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Remoxipride
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| Clinical data | |
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| Trade names | Roxiam |
| Routes of administration | Oral |
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| Pharmacokinetic data | |
| Bioavailability | 96%[1] |
| Protein binding | 89-98% |
| Metabolism | Hepatic[1] |
| Elimination half-life | 4-7 hours[1] |
| Excretion | Renal[1] |
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| Chemical and physical data | |
| Formula | C16H23BrN2O3 |
| Molar mass | 371.275 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a typical antipsychotic) which was previously used in Europe for the treatment of schizophrenia and acute mania but was withdrawn due to toxicity concerns (incidence of aplastic anemia in 1/10,000 patients).[2] It was initially launched by AstraZeneca in 1990 and suspension of its use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]
- ^ 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.
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