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Amisulpride (sold as Amazeo, Amipride (AU), Amival, Solian (AU, IE, RU, UK, ZA), Soltus, Sulpitac (IN), Sulprix (AU)), is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. In Italy, it is also used as a treatment for dysthymia.^[5]

It was introduced by Sanofi-Aventis in the 1990s. Its patent had expired by 2008 and hence generic formulations are now available.^[6]

Medical Uses

Schizophrenia

It appears to have comparable efficacy to olanzapine in the treatment of schizophrenia.^[7]^[8]^[9] Amisulpride augmentation, similarly to sulpiride augmentation, has been considered a viable treatment option (although, it is worth noting that the supporting evidence is limited to the theory, case reports, a small randomised double-blind placebo-controlled trial^[10] and a couple of open-label studies^[11]^[12]) in clozapine-resistant cases of schizophrenia.^[13]^[14] A randomised, double-blind, placebo-controlled clinical trial has been conducted to evaluate the efficacy of celecoxib as an adjunct to amisulpride, with significant success.^[15] Another recent study concluded that amisulpride is an appropriate first-line treatment for the management of acute psychosis.^[16]

Bipolar disorder

Amisulpride has been tried as a treatment for acute mania in a few open-label studies.^[17]^[18] These findings should be interpreted with caution, not just due to the fact that these clinical trials were all open-label and hence low-quality but also because several case reports have been made documenting the precipitation of mania in schizophrenia patients that received amisulpride.^[2]^[19]

Dysthymia

At low doses, it is also used to treat dysthymia where it appears to be at least as effective as conventional antidepressants according to a recent Cochrane review. Studies showed that at dose < 50 mg amisulpride has preferential affinity for pre-synaptic dopamine D2 and D3 autoreceptor subtypes (pre-synaptics autoreceptors serves as a negative feedback loop control). By blocking these autoreceptors amisulpride is preventing neurons to stop firing dopamine, leading to an increase of dopamine concentration in the brain. This mode of action could explain its strong antidepressant properties.^[4]^[20]^[21] In this indication, amisulpride is significantly more effective than:

Sertraline^[22]
Imipramine^[23]

and equal to:

Amitriptyline^[24]
Amineptine^[25]

Investigational

Low-dose amisulpride has been found to be an effective treatment for postoperative emesis in a recent randomised, double-blind, placebo-controlled clinical trial.^[26] In a small (N=11) clinical trial amisulpride combined with either mirtazapine or citalopram was found an effective treatment for psychotic depression in elderly patients, although it should be noted that this trial was not placebo-controlled and hence the level of evidence it provides to amisulpride's efficacy in this indication is low.^[27] In a medium-sized (N=106) single-blind study it was found efficacious and well-tolerated in improving depressive symptoms in cancer patients undergoing chemotherapy.^[28]

Adverse effects

Very Common (≥10% incidence)^[29]

Extrapyramidal side effects (EPS; including dystonia, tremor, akathisia, parkinsonism). Produces a moderate degree of EPS; more than aripiprazole (not significantly, however), clozapine, iloperidone (not significantly), olanzapine (not significantly), quetiapine (not significantly) and sertindole; less than chlorpromazine (not significantly), haloperidol, lurasidone (not significantly), paliperidone (not significantly), risperidone (not significantly), ziprasidone (not significantly) and zotepine (not significantly).^[9]

Common (≥1%, <10% incidence)^[2]^[30]^[31]^[32]

Insomnia
Hypersalivation
Nausea
Headache
Hyperactivity
Anxiety
Vomiting

Hyperprolactinaemia (which can lead to galactorrhoea, breast enlargement and tenderness, sexual dysfunction, etc.)
Weight gain (produces less weight gain than chlorpromazine, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, sertindole, zotepine and more (although not statistically significantly) weight gain than haloperidol, lurasidone, ziprasidone and approximately as much weight gain as aripiprazole and asenapine)^[9]
Anticholinergic side effects (although it does not bind to the muscarinic acetylcholine receptors and hence these side effects are usually quite mild) such as

