Aripiprazole 5mg
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Aripiprazole 5mg: Efficacy, Safety, and Pharmacokinetics
Introduction to Aripiprazole 5mg
Aripiprazole is an atypical antipsychotic known for its unique pharmacological profile, including partial agonism at dopamine D2 receptors and serotonin 5-HT1A receptors, and antagonism at serotonin 5-HT2A receptors. This medication is used to treat various psychiatric conditions, including schizophrenia, bipolar disorder, and irritability associated with autistic disorder.
Efficacy in Treating Hyperprolactinemia
Hyperprolactinemia Management
Hyperprolactinemia is a common side effect of antipsychotic medications like risperidone. A study evaluated the efficacy of adjunctive aripiprazole in reducing prolactin levels in patients with schizophrenia experiencing risperidone-induced hyperprolactinemia. Patients were administered aripiprazole at doses of 5mg, 10mg, or 20mg daily. The study found that all doses significantly reduced prolactin levels compared to placebo, with the 10mg and 20mg doses being more effective than the 5mg dose1.
Pharmacokinetics of Aripiprazole 5mg
Combination with Divalproex Sodium
A pilot pharmacokinetic study assessed the fixed-dose combination (FDC) of aripiprazole 5mg with divalproex sodium 500mg. The study found that the combination increased the peak plasma concentration (Cmax) and area under the curve (AUC) of both drugs while decreasing their half-lives. This suggests that the FDC could potentially improve patient compliance by simplifying the medication regimen2.
Efficacy in Pediatric Populations
Treatment of Irritability in Autism
Aripiprazole has also been studied for its efficacy in treating irritability in children and adolescents with autistic disorder. In a placebo-controlled study, aripiprazole at doses of 5mg, 10mg, and 15mg daily significantly improved irritability symptoms compared to placebo. The 5mg dose was effective, but higher doses showed greater improvements. The medication was generally well-tolerated, with sedation being the most common adverse event leading to discontinuation3.
Receptor Occupancy and Mechanism of Action
PET Study Insights
A positron emission tomography (PET) study investigated the receptor occupancy of aripiprazole at different doses. The study revealed high occupancy at D2 receptors even at the lowest dose of 10mg, with lower occupancy at 5-HT2 and 5-HT1A receptors. This high D2 receptor occupancy is consistent with aripiprazole's efficacy in treating schizophrenia, while the lower 5-HT2 occupancy may contribute to its lower incidence of extrapyramidal side effects4.
Conclusion
Aripiprazole 5mg is effective in managing risperidone-induced hyperprolactinemia, treating irritability in children with autism, and has a favorable pharmacokinetic profile when combined with divalproex sodium. Its unique receptor occupancy profile supports its efficacy and safety in treating various psychiatric conditions. Further studies are needed to fully understand its long-term effects and comparative efficacy with other antipsychotics.
Sources and full results
Most relevant research papers on this topic
Adjunctive aripiprazole in the treatment of risperidone-induced hyperprolactinemia: A randomized, double-blind, placebo-controlled, dose–response study
Adjunctive aripiprazole effectively and safely reduces risperidone-induced hyperprolactinemia in schizophrenia patients without significant effects on psychopathology or side effects.
RCTFixed Dose Combination Tablets of Aripiprazole and Divalproex Sodium: a Pilot Pharmacokinetic Study in Human Volunteers
Fixed dose combination tablets of aripiprazole and divalproex sodium show a comparable pharmacokinetic profile to their individual components, potentially improving patient compliance.
RCTA placebo-controlled, fixed-dose study of aripiprazole in children and adolescents with irritability associated with autistic disorder.
Aripiprazole is an effective and generally safe treatment for irritability in children and adolescents with autistic disorder.
RCT
Highly CitedDifferential effects of aripiprazole on D(2), 5-HT(2), and 5-HT(1A) receptor occupancy in patients with schizophrenia: a triple tracer PET study.
Aripiprazole exhibits a unique occupancy profile in schizophrenia patients, with high D(2) receptor occupancy and low 5-HT(2) receptor occupancy, and uncommon extrapyramidal side effects.
RCTHighly CitedEfficacy of brexpiprazole in patients with acute schizophrenia: Review of three randomized, double-blind, placebo-controlled studies
Brexpiprazole 2mg and 4mg are effective in treating acute schizophrenia, with minimal changes in PANSS total score and suboptimal improvement in 1mg group.
RCT
Large Human TrialOpen Labeled, Randomized, Switch-Over Study of Two Fixed Doses (10/15mg) Of Aripiprazole : To Evaluate its Safety And Efficacy in the Treatment of Indian Patients of Schizophrenia.
Aripiprazole is a safe and effective antipsychotic for Indian patients with schizophrenia, improving symptoms and reducing side effects.
RCTAripiprazole: a review of its use in schizophrenia and schizoaffective disorder.
Aripiprazole is an effective and well-tolerated atypical antipsychotic drug for treating schizophrenia and schizoaffective disorder, with a low potential for bodyweight gain and no dosage titration needed.
Literature ReviewHighly CitedThe antipsychotic aripiprazole selectively prevents the stimulant and rewarding effects of morphine in mice.
Aripiprazole selectively inhibits the abuse-related effects of morphine in mice, potentially offering a potential substitute therapy for opioid addiction.
Non-RCT
Animal Study
Rigorous JournalEfficacy and safety of aripiprazole vs. haloperidol for long-term maintenance treatment following acute relapse of schizophrenia.
Aripiprazole shows comparable or superior long-term efficacy to haloperidol for schizophrenia treatment, with better safety and tolerability.
Meta-AnalysisHighly CitedSafety and Efficacy of Aripiprazole 2-Month Ready-to-Use 960 mg: Secondary Analysis of Outcomes in Adult Patients With Schizophrenia in a Randomized, Open-label, Parallel-Arm, Pivotal Study.
Ari 2MRTU 960 is well-tolerated and has similar efficacy to AOM 400 in clinically stable patients with schizophrenia.
RCT