The Sound of Evolution
Paliperidone
Mechanism of action:
Paliperidone has a multi-receptor antagonistic pharmacologic profile. Paliperidone antagonizes dopamine D2 receptors in the mesolimbic pathway, suppressing excessive dopamine activity. At the same time, it also inhibits D2 receptors in the nigrostriatal pathway, which can cause extrapyramidal symptoms (EPS). In addition, paliperidone antagonizes serotonin 5-HT2A receptors, reducing the inhibitory effect of 5-HT2A receptors on dopamine and lowering the risk of extrapyramidal symptoms. Paliperidone also has partial antagonistic effects on alpha1-, alpha2-adrenergic receptors and H1 histamine receptors, producing adverse effects associated with these receptors.
Reference(s):
1. Jones MP et al. (2010). Efficacy and tolerability of paliperidone ER and other oral atypical antipsychotics in schizophrenia. Int J Clin Pharmacol Ther.
2. Urichuk L et al. (2008). Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab.