Peringatan Keamanan

In mice, oral LD50 is 1024 mg/kg, intraperitoneal LD50 is 175 mg/kg, and subcutaneous LD50 is 224 mg/kg. The Lowest published toxic dose (TDLo) following subcutaneous administration is 0.24 mg/kg in rats. The oral TDLo in men is 4.3 mg/kg.L32769

Oral doses of amisulpride above 1200 mg/day are associated with adverse effects related to dopamine-2 (D2) antagonism. Cardiovascular adverse reactions include prolongation of the QT interval, torsades de pointes, bradycardia, and hypotension. Neuropsychiatric adverse reactions include sedation, coma, seizures, and dystonic and extrapyramidal reactions. As there is no specific antidote for amisulpride overdosage, management includes cardiac monitoring and treatment of severe extrapyramidal symptoms. Drug elimination with the use of hemodialysis is effective.L32759 Severe extrapyramidal effects may be managed with anticholinergic drugs.L32764

Amisulpride

DB06288

small molecule approved investigational

Deskripsi

Amisulpride is a benzamide derivative and a dopamine receptor antagonist that selectively works on dopamine D2 and D3 receptors. As an antipsychotic agent, amisulpride alleviates both positive and negative symptoms of schizophrenia, and it exhibits antidepressant properties in patients with psychiatric disorders, dysthymia, and major depression.A6755 Amisulpride predominantly works in the limbic system, which explains its relatively lower risk of extrapyramidal adverse effects compared to other atypical antipsychotic agents.A6752, L32764 Oral tablets of amisulpride is used in European countries as a treatment for acute and chronic schizophrenic disorders, as well as secondary negative symptoms in mental health disorders such as affective disorders, depressive mood, and mental retardation.L32764

Amisulpride is also used as an antiemetic agent. In the US, the intravenous formulation of amisulpride is used to treat and prevent postoperative nausea and vomiting in adults, either as monotherapy or in combination with another antiemetic agent of a different drug class.L32759 It is marketed under the brand name Barhemsys.

Struktur Molekul 2D

Berat 369.479
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Elimination is biphasic.[A232269] The elimination half-life of amisulpride is approximately 12 hours after an oral dose.[L32764] The mean elimination half-life is approximately four to five hours in both healthy subjects and patients undergoing surgery receiving intravenous amisulpride.[L32759]
Volume Distribusi Following oral administration, the volume of distribution is 5.8 L/kg.[L32764] Following intravenous infusion, the mean volume of distribution of amisulpride is estimated to be 127 to 144 L in surgical patients and 171 L in healthy subjects.[L32759]
Klirens (Clearance) The plasma clearance of amisulpride is 20.6 L/h in surgical patients and 24.1 L/h in healthy subjects following intravenous administration. Renal clearance was estimated to be 20.5 L/hr (342 mL/min) in healthy subjects.[L32759]

Absorpsi

Following oral administration, amisulpride is rapidly absorbed with absolute bioavailability of 48%.A6751 Amisulpride has two absorption peaks, with one rapidly achieved within one hour post-dose and a second peak occurring between three to four hours post-dose. Following oral administration of a 50 mg dose, two peak plasma concentrations were 39 ± 3 and 54 ± 4 ng/mL.L32764 Following intravenous administration, the peak plasma concentration of amisulpride is achieved at the end of the infusion period and the plasma concentration decreases by 50% within approximately 15 minutes. The AUC(0-?) increases dose-proportionally in the dose range from 5 mg to 40 mg, which is about four times the maximum recommended dose. In healthy patients receiving intravenous amisulpride, the mean (SD) Cmax was 200 (139) ng/mL at the dose of 5 mg and 451 (230) ng/mL at the dose of 10 mg. The AUC ranged from 136 to 154 ng x h/mL in the dose range of 5 mg to 10 mg. In patients undergoing surgery, the mean (SD) Cmax ranged from 127 (62) to 161 (58) ng/mL at the dose of 5 mg. At the dose of 10 mg, it was 285 (446) ng/mL. The AUC ranged from 204 to 401 ng x h/mL.L32759

Metabolisme

Amisulpride undergoes minimal metabolism A6751 and its metabolites in plasma are largely undetectable. Two identified metabolites, formed by de-ethylation and oxidation, are pharmacologically inactive A232269 and account for approximately 4% of the dose.L32764 Metabolites remain largely uncharacterized. Metabolism of amisulpride does not involve cytochrome P450 enzymes.L32759

Rute Eliminasi

Following intravenous administration, about 74% of amisulpride is excreted in urine, where 58% of the recovered dose was excreted as unchanged amisulpride. About 23% of the dose is excreted in feces, with 20% of the excreted dose as unchanged parent drug. Following intravenous administration, about four metabolites were identified in urine and feces, accounting for less than 7% of the total dose administered.L32759 About 22 to 25% of orally administered amisulpride is excreted in urine, mostly as the unchanged parent drug.A6751

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Amisulpride may enhance the effects of alcohol.
  • 2. Take with or without food. A high fat meal does not significantly affect drug pharmacokinetics, although a carbohydrate rich meal decreases drug absorption and levels.

