Chemistry:Remoxipride

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Short description: Antipsychotic medication
Remoxipride
Remoxipride.svg
Clinical data
Trade namesRoxiam
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • Withdrawn
Pharmacokinetic data
Bioavailability96%[1]
Protein binding89-98%
MetabolismHepatic[1]
Elimination half-life4-7 hours[1]
ExcretionRenal[1]
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC16H23BrN2O3
Molar mass371.275 g·mol−1
3D model (JSmol)
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Remoxipride (Roxiam) is an atypical antipsychotic (although according to some sources it is a typical antipsychotic) which was previously used in Europe for the treatment of schizophrenia and acute mania but was withdrawn due to toxicity concerns (incidence of aplastic anemia in 1/10,000 patients).[2] It was initially launched by AstraZeneca in 1990 and suspension of its use began in 1993.[2] Remoxipride acts as a selective D2 and D3 receptor antagonist and also has high affinity for the sigma receptor, possibly playing a role in its atypical neuroleptic action.[3]

Due to its short half-life twice daily (bid) dosing is required, although a once-daily controlled-release tablet has been developed.[4] There was some interest in its use in the treatment of treatment-resistant schizophrenia.[5][6]

See also

References

  1. 1.0 1.1 1.2 1.3 "Remoxipride--a new potential antipsychotic compound. Tolerability and pharmacokinetics after single oral and intravenous administration in healthy male volunteers". Psychopharmacology 98 (3): 304–9. 1989. doi:10.1007/bf00451679. PMID 2568653. 
  2. 2.0 2.1 Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application. Weinheim: Wiley-VCH. 2007. ISBN 978-3-527-31058-6. 
  3. "Biochemical pharmacology of the atypical neuroleptic remoxipride". Acta Psychiatrica Scandinavica. Supplementum 358: 27–36. 1990. doi:10.1111/j.1600-0447.1990.tb05282.x. PMID 1978484. 
  4. "Once-daily controlled release remoxipride is equieffective with twice-daily immediate release remoxipride in the treatment of schizophrenia". Journal of Psychopharmacology 7 (3): 276–82. January 1993. doi:10.1177/026988119300700307. PMID 22290842. 
  5. "Remoxipride therapy in treatment resistant schizophrenia". Schizophrenia Research 9 (2–3): 235–236. April 1993. doi:10.1016/0920-9964(93)90521-J. 
  6. "Remoxipride therapy in poorly responsive schizophrenics". Schizophrenia Research 4 (3): 316. April 1993. doi:10.1016/0920-9964(91)90208-9. 

External links