Minimal Effects of Cariprazine on Prolactin Levels in Bipolar Disorder and Schizophrenia

BACKGROUND: Many medications used to treat schizophrenia and bipolar I disorder are linked to hyperprolactinemia. The effects of cariprazine, a dopamine D(3)/D(2) receptor partial agonist, on prolactin levels in patients with schizophrenia or bipolar I disorder were evaluated. METHODS: Effects on prolactin were evaluated using pooled data from randomized, double-blind, placebo-controlled studies in patients with schizophrenia (4 studies; 6-week duration; cariprazine 1.5–3 mg/d, 4.5–6 mg/d, and 9–12 mg/d), bipolar mania (3 studies; 3-week duration; cariprazine 3–6 and 9–12 mg/d), and bipolar depression (3 studies; 6- to 8-week duration; cariprazine 1.5 and 3 mg/d). Long-term effects were analyzed using open-label studies in patients with schizophrenia (2 studies; 48-week duration) and patients with bipolar mania (1 study; 16-week duration). Change in prolactin levels (ng/mL) from baseline to study endpoint was evaluated in subsets of sex and prior medication use. RESULTS: In patients with schizophrenia (male, n = 1377; female, n = 558), median prolactin changes were −1.2 for males and −7.4 for females on placebo, and ranged from −4.2 to −3.6 for males and −12.4 to +0.2 for females in the cariprazine-treatment groups. In patients with bipolar mania (male, n = 570; female, n = 395), median prolactin changes were −0.2 for males and −1.1 for females on placebo and ranged from −2.1 to −3.0 for males and 0 to +1.8 for females in the cariprazine-treatment groups. Median decreases were also seen in the long-term studies of schizophrenia (range, −14.6 to −2.0) and bipolar mania (range, −0.8 to +1.9). In patients with bipolar depression (male, n = 485; female, n = 780), median prolactin changes were +0.3 for males and +0.7 for females on placebo and ranged from +0.4 to +0.5 for males and +3.0 to +3.1 for females in the cariprazine-treatment groups. CONCLUSION: Treatment with cariprazine for schizophrenia or bipolar I disorder was associated with minimal effects on prolactin levels.