Interaksi Obat

1039 Data
Buprenorphine Amisulpride may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Amisulpride.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Amisulpride.
Hydrocodone Amisulpride may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Amisulpride can be increased when used in combination with Magnesium sulfate.
Metyrosine Amisulpride may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Amisulpride.
Mirtazapine Amisulpride may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Amisulpride.
Orphenadrine Amisulpride may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Amisulpride may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Amisulpride.
Rotigotine Amisulpride may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Amisulpride.
Sodium oxybate Amisulpride may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Amisulpride may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Amisulpride.
Thalidomide Amisulpride may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Amisulpride may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Reserpine Reserpine may increase the antipsychotic activities of Amisulpride.
Ziprasidone Ziprasidone may increase the antipsychotic activities of Amisulpride.
Olanzapine Olanzapine may increase the antipsychotic activities of Amisulpride.
Clozapine Clozapine may increase the antipsychotic activities of Amisulpride.
Thiethylperazine Thiethylperazine may increase the antipsychotic activities of Amisulpride.
Sulpiride Sulpiride may increase the antipsychotic activities of Amisulpride.
Loxapine Loxapine may increase the antipsychotic activities of Amisulpride.
Remoxipride Remoxipride may increase the antipsychotic activities of Amisulpride.
Promazine Promazine may increase the antipsychotic activities of Amisulpride.
Prochlorperazine Prochlorperazine may increase the antipsychotic activities of Amisulpride.
Chlorpromazine Chlorpromazine may increase the antipsychotic activities of Amisulpride.
Haloperidol Haloperidol may increase the antipsychotic activities of Amisulpride.
Triflupromazine Triflupromazine may increase the antipsychotic activities of Amisulpride.
Amoxapine Amoxapine may increase the antipsychotic activities of Amisulpride.
Fluphenazine Fluphenazine may increase the antipsychotic activities of Amisulpride.
Thioridazine Thioridazine may increase the antipsychotic activities of Amisulpride.
Moricizine Moricizine may increase the antipsychotic activities of Amisulpride.
Risperidone Risperidone may increase the antipsychotic activities of Amisulpride.
Trifluoperazine Trifluoperazine may increase the antipsychotic activities of Amisulpride.
Perphenazine Perphenazine may increase the antipsychotic activities of Amisulpride.
Flupentixol Flupentixol may increase the antipsychotic activities of Amisulpride.
Mesoridazine Mesoridazine may increase the antipsychotic activities of Amisulpride.
Acetophenazine Acetophenazine may increase the antipsychotic activities of Amisulpride.
Promethazine Promethazine may increase the antipsychotic activities of Amisulpride.
Pimozide Pimozide may increase the antipsychotic activities of Amisulpride.
Quetiapine Quetiapine may increase the antipsychotic activities of Amisulpride.
Aripiprazole Aripiprazole may increase the antipsychotic activities of Amisulpride.
Chlorprothixene Chlorprothixene may increase the antipsychotic activities of Amisulpride.
Alimemazine Alimemazine may increase the antipsychotic activities of Amisulpride.
Paliperidone Paliperidone may increase the antipsychotic activities of Amisulpride.
Lithium cation Lithium cation may increase the antipsychotic activities of Amisulpride.
Methotrimeprazine Methotrimeprazine may increase the antipsychotic activities of Amisulpride.
Periciazine Periciazine may increase the antipsychotic activities of Amisulpride.
Acepromazine Acepromazine may increase the antipsychotic activities of Amisulpride.
Aceprometazine Aceprometazine may increase the antipsychotic activities of Amisulpride.
Molindone Molindone may increase the antipsychotic activities of Amisulpride.
Pipotiazine Pipotiazine may increase the antipsychotic activities of Amisulpride.
Thioproperazine Thioproperazine may increase the antipsychotic activities of Amisulpride.
Thiothixene Thiothixene may increase the antipsychotic activities of Amisulpride.
Zuclopenthixol Zuclopenthixol may increase the antipsychotic activities of Amisulpride.
Fluspirilene Fluspirilene may increase the antipsychotic activities of Amisulpride.
Osanetant Osanetant may increase the antipsychotic activities of Amisulpride.
Bifeprunox Bifeprunox may increase the antipsychotic activities of Amisulpride.
Iloperidone Iloperidone may increase the antipsychotic activities of Amisulpride.
BL-1020 BL-1020 may increase the antipsychotic activities of Amisulpride.
Cariprazine Cariprazine may increase the antipsychotic activities of Amisulpride.
Lumateperone Lumateperone may increase the antipsychotic activities of Amisulpride.
Sertindole Sertindole may increase the antipsychotic activities of Amisulpride.
Asenapine Asenapine may increase the antipsychotic activities of Amisulpride.
Lurasidone Lurasidone may increase the antipsychotic activities of Amisulpride.
Perospirone Perospirone may increase the antipsychotic activities of Amisulpride.
Amperozide Amperozide may increase the antipsychotic activities of Amisulpride.
Cyamemazine Cyamemazine may increase the antipsychotic activities of Amisulpride.
Brexpiprazole Brexpiprazole may increase the antipsychotic activities of Amisulpride.
Blonanserin Blonanserin may increase the antipsychotic activities of Amisulpride.
Melperone Melperone may increase the antipsychotic activities of Amisulpride.
Zotepine Zotepine may increase the antipsychotic activities of Amisulpride.
Brilaroxazine Brilaroxazine may increase the antipsychotic activities of Amisulpride.
Methylene blue Methylene blue may increase the antipsychotic activities of Amisulpride.
Pipamperone Pipamperone may increase the antipsychotic activities of Amisulpride.
Azaperone Azaperone may increase the antipsychotic activities of Amisulpride.
Propiopromazine Propiopromazine may increase the antipsychotic activities of Amisulpride.
Tetrahydropalmatine Tetrahydropalmatine may increase the antipsychotic activities of Amisulpride.
Ecopipam Ecopipam may increase the antipsychotic activities of Amisulpride.
Bromperidol Bromperidol may increase the antipsychotic activities of Amisulpride.
Raclopride Raclopride may increase the antipsychotic activities of Amisulpride.
Ritanserin Ritanserin may increase the antipsychotic activities of Amisulpride.
Perazine Perazine may increase the antipsychotic activities of Amisulpride.
Benperidol Benperidol may increase the antipsychotic activities of Amisulpride.
Prothipendyl Prothipendyl may increase the antipsychotic activities of Amisulpride.
Tiapride Tiapride may increase the antipsychotic activities of Amisulpride.
Butaperazine Butaperazine may increase the antipsychotic activities of Amisulpride.
Clothiapine Clothiapine may increase the antipsychotic activities of Amisulpride.
Sultopride Sultopride may increase the antipsychotic activities of Amisulpride.
Chlorproethazine Chlorproethazine may increase the antipsychotic activities of Amisulpride.
Oxypertine Oxypertine may increase the antipsychotic activities of Amisulpride.
Thiazinam Thiazinam may increase the antipsychotic activities of Amisulpride.
Veralipride Veralipride may increase the antipsychotic activities of Amisulpride.
Trifluperidol Trifluperidol may increase the antipsychotic activities of Amisulpride.
Moperone Moperone may increase the antipsychotic activities of Amisulpride.
Thiopropazate Thiopropazate may increase the antipsychotic activities of Amisulpride.

