Remoxipride
- N05AL04 (WHO)
- Withdrawn
- 3-bromo-N-[[(2S)-1-ethylpyrrolidin-2-yl]methyl]-2,6-dimethoxybenzamide
- 80125-14-0 N
- 54477
- DB00409 Y
- 49195 Y
- 0223RD59PE
- D02683 Y
- ChEMBL22242 Y
- DTXSID6045668
- Interactive image
- CCN2CCC[C@H]2CNC(=O)c1c(OC)ccc(Br)c1OC
- InChI=1S/C16H23BrN2O3/c1-4-19-9-5-6-11(19)10-18-16(20)14-13(21-2)8-7-12(17)15(14)22-3/h7-8,11H,4-6,9-10H2,1-3H3,(H,18,20)/t11-/m0/s1 Y
- Key:GUJRSXAPGDDABA-NSHDSACASA-N Y
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a typical antipsychotic) which was previously used in Europe for the treatment of schizophrenia and acute mania but was withdrawn due to toxicity concerns (incidence of aplastic anemia in 1/10,000 patients).[2] It was initially launched by AstraZeneca in 1990 and suspension of its use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
- ^ a b c d 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): 304–9. doi:10.1007/bf00451679. PMID 2568653. S2CID 27357548.
- ^ a b Vela JM, Buschmann H, Holenz J, Párraga A, Torrens A (2007). Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application. Weinheim: Wiley-VCH. ISBN 978-3-527-31058-6.
- ^ 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. doi:10.1111/j.1600-0447.1990.tb05282.x. PMID 1978484. S2CID 144567193.
- ^ 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. S2CID 23518319.
- ^ Conley R, Dixon L, Nguyen JA, Tamminga C, Raymond R (April 1993). "Remoxipride therapy in treatment resistant schizophrenia". Schizophrenia Research. 9 (2–3): 235–236. doi:10.1016/0920-9964(93)90521-J. S2CID 54386181.
- ^ Conley R, Dixon L, Nguyen JA, Tamminga C, Raymond R (April 1993). "Remoxipride therapy in poorly responsive schizophrenics". Schizophrenia Research. 4 (3): 316. doi:10.1016/0920-9964(91)90208-9. S2CID 54317014.
External links
- Herbert Y. Meltzer, Atypical Antipsychotic Drugs, 2000 Archived 2006-04-26 at the Wayback Machine
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