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Paliperidone ER - A novel antipsychotic

机译：Paliperidone ER-新型抗精神病药

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Paliperidone ER is metabolite of risperidone (9-hydroxy-risperidone) formulated as OROS extended release system, which facilitates its once daily use and improves treatment compliance. It is indicated not only in schizophrenia but also in schizoaffective disorder and bipolar mania. Due to lack of interactions of CYP enzymes, minimal or no pharmacological interactions are evident. Due to favorable pharmacodynamic profile i.e. antagonism of 5HT2A, α1 and D2; it has improved positive and negative symptoms (reduction in PANSS score), reduced extra pyramidal side effects and efficacy. Only renal failure patients demand dose reduction. In various therapeutic trials, paliperidone ER has shown better efficacy than placebo and olanzapine, also delays symptoms recurrence of schizophrenia. Paliperidone ER has caused various adverse effects like akathisia, headache, increase serum prolactin level and weight gain but serum lipid, glucose and insulin level remained unaffected. Paliperidone ER has increased the number of annual stable days and more cost effective than other atypical antipsychotics. Introduction Schizophrenia is devastating illness with significant psychological, physical, social and economic impact, affecting about 1% of the population. [1] Disease course is variable and mostly chronic, characterized by ongoing functional impairment and the frequent recurrence of acute psychotic symptoms. Thus, the general goals of the treatment are to quickly reduce symptoms severity, improve patient functioning, prevent recurrences of the symptomatic episodes and associated deterioration of the functioning. Atypical antipsychotics are currently the most frequently prescribed class of drugs for schizophrenia, as they have good efficacy with lower risk of extra pyramidal side effects. [2] These agents are associated with varying degrees of metabolic adverse effects like weight gain, impaired glucose metabolism, dyslipidemia and in some cases serious morbidity, such as cardiovascular diseases. Paliperidone is new molecule in list of atypical antipsychotics, which has low propensity to interfere with metabolic parameters. In addition, receptor antagonism profile is favorable, leading to very few adverse effects.
机译：Paliperidone ER是利培酮（9-羟基-利培酮）的代谢产物，配制成OROS缓释系统，有利于每天使用一次并改善治疗依从性。它不仅适用于精神分裂症，而且适用于精神分裂性情感障碍和躁郁症。由于缺乏CYP酶的相互作用，因此很少或没有药理学相互作用是显而易见的。由于有利的药效学特征，即5HT2A，α1和D2的拮抗作用;它具有改善的阳性和阴性症状（PANSS评分降低），减少了额外的锥体束副作用和功效。只有肾衰竭患者需要降低剂量。在各种治疗试验中，帕潘立酮ER已显示出比安慰剂和奥氮平更好的疗效，也延迟了精神分裂症的症状复发。 Paliperidone ER引起了多种不良反应，如静坐症，头痛，血清催乳素水平增加和体重增加，但血清脂质，葡萄糖和胰岛素水平未受影响。与其他非典型抗精神病药相比，帕潘立酮ER增加了年度稳定天数，并且更具成本效益。简介精神分裂症是具有重大心理，身体，社会和经济影响的毁灭性疾病，影响了约1％的人口。 [1]疾病过程是可变的，并且大多数是慢性的，其特征是持续的功能障碍和急性精神病性症状的频繁复发。因此，治疗的总体目标是迅速减轻症状的严重程度，改善患者的机能，防止症状发作的复发和相关的机能恶化。目前，非典型抗精神病药是治疗精神分裂症的最常用处方药，因为它们具有良好的疗效，且具有较低的锥体束副作用风险。 [2]这些药物与不同程度的代谢不良反应有关，例如体重增加，葡萄糖代谢受损，血脂异常，在某些情况下还包括心血管疾病等严重的疾病。帕潘立酮是非典型抗精神病药清单中的新分子，具有低干扰代谢参数的倾向。此外，受体拮抗作用是有利的，几乎没有副作用。

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