Paliperidone palmitate long-acting injection compared to risperidone for schizophrenia
When flexibly dosed every four weeks, 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.
Findings in words
Findings in numbers
Quality of evidence
Global state: No clinically important change
No 30% improvement on PANSS score. Follow-up: 13-53 weeks
There is no clear difference between people given paliperidone palmitate and those receiving risperidone for this outcome. These findings are based on data of low quality.
Recurrence of psychotic symptoms. Follow up: 13-53 weeks
There is no clear difference between people given paliperidone palmitate and those receiving risperidone for the outcome of 'relapse'. Data supporting this finding are based on moderate quality evidence.
RR 1.23 (0.98 to 1.53)
Leaving the study early
- For any reason. Follow up: 13-53 weeks
Paliperidone palmitate causes little or no increase to the chance of leaving the study.
RR 1.12 (1 to 1.25)
- Because of lack of efficacy. Follow up: 13-53 weeks
Paliperidone palmitate may increase the risk of finding treatment unacceptable or being withdrawn from treatment outcome for the reason of perceived lack of efficacy compared with risperidone. Data are based on moderate quality evidence.
RR 1.35 (1.06 to 1.71)
Adverse event: death
Follow up: 13-53 weeks
There was no clear difference between people given paliperidone palmitate and those receiving risperidone for this rare outcome. These findings are based on data of low quality.
RR 3.62 (0.6 to 21.89)
Outcomes of 'cost' and 'quality of life' are not reported in the included randomized trials.
The British National Formulary recommends a gradual withdrawal when discontinuing antipsychotics to avoid acute withdrawal syndrome or rapid relapse. Symptoms of withdrawal commonly include nausea, vomiting, and loss of appetite. Other symptoms may include restlessness, increased sweating, and trouble sleeping. Less commonly there may be a feeling of the world spinning, numbness, or muscle pains. Symptoms generally resolve after a short period of time.
There is tentative evidence that discontinuation of antipsychotics can result in psychosis. It may also result in reoccurrence of the condition that is being treated. Rarely tardive dyskinesia can occur when the medication is stopped.
In April 2014, it was reported that 21 Japanese people who had received shots of the long-acting injectable paliperidone to date had died, out of 10,700 individuals prescribed the drug.
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.
Paliperidone is the primary active metabolite of the older antipsychotic risperidone. While its specific mechanism of action is unknown, it is believed paliperidone and risperidone act via similar, if not identical, pathways. Its efficacy is believed to result from central dopaminergic and serotonergic antagonism. Food is known to increase the absorption of Invega type ER OROS prolonged-release tablets. Food increased exposure of paliperidone by up to 50-60%, however, half-life was not significantly affected. The effect was probably due to a delay in the transit of the ER OROS formulation in the upper part of the GI channel, resulting in increased absorption.
Paliperidone (as Invega) was approved by the Food and Drug Administration (FDA) 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 name "Palimax ER" manufactured & 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.
On May 18, 2015, a new formulation of paliperidone palmitate was approved by the FDA under the brand name Invega Trinza. 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.
^ abcdeLeucht S, Cipriani A, Spineli L, Mavridis D, Orey D, Richter F, Samara M, Barbui C, Engel RR, Geddes JR, Kissling W, Stapf MP, Lässig B, Salanti G, Davis JM (September 2013). "Comparative efficacy and tolerability of 15 antipsychotic drugs in schizophrenia: a multiple-treatments meta-analysis". Lancet. 382 (9896): 951–62. doi:10.1016/S0140-6736(13)60733-3. PMID23810019.
^Joint Formulary Committee, BMJ, ed. (March 2009). "4.2.1". British National Formulary (57 ed.). United Kingdom: Royal Pharmaceutical Society of Great Britain. p. 192. ISBN978-0-85369-845-6. Withdrawal of antipsychotic drugs after long-term therapy should always be gradual and closely monitored to avoid the risk of acute withdrawal syndromes or rapid relapse.