Bookmark
Forward
QuickView for Paliperidone (compound)
DrugBank
Identification
| Name: | paliperidone |
|---|---|
| Name (isomeric): | DB01267 |
| Drug Type: | small molecule |
| Synonyms: |
9-Hydroxyrisperidone
|
| Brand: | Invega |
| Category: | Antipsychotic Agents |
| CAS number: | 144598-75-4 |
Pharmacology
| Indication: | For the treatment of schizophrenia. |
|---|---|
| Pharmacology: | Paliperidone is an atypical antipsychotic developed by Janssen Pharmaceutica. Chemically, paliperidone is primary active metabolite of the older antipsychotic risperidone (paliperidone is 9-hydroxyrisperidone). While its specific mechanism of action is unknown, it is believed paliperidone and risperidone act via similar, if not the same, pathways. |
| Mechanism of Action: |
Paliperidone is the major active metabolite of risperidone. The mechanism of action of paliperidone, as with other drugs having efficacy in schizophrenia, is unknown, but it has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor ...
show more » |
| Absorption: | The absolute oral bioavailability of paliperidone following paliperidone administration is 28%. |
| Protein binding: | The plasma protein binding of racemic paliperidone is 74%. |
| Biotransformation: | Although in vitro studies suggested a role for CYP2D6 and CYP3A4 in the metabolism of paliperidone, in vivo results indicate that these isozymes play a limited role in the overall elimination of paliperidone. Four primary metabolic pathways have been identified in vivo, none of which could be shown to account for more than 10% of the dose: dealkylation, hydroxylation, dehydrogenation, and benzisoxazole scission. Paliperidone does not undergo extensive metabolism and a significant portion of its metabolism occurs in the kidneys. |
| Route of elimination: | One week following administration of a single oral dose of 1 mg immediate-release 14C-paliperidone to 5 healthy volunteers, 59% (range 51% – 67%) of the dose was excreted unchanged into urine, 32% (26% – 41%) of the dose was recovered as metabolites, and 6% – 12% of the dose was not recovered. |
| Half Life: | The terminal elimination half-life of paliperidone is approximately 23 hours. |
| Toxicity: | The possibility of obtundation, seizures, or dystonic reaction of the head and neck following overdose may create a risk of aspiration with induced emesis. |
| Affected organisms: | Humans and other mammals |
Interactions
| Food interaction: |
| ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Drug interaction: |
|
Targets
