Antipsychotics are the standard of care when it comes to the treatment of
Schizophrenia, and they are often used in Bipolar as well. Their use can come with adverse effects such as extrapyramidal movements, metabolic complications as well as cardiovascular complications such as a prolonged QT interval. Treatment for these side effects ranges from the treatment of the complications up to the cessation of the medication, which could come at the expense of the user's stability. Both
schizophrenia and
bipolar disorder have an increased risk of suicide and increased morbidity. The purpose of this review presents the background, evidence, and indications for the use of the new second-generation
antipsychotic Cariprazine, which has a primary function as a D3 and D2 partial agonist, with higher selectivity for the D3 receptor type.
Recent Findings:
Schizophrenia is currently teated by
dopamine antagonists and/or 5HT modulators, each with their own set of side effects.
Bipolar disorder is mostly treated with mood stabilizers. Studies looking at the efficacy and safety of
cariprazine have shown in two phase II trials and phase III trials the decrease in PANSS scores in
schizophrenia. The most common adverse effects were
akathisia,
insomnia,
constipation, and other extrapyramidal side effects. A unique side effect of
Cariprazine caused bilateral
cataract and cystic degeneration of the retina in the dog following daily
oral administration for 13 weeks and/or 1 year and
retinal degeneration in rats following daily
oral administration for 2 years. Another study showed that
cariprazine had significant efficacy in preventing relapse in patients with
schizophrenia. The time to the loss of sustained remission was significantly longer (P = .0020) for
cariprazine compared to placebo (hazard ratio = 0.51) during the double-blind treatment. 60.5% of patients treated with
cariprazine and 34.9% of patients treated with placebo sustained remission through the final visit (odds ratio [OR] = 2.85; P = .0012; number needed to treat [NNT] = 4. Another Phase IIIb study looked at negative symptoms and used the Positive and Negative Syndrome Scale Factor Score for Negative Symptoms (PANSS-FSNS), and it found that the use of
cariprazine, from baseline to week 26, led to a greater least-squares mean change in PANSS-FSNS than did
risperidone. Another study looked at the quality of life years with the treatment of
cariprazine and showed those treated with
cariprazine had superior quality of life compared to those treated with
risperidone. In terms of
bipolar disorder, it showed a decrease in depressive symptoms as measured by decreased MADRs scores with a dose of 3.0mg/day. A phase II study looked at the use of
cariprazine in
mania or mix states and showed
cariprazine significantly decreased YMRS scores compared to placebo, least-square mean difference of -6.1 (p < 0.001). The metabolic parameters demonstrated comparable changes except for fasting
glucose in which
cariprazine was associated with elevations in
glucose levels compared to placebo (p < 0.05). Another phase III study showed significant differences in YMRS total score mean change between
cariprazine versus placebo-treated group. Changes in metabolic profiles in all mentioned studies were minimal.
Summary: