Long-Acting Injectable Aripiprazole

Abstract

Schizophrenia is a severe mental illness with a lifetime prevalence of approximately one percent worldwide. Maintenance antipsychotic treatment has been effective in preventing relapses in long-term follow-up studies. Logically it can be proposed that long-acting injectable antipsychotics (LAI) might reduce both unintentional and intentional nonadherence. Long-acting injectable aripiprazole was approved for the treatment of schizophrenia by the U.S. FDA on 28th February 2013 and will be marketed under the name Abilify Maintena. Aripiprazole LAI (ALAI) is a lyophilized powder that needs to be reconstituted with sterile water to form an injectable suspension without affecting the original molecule. The monthly injection interval is very attractive since patients prefer fewer injections. From a tolerability perspective, ALAI appears to be both weight neutral and lacking metabolic side effects. This can confer an advantage over the other currently available second-generation antipsychotic LAIs. Simple constitution with sterile water and no requirement to refrigerate make storage and administration easier. Like all medications, there are always potential disadvantages to ALAI. There is a period of oral coverage, while not as long as for long-acting risperidone microspheres (RLAI), that is required. Care must be taken to review concomitant medications for the presence of metabolic inducers and inhibitors. One would also expect some patients to be sensitive to extrapyramidal symptoms, especially akathisia which is well documented in the oral preparation. All things considered, we welcome our new tool, ALAI, to our work-place and predict both clinical practice and post marketing analysis and studies will discover its true value.

Discovery of G Protein-Biased D2 Dopamine Receptor Partial Agonists

“…10 Thus, safer and more effective drugs that target D2R are needed not only to treat the positive and negative symptoms of schizophrenia, 11 but also to minimize the motor side-effects commonly observed with chronic antipsychotic treatment. 12 Newer generation antipsychotics such as aripiprazole 13 possess partial agonist actions at D2R 14 and have less propensity to produce motor side-effects, 15 but mounting evidence in the last decade has suggested that aripiprazole, which is a balanced D2R agonist, 16 can activate a plethora of downstream signaling pathways. 17–18 …”

Spotlight on once-monthly long-acting injectable aripiprazole and its potential as maintenance treatment for bipolar I disorder in adult patients

“…The drug is absorbed from the surface of the depot injection, and in the case of haloperidol, no overlap with oral medication is required when a loading dose strategy is used. 35 …”

“…Risperidone, the first atypical LAI, is delivered in the form of a biodegradable microsphere preparation. 35 , 36 It has a similar side-effect profile as oral risperidone, and the main challenges in the clinical setting have been the need for refrigeration as well as the need to dose the medication every 2 weeks. 36 A period of overlap with oral medication is required with LAI risperidone.…”

Aripiprazole: from pharmacological profile to clinical use

“…Aripiprazole LAI is more effective than placebo, and non-inferior to oral aripiprazole, in delaying relapse and in reducing relapse rates in schizophrenia. 66 , 67 …”