): 81–94. February 1995. doi:10.1016/1043-6618(95)80052-2. PMID 7596959. 
  5. ↑ 5.0 5.1 "5-HT4 receptors contribute to the motor stimulating effect of levosulpiride in the guinea-pig gastrointestinal tract". Dig Liver Dis 35 (4): 244–250. April 2003. doi:10.1016/s1590-8658(03)00061-6. PMID 12801035. 
  6. ↑ "Levosulpiride for Premature Ejaculation: A Systematic Review and Meta-Analysis". Am J Mens Health 16 (5). 2022. doi:10.1177/15579883221124832. PMID 36154321. 
  7. ↑ "Levosulpiride: a new solution for premature ejaculation?". Int J Impot Res 14 (4): 308–309. August 2002. doi:10.1038/sj.ijir.3900901. PMID 12152121. 
  8. ↑ 8.0 8.1 "Antipsychotics and torsadogenic risk: signals emerging from the US FDA Adverse Event Reporting System database". Drug Safety 36 (6): 467–79. June 2013. doi:10.1007/s40264-013-0032-z. PMID 23553446. 
  9. ↑ "Levosulpiride drug information". DrugsUpdate India. http://www.drugsupdate.com/generic/view/860. 
  10. ↑ "Rapid onset resistant dystonia with low dose of Levosulpiride.". British Journal of Psychiatry 190 (1): 81. January 2007. doi:10.1192/bjp.190.1.81a. 



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