Paliperidone
Drug class: Atypical Antipsychotic
Paliperidone (INVEGA)（中文：帕利哌酮）
Common Strengths of Paliperidone Tablet
Paliperidone are available in the following strengths:
- 3 mg, 6 mg, 9 mg extended-release tablets
Drug Trade Names of Paliperidone Tablet
- Invega
- Invega Sustenna (injectable form)
Drug Usage
Treatment of schizophrenia in adults and adolescents (12 years and older)
Mechanism of Action
It is a centrally-acting dopamine D2 antagonist and serotonin 5-HT2A antagonist.
Route of Administration
- Oral (extended-release tablets)
- Intramuscular injection (long-acting injectable form)
Dosages
- Schizophrenia (adults): Initial dose 6 mg once daily, with a recommended dose range of 3 - 12 mg once daily
Renal dose based on eGFR:
- Mild renal impairment (eGFR 50 - 80 mL/min): 3 mg once daily
- Moderate to severe renal impairment (eGFR 10 - 50 mL/min): 1.5 once daily
Side Effects
| Frequency | Adverse reactions |
|---|---|
| Common | Insomnia |
| Headche | |
| Akathisia | |
| Dizziness | |
| Extrapyramidal symptoms | |
| Tachycardia | |
| Weight gain | |
| Uncommon | QT prolongation: This condition affect heart rhythm and can cause irregular heartbeats |
| Tardive dyskinesia: A movement disorder especially in older adults | |
| Neuroleptic Malignant Syndrome (NMS): is characterized by high fever, muscle stiffness, and confusion | |
| Hyperglycemia and diabetes: can raise blood sugar levels, posing a risk for diabetes | |
| Increased prolactin levels: can lead to unwanted breast milk prodction, missed periods, or difficulty becoming pregnant in females, and decreased sexual ability or enlarged breast in males | |
| Seizures: There is an increased risk of seizures, particularly at higher doses | |
| Orthostatic hypotension: Sudden drops in blood pressure when standing up, leading to dizziness and fainting | |
| Difficulty swallowing |
Pharmacokinetics
- Absorption: Well absorbed after oral adminstration
- Metabolism: Limited hepatic metabolism
- Elimination: Approximately 80% excreted unchanged in urine
- Onset of action may be seen within 4 - 8 days, with full effects typically observed within 4 - 6 weeks
Drug Precautions
Pregnancy
Use with caution
Breastfeeding
Not recommended; paliperidone is excreted in human milk
Children and Elderly
Not approved for use in children under 12; use with caution in elderly patients
Renal Impairment
Dose adjustment required (see item 6)
Monitoring Requirements
Due to the potential severity of these side effects, patients on paliperidone require regular monitoring, including:
- Cardiac monitoring to detect any changes in heart rhythm.
- Regular metabolic assessments to check for weight gain, blood sugar levels, and lipid profiles.
- Monitoring for signs of infection due to potential decreases in white blood cell counts.
Drug Interaction
May enhance the effects of other CNS depressants; caution with drugs that prolong QT interval such as citalopram, domperidone or azithromycin.
FAQ
How Should I Take the Tablet?
Take the tablet once daily in the morning, with or without food. Swallow the tablet whole; do not chew, divide, or crush.
What should I avoid while taking?
Avoid alcohol and activities requiring mental alertness until you know how paliperidone affect you.
What Happens if I Miss a Dose?
If you miss a dose, take it as soon as you remember. If it's almost time for your next dose, skip the missed dose and continue your regular dosing schedule. Do not take two doses at once.
