Remoxipride

Remoxipride

Remoxipride
Systematic (IUPAC) name
(S)-3-bromo-N-[(1-ethylpyrrolidin-2-yl)methyl]-2,6-dimethoxy-benzamide
Clinical data
Trade names Roxiam
Legal status
  • Withdrawn
Routes of
administration
Oral
Pharmacokinetic data
Bioavailability 96%[1]
Protein binding 89-98%
Metabolism Hepatic[1]
Biological half-life 4-7 hours[1]
Excretion Renal[1]
Identifiers
CAS Registry Number  N
ATC code N05
PubChem CID:
DrugBank  YesY
ChemSpider  YesY
UNII  YesY
KEGG  YesY
ChEMBL  YesY
Chemical data
Formula C16H23BrN2O3
Molecular mass 371.27 g/mol
 N   

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a typical antipsychotic) which was previously used in Europe for the treatment of schizophrenia and acute mania but was withdrawn due to toxicity concerns (incidence of aplastic anemia in 1/10,000 patients).[2] It was initially launched by AstraZeneca in 1990 and suspension of its use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. ^ a b c d
  2. ^ a b
  3. ^
  4. ^
  5. ^
  6. ^

External links

  • Herbert Y. Meltzer, Atypical Antipsychotic Drugs, 2000