4. FDA APPROVED INDICATIONS :
Schizophrenia (age 13 and above)
Maintaining stability in schizophrenia
Acute mania/mixed mania ( age 10 and above)
Bipolar maintainance ( mono therapy and adjunct)
Depression(adjunct)
Autism-related irritability in children ages 6 to 18
Acute agitation associated with schizophrenia or bipolar disorder
Tourette‘s disorder ( age 6 to 18 )
5. Side Effects:
Weight Gain.
Postural Hypotension
Extrapyramidal Symptoms
Tardive dyskinesia on long-term administration
Lightheadedness and drowsiness ,dizziness.
Constipation
Headache ,asthenia,sedation.
Hyperglycemia and sometimes diabetes.
Increased risk of hyperlipidemia.
6. Cautions:
Hepatic Impairment because Aripiprazole is metabolized by hepatic
enzymes (CYP3A4 and CYP2D6).
Elderly patients with dementia related psychosis.
Pregnancy because Aripiprazole is Category C.
Patients with cardiovascular Disease.
Patients predisposed to hypotension.
7. Contraindications
Hypersensitivity to Aripiprazole has been documented. Therefore avoid in
patients with hypersensitivity.
Operating Heavy Machinery and work that requires skill (eg. driving)
probably because Aripiprazole causes sedation.
In breast-feeding. Aripiprazole is secreted in breast milk.
8. Pharmacokinetics
Plasma Half- life: Parent Drug, 75 hr.; metabolite, 94 hr.
Plasma Peak Time: 3-5 hours.
Protein Bound: 99%.
Absorption: Oral (3-5 hr.); IM (1-3 hr.).
Metabolism: Aripiprazole is metabolized largely by hepatic CYP2D6 and
CYP3A4.
Excretion: Faeces (55%) and Urine. (25%)
Dosage Form: Oral or IM.
9. DrugInteractions
Drug Cause Reason
Ritonavir Increased concentration of
Aripiprazole.
Ritonavir is a CYP3A4
(involved in the metabolism
of Aripiprazole) inhibitor.
Serotonin Reuptake
Inhibitors (fluoxetine,
sertraline, fluvoxamine)
Increased concentration of
Aripiprazole.
Serotonin reuptake
inhibitors are CYP2D6
(involved in the metabolism
of Aripiprazole) inhibitors.
Carbinoxamine Sedation Carbinoxamine and
Aripiprazole both cause
sedation. Additive Effect.
10. Switching from Oral Antipsychotics to
Aripiprazole.
It is advisable to begin aripiprazole at an intermediate dose and build the
dose rapidly over 3-7 days.
Clinical experience has shown that asenapine, quetiapine, and olanzapine
should be tapered off slowly over a period of 3-4 weeks, to allow patients
to readapt to the withdrawal of blocking cholinergic, histaminergic, and
alpha-1 receptors
Clozapine should always be tapered off slowly, over a period of 4 weeks or
more
Benzodiazepine or anticholinergic medication can be administered during
cross-titration to help alleviate side effects such as insomnia, agitation,
and/or psychosis.
11.
12.
13. Conclusion
Aripiprazole is a second-generation (atypical)
antipsychotic drug used in the treatment of
various mental conditions such as:
schizophrenia, mania, and control of
agitation and disturbed behavior. In my
opinion, it is better than other antipsychotic
drugs such as chlorpromazine as it has mild
extrapyramidal side effects due to its unique
D2 PA activity.