Target Protein

5-hydroxytryptamine receptor 7 HTR7
5-hydroxytryptamine receptor 2A HTR2A
D(2) dopamine receptor DRD2
D(3) dopamine receptor DRD3
Mu-type opioid receptor OPRM1
Delta-type opioid receptor OPRD1
Kappa-type opioid receptor OPRK1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 12404702
    Rosenzweig P, Canal M, Patat A, Bergougnan L, Zieleniuk I, Bianchetti G: A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers. Hum Psychopharmacol. 2002 Jan;17(1):1-13.
  • PMID: 14642970
    Moller HJ: Amisulpride: limbic specificity and the mechanism of antipsychotic atypicality. Prog Neuropsychopharmacol Biol Psychiatry. 2003 Oct;27(7):1101-11.
  • PMID: 14575800
    Weizman T, Pick CG, Backer MM, Rigai T, Bloch M, Schreiber S: The antinociceptive effect of amisulpride in mice is mediated through opioid mechanisms. Eur J Pharmacol. 2003 Oct 8;478(2-3):155-9.
  • PMID: 11823257
    Leucht S, Pitschel-Walz G, Engel RR, Kissling W: Amisulpride, an unusual "atypical" antipsychotic: a meta-analysis of randomized controlled trials. Am J Psychiatry. 2002 Feb;159(2):180-90.
  • PMID: 21176108
    Rehni AK, Singh TG, Chand P: Amisulpride-induced seizurogenic effect: a potential role of opioid receptor-linked transduction systems. Basic Clin Pharmacol Toxicol. 2011 May;108(5):310-7. doi: 10.1111/j.1742-7843.2010.00655.x. Epub 2010 Dec 22.
  • PMID: 11735643
    Curran MP, Perry CM: Amisulpride: a review of its use in the management of schizophrenia. Drugs. 2001;61(14):2123-50. doi: 10.2165/00003495-200161140-00014.
  • PMID: 30725818
    MacDougall MR, Sharma S: Physiology, Chemoreceptor Trigger Zone .
  • PMID: 19337725
    Abbas AI, Hedlund PB, Huang XP, Tran TB, Meltzer HY, Roth BL: Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo. Psychopharmacology (Berl). 2009 Jul;205(1):119-28. doi: 10.1007/s00213-009-1521-8. Epub 2009 Apr 1.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 1 • International brands: 2
Produk
  • Barhemsys
    Injection, solution • 2.5 mg/1mL • Intravenous • US • Approved
International Brands
  • Deniban — Sanofi-Aventis
  • Solian — Sanofi-Aventis

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul