Pharmacy Department, South London and Maudsley NHS Foundation Trust, London, United Kingdom.
Neuropsychiatr Dis Treat. 2010 Sep 7;6:561-72. doi: 10.2147/NDT.S8505.
Paliperidone palmitate is a new long-acting antipsychotic injection for the treatment of acute and maintenance therapy in schizophrenia. Paliperidone (9-hydroxyrisperidone) is the major active metabolite of risperidone and acts at dopamine D(2) and serotonin 5HT(2A) receptors. As with other atypical antipsychotics, it exhibits a high 5HT(2A):D(2) affinity ratio. It also has binding activity as an antagonist at α(1)-and α(2) adrenergic receptors and H(1) histaminergic receptors, but has virtually no affinity for cholinergic receptors. Paliperidone palmitate has been shown to be effective in reducing Positive and Negative Syndrome Scale total scores in four short-term trials in acute schizophrenia. It was also effective as maintenance therapy in a long-term trial in which time to recurrence of symptoms was significantly longer in paliperidone-treated patients compared with placebo. In addition, paliperidone was shown to be noninferior to risperidone long-acting injection in one study, but this noninferiority was not established in another longer study comparing the two drugs. Treatment should be initiated with 234 mg on day 1 and 156 mg on day 8, followed by a recommended monthly maintenance dose of 39-234 mg based on efficacy and tolerability. Paliperidone palmitate is generally well tolerated, although it can cause weight gain and a rise in prolactin levels, which is generally greater in women than in men. Overall, paliperidone palmitate may have advantages over other currently available long-acting injections, and therefore may be a useful alternative for the treatment of schizophrenia, although further long-term trials comparing it with active treatments are warranted.
棕榈酸帕利哌酮是一种新型长效抗精神病注射剂，用于治疗精神分裂症的急性和维持治疗。帕利哌酮（9-羟基利培酮）是利培酮的主要活性代谢物，作用于多巴胺 D2 和 5HT2A 受体。与其他非典型抗精神病药一样，它表现出高 5HT2A:D2 亲和力比。它还具有作为 α1-和 α2 肾上腺素能受体和 H1 组胺能受体拮抗剂的结合活性，但对胆碱能受体几乎没有亲和力。棕榈酸帕利哌酮已被证明在四项急性精神分裂症短期试验中可有效降低阳性和阴性综合征量表总分。在一项长期试验中，棕榈酸帕利哌酮治疗组的症状复发时间明显长于安慰剂组，也作为维持治疗有效。此外，在一项研究中，帕利哌酮显示非劣效于利培酮长效注射剂，但在另一项比较两种药物的更长研究中，这种非劣效性未得到证实。治疗应从第 1 天的 234mg 和第 8 天的 156mg 开始，然后根据疗效和耐受性推荐每月维持剂量为 39-234mg。棕榈酸帕利哌酮通常具有良好的耐受性，尽管它可能导致体重增加和催乳素水平升高，在女性中通常比男性更明显。总的来说，棕榈酸帕利哌酮可能优于其他目前可用的长效注射剂，因此可能是治疗精神分裂症的有用选择，尽管需要进一步的长期试验来比较它与活性治疗的效果。
