Paliperidone for schizophrenia

Dolder, Christian R.; Nelson, Michael; Deyo, Zachariah

doi:10.2146/ajhp070261

Cited by 68 publications

(40 citation statements)

References 36 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Paliperidone is the 9-hydroxy metabolite of risperidone and a benzisoxazole derivate with highest concentrations present in the cortex and striatum (Karlsson et al 2005). Additionally, paliperidone shares comparable pharmacodynamic properties and antagonistic profile with risperidone (Mannens et al 1993;Citrome 2007;Dolder et al 2008). For example, paliperidone and risperidone have similar affinities for serotonin-2A (5-HT 2A ) receptor subtype with inhibition constants (K i ) of 0.25 and 0.16, respectively, and with dopamine-2 (D 2 ) receptor subtype with K i of 4.0 (paliperidone) and 3.3 (risperidone; Schotte et al 1996;Dolder et al 2008).…”

Section: Introductionmentioning

confidence: 99%

“…Additionally, paliperidone shares comparable pharmacodynamic properties and antagonistic profile with risperidone (Mannens et al 1993;Citrome 2007;Dolder et al 2008). For example, paliperidone and risperidone have similar affinities for serotonin-2A (5-HT 2A ) receptor subtype with inhibition constants (K i ) of 0.25 and 0.16, respectively, and with dopamine-2 (D 2 ) receptor subtype with K i of 4.0 (paliperidone) and 3.3 (risperidone; Schotte et al 1996;Dolder et al 2008). Furthermore, 5-HT 2A /D 2 affinity ratio has been shown to be very similar between paliperidone (K i =0.06) and risperidone (K i =0.05; Schotte et al, 1996).…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Paliperidone suppresses the development of the aggressive phenotype in a developmentally sensitive animal model of escalated aggression

et al. 2008

View full text Add to dashboard Cite

Rationale Atypical antipsychotics are commonly prescribed to clinically referred youngsters for treatment of heightened aggressive behavior associated with various psychiatric disorders. Previously, we demonstrated risperidone's antiaggressive effects using a well-validated animal model of offensive aggression. Paliperidone, the main active metabolite of risperidone, is a potent serotonin-2A and dopamine-2 receptor antagonist with slightly different pharmacodynamic properties compared to risperidone. Given that much of risperidone's therapeutic efficacy is due to its active metabolite, paliperidone may effectively suppress aggression with fewer adverse side effects. Objectives Investigate whether paliperidone administration would reduce heightened aggressive behavior induced by low-dose cocaine exposure in a developmentally sensitive model of offensive aggression. Materials and methods Male Syrian hamsters (n=12/group) were administered an acute dose of paliperidone (0.05, 0.1, 0.2, and 0.3 mg/kg) and then tested for aggressive behavior using the resident-intruder paradigm. To investigate the effects of chronic paliperidone administration, a separate set of animals (n=12/group) was exposed to repeated paliperidone administration (0.1 mg kg −1 day −1 ) during different developmental periods and varying lengths of time (1-4 weeks). Results Experiment 1 results revealed a dose-dependent decrease in bite and attack behaviors with an effective dose observed at 0.1 mg/kg. In Experiment 2, the maximal reduction in aggressive behavior in response to chronic paliperidone treatment was observed in animals treated during the third week of adolescence, and this reduction occurred without concomitant alterations in non-aggressive behaviors.Conclusions These results support the specific aggressionsuppressing properties of paliperidone and the potential use of this compound in the treatment of maladaptive aggression in clinical settings.

show