Search
paliperidone (9-hydroxyrisperidone, Invega, Invega Sustenna)
Indications:
- schizophrenia
- psychosis & agitation in the elderly [4]
Dosage:
- schizophrenia:
- start 6 mg PO QD [3]
- maintenance dose: 9 mg QD average [3]
- elderly: 1.5-12 mg PO [4]
Tabs: sustained release
Injection: Invega Sustenna once a month IM injection
Pharmacokinetics:
1) active metabolite, thus hepatic activation not needed
2) presumably conjugated for renal or biliary excretion
3) 1/2life of 24 hours
Dosage adjustment in renal failure:
- yes [4]
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 interactions:
1) see risperidone
2) less interaction with inhibitors & inducers of cyt P450 2D6 than risperidone
Mechanism of action:
1) active metabolite of risperidone
2) blocks dopamine D2 receptors, serotonin 5HT2A receptors, alpha-1 adrenergic receptors, alpha-2 adrenergic receptors, & histamine H1 receptors [2]
Interactions
drug interactions
drug adverse effects (more general classes)
monitor with atypical antipsychotic agents
General
atypical antipsychotic agent; second generation antipsychotic
dopaminergic receptor antagonist
serotonin antagonist
Database Correlations
PUBCHEM cid=115237
References
- Prescriber's Letter 14(2): 2007
Follow-on Drugs: Therapeutic benefit of economic burden?
Detail-Document#: 230201
(subscription needed) http://www.prescribersletter.com
- Prescriber's Letter 14(5): 2007
New Drug: Invega (Paliperidone Extended-release Tablets)
Detail-Document#: 230512
(subscription needed) http://www.prescribersletter.com
- 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
- Geriatric Review Syllabus, 8th edition (GRS8)
Durso SC and Sullivan GN (eds)
American Geriatrics Society, 2013