Improvement in antipsychotic-induced hyperprolactinemia with the addition of aripiprazole in schizophrenic patients

Abstract

Purpose: Hyperprolactinemia, a common adverse effect of antipsychotics, frequently impacts patients' quality of life. Aripiprazole is a potent dopamine D2 receptor partial agonist and rarely increases the serum prolactin concentration. The authors investigated the effect of aripiprazole coadministration on antipsychotic-induced hyperprolactinemia and associated symptoms in patients with schizophrenia. Method: The subjects were 9 patients (8 females, 1 male) with hyperprolactinemia induced by risperidone, olanzapine, haloperidol, zotepine, bromperidol, levomepromazine, and quetiapine; 6 of the females had oligomenorrhea and 2 amenorrhea, and the male had erectile dysfunction. All of the patients received concomitant aripiprazole for more than 8 weeks at a mean dose (range) of 7.7 (3-18) mg/day. The doses of all other medications, including the hyperprolactinemia-inducing antipsychotics, remained fixed throughout the study period. Results: The mean serum concentration (range) of prolactin during aripiprazole coadministration (29.9 (9.8-53) ng/ml) was significantly (p=0.008) lower than that before aripiprazole coadministration (81.1 (27-153) ng/ml). The associated symptoms were improved in 4 females (regularized or regained menstruation) and the male (normalized erectile function), while no changes were observed in the other clinical symptoms of schizophrenia. Discussion: The results of the present study suggest that even small doses of coadministered aripiprazole effectively limit excessive prolactin response to antipsychotics without interfering with the benefits of existing prescriptions.

Effects of Genetic Polymorphisms of CYP2D6, CYP3A5, and ABCB1 on the Steady-State Plasma Concentrations of Aripiprazole and Its Active Metabolite, Dehydroaripiprazole, in Japanese Patients With Schizophrenia

“…3,4 Furthermore, the addition of aripiprazole can resolve hyperprolactinemia induced by other antipsychotic drugs. 5 Aripiprazole undergoes N-dealkylation, hydroxylation, and dehydrogenation, yielding its active metabolite, dehydroaripiprazole. 6 Dehydroaripiprazole is further hydroxylated and N-dealkylated.…”

Lack of Correlation Between the Steady-State Plasma Concentrations of Aripiprazole and Haloperidol in Japanese Patients With Schizophrenia

“…1 The efficacy of aripiprazole has been established for the treatment of psychiatric disorders, especially of schizophrenia. [1][2][3] Aripiprazole undergoes N-dealkylation, hydroxylation, and dehydrogenation, yielding its active metabolite, dehydroaripiprazole. [1][2][3] Aripiprazole undergoes N-dealkylation, hydroxylation, and dehydrogenation, yielding its active metabolite, dehydroaripiprazole.…”

Prolactin concentrations during aripiprazole treatment in relation to sex, plasma drugs concentrations and genetic polymorphisms of dopamine D2 receptor and cytochrome P450 2D6 in Japanese patients with schizophrenia

“…Also, aripiprazole rather decreases prolactin concentrations in the treatment of schizophrenia through the intrinsic activity on dopamine receptor in the pituitary . Furthermore, the addition of aripiprazole can resolve hyperprolactinemia induced by other antipsychotic drugs …”