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Antipsychotic medication From Wikipedia, the free encyclopedia
Sertindole, sold under the brand name Serdolect among others, is an antipsychotic medication. Sertindole was developed by the Danish pharmaceutical company Lundbeck and marketed under license by Abbott Labs. Like 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.
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Trade names | Serdolect, Serlect |
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Routes of administration | By mouth |
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Pharmacokinetic data | |
Bioavailability | 75%[1] |
Protein binding | 99.5%[1] |
Metabolism | Liver (mostly via CYP2D6 and CYP3A4)[2][3] |
Elimination half-life | 3 days[2] |
Excretion | Faecal (the majority), Kidney (4% metabolites; 1% unchanged)[2] |
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ECHA InfoCard | 100.162.562 |
Chemical and physical data | |
Formula | C24H26ClFN4O |
Molar mass | 440.95 g·mol−1 |
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Sertindole is not approved for use in the United States and was discontinued in Australia in January 2014.[citation needed]
Sertindole appears effective as an antipsychotic in schizophrenia.[4] In a 2013 study in a comparison of 15 antipsychotic drugs in effectivity in treating schizophrenic symptoms, sertindole was found to be slightly less effective than haloperidol, quetiapine, and aripiprazole, as effective as ziprasidone, approximately as effective as chlorpromazine and asenapine, and slightly more effective than lurasidone and iloperidone.[5]
Very common (>10% incidence) adverse effects include:[2]
Common (1–10% incidence) adverse effects include:[2]
Uncommon (0.1–1% incidence) adverse effects include:[2]
Rare (<0.1% incidence) adverse effects include:[2]
Unknown frequency adverse events include:[2]
Biologic protein | Binding affinity (Ki[nM])[7] | Notes |
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5-HT1A | 280 | |
5-HT1B | 60 | |
5-HT1D | 96 | |
5-HT1E | 430 | |
5-HT1F | 360 | |
5-HT2A | 0.39 | The receptor believed to mediate the atypicality of atypical antipsychotics.[8] |
5-HT2C | 0.9 | Likely responsible for its propensity for causing weight gain.[8] |
5-HT6 | 5.4 | |
5-HT7 | 28 | |
α1A | 1.8 | Likely responsible for the orthostatic hypotension seen in patients on sertindole.[8] |
α2A | 640 | |
α2B | 450 | |
α2C | 450 | |
β1 | 5000 | |
β2 | 5000 | |
M1 | >10000 | [8] |
M3 | 2692 | |
D2 | 2.35 | Believed to be responsible for the drug's efficacy against positive symptoms.[8] |
D3 | 2.30 | |
D4 | 4.92 | |
hERG | 3 | Responsible for the QT interval prolongation and torsade de pointes |
H1 | 130 | |
NK1 | 1000 |
Sertindole is metabolized in the body to dehydrosertindole.[9]
Abbott Labs first applied for U.S. Food and Drug Administration (FDA) approval for sertindole in 1996,[10] but withdrew this application in 1998 following concerns over the increased risk of sudden death from QTc prolongation.[11] In a trial of 2000 patients on taking sertindole, 27 patients died unexpectedly, including 13 sudden deaths.[12] Lundbeck cites the results of the Sertindole Cohort Prospective (SCoP) study of 10,000 patients to support its claim that although sertindole does increase the QTc interval, this is not associated with increased rates of cardiac arrhythmias, and that patients on sertindole had the same overall mortality rate as those on risperidone.[13] Nevertheless, in April 2009 an FDA advisory panel voted 13-0 that sertindole was effective in the treatment of schizophrenia but 12-1 that it had not been shown to be acceptably safe.[14] As of October 2010[update], the drug has not been approved by the FDA for use in the USA.[15][failed verification]
In the European Union, sertindole was approved and marketed in 19 countries from 1996,[12] but its marketing authorization was suspended by the European Medicines Agency in 1998[16] and the drug was withdrawn from the market. In 2002, based on new data, the EMA's CHMP suggested that Sertindole could be reintroduced for restricted use in clinical trials, with strong safeguards including extensive contraindications and warnings for patients at risk of cardiac dysrhythmias, a recommended reduction in maximum dose from 24 mg to 20 mg in all but exceptional cases, and extensive ECG monitoring requirement before and during treatment.[17][18] As of September 2020[update], sertindole is authorized in several states of the European Union.[19]
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