Paliperidone is an antipsychotic medication. It works by changing the effects of chemicals in the brain. Paliperidone was approved by the FDA for the treatment of schizophrenia in 2006. It is marketed for the treatment of schizophrenia and bipolar mania.
Abstract
Paliperidone is an antipsychotic medication. It works by changing the effects of chemicals in the brain.
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Brand Names
Invega
Invega Sustenna
Xeplion (Europe)
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Manufacturers
JANSSEN PHARMA
QUALITY CARE
[1]
History
Paliperidone was approved by the FDA for the treatment of schizophrenia in 2006. It is marketed for the treatment of schizophrenia and bipolar mania. Recently, the long-acting injectable form of paliperidone, marketed as INVEGA Sustenna in U.S. and Xeplion in Europe, was approved by the FDA on July 31, 2009. It was approved in Europe in 2011 for schizophrenia. In Europe the monthly (every 28 days) injection comes in 50 mg, 75 mg, 100 mg, and 150 mg of paliperidone without the 25 mg injection that is available in the U.S.
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Uses
Paliperidone is used to treat schizophrenia.
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Pharmacology
Paliperidone is the primary active metabolite of the older antipsychotic risperidone. While its specific mechanism of action is unknown, it is believed paliperidone and risperidone act via similar, if not identical, pathways.
Paliperidone has antagonist effect at α1 and α2 adrenergic receptors and at H1 histamine receptors.It does not bind to muscarinic acetylcholine receptors. In addition it binds with dopamine and serotonin receptors.
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Schedule
It is not a controlled substance in the US.
Dosage
The dosage depends on the reason why it is prescribed for an individual. In general,
Oral:
6 mg PO qAM; may titrate up or down, not to exceed 12 mg/day
Titrate by dose increment of 3 mg/day at intervals of at least 5 days
IM:
Initial: 234 mg IM in deltoid muscle on treatment day 1, THEN 156 mg 1 week later
Maintenance: 117 mg IM qMonth, some patients may require lower or higher doses (dose range 39-234 mg/month)
Adolesents: 3 mg PO qDay initially; may increase dose if needed, not to exceed 12 mg/day
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Drug Interactions
Contraindicated interactions with:
None
Serious interactions with:
amiodarone
apomorphine
arsenic trioxide
astemizole
bepridil
bromocriptine
cabergoline
cisapride
ibutilide
indapamide
levodopa
lisuride
methyldopa
ondansetron
sodium oxybate
sotalol
terfenadine
vandetanib
vemurafenib
Significant interactions with:
abobotulinumtoxina
acarbose
aclidinium
albuterol
butalbital
butorphanol
caffeine
carbamazepine
desipramine
dexchlorpheniramine
dexfenfluramine
dexmedetomidine
melatonin
mepenzolate
meperidine
mephentermine
mephenytoin
yohimbine
ziconotide
ziprasidone
zotepine
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Adverse Effects
Akathisia
Somnolence
Tachycardia
Hyperprolactinemia
Dystonia
Extrapyramidal symptoms
Orthostatic hypotension
QT prolongation
Sialorrhea
Priapism
Weight gain
Constipation
Indigestion
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Contraindications
Documented hypersensitivity to paliperidone or risperidone
Any condition or drugs that prolong QT interval
Severe preexisting GI stenosis
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Cautions
Avoid overheating and dehydration
History of seizures
Hyperprolactinemia occurs and persists during chronic administration
Prolongs QT interval modestly
Potential risk of neuroleptic malignant syndrome
Risk of orthostatic hypotension
FDA Warning regarding off-label use for dementia in elderly
Discontinue drug at first sign of a clinically significant decline <1000/mm³ in WBC in absence of other causative factors and continue monitoring WBC until recovery)
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Pricing
The pricing varies depending on what form one would like to buy, and the brand.
The 3mg tablet is priced in between $26.51 to $28.86. The prices for 6mg tablet vary from $28.86 to $52.35. No pricing information is available for 1.5mg and 9mg tablet.
[1]
Referenecs
[1] http://reference.medscape.com/drug/invega-sustenna-paliperidone-342992#90
[2] http://www.drugs.com/mtm/paliperidone.html
[3] http://www.invegasustenna.com/
[4] http://www.drugbank.ca/drugs/DB01267
[5] http://reference.medscape.com/drug/invega-sustenna-paliperidone-342992#0
[6] http://reference.medscape.com/drug/invega-sustenna-paliperidone-342992#3
[7] http://reference.medscape.com/drug/zyprexa-relprevv-olanzapine-342979#4
[8] http://reference.medscape.com/drug/zyprexa-relprevv-olanzapine-342979#5
