Amisulpride, sold under the brand names Solian and Barhemsys, is a medication used in the treatment of schizophrenia, acute psychotic episodes, depression, and nausea and vomiting.
[12][13][14] Amisulpride is indicated for use in the United States in adults for the prevention of postoperative nausea and vomiting (PONV), either alone or in combination with an antiemetic of a different class; and to treat PONV in those who have received antiemetic prophylaxis with an agent of a different class or have not received prophylaxis.
The effectiveness of amisulpride in treating dysthymia and the negative symptoms of schizophrenia is believed to stem from its blockade of the presynaptic dopamine D2 and D3 autoreceptors.
[14] Although according to other studies it appears to have comparable efficacy to olanzapine in the treatment of schizophrenia,[16] amisulpride augmentation, similarly to sulpiride augmentation, has been considered a viable treatment option (although this is based on low-quality evidence) in clozapine-resistant cases of schizophrenia.
[17][18] Another recent study concluded that amisulpride is an appropriate first-line treatment for the management of acute psychosis.
[19] Amisulpride is approved and used at low doses in the treatment of dysthymia and major depressive disorder.
[11][10] Amisulpride is indicated for use in the United States in adults for the prevention of postoperative nausea and vomiting (PONV), either alone or in combination with an antiemetic of a different class; and to treat PONV in those who have received antiemetic prophylaxis with an agent of a different class or have not received prophylaxis.
[6] Hyperprolactinaemia results from antagonism of the D2 receptors located on the lactotrophic cells found in the anterior pituitary gland.
[41][42] Amisulpride should not be used in conjunction with drugs that prolong the QT interval (such as citalopram, bupropion, clozapine, tricyclic antidepressants, sertindole, ziprasidone, etc.
Likewise it is imprudent to combine antipsychotics due to the additive risk for tardive dyskinesia and neuroleptic malignant syndrome.
[47] Though it was long widely assumed that dopaminergic modulation is solely responsible for the respective antidepressant and antipsychotic properties of amisulpride, it was subsequently found that the drug also acts as a potent antagonist of the serotonin 5-HT7 receptor (Ki = 11.5 nM).
[44] Amisulpride also appears to bind with high affinity to the serotonin 5-HT2B receptor (Ki = 13 nM), where it acts as an antagonist.
It is structurally related to other benzamide dopamine receptor antagonists employed as antipsychotics and antiemetics including levosulpiride, metoclopramide, nemonapride, remoxipride, sulpiride, sultopride, tiapride, and veralipride.
[51] Subjects were randomly assigned to receive either amisulpride or a placebo drug at the beginning of general anesthesia.
LB Pharmaceuticals is developing N-methyl amisulpride for the use in the treatment of schizophrenia; a Phase 2 first-in-patient study is planned for 2023.
[55][56] An IV formulation of Amisulpride was approved for the treatment of postoperative nausea and vomiting ("PONV") in the United States in February 2020.
[57][9][51] SEP-4199 (non-racemic amisulpride), an 85:15 ratio of aramisulpride ((R)-amisulpride) to esamisulpride ((S)-amisulpride), which is theorized to provide more balanced serotonin 5-HT7 and dopamine D2 receptor antagonism than racemic amisulpride (a 50:50 ratio of its (R)- and (S)-enantiomers), is or was under development by Sunovion Pharmaceuticals for the treatment of bipolar depression in the United States and other countries.
[61] A more lipophilic and centrally permeable derivative of amisulpride, N-methylamisulpride (developmental code name LB-102), is under development by LB Pharmaceuticals for the treatment of schizophrenia in the United States and other countries.