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|Systematic (IUPAC) name|
|Biological half-life||4-7 hours|
|CAS Registry Number|
|Molecular mass||371.27 g/mol|
|(what is this?)|
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a typical antipsychotic) which was previously used in Europe for the treatment of schizophrenia and acute mania but was withdrawn due to toxicity concerns (incidence of aplastic anemia in 1/10,000 patients). It was initially launched by AstraZeneca in 1990 and suspension of its use began in 1993. 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.
Due to its short half-life twice daily (bid) dosing is required, although a once-daily controlled-release tablet has been developed. There was some interest in its use in the treatment of treatment-resistant schizophrenia.
Specific dopamine D2-receptor antagonist.
Bromination of acid 1' followed by reaction of the product (2), as its acid chloride, with the (S)-(–)-aminomethylpyrrolidine, gives remoxipride with (S)-configuration.
- 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.
- 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.
- G. L. Florvall, S. O. Ogren, EP 4831 ; eidem, U.S. Patent 4,232,037 (1979, 1980 both to Astra).
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