Xeplion (paliperidone palmitate)
Paliperidone is the active metabolite of the atypical antipsychotic risperidone, and is already on the market as the extended-release tablets Invega (paliperidone). As of recently, an ester of paliperidone, Xeplion (paliperidone palmitate), has been approved as an extended-release injection (i.m.) for the treatment of schizophrenia. The injection is given monthly.
Xeplion is indicated for maintenance treatment of schizophrenia in adult patients stabilised with paliperidone or risperidone. In selected adult patients with schizophrenia and previous responsiveness to oral paliperidone or risperidone, Xeplion may be used without prior stabilisation with oral treatment, if psychotic symptoms are mild to moderate and a long-acting injectable treatment is needed.
Paliperidone palmitate (50-150 mg/month) has shown a significantly better effect than placebo after 8 days of treatment. In a 13-week randomized controlled trial, Xeplion (50-150 mg) and risperidone injection (25-50 mg/month) were equally effective. In other studies, i.e. with an older dosage regime, Xeplion did not show the same effect as risperidone. Furthermore, the drug has not been compared to oral paliperidone (Invega). Looking at the existing data material, the magnitude of Xeplion’s clinical effect is, at this point in time, not yet determined. Doctors need to be aware that some patients will have a need for dosage adjustments or supplemental oral treatment for a period of time.
The effect of combining Xeplion and oral risperidone is unknown, as well as the effect of Xeplion in patients, who are non-respondent to treatment with either risperidone or paliperidone. Due to other exclusion criteria (i.e. patients, who have had no effect of other antipsychotics, polydrug patients), the use of Xeplion should be limited to the approved patient population.
The most common side effects of Xeplion is headaches, tachycardia, insomnia, dizziness, orthostatic hypotension, and, when high doses are given, extra-pyramidal symptoms (EPS) and weight gain. Local reactions on the site of injection, as well as anxiety, were experienced more frequently with Xeplion than with risperidone or placebo.
The normal maintenance dose of Xeplion is 75 mg per month, in total 3.483 Dkr. A start-up fee of 9.072 Dkr. is to be expected. In comparison, Risperdal extended-release injection (25 mg x2 per month) costs 2.454 Dkr a month, while tablet treatment with oral paliperidone costs 1.183 Dkr. for 28 days (6 mg daily), and oral risperidone costs between 25,80 and 57,- Dkr. a month (4-6 mg daily).
IRF finds, that extended release injection treatment with typical antipsychotics is, in many cases, a good treatment for schizophrenic patients. Both the effect and side effects of Xeplion are, at the most, equal to those of risperidone, and the price for Xeplion is higher than for oral treatment. Therefore, IRF does not recommend Xeplion as a first-line agent for extended release treatment of schizophrenia. Xeplion can be considered when other, equally effective and cheaper, oral and injectable antipsychotics have been tried, or if there are issues with patient compliance.
Xeplion (paliperidone palmitate) was marketed on May 2nd, 2011. There is general reimbursement for Xeplion.
The Institute for Rational Pharmacotherapy, July 11th, 2011.