Products
Sertindole is commercially available in the form of film-coated tablets (Serdolect). It has been approved in many countries since 1997.
Structure and properties
Sertindole (C24H26ClFN4O, Mr = 440.9 g/mol) was developed as the first neuroleptic with a phenylindole structure.
Effects
Sertindole (ATC N05AE03) has antipsychotic properties. The effects are due to antagonism at dopamine D2 receptors, serotonin 5HT2 receptors, and α1-adrenoceptors. Sertindole is not anticholinergic, not depressant, and not antihistamine. The substance has a long half-life of two to four days.
Indications
As a second-line agent for the treatment of schizophrenia.
Dosage
According to the prescribing information. Tablets are usually taken once daily, independent of meals. Treatment is started gradually.
Contraindications
- Hypersensitivity
- Untreated hypokalemia or hypomagnesemia.
- Severe hepatic insufficiency
- Certain cardiovascular diseases
- Congenital or acquired QT prolongation.
- Combination with drugs that prolong the QT interval.
- Combination with CYP3A4 inhibitors.
Full precautions can be found in the drug label.
Interactions
Sertindole is metabolized by CYP2D6 and CYP3A, and corresponding drug interactions with CYP inhibitors or inducers are possible. Additional interactions may occur with agents that prolong the QT interval.
Adverse effects
The most common potential adverse effects include rhinitis, dizziness, dry mouth, decreased ejaculatory volume, weight gain, orthostatic hypotension, and joint pain. Sertindole may prolong the QT interval and cause cardiac arrhythmias. It is controversial because of the potential cardiovascular side effects. Sertindole is one of the atypical neuroleptics and therefore has profound potential for extrapyramidal disorders.