Paliperidone

Antipsychotic Drug

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.