Drug intelligence / Profile preview

paliperidone + carbamazepine

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intramuscular, Intravenous
01

Overview

Paliperidone + carbamazepine refers to the concomitant use of two pharmaceutical drugs, paliperidone and carbamazepine. Paliperidone is an atypical antipsychotic primarily used for the treatment of schizophrenia and schizoaffective disorders. It acts mainly as a dopamine D2 receptor antagonist and serotonin 5-HT2A receptor antagonist, modulating neurotransmission in the brain[5][6][8]. Carbamazepine is an anticonvulsant and mood stabilizer commonly used to treat epilepsy, bipolar disorder, and trigeminal neuralgia; it works by inhibiting voltage-gated sodium channels in neuronal membranes. When administered together, carbamazepine induces drug-metabolizing enzymes (notably CYP3A4) and drug transporters such as P-glycoprotein. This induction leads to a significant reduction in plasma concentrations of paliperidone—by up to 37%—which may decrease its therapeutic efficacy[1][2][3][4]. The interaction is dose-dependent with effects plateauing at higher doses of carbamazepine. Clinical studies have shown that this combination may require dose adjustments for optimal management.

02

Targets

DRD4 (Dopamine D4 Receptor)HTR2A (Serotonin receptor 5-HT2A)HRH1 (Histamine H1 Receptor)ADRA2A (α2A)SCN2A (Voltage-gated sodium channel protein type 2 subunit alpha)DRD2 (Dopamine D2 Receptor)HTR2C (5-hydroxytryptamine 2C receptor)DRD3 (Dopamine receptor D3)ADRA1A (α1A)

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