Remoxipride

Remoxipride
Clinical data
Trade names Roxiam
Routes of
administration		 Oral
ATC code N05AL04 (WHO)
Legal status
Legal status
  • Withdrawn
Pharmacokinetic data
Bioavailability 96%[1]
Protein binding 89-98%
Metabolism Hepatic[1]
Biological half-life 4-7 hours[1]
Excretion Renal[1]
Identifiers
CAS Number 80125-14-0 N
PubChem (CID) 54477
DrugBank DB00409 YesY
ChemSpider 49195 YesY
UNII 0223RD59PE YesY
KEGG D02683 YesY
ChEMBL CHEMBL22242 YesY
Chemical and physical data
Formula C16H23BrN2O3
Molar mass 371.27 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

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a typical antipsychotic) which was previously used in Europe for the treatment of schizophrenia and acute mania but was withdrawn due to toxicity concerns (incidence of aplastic anemia in 1/10,000 patients).[2] It was initially launched by AstraZeneca in 1990 and suspension of its use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 2 3 4 Grind, M; Nilsson, MI; Nilsson, L; Oxenstierna, G; Sedvall, G; Wahlén, A (1989). "Remoxipride - a new potential antipsychotic compound: tolerability and pharmacokinetics after single oral and intravenous administration in healthy male volunteers". Psychopharmacology. 98 (3): 304–309. doi:10.1007/bf00451679. PMID 2568653.
  2. 1 2 José Miguel Vela; Helmut Buschmann; Jörg Holenz; Antonio Párraga; Antoni Torrens (2007). Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application. Weinheim: Wiley-VCH. ISBN 3-527-31058-4.
  3. ↑ Köhler C, Hall H, Magnusson O, Lewander T, Gustafsson K (1990). "Biochemical pharmacology of the atypical neuroleptic remoxipride". Acta Psychiatrica Scandinavica. Supplementum. 358: 27–36. PMID 1978484.
  4. ↑ Alexander, MS; Chakravarti, SK; Sundararajan, K; Mullin, JM; Shaw, SH; Blomqvist, M; Lockett, CM (January 1993). "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. doi:10.1177/026988119300700307. PMID 22290842.
  5. ↑ Conley, R; Dixon, L; An Nguyen, R; Taminga, C; Hain, R (April 1993). "Remoxipride therapy in treatment resistant schizophrenia". Schizophrenia Research. 9 (2-3): 235–236. doi:10.1016/0920-9964(93)90521-J.
  6. ↑ Conley, R; Dixon, L; An Nguyen, R; Taminga, C; Raymond, R (April 1993). "Remoxipride therapy in poorly responsive schizophrenics". Schizophrenia Research. 4 (3): 316. doi:10.1016/0920-9964(91)90208-9.


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