- constipation; - dry mouth; - disorder of accommodation; - Blurred vision
Rare (<1% incidence)^[2]^[30]^[31]^[32]

Bradycardia
Hypotension
Palpitations
Urticaria
Seizures
Mania
Oculogyric crisis
Tardive dyskinesia

Blood dyscrasias such as leucopenia, neutropenia and agranulocytosis
QT interval prolongation (in a recent meta-analysis of the safety and efficacy of 15 antipsychotic drugs amisulpride was found to have the 2nd highest effect size for causing QT interval prolongation^[9])

Hyperprolactinaemia results from antagonism of the D₂ receptors located on the lactotrophic cells found in the anterior pituitary gland. Amisulpride has a high propensity for elevating plasma prolactin levels as a result of its poor blood-brain barrier penetrability and hence the resulting greater ratio of peripheral D₂ occupancy to central D₂ occupancy. This means that to achieve the sufficient occupancy (~60-80%^[33]) of the central D₂ receptors in order to elicit its therapeutic effects a dose must be given that is enough to saturate peripheral D₂ receptors including those in the anterior pituitary.^[34]^[35]

Somnolence. It produces minimal sedation due to its absence of cholinergic, histaminergic and alpha adrenergic receptor antagonism. It is one of the least sedating antipsychotics.^[9]

Contraindications

Amisulpride's use is contraindicated in the following disease states^[2]^[31]^[32]

Phaeochromocytoma
Concomitant Prolactin dependent tumours e.g. Prolactinoma, Breast cancer
Movement disorders (e.g. Parkinson's disease and dementia with lewy bodies)
Lactation
Children before the onset of puberty

neither is it recommended to use amisulpride in patients with hypersensitivities to amisulpride or the excipients found in its dosage form.^[2]

Interactions

Amisulpride should not be used in conjunction with drugs that prolong the QT interval (such as citalopram, venlafaxine, bupropion, clozapine, tricyclic antidepressants, sertindole, ziprasidone, etc.),^[36] reduce heart rate and those that can induce hypokalaemia. Likewise it is imprudent to combine antipsychotics due to the additive risk for tardive dyskinesia and neuroleptic malignant syndrome.^[36]

Overdose

Torsades de Pointes is common in overdose.^[37]^[38] Amisulpride is moderately dangerous in overdose (with the TCAs being very dangerous and the SSRIs being modestly dangerous).^[36]^[39]

Pharmacology

Amisulpride function primarily as a D₂ and D₃ receptor antagonist. It has high affinity for these receptors with dissociation constants of 2.2 nM and 2.4 nM, respectively. Although standard doses used to treat psychosis inhibit dopaminergic neurotransmission, low doses preferentially block inhibitory pre-synaptic autoreceptors. This results in a facilitation of dopamine activity, and for this reason, low dose amisulpride has also been used to treat dysthymia.^[2]

Amisulpride and its relative sulpiride have been shown to bind to and activate the GHB receptor at doses that are used for therapeutic purposes.^[40]

Though it has long been widely assumed that dopaminergic modulation is solely responsible for the respective antidepressant and antipsychotic properties of amisulpride, it has recently been shown that it also acts as a potent antagonist at the 5-HT₇ receptor.^[41] Several of the other atypical antipsychotics such as risperidone and ziprasidone are potent antagonists at the 5-HT₇ receptor as well, and selective antagonists of the receptor show antidepressant properties themselves. To characterize the role of the 5-HT₇ receptor in the antidepressant effects of amisulpride, a study prepared 5-HT₇ receptor knockout mice.^[41] The study found that in two widely used rodent models of depression, the tail suspension test, and the forced swim test, those mice did not exhibit an antidepressant response upon treatment with amisulpride.^[41] These results suggest that 5-HT₇ receptor antagonism mediates the antidepressant effects of amisulpride.^[41]

Amisulpride also appears to bind with high affinity to the 5-HT_2B receptor (see below table), though the clinical implications of this, if any, are unclear.

