Amisulpride

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Amisulpride
Systematic (IUPAC) name
4-amino-N-[(1-ethylpyrrolidin-2-yl)methyl]-
5-ethylsulfonyl-2-methoxy-benzamide
Identifiers
CAS number 53583-79-2
[1]
ATC code N05AL05
PubChem 2159
DrugBank none
Chemical data
Formula C17H27N3O4S 
Mol. mass 369.48 g/mol
Pharmacokinetic data
Bioavailability 48%[2]
Metabolism  ?
Half life 12 h[2]
Excretion Renal[2]
Therapeutic considerations
Pregnancy cat.

B3(AU)
Legal status

℞ Prescription only
Routes Oral, intramuscular[1]

Amisulpride (brand-name Solian) is an antipsychotic drug sold by Sanofi-Aventis. Amisulpride is a selective dopamine antagonist. It has a high affinity for D2 (Ki 2.8 nM) and D3 (Ki 3.2 nM) dopaminergic receptors. Its dosage ranges from 200 to 1200 mg/day. Lower doses (less than 50 mg) preferentially block D2 autoreceptors that control the synthesis and release of dopamine. This results in an increase in dopaminergic transmission. This dopamine increase is hypothesized to cause a reduction in both depressive and negative symptoms. Higher doses of the drug block the postsynaptic dopamine receptors resulting in an improvement in psychoses. Its low incidence of extrapyramidal side effects (EPS) is characteristic of atypical antipsychotics.[3]

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, the UK, ...) and Australia to treat psychoses and schizophrenia.[4][5] In Italy, in 50 mg doses, it is also used as a treatment for dysthymia (under the brand name Deniban).

In one study, anxiety measured by HAM-A total mean score decreased significantly more with amisulpride 50 mg/day (63%) than with fluoxetine 20 mg/day (54%; P = 0.021).[6] Another recent study[7] concludes that amisulpride is an appropriate first-line treatment for the management of acute psychosis.

Contents

[edit] Side effects

Prolactin induction, thereby causing amenorrhoea and galactorrhoea in women, nausea, weight gain, although much less than similar drugs in its class, and less commonly QT interval prolongation (which can lead to serious heart arrhythmias). Overdoses of amisulpride have been linked with torsades de pointes.[8]

[edit] GHB receptor

The benzamide neuroleptics (including amisulpride and sulpiride) have been shown to activate the endogenous gamma-hydroxybutyrate receptor in vivo at theraputic concentrations.[9] GHB has neuroleptic properties and it is believed binding to this receptor may contribute to the effects of these neuroleptics.

[edit] See also

[edit] References

  1. ^ a b BIAM (2000) AMISULPRIDE, (HTML) Banque de Données Automatisée sur les Médicaments [online] Available from: http://www.biam2.org/www/Sub393.html Accessed on 25 November 2005. (French)
  2. ^ 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. 
  3. ^ Mortimer A.M. (2004). "Atypical Antipsychotics as First-Line Treatments for Schizophrenia: Advantages for Stakeholders in the UK Healthcare System". Disease Management & Health Outcomes 12 (3): 169–179. doi:10.2165/00115677-200412030-00003. 
  4. ^ Lecrubier Y, et al. (2001). "Consensus on the Practical Use of Amisulpride, an Atypical Antipsychotic, in the Treatment of Schizophrenia.". Neuropsychobiology 44: 41–46. doi:10.1159/000054913. 
  5. ^ Kaplan, Arline. (2004). "Psychotropic Medications Around the World". Psychiatric Times 21 (5). 
  6. ^ Smeraldi E (1998). "Amisulpride versus fluoxetine in patients with dysthymia or major depression in partial remission: a double-blind, comparative study". J Affect Disord 48 (1): 47–56. doi:10.1016/S0165-0327(97)00139-0. PMID 9495601. 
  7. ^ Nuss, Philippe; Martina Hummer and Cédric Tessier (2007). "The use of amisulpride in the treatment of acute psychosis". Therapeutics and Clinical Risk Management 3 (1). doi:10.2147/tcrm.2007.3.1.3. 
  8. ^ Isbister G, Murray L, John S, Hackett L, Haider T, O'Mullane P, Gosselin S, Daly F (2006). "Amisulpride deliberate self-poisoning causing severe cardiac toxicity including QT prolongation and torsades de pointes". Med J Aust 184 (7): 354–6. PMID 16584372.  Free full text
  9. ^ Displacement of [3H] gamma-hydroxybutyrate binding...[Eur J Pharmacol. 1994] - PubMed Result
v • d • e
Psycholeptics: antipsychotics (N05A)
Phenothiazine typical antipsychotics
Other typical antipsychotics
Atypical antipsychotics