Paliperidone

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Paliperidone, sold under the brand name Invega among others, is an atypical antipsychotic.[13] It is used for the treatment of schizophrenia and schizoaffective disorder.[13][14] It is marketed by Janssen Pharmaceuticals.[9]

Paliperidone was approved by the US Food and Drug Administration (FDA) for the treatment of schizophrenia in December 2006,[9] and in the European Union in June 2007.[3] Paliperidone palmitate is a long-acting injectable formulation of paliperidone palmitoyl ester.[13][15] It is on the World Health Organization's List of Essential Medicines.[16] Paliperidone is available as a generic medication.[8]

Medical use

In the United States, paliperidone is indicated for the treatment of schizophrenia and for the treatment of schizoaffective disorder as monotherapy and as an adjunct to mood stabilizers and/or antidepressants.[9]

In the European Union, paliperidone is indicated for the treatment of schizophrenia in adults and in adolescents fifteen years of age and older and for the treatment of schizoaffective disorder in adults.[3]

Paliperidone is used for the treatment of schizophrenia and schizoaffective disorder.[14]

Adverse effects

The most common side effects include headache, insomnia, sleepiness, parkinsonism (effects similar to Parkinson's disease such as shaking, muscle stiffness and slow movement), dystonia (involuntary muscle contractions), tremor (shaking), dizziness, akathisia (restlessness), agitation, anxiety, depression, weight gain, nausea, vomiting, constipation, dyspepsia (heartburn), diarrhea, dry mouth, tiredness, toothache, muscle and bone pain, back pain, asthenia (weakness), tachycardia (increased heart rate), high blood pressure, prolonged QT interval (an alteration of the electrical activity of the heart), upper respiratory tract infection (nose and throat infections) and cough.[3]

A 2023 study found that paliperidone may worsen verbal learning and memory compared to placebo in the early months of psychosis treatment.[17]

Other symptoms may include restlessness, increased sweating, and trouble sleeping.[18] Less commonly there may be a feeling of the world spinning, numbness, or muscle pains.[18]

Pharmacology

Paliperidone is the primary active metabolite of the older antipsychotic risperidone.[19]Template:Unreliable medical source While its specific mechanism of action is unknown, it is believed paliperidone and risperidone act via similar, if not identical, pathways.[20] Its efficacy is believed to result from central dopaminergic and serotonergic antagonism except paliperidone, like its parent compound risperidone, functions as an inverse agonist at 5-HT2A 15. Paliperidone also acts as an antagonist of alpha-1 and alpha-2 adrenergic receptors as well as H1 histaminergic receptors.[19] Food is known to increase the absorption of Invega type ER OROS prolonged-release tablets. Food increased exposure of paliperidone by up to 50-60%; however, half-life was not significantly affected. The effect was probably due to a delay in the transit of the ER OROS formulation in the upper part of the GI tract, resulting in increased absorption.[21]

Risperidone and its metabolite paliperidone are reduced in efficacy by P-glycoprotein inducers such as St John's wort[22][23]

Template:Pharmacokinetics of long-acting injectable antipsychotics

Paliperidone[20]
Site Ki (nM)
5-HT1A 6.17
5-HT2A 1
5-HT2C 48
5-HT6 24
5-HT7 2.7
α1A 2.5
α2A 3.9
α2C 2.7
D1 41
D2 1.6
D3 3.5
D4 54[24]
D5 29
H1 19
H2 121
mACh >10,000

Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.

History

Paliperidone (as Invega) was approved by the US Food and Drug Administration (FDA) for the treatment of schizophrenia in 2006. Paliperidone was approved by the FDA for the treatment of schizoaffective disorder in 2009. The long-acting injectable form of paliperidone, marketed as Invega Sustenna in the US,[11] and Xeplion in the EU,[7] was approved by the FDA in July 2009.

It was initially approved in the European Union in 2007, for schizophrenia, the extended release form and use for schizoaffective disorder were approved in the EU in 2010, and extension to use in adolescents older than 15 years old was approved in 2014.[25]

Society and culture

Deaths

In April 2014, it was reported that 21 Japanese people who had received shots of the long-acting injectable paliperidone palmitate had died, out of 10,700 individuals prescribed the drug.[26][27][28][29][30][31][32]Template:Excessive citations inline

Brand names

In May 2015, a formulation of paliperidone palmitate was approved by the US Food and Drug Administration under the brand name Invega Trinza.[33][12] A similar prolonged release suspension was approved in 2016 by the European Medicines Agency originally under the brand name Paliperidone Janssen, later renamed to Trevicta.[34] In September 2021, a newer formulation of paliperidone palmitate, Invega Hafyera, was approved by the US FDA.[10]

References

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  8. ↑ a b Script error: No such module "citation/CS1".
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  33. ↑ Script error: No such module "citation/CS1".
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External links

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