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 | [1] |
| ATC code | N05 |
| PubChem | |
| DrugBank | |
| ChemSpider | |
| 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), or Sultopride, is an atypical 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, Russia, United Kingdom, ...) 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.
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[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 therapeutic concentrations.[9] GHB has neuroleptic properties and it is believed binding to this receptor may contribute to the effects of these neuroleptics.
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