Which of the two initial intramuscular injections of Invega Sustenna (paliperidone palmitate) given a week apart is considered the loading dose?

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Which Initial Invega Sustenna Dose is the Loading Dose?

Both initial doses function together as a loading regimen, but the Day 1 dose of 234 mg (150 mg eq) administered in the deltoid is specifically designed as the primary loading dose to rapidly achieve therapeutic concentrations. 1, 2

Understanding the Two-Dose Initiation Regimen

The recommended initiation protocol for Invega Sustenna consists of:

  • Day 1: 234 mg (150 mg eq) deltoid injection - This is the loading dose that initiates rapid therapeutic blood levels 1, 2
  • Day 8: 156 mg (100 mg eq) deltoid injection - This is the second initiation dose that maintains and continues the therapeutic effect 1, 2

Why Day 1 is Considered the Loading Dose

The 234 mg Day 1 injection achieves significantly greater symptom improvement compared to placebo by Day 8, demonstrating its role as the primary loading dose. 3 This design allows therapeutic concentrations to be reached rapidly without requiring oral antipsychotic supplementation, which distinguishes it from other long-acting injectable formulations. 1, 4

The pharmacokinetic profile shows that:

  • Release begins as early as Day 1 following the initial injection 2
  • Maximum plasma concentrations are reached at approximately 13 days 2
  • The onset of clinical response occurs by Day 8 in patients receiving the 234 mg initial dose 4

Clinical Significance of Both Doses

While Day 1 serves as the loading dose, both injections must be administered in the deltoid muscle during initiation because deltoid injection produces approximately 28% higher maximum concentrations compared to gluteal injection. 2 This is critical for achieving rapid therapeutic levels.

After the Day 8 injection of 156 mg, continued symptom improvement is observed at Day 22 and Day 36, with evidence of a dose-dependent response trend. 3 This demonstrates that the Day 8 dose is essential for maintaining the therapeutic effect initiated by the loading dose.

Common Pitfall to Avoid

Do not administer either initiation dose in the gluteal muscle - both Day 1 and Day 8 injections must be given deltoid to ensure proper therapeutic concentrations are achieved rapidly. 2 Subsequent monthly maintenance doses (starting Day 36 onward) can be administered in either deltoid or gluteal sites. 1, 4

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Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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