Aliwei Aripiprazole Microspheres for Injection

1. Indications and Usage
Schizophrenia:
Treatment of schizophrenia in adults.
Note: This medication is indicated for patients who have been stabilized on oral aripiprazole or another antipsychotic medication.
2. Dosage and Administration
Route of Administration:
For Intramuscular (IM) Injection ONLY.
Administered by a healthcare professional into the deltoid or gluteal muscle.
Recommended Dosage:
Dosing Options: Available in doses administered every 4 weeks, every 6 weeks, or every 8 weeks (e.g., 441 mg/4 weeks, 662 mg/4 weeks, 882 mg/4 weeks, 1064 mg/6 weeks, 1324 mg/8 weeks).
Critical Administration Instructions (Loading Dose):
Initial Treatment: A loading dose injection (deltoid) is required immediately after the first injection to achieve therapeutic levels rapidly.
Oral Supplementation: Oral aripiprazole supplementation (e.g., 10–20 mg/day) is required for 14 days following the initiation of therapy to cover the gap until steady-state is reached.
Missed Dose: Protocol varies significantly based on the time elapsed since the last dose (ranging from 4 days to 8 weeks); strictly follow the prescribing guide for missed doses to prevent relapse.
3. Mechanism of Action
Receptor Profile:
Aripiprazole is an atypical antipsychotic with high affinity for dopamine D2 and serotonin 5-HT1A receptors, and moderate affinity for 5-HT2A receptors.
Partial Agonist Activity:
Acts as a partial agonist at D2 and 5-HT1A receptors.
Acts as an antagonist at 5-HT2A receptors.
Microsphere Technology:
The drug is formulated in biodegradable polymer microspheres. Upon IM injection, the polymer slowly degrades, releasing arripiprazole gradually into the systemic circulation over weeks, maintaining stable plasma concentrations.
4. Safety and Warnings
Increased Mortality in Elderly with Dementia (Boxed Warning):
Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death.
Suicidal Thoughts and Behaviors:
Monitor for the emergence of suicidal ideation and behavior.
Injection Site Reactions:
Pain, erythema, and induration at the injection site may occur.
Metabolic Changes:
Hyperglycemia, weight gain, and dyslipidemia may occur; monitor metabolic parameters regularly.
Neuroleptic Malignant Syndrome (NMS):
Monitor for NMS, a potentially fatal reaction.
Tardive Dyskinesia:
Risk of developing abnormal involuntary movements.
5.Adverse Reactions
Most Common:
Injection site pain, headache, akathisia (inner restlessness), insomnia, and anxiety.
6.Drug Interactions
CYP3A4 and CYP2D6 Substrate:
Aripiprazole is metabolized by CYP3A4 and CYP2D6 enzymes.
Strong CYP3A4 Inhibitors:
Dose reduction is required (e.g., ketoconazole, itraconazole).
Strong CYP2D6 Inhibitors:
Dose reduction is required (e.g., quinidine, fluoxetine).
CYP3A4 Inducers:
Dose increase is required (e.g., carbamazepine, rifampin).
7.Pharmaceutical Information
Chemical Composition:
Active Ingredient: Aripiprazole.
Excipients: Poly(lactic-co-glycolic acid) (PLGA) – biodegradable polymer.
Appearance: Sterile, lyophilized (freeze-dried) powder in a vial; must be reconstituted with the provided solvent (NMP-based) prior to injection.
Storage: Store at 25°C (77°F); excursions permitted to 15–30°C (59–86°F).