Paliperidone

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Invega; Belgium: Invega; Bulgaria: Invega; Cyprus: Invega; Czech Republic: Invega; Denmark: Invega; Estonia: Invega; Finland: Invega; France: Invega; Germany: Invega; Greece: Invega; Hungary: Invega; Ireland: Invega; Italy: Invega; Latvia: Invega; Lithuania: Invega; Malta: Invega; Netherlands: Invega; Poland: Invega; Portugal: Invega; Romania: Invega; Slovakia: Invega; Slovenia: Invega; Spain: Invega; Sweden: Invega; UK: Invega.

North America

Canada: Invega; USA: Invega.

Latin America

Argentina: Invega; Mexico: Invega.

Asia

Japan: Invega.

Drug combinations

Chemistry

Paliperidone: C~23~H~27~FNH~4~O~3~. Mw: 388.50. (1) 4H-Pyrido[1,2-a]pyrimidin-4-one, 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-; (2)(9RS)-3-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one. CAS-144598-75-4 (2004).

Pharmacologic Category

Atypical Antipsychotics. (ATC-Code: N05AX13).

Mechanism of action

Therapeutic efficacy of paliperidone believed to result from mixed central serotonergic and dopaminergic antagonism. Demonstrates high affinity to α~1~, D~2~, H~1~, and 5-HT~2C~ receptors, and low affinity for muscarinic and 5-HT~1A~ receptors.

Therapeutic use

Treatment of schizophrenia.

Pregnancy and lactiation implications

Animal studies indicate increase in fetal mortality. There are no adequate, well-controlled studies in pregnant women. Enters breast milk (use caution).

Unlabeled use

Psychosis/agitation related to Alzheimer’s dementia.

Contraindications

Hypersensitivity to paliperidone, risperidone, or any component of the formulation.

Warnings and precautions

May alter cardiac conduction and prolong QTc interval (avoid use in combination with QTc-prolonging drugs, in congenital long-QT syndrome and in history of cardiac arrhythmia). Antipsychotic use associated with esophageal dysmotility and aspiration (use with caution in risk of pneumonia, and in patients unable to swallow tablet whole). May cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia. Risk of tardive dyskinesia may be increased in the elderly, particularly women. Risk of dystonia may be greater with increased doses, use of conventional antipsychotics, males, and younger patients. Atypical antipsychotics associated with development of hyperglycemia (use with caution in diabetes (or risk factors) or other disorders of glucose regulation). Use may be associated with neuroleptic malignant syndrome (risk may be increased in Parkinson’s disease or Lewy body dementia). May cause orthostatic hypotension (use with caution in cerebrovascular disease, cardiovascular disease, hypovolemia, or concurrent medication use which may predispose to hypotension/bradycardia). May be low-to-moderately sedating. Possibility of suicide attempt inherent in psychotic illness or bipolar disorder. Impaired core body temperature regulation may occur. Significant weight gain observed with antipsychotic therapy. Elderly patients with dementia-related psychosis treated with atypical antipsychotics are at increased risk of death compared to placebo. Not approved for treatment of dementia-related psychosis. Use not recommended in pre-existing severe gastrointestinal narrowing disorders. Use with caution in Parkinson’s disease, in breast cancer or other prolactin-dependent tumors (elevates prolactin levels), in renal disease, and in risk of seizures (the elderly may be at increased risk of seizures). May mask toxicity of other drugs or conditions (e.g. intestinal obstruction, Reye’s syndrome, brain tumor) due to antiemetic effects.

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