关键词: D3 receptor atypical antipsychotics cariprazine negative symptoms pharmacology schizophrenia socializing drug third-generation antipsychotics

来  源:   DOI:10.3389/fpsyt.2024.1385925   PDF(Pubmed)

Abstract:
Management of negative symptoms is one of the most challenging and important unmet needs of schizophrenia treatment. Negative symptoms together with positive symptoms result in significant psychosocial impairment and poor quality of life. Existing studies on atypical antipsychotics reported limited treatment adherence due to higher prevalence of treatment-emergent adverse events, such as diabetes, weight gain, hyperlipidemia, hyperprolactinemia and hypertension. A compound with greater affinity for dopamine D2/D3 receptors may improve negative symptoms, mood, and cognitive impairment associated with schizophrenia. In 2015, the US FDA has approved cariprazine, a partial D2/D3 agonist for treatment of schizophrenia, mania or mixed episodes. Midlands and Lancashire Commissioning Support Unit, UK (2019) has particularly suggested cariprazine for the treatment of predominant negative symptoms of schizophrenia. India\'s Central Drugs Standard Control Organization (CDSCO) has approved cariprazine in 2021 for the treatment of schizophrenia, manic or mixed episodes associated with bipolar I disorder. A ten-fold greater affinity for D3 receptors and partial agonism to serotonin receptors, along with longer half-life make cariprazine distinct when compared with other atypical antipsychotics. Cariprazine is also reported to have fewer incidents of metabolic and hormonal adverse events, and has been shown to provide better relapse prevention. Recent evidence indicates promising effect of cariprazine in ameliorating negative symptoms as well as psychotic symptoms in patients with schizophrenia. In addition, improved adherence to treatment (adjunctive/monotherapy) with cariprazine in patients having inadequate response to an ongoing antipsychotic treatment has also been clinically established. This review presents the evidence-based safety and efficacy of cariprazine for treatment of predominant negative symptoms of schizophrenia.
摘要:
阴性症状的管理是精神分裂症治疗中最具挑战性和重要的未满足需求之一。阴性症状与阳性症状一起导致显著的心理社会损害和不良的生活质量。关于非典型抗精神病药物的现有研究报告称,由于治疗引起的不良事件发生率较高,因此治疗依从性有限。比如糖尿病,体重增加,高脂血症,高催乳素血症和高血压。对多巴胺D2/D3受体具有更大亲和力的化合物可以改善阴性症状,心情,以及与精神分裂症相关的认知障碍。2015年,美国FDA批准卡利拉嗪,用于治疗精神分裂症的部分D2/D3激动剂,躁狂症或混合发作。中部和兰开夏郡调试支持股,英国(2019)特别建议卡利拉嗪用于治疗精神分裂症的主要阴性症状。印度的中央药物标准控制组织(CDSCO)于2021年批准卡利拉嗪用于治疗精神分裂症,躁狂或混合发作与双相I型障碍相关。对D3受体的亲和力高十倍,对5-羟色胺受体有部分激动作用,与其他非典型抗精神病药物相比,卡利拉嗪的半衰期更长,因此与众不同。据报道,卡利哌嗪的代谢和激素不良事件也较少,并已被证明可以更好地预防复发。最近的证据表明,卡利拉嗪可改善精神分裂症患者的阴性症状和精神病症状。此外,在对正在进行的抗精神病药物治疗反应不足的患者中,卡利拉嗪治疗(辅助/单药治疗)的依从性也得到了临床证实.这篇综述介绍了卡利拉嗪治疗精神分裂症主要阴性症状的循证安全性和有效性。
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