Remoxipride
 | |
| Systematic (IUPAC) name | |
|---|---|
|
3-bromo-N-[[(2S)-1-ethylpyrrolidin-2-yl]methyl]-2,6-dimethoxybenzamide | |
| Clinical data | |
| Trade names | Roxiam |
| Legal status |
|
| 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 Number |
117591-79-4  |
| ATC code | N05AL04 |
| PubChem | CID 54477 |
| DrugBank |
DB00409  |
| ChemSpider |
49195 |
| UNII |
0223RD59PE |
| KEGG |
D02683 |
| ChEMBL |
CHEMBL22242 |
| Chemical data | |
| Formula | C16H23BrN2O3 |
| Molar mass | 371.27 g/mol |
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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a typical antipsychotic) which was previously used in Europe for the treatment of schizophrenia and acute mania but was withdrawn due to toxicity concerns (incidence of aplastic anemia in 1/10,000 patients).[2] It was initially launched by AstraZeneca in 1990 and suspension of its use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 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.
- 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
External links
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