Sertindole
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Sertindole
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| Systematic (IUPAC) name | |
| 1-[2-[4-[5-chloro-1-(4-fluorophenyl)- indol-3-yl]-1-piperidyl]ethyl] imidazolidin-2-one |
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| Identifiers | |
| CAS number | |
| ATC code | N05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C24H26ClFN4O |
| Mol. mass | 440.941 |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | 3 days |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status |
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| Routes | ? |
Sertindole (brand names: Serdolect, and Serlect in Mexico) is one of the newer antipsychotic medications available. Serdolect is developed by the Danish pharmaceutical company H. Lundbeck. Like the other atypical antipsychotics, it has activity at dopamine and serotonin receptors in the brain. It is used in the treatment of schizophrenia. It is classified chemically as a phenylindole derivative. it is not currently available in Australia but will be released in 2007 or 2008.
Sertindole promises a restricted receptor and brain site activity. It mainly affects dopamine D2, serotonin 5-HT2 and α1-adrenergic receptors. The effect on D2 receptors is more pronounced in the limbic dopamine system compared with the nigrostriatal system. This is supported by findings from clinical trials that provide evidence for significantly fewer extra pyramidal side effects than haloperidol and risperidone.[citation needed] Weight gain is moderate, there is no diabetogenic effect, or effects on cholesterol and triglycerides, or prolactin reported.
In contrast to other antipsychotics, sertindole is not associated with sedative effects; sedation may add to the cognitive problems inherent in schizophrenia. Further to that, studies show that sertindole effectively normalizes laboratory induced cognitive impairment in animals, and that sertindole treatment has shown long lasting improvements in elementary cognitive processes in humans. This advantage may be linked to the high 5HT6a receptor affinity.[citation needed]
Sertindole was voluntarily withdrawn from the market late 1998 due to concerns over the risk of cardiac arrhythmia and sudden death, which may be caused by a QTc prolongation reported in some individuals.
However, large cohort analyses, as well as non-clinical evidence, has proven that all-cause mortality with sertindole is comparable with risperidone or olanzapine, and that the risk/benefit profile of sertindole did not motivate a permanent withdrawal from the market.[citation needed] These data also indicate that Serdolect treatment may be associated with lower suicidal rates than risperidone or olanzapine.[citation needed]
The suspension was lifted in 2002 for the Sertindole Cohort Prospective (SCoP) study. This large post-marketing obeservational study revealed no increase in overall or cardiac mortality.[citation needed]Based on an evaluation by the Committee for Human Medicinal Products (CHMP), the European Commission recommended lifting the marketing restrictions on sertindole in 2005 with a regulatory requirement of ECG monitoring.
The regulatory agencies in many countries have now implemented the approval of sertindole on a national level, and sertindole is available in more than 20 countries across the world.[citation needed]
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Clinical experience and data suggests high efficacy in the treatment of schizophrenia based on the unique pharmacodynamic profile. There’s potential superiority for effects on cognition because of the freedom of sedative effects, no need for anticholinergic control of side effects, and the high 5HT6a receptor affinity. In terms of economy, it compares well with risperidone and costs less than, for example, olanzapine.
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