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Chapter 31. Aripiprazole

Zafar A. Sharif, M.D.; Jeffrey A. Lieberman, M.D.
DOI: 10.1176/appi.books.9781585623860.430665

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Excerpt

Aripiprazole is a dihydroquinolinone antipsychotic agent. Chemically, it is unrelated to phenothiazine, butyrophenone, thienobenzodiazepine, or other antipsychotic agents. Pharmacologically, it exhibits a novel mechanism of action, combining partial agonist activity at dopamine2 (D2), dopamine3 (D3), and serotonin1A (5-HT1A) receptors with antagonist activity at serotonin2A (5-HT2A) and D2 receptors (Burris et al. 2002; Jordan et al. 2002). The development and approval of aripiprazole represent a significant event in the history of antipsychotic agents, as it potentially represents another significant innovation following the introduction of first-generation, or typical, antipsychotic drugs and second-generation, or atypical, antipsychotic drugs in the pharmacology and mechanism of action of therapeutic agents for psychotic disorders.

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FIGURE 31–1. Conventional dopamine (DA) antagonist activity: effect on positive symptoms, extrapyramidal side effects (EPS), and prolactin levels.

FIGURE 31–2. Dopamine (DA) partial agonist activity: effect on positive symptoms, extrapyramidal side effects (EPS), and prolactin levels.

FIGURE 31–3. Chemical structure of aripiprazole.
Table Reference Number
TABLE 31–1. Receptor-binding profile of aripiprazole

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A unique mechanism of action of aripiprazole that distinguishes it from all other available antipsychotic agents is
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The most frequently reported adverse effect associated with aripiprazole treatment is
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Aripiprazole is metabolized primarily by hepatic cytochrome P450 (CYP) enzymes in the liver. As a consequence, aripiprazole blood levels may be increased by
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