Paliperidone, sold under the trade name Invega among others, is an atypical antipsychotic. It is mainly used to treat schizophrenia and schizoaffective disorder.

It is marketed by Janssen Pharmaceuticals. 提供使用 OROS 缓释系统的缓释制剂,允许每天给药一次. 帕潘立酮棕榈酸酯是帕潘立酮棕榈酸酯的长效注射剂,适用于一次 28 初始滴定期后注射天数.

医疗用途
用于治疗精神分裂症和分裂情感性障碍. [4]

帕潘立酮棕榈酸酯长效注射液与利培酮治疗精神分裂症的比较[5]
每四个星期灵活给药时, paliperidone palmitate appears comparable in efficacy and tolerability to risperidone. In short-term studies, paliperidone palmitate – the longer-acting injection – has a similar adverse effect profile to related compounds such as risperidone by mouth. No difference was found in the high rate of reported adverse sexual outcomes and paliperidone palmitate is associated with an increase in serum prolactin.[5]
Outcome Findings in words Findings in numbers Quality of evidence
Adverse effects
Sources:[6][7][8][9][10]

Very Common (>10% incidence)
Headache
Tachycardia
Somnolence (causes less sedation than most atypical antipsychotics)[4]
Insomnia
Hyperprolactinaemia (seems to cause comparable prolactin elevation to its parent drug, risperidone)[4]
Sexual Dysfunction
Common (1–10% incidence)
Cough
Extrapyramidal side effects (EPSE; e.g. dystonia, akathisia, muscle rigidity, parkinsonism. It appears to produce similar EPSE to risperidone, asenapine and ziprasidone and more EPSE than olanzapine, clozapine, aripiprazole, quetiapine, amisulpride and sertindole)[4]
Orthostatic hypotension
Weight gain (tends to produce a moderate degree of weight gain, possibly related to its potent blockade of the 5-HT2C receptor)
QT interval prolongation (tends to produce less QT interval prolongation than most other atypical antipsychotics and approximately as much QT interval prolongation as aripiprazole and lurasidone)[4]
Nasopharyngitis
Anxiety
Indigestion
Constipation
Discontinuation
The British National Formulary recommends a gradual withdrawal when discontinuing antipsychotics to avoid acute withdrawal syndrome or rapid relapse.[11] Symptoms of withdrawal commonly include nausea, vomiting, and loss of appetite.[12] Other symptoms may include restlessness, increased sweating, and trouble sleeping.[12] Less commonly there may be a feeling of the world spinning, numbness, or muscle pains.[12] Symptoms generally resolve after a short period of time.[12]

There is tentative evidence that discontinuation of antipsychotics can result in psychosis.[13] It may also result in reoccurrence of the condition that is being treated.[14] 停药后很少会出现迟发性运动障碍。[12]

死亡人数
在四月份 2014, 据报道, 21 迄今为止接受过长效注射帕潘立酮注射的日本人已经死亡, 在......之外 10,700 个人开了药。[15][16][17][18][19][20][21]

药理
Paliperidone[22]
站点 Ki (纳米)
5-HT1A 617
5-HT2A 1.1
5-HT2C 48
5-HT7 2.7
α1A 2.5
α2A 3.9
α2C 2.7
值是 Ki (纳米). 值越小, 药物与该部位的结合越强.
帕潘立酮是老款抗精神病药利培酮的主要活性代谢物。[23] 虽然其具体作用机制尚不清楚, 据信帕潘立酮和利培酮通过类似的作用, 如果不相同, 途径。[22] 其功效被认为是由中枢多巴胺能和血清素能拮抗作用引起的. 已知食物可增加 Invega 型 ER OROS 缓释片的吸收. 食物会增加帕潘立酮的暴露量 50-60%, 然而, 半衰期没有显着影响. 该效应可能是由于 ER OROS 制剂在 GI 通道上部的转运延迟, 导致吸收增加。[24]

The half-life is 23 hours.[24]

Risperidone and its metabolite paliperidone are reduced in efficacy by P-glycoprotein inducers such as St John’s wort[25][26]

vte Pharmacokinetics of long-acting injectable antipsychotics
History
Paliperidone (as Invega) was approved by the Food and Drug Administration (食品药品监督管理局) for the treatment of schizophrenia in 2006. Paliperidone was approved by the FDA for the treatment of schizoaffective disorder in 2009. The long-acting injectable form of paliperidone, marketed as Invega Sustenna in U.S. and Xeplion in Europe, was approved by the FDA on July 31, 2009. It is the only available brand in Bangladesh under the brand namePalimax ERmanufactured & marketed by ACI Pharmaceuticals.

It was initially approved in Europe in 2007 for schizophrenia, the extended release form and use for schizoaffective disorder were approved in Europe in 2010, and extension to use in adolescents older than 15 years old was approved in 2014.[37]

Brand names
On May 18, 2015, a new formulation of paliperidone palmitate was approved by the FDA under the brand name Invega Trinza.[38] A similar 3 -monthly injection of prolonged release suspension was approved in 2016 by the European Medicines Agency originally under the brand name Paliperidone Janssen, later renamed to Trevicta.[39]


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干细胞疗法