HALF-LIFE: Aripiprazole 74 hours; Active metabolite 94 hours
METABOLISM: Hepatic. Metabolized by CYP2D6 and CYP3A4
STARTING DOSE: 2mg-15mg daily
TARGET DOSING RANGE: 2mg-30mg PO daily
BEST TIME TO DOSE: Any
HOW TO DOSE:
Schizophrenia and Bipolar Mania: Initial 10mg-15mg PO daily. Max dose 30mg PO daily
Adjunct for depression: Initial 2mg-5mg PO daily. Increase dose by 5mg per day at intervals of >1 week. Max dose 15mg PO daily
Autism and Tourette’s disorder: Initial 2mg PO daily. Increase dose by 5mg/day at intervals of >1 week. Max dose 10mg-15mg PO daily
PREGNANCY: Minimal data on safety
BREASTFEEDING: Minimal data on safety
Akathisia (inner feeling of restlessness or urge to move), sedation, drowsiness, nausea, upset stomach, heartburn, diarrhea, tremors, muscle weakness, movement disorders, muscle cramping, restlessness, increased appetite, dry mouth, emotional “blunting,” seizures (very rare), lethargy, fatigue, headache, Neuroleptic Malignant Syndrome (Very rare), compulsive behaviors (such as compulsive gambling). Some of these side effects (e.g., nausea, jitteriness, restlessness, increased anxiety, upset stomach, headache, sedation, dry mouth, daytime fatigue) are common initially but typically go away after 5-7 days of consistently taking the medication as prescribed.
1) Schizophrenia, 13yo and older
2) Acute mania/mixed episodes, 10yo and older
3) Bipolar maintenance
4) Adjunct for Unipolar depression
5) Autism-related irritability, 6-17yo
6) Tourette’s disorder, 6-18yo
7) Acute agitation associated with schizophrenia or bipolar disorder (IM)
Off Label Uses: Bipolar Depression, Obsessive Compulsive Disorder, PTSD, Personality Disorders
Mechanism(s) of Action
Aripiprazole’s antipsychotic effects are hypothetically related to partial agonist actions at D2 receptor
Aripiprazole’s 5HT2A affinity is less than D2 affinity
Aripiprazole’s 5HT1A partial agonist actions are more potent than 5HT2A antagonist actions
Aripiprazole’s antidepressant effects are partially explained by 5HT1A partial agonism and 5HT7 antagonism
- Usually not sedating (lacks M1 and H1 antagonism)
- Minimal weight gain, rare dyslipidemia, rare insulin resistance (except in some children and adolescents)
- Minimal to no QTc prolongation
- Lower doses may be more activating than higher doses
- Long acting depot formulations available (Maintena (monthly injection), Aristada (injection every 2-3 months)
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