Substrate to Cyps 2D6 and 3A4 but probably insignificant hepatic exposure. In spite of a molecular structure with amine functions of possible Cyp TDI relevance, there is no conclusive evidence of irreversible Cyp inhibition in therapeutic use. No potentially porphyrogenic pharmacodynamic actions or side effects.

Indol neuroleptic: fluoropheny-indolpiperidine imdiazol derivative. Large pentacyclic molecule with three cyclic tertiary and one cyclic secondary amine functions. M=441. Therapeutic plasma concentrations are below 140 ng/ml (<320 nMol/l).

Schizophrenia. Peroral administration. Starting dose 4 mg/d , with 4-5 days intervals escalating to the ususal theraputic dose 10-20 mg/d, or the exceptional maximal dose 24 mg/d. Selective inhibitor of mesolimbic dopamine neurons through balanced inhibing effects on central dopamine D2 and serotonin 5HT2 receptors, as well as alpha1-adrenergic receptors. The serum prolactine increase observed with other antipsychotic drug is not seen. None conceivable physiological porphyrogenic effects.

Probably insignificant.

Metabolized ny Cyps 2D6 and 3A4. Multiple amine functions associated with irreversible Cyp-inhibition, but sertinol are not included in lists over Cyp-TDI drugs. Pharmacokinetic interactions are studied but no effects on Cyp-metabolism of other drugs stated. Clearence for sertinol decreases in repeated aministration to a mean of 14 l/h. Dependent on increased bioavaliability, accumualtion of sertinol therefore takes place out of proportion to dose in repeated administration , while in steady state plasma concentrations are proportional to dose.