Molecular target	Binding Affinity (K_i in nM)^[42]
SERT	>10000
NET	>10000
DAT	>10000
5-HT_1A	>10000
5-HT_1B	1744
5-HT_1D	1341
5-HT_1E	>10000
5-HT_2A	8304
5-HT_2B	13
5-HT_2C	>10000
5-HT₃	>10000
5-HT_5A	>10000
5-HT₆	4154
5-HT₇	11.5^[41]
α_1A	>10000
α_1B	>10000
α_1D	>10000
α_2A	1114
α_2C	1540
β₁	>10000
β₂	>10000
β₃	>10000
M₁	>10000
M₂	>10000
M₃	>10000
M₄	>10000
M₅	>10000
D₁	>10000
D₂	2.2
D₃	2.4
D₄	2370
D₅	>10000
H₁	>10000
H₂	>10000
H₄	>10000
δ opioid	>10000
κ opioid	>10000
μ opioid	>10000
Prostaglandin E3 receptor	>10000
Prostaglandin E4 receptor	>10000

Availability

Amisulpride is not approved by the Food and Drug Administration for use in the United States, but it is used in Europe (France, Germany, Italy, Switzerland, Russia, United Kingdom, etc.), Israel, India, New Zealand and Australia (TGA approved in February 2002^[2]) to treat psychosis and schizophrenia.^[43]^[44]

Synthesis

Dopamine receptor antagonist.

Amisulpride synthesis: M. Thominet et al., BE 872585; eidem, U.S. Patent 4,401,822 (1979, 1983 both to Soc. d'Etudes Sci. Ind. de l'Ile-de-France).

4-amino-5-mercapto-2-methoxybenzoic acid (1) is alkylated with diethyl sulfate to 4-amino-5-(ethylthio)-2-methoxybenzoic acid (2) and then this is oxidized with H2O2 to 4-amino-5-(ethylsulfonyl)-2-methoxybenzoic acid (3). A mixed anhydride is prepared via reaction with ethyl chloroformate (4) and then amidation with 1-ethyl-(2-aminoethyl)pyrrolidine (5) to give Amisulpride as the product (6).

