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Levosulpiride, sold under the brand name SULPEPTA , is a potent prokinetic agent of the benzamide class.[1] It is a selective antagonist of the dopamine D2 receptors and 5HT4 Agonism [2] on both central and peripheral nervous systems. Levosulpiride is claimed to have mood elevating properties.

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 effects

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.[3] A case of rapid onset resistant dystonia caused by low dose levosulpiride was reported in India.[5]

Mechanism of action

In contrast to most other neuroleptics which block both D1 and D2 receptors, levosulpiride is more selective and acts primarily as a D2 antagonist. Levosulpiride appears to lack effects on norepinephrine, acetylcholine, serotonin, histamine, and gamma-aminobutyric acid (GABA) receptors.[6]

Pharmacodynamics

Levosulpiride is a substituted benzamide derivative and a selective dopamine D2 antagonist with antipsychotic and antidepressant activity. Other benzamide derivatives include metoclopramide, tiapride, and sultopride.[6]

See also

References

  1. ^ "Levosulpiride - S-(-)-Sulpiride". Generon. Retrieved 2016-08-31.
  2. ^ "Levosulpiride". Stratech Scientific Ltd. Retrieved 2016-08-31.
  3. ^ a b 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.
  4. ^ "Levosulpiride drug information". DrugsUpdate India.
  5. ^ 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.
  6. ^ a b "Sulpiride". DrugBank. DB00391.
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