Other events since the product launch of aripiprazole have been the emergence of second-generation antipsychotics as mood stabilizers, with almost all of them, including aripiprazole, being approved by regulatory authorities for the indication of bipolar mania. Since then, there has been greater appreciation of the more complex nature of receptor binding affinities, and aripiprazole can also be classified as a medication with significant 5HT2A-antagonism, and with still other additional secondary binding characteristics which may be clinically important in individual patients. Its introduction was heralded by some as a “third-generation” antipsychotic, as it was the first dopamine partial agonist anti-schizophrenia drug to be marketed. Aripiprazole appears to have a low propensity for weight gain, a favorable metabolic profile, and no association with hyperprolactinemia.Īripiprazole was approved by the United States Food and Drug Administration in November 2002 for the treatment of schizophrenia. Appropriate dosing may also be important in individualizing therapy to improve tolerability, with lower starting doses becoming more important when adding to, or switching from, another antipsychotic. Among some patients with bipolar disorder, akathisia and gastrointestinal (GI) complaints can emerge at the start of treatment however, the GI symptoms were time-limited in many instances. Efficacy in treating manic or mixed states was established in placebo-controlled trials.
Its tolerability profile in patients with schizophrenia appears superior to haloperidol, perphenazine, risperidone, and olanzapine. The evidence so far suggests that in terms of efficacy for schizophrenia, aripiprazole is superior to placebo and haloperidol (long term), similar to perphenazine and risperidone, and inferior to olanzapine.
Relatively few comparative trials with other second-generation antipsychotics have been published for schizophrenia, with none available for bipolar disorder. Several double-blind randomized clinical trials have established the efficacy and tolerability of aripiprazole within the dose range of 10–30 mg/day for schizophrenia, and 15–30 mg/day for manic or mixed states associated with bipolar I disorder.
Although it is a dopamine partial agonist, it also has substantial binding affinity for the serotonin 5HT2A receptor. Aripiprazole has been approved by regulatory agencies for the treatment of schizophrenia and bipolar I disorder.
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