Comparative Pharmacology of Risperidone and Paliperidone.
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Corena-McLeod M
Comparative Pharmacology of Risperidone and Paliperidone.
Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x.
- PubMed ID
- 25943458 [ View in PubMed]
- Abstract
Antipsychotics, risperidone, and risperidone's active metabolite, paliperidone (9-hydroxyrisperidone), are related molecules used for the treatment of schizophrenia and related disorders. Differences in receptor binding, 5-HT2A/D2 (serotonin/dopamine) binding ratios, and mitochondrial proteomics suggest that the effects of risperidone and paliperidone on neuronal firing, regulation of mitochondrial function, and movement are different. This review seeks to explore the most significant differences at the molecular level between risperidone and paliperidone, as reported in preclinical studies. Although risperidone shows higher affinity for 5-HT receptors, paliperidone does not fit this profile. Thus, the risperidone 5-HT2A/D2 binding ratio is significantly lower than the paliperidone 5-HT2A/D2 binding ratio. Paliperidone, similar to lithium and valproate, affects expression levels and phosphorylation of complex I and V proteins in synaptoneurosomal preparations of rat prefrontal cortex, suggesting that paliperidone behaves as a mood stabilizer. It is apparent that the presence of a hydroxyl group in the paliperidone molecule confers increased hydrophilicity to this drug compared with its parent, risperidone; thus, this contributes to differential effects on mitochondrial movement, protein expression, and phosphorylation. These differences are reflected in synaptic plasticity and neuronal firing and have only recently been implicated in the mechanisms of mitochondrial function and movement.
DrugBank Data that Cites this Article
- Drugs
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Risperidone 5-hydroxytryptamine receptor 2A Protein Humans YesAntagonistDetails Risperidone 5-hydroxytryptamine receptor 2C Protein Humans UnknownAntagonistDetails Risperidone 5-hydroxytryptamine receptor 7 Protein Humans UnknownAntagonistDetails Risperidone Alpha-1A adrenergic receptor Protein Humans UnknownAntagonistDetails Risperidone Alpha-1B adrenergic receptor Protein Humans UnknownAntagonistDetails Risperidone Alpha-2B adrenergic receptor Protein Humans UnknownAntagonistDetails Risperidone Alpha-2C adrenergic receptor Protein Humans UnknownAntagonistDetails Risperidone D(2L) dopamine receptor Protein Humans UnknownAntagonistDetails Risperidone Dopamine D2 receptor Protein Humans YesAntagonistDetails Risperidone Histamine H1 receptor Protein Humans UnknownAntagonistDetails - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwarePaliperidoneLevothyroxine The serum concentration of Paliperidone can be decreased when it is combined with Levothyroxine. PaliperidoneMifepristone The serum concentration of Paliperidone can be decreased when it is combined with Mifepristone. PaliperidoneRifampicin The serum concentration of Paliperidone can be decreased when it is combined with Rifampicin. PaliperidoneLorlatinib The serum concentration of Paliperidone can be decreased when it is combined with Lorlatinib. PaliperidoneLumacaftor The serum concentration of Paliperidone can be decreased when it is combined with Lumacaftor.