Products
Paliperidone is commercially available as sustained-release tablets (Invega, generic) and as a sustained-release suspension for intramuscular injection (Xeplion, Trevicta, generic). It has been approved in many countries since 2008.
Structure and properties
Paliperidone (C23H27FN4O3, Mr = 426.5 g/mol) exists as a racemate and is practically insoluble in water. It belongs to the group of benzisoxazoles. Paliperidone corresponds to 9-hydroxyrisperidone, the active metabolite of risperidone (Risperdal) and differs from the parent compound only in one hydroxyl group. In the retard suspension, it is present as paliperidone palmitate.
Effects
Paliperidone (ATC N05AX13) has antipsychotic properties. The effects are due to antagonism at dopamine D2 receptors and serotonin 5HT2A receptors. Unlike risperidone, paliperidone does not require activation by CYP2D6 and therefore has a lower potential for drug-drug interactions and interindividual differences in metabolism.
Indications
For the treatment of schizophrenia.
Dosage
According to the professional information. Tablets are taken once daily and always at the same time of day, regardless of meals.
Contraindications
- Hypersensitivity (including to risperidone).
- Parkinson’s disease
- Lewy body dementia
Full details of precautions and interactions can be found in the drug label.
Adverse effects
The most common possible adverse effects include headache, motor agitation, drowsiness, fatigue, dullness, dizziness, extrapyramidal disorders, rapid pulse, agitation, constipation, nausea, tremor, dyspepsia, vomiting, dry mouth, low blood pressure, and weight gain.
