Aripiprazole: an overview of a novel antipsychotic.
Aripiprazole exhibits high affinity for dopamine D2 and D3, serotonin 5-HT1A and 5-HT2A receptors, moderate affinity for dopamine D4, serotonin 5-HT2C and 5-HT7, alpha1-adrenergic and histamine H1 receptors. The mean elimination half-lives are about 75 hours and 94 hours for aripiprazole and dehydroaripiprazole, respectively. Steady-state concentrations are attained within 14 days of dosing for both active moieties. At least 1 to 2 weeks, and sometimes up to 4 weeks, may pass before aripiprazole reaches its full effect. The efficacy of aripiprazole was investigated in the treatment of schizophrenia, in the treatment of acute manic episode associated with Bipolar I Disorder, and in the treatment of psychosis associated with Alzheimer's dementia. Aripiprazole has demonstrated superiority to placebo in clinical studies of the treatment of both schizophrenia and acute bipolar mania. Aripiprazole has been evaluated for safety in 5592 patients who participated in multiple dose, premarketing trials in schizophrenia, bipolar mania, and dementia of the Alzheimer's type. The recommended starting and target dose for aripiprazole is 10 or 15 mg/day administered on a once-a-day schedule without regard to meals. Aripiprazole has been systematically evaluated and shown to be effective in a dose range of 10 to 30 mg/day. Dosage increases should not be made before 2 weeks of continuous therapy, the time needed to achieve steady state. At least 1 to 2 weeks, and sometimes up to 4 weeks, may pass before aripiprazole reaches its full effect. In this presentation was given an overview of novel antipsychotic aripiprazole.
Uzun
Suzana
S
University Department of Psychiatry, School of Medicine, University of Zagreb, Psychiatric Hospital Vrapce, Zagreb, Croatia.
Kozumplik
Oliver
O
Mimica
Ninoslav
N
Folnegović-Smalc
Vera
V
D000544:Alzheimer Disease / Q000097:blood / Q000188:drug therapy*; D014150:Antipsychotic Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000068180:Aripiprazole; D001921:Brain / Q000187:drug effects; D002986:Clinical Trials as Topic; D006207:Half-Life; D006801:Humans; D008657:Metabolic Clearance Rate / Q000502:physiology; D010879:Piperazines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011618:Psychotic Disorders / Q000097:blood / Q000188:drug therapy*; D015363:Quinolones / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D017981:Receptors, Neurotransmitter / Q000187:drug effects; D016896:Treatment Outcome
D014150:Antipsychotic Agents; D010879:Piperazines; D015363:Quinolones; D017981:Receptors, Neurotransmitter; C517414:dehydroaripiprazole; D000068180:Aripiprazole