References

^ ^a ^b ^c Rosenzweig, P.; Canal, M.; Patat, A.; Bergougnan, L.; Zieleniuk, I.; Bianchetti, G. (2002). "A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers.". Human Psychopharmacology 17 (1): 1–13. doi:10.1002/hup.320. PMID 12404702.
^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k "PRODUCT INFORMATION SOLIAN® TABLETS and SOLUTION" (PDF). TGA eBusiness Services. Sanofi-Aventis Australia Pty Ltd. 9 September 2013. Retrieved 17 October 2013.
^ Caccia, S (May 2000). "Biotransformation of Post-Clozapine Antipsychotics Pharmacological Implications". Clinical Pharmacokinetics 38 (5): 393–414. doi:10.2165/00003088-200038050-00002.
^ ^a ^b Noble, S; Benfield, P (December 1999). "Amisulpride: A Review of its Clinical Potential in Dysthymia". CNS Drugs 12 (6): 471–483. doi:10.2165/00023210-199912060-00005.
^ Pani, L; Gessa, GL (2002). "The substituted benzamides and their clinical potential on dysthymia and on the negative symptoms of schizophrenia" (PDF). Molecular Psychiatry 7 (3): 247–253. doi:10.1038/sj/mp/4001040. PMID 11920152.
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^ Vieta, E; Ros, S; Goikolea, JM; Benabarre, A; Popova, E; Comes, M; Capapey, J; Sánchez-Moreno, J (May 2005). "An open-label study of amisulpride in the treatment of mania". Journal of Clinical Psychiatry 66 (5): 575–578. doi:10.4088/jcp.v66n0505. PMID 15889942.
^ Thomas, P; Vieta, E (June 2008). "Amisulpride plus valproate vs haloperidol plus valproate in the treatment of acute mania of bipolar I patients: a multicenter, open-label, randomized, comparative trial". Neuropsychiatric disease and treatment 4 (3): 675–686. doi:10.2147/NDT.S3135. PMC 2526384. PMID 18830442.
^ Aggarwal, A; Jain, M; Khandelwal, A; Jiloha, RC (April 2010). "Amisulpride induced mania". Indian Journal of Pharmacology 42 (2): 112–113. doi:10.4103/0253-7613.64496. PMC 2907009. PMID 20711379.
^ Komossa, K; Depping, AM; Gaudchau, A; Kissling, W; Leucht, S (December 2010). "Second-generation antipsychotics for major depressive disorder and dysthymia." (PDF). The Cochrane Database of Systematic Reviews (12): CD008121. doi:10.1002/14651858.CD008121.pub2. PMID 21154393.
^ Pani, L; Gessa, GL (2002). "The substituted benzamides and their clinical potential on dysthymia and on the negative symptoms of schizophrenia" (PDF). Molecular Psychiatry 7 (3): 247–253. doi:10.1038/sj/mp/4001040. PMID 11920152.
^ Amore, M.; Jori, M. C.; Amisert investigators (2001). "Faster response on amisulpride 50 mg versus sertraline 50-100 mg in patients with dysthymia or double depression: A randomized, double-blind, parallel group study". International Clinical Psychopharmacology 16 (6): 317–324. doi:10.1097/00004850-200111000-00001. PMID 11712619.
^ Papp, M.; Wieronska, J. (2000). "Antidepressant-like activity of amisulpride in two animal models of depression". Journal of Psychopharmacology (Oxford, England) 14 (1): 46–52. doi:10.1177/026988110001400106. PMID 10757253.
^ Ravizza, L.; AMILONG investigators (1999). "Amisulpride in medium-term treatment of dysthymia: A six-month, double-blind safety study versus amitriptyline". Journal of Psychopharmacology (Oxford, England) 13 (3): 248–254. doi:10.1177/026988119901300307. PMID 10512080.
^ Boyer, P.; Lecrubier, Y.; Stalla-Bourdillon, A.; Fleurot, O. (1999). "Amisulpride versus amineptine and placebo for the treatment of dysthymia". Neuropsychobiology 39 (1): 25–32. doi:10.1159/000026556. PMID 9892856.
^ Kranke, P; Eberhart, L; Motsch, J; Chassard, D; Wallenborn, J; Diemunsch, P; Liu, N; Keh, D; Bouaziz, H; Bergis, M; Fox, G; Gan, TJ (July 2013). "I.V. APD421 (amisulpride) prevents postoperative nausea and vomiting: a randomized, double-blind, placebo-controlled, multicentre trial". British Journal of Anaesthesia 111 (6): 938–45. doi:10.1093/bja/aet251. PMID 23872464.
^ Torta, R; Berra, C; Binaschi, L; Borio, R (July 2008). "Combination therapy with amisulpride and antidepressants: Clinical observations in case series of elderly patients with psychotic depression". Progress in Neuro-Psychopharmacology & Biological Psychiatry 32 (5): 1227–1230. doi:10.1016/j.pnpbp.2008.03.011. PMID 18442877.
^ Torta, R; Berra, C; Binaschi, L; Borio, R (May 2007). "Amisulpride in the short-term treatment of depressive and physical symptoms in cancer patients during chemotherapies". Support Care Cancer 15 (5): 539–546. doi:10.1007/s00520-006-0194-7. PMID 17406919.
^ Sandoz Limited Summary of Product Characteristics, archived from the original on 2014-08-17, retrieved 2014-08-17
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UpToDate Contents

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1. 成人における単極性うつ病：第2世代抗精神病薬による治療 unipolar depression in adults treatment with second generation antipsychotics
2. 治療抵抗性統合失調症 treatment resistant schizophrenia
3. 成人における単極性うつ病：初期治療の選択 unipolar major depression in adults choosing initial treatment
4. 高プロラクチン血症の原因 causes of hyperprolactinemia

English Journal

Beta-glucan from Saccharomyces cerevisiae reduces plasma lipid peroxidation induced by haloperidol.

Dietrich-Muszalska A, Olas B, Kontek B, Rabe-Jab?o?ska J.SourceDepartment of Affective and Psychotic Disorders, Medical University of Lodz, Czechoslowacka 8/10, 92-216 Lodz, Poland.
International journal of biological macromolecules." abstractLink="yes" alsec="jour" alterm="Int J Biol Macromol.2011 Jul 1;49(1):113-6. Epub 2011 Mar 21.
Since oxidative stress observed in schizophrenia may be caused partially by the treatment of patients with various antipsychotics, the aim of the study was to establish the effects of beta-d-glucan, polysaccharide derived from the yeast cell walls of species such as Saccharomyces cerevisiae, and the
PMID 21421004

Functional potencies of dopamine agonists and antagonists at human dopamine D(2) and D(3) receptors.

Tadori Y, Forbes RA, McQuade RD, Kikuchi T.SourceQuests Research Institute, Otsuka Pharmaceutical Co., Ltd., Tokushima, 771-0192, Japan.
European journal of pharmacology." abstractLink="yes" alsec="jour" alterm="Eur J Pharmacol.2011 Jun 1. [Epub ahead of print]
We measured the functional agonist potencies of dopamine agonists including antiparkinson drugs, and functional antagonist potencies of antipsychotics at human dopamine D(2) and D(3) receptors. In vitro pharmacological assessment included inhibition of forskolin-stimulated cAMP accumulation and the
PMID 21658377

Japanese Journal

Development and Validation of Spectrophotometric Methods for Estimating Amisulpride in Pharmaceutical Preparations

SHARMA Sangita,NEOG Madhurjya,PRAJAPATI Vipul,PATEL Hiren,DABHI Dipti
Analytical sciences : the international journal of the Japan Society for Analytical Chemistry 26(4), 485-489, 2010-04-10
NAID 10026783156

Selective and sensitive determination of amisulpride in human plasma by liquid chromatography-tandem mass spectrometry with positive electrospray ionisation and multiple reaction monitoring

GSCHWEND M. H.,ARNOLD P.,RING J.,MARTIN W.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 831(1), 132-139, 2006-02-02
NAID 10025779271

「アミスルプリド」

Amisulpride
Systematic (IUPAC) name
	RS-4-amino-N-[(1-ethylpyrrolidin-2-yl)methyl]-; 5-ethylsulfonyl-2-methoxy-benzamide
Clinical data
Trade names	Solian
AHFS/Drugs.com	International Drug Names
Pregnancy; category	AU: C; ;
Legal status	AU: Prescription Only (S4); UK: Prescription-only (POM);
Routes of; administration	Oral, intravenous
Pharmacokinetic data
Bioavailability	48%
Protein binding	16%
Metabolism	Hepatic (minimal; most excreted unchanged)
Biological half-life	12 hours
Excretion	Renal (23-46%), Faecal
Identifiers
CAS Registry Number	71675-85-9
ATC code	N05AL05
PubChem	CID: 2159
IUPHAR/BPS	963
DrugBank	DB06288
ChemSpider	2074
UNII	8110R61I4U
KEGG	D07310
ChEBI	CHEBI:64045
ChEMBL	CHEMBL243712
Chemical data
Formula	C17H27N3O4S
Molecular mass	369.48 g/mol
	SMILES O=S(=O)(c1cc(c(OC)cc1N)C(=O)NCC2N(CC)CCC2)CC ;
	InChI InChI=1S/C17H27N3O4S/c1-4-20-8-6-7-12(20)11-19-17(21)13-9-16(25(22,23)5-2)14(18)10-15(13)24-3/h9-10,12H,4-8,11,18H2,1-3H3,(H,19,21) ; Key:NTJOBXMMWNYJFB-UHFFFAOYSA-N ;
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　　[★]

英: amisulpride
関: スルトプリド、塩酸スルトプリド

-amisulpride

「sultopride」

　　[★]

スルトプリド

関: amisulpride、sultopride hydrochloride

「sultopride hydrochloride」

　　[★]

塩酸スルトプリド

関: amisulpride、sultopride

[Rosenzweig-1] Rosenzweig, P.; Canal, M.; Patat, A.; Bergougnan, L.; Zieleniuk, I.; Bianchetti, G. (2002). "A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers.". Human Psychopharmacology 17 (1): 1–13. doi:10.1002/hup.320. PMID 12404702.

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amisulpride