paliperidone (9-hydroxyrisperidone, Invega, Invega Sustenna)
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Indications
Dosage
Tabs: sustained release
Injection: Invega Sustenna once a month IM injection
Dosage adjustment in renal failure
- yes[4]
Pharmacokinetics
- active metabolite, thus hepatic activation not needed
- presumably conjugated for renal or biliary excretion
- 1/2life of 24 hours
Adverse effects
- sedation, fatigue
- GI distress
- extrapyramidal symptoms
- black box warning[4]
- increased risk of hyperglycemia
- increased risk of cerebrovascular events
- increased risk of mortality in patients with dementia
- drug adverse effects of antipsychotic agents
- drug adverse effects of atypical antipsychotic agents
- drug adverse effects of psychotropic agents
- drug adverse effects of dopaminergic receptor antagonists
- drug adverse effects of antihypertensive agents
Drug interactions
- see risperidone
- less interaction with inhibitors & inducers of cyt P450 2D6 than risperidone
- drug interaction(s) of antipsychotics & dopamine receptor agonists
- drug interaction(s) of antipsycotics with benzodiazepines
- drug interaction(s) of NSAIDs & antihypertensives
Mechanism of action
- active metabolite of risperidone
- blocks dopamine D2 receptors, serotonin 5HT2A receptors, alpha-1 adrenergic receptors, alpha-2 adrenergic receptors, & histamine H1 receptors[2]
More general terms
- atypical antipsychotic agent; second generation antipsychotic
- dopaminergic receptor antagonist
- serotonin antagonist
References
- ↑ Prescriber's Letter 14(2): 2007 Follow-on Drugs: Therapeutic benefit of economic burden? Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230201&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 2.0 2.1 Prescriber's Letter 14(5): 2007 New Drug: Invega (Paliperidone Extended-release Tablets) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230512&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 3.0 3.1 3.2 Canuso CM et al. Randomized, double-blind, placebo-controlled study of paliperidone extended-release and quetiapine in inpatients with recently exacerbated schizophrenia. Am J Psychiatry 2009 May 1; [e-pub ahead of print] http://dx.doi.org/10.1176/appi.ajp.2009.08040613
- ↑ 4.0 4.1 4.2 4.3 4.4 Geriatric Review Syllabus, 8th edition (GRS8) Durso SC and Sullivan GN (eds) American Geriatrics Society, 2013