Levosulpiride

Levosulpiride is a substituted benzamide antipsychotic,[1] reported to be a selective antagonist of dopamine D2 receptor activity[2] on both central and peripheral levels. It is an atypical neuroleptic and a prokinetic agent.[2] Levosulpiride is also claimed to have mood elevating properties.

Levosulpiride
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Chemical and physical data
FormulaC15H23N3O4S
Molar mass341.43 g·mol−1
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Chemically, it is the (S)-(−)-enantiomer of sulpiride.

Uses

Levosulpiride is used in the treatment of:

Levosulpiride is not currently licensed for treatment of premature ejaculation in the UK or other European countries.[3]

Side effect

Side effects include amenorrhea, gynecomastia, galactorrhea, changes in libido, and neuroleptic malignant syndrome.[4] In the U.S., as of 2013 only one case of adverse reaction to Levosulpiride had been recorded on the FDA Adverse Event Reporting System Database.[5] A case of rapid onset resistant dystonia caused by low dose levosulpiride was reported in India.[6]

Mechanism of action

In contrast to most other neuroleptics which block both dopamine D1 and D2 receptors, sulpiride is more selective and acts primarily as a dopamine D2 antagonist. Sulpiride appears to lack effects on norepinephrine, acetylcholine, serotonin, histamine, or gamma-aminobutyric acid (GABA) receptors.[7]

Pharmacodynamics

Sulpiride is a substituted benzamide derivative and a selective dopamine D2 antagonist with antipsychotic and antidepressant activity. Other benzamide derivatives include metoclopramide, tiapride, and sultopride.[7]

References
  1. Generon. "Levosulpiride - S-(-)-Sulpiride - >98% Generon". www.generon.co.uk. Retrieved 2016-08-31.
  2. http://www.stratech.co.uk/. "Levosulpiride | Stratech Scientific Ltd". www.stratech.co.uk. Retrieved 2016-08-31.
  3. Poluzzi, Elisabetta; Raschi, Emanuel; Koci, Ariola; Moretti, Ugo; Spina, Edoardo; Behr, Elijah R.; Sturkenboom, Miriam; Ponti, Fabrizio De (2013-04-04). "Antipsychotics and Torsadogenic Risk: Signals Emerging from the US FDA Adverse Event Reporting System Database". Drug Safety. 36 (6): 467–479. doi:10.1007/s40264-013-0032-z. ISSN 0114-5916. PMC 3664739. PMID 23553446.
  4. "Levosulpiride drug information | DrugsUpdate India".
  5. Poluzzi, Elisabetta; Raschi, Emanuel; Koci, Ariola; Moretti, Ugo; Spina, Edoardo; Behr, Elijah R.; Sturkenboom, Miriam; Ponti, Fabrizio De (2013-04-04). "Antipsychotics and Torsadogenic Risk: Signals Emerging from the US FDA Adverse Event Reporting System Database". Drug Safety. 36 (6): 467–479. doi:10.1007/s40264-013-0032-z. ISSN 0114-5916. PMC 3664739. PMID 23553446.
  6. "Rapid onset resistant dystonia with low dose of Levosulpiride". 2016-08-24. Cite journal requires |journal= (help)
  7. "Sulpiride". Drugbank.ca. DB00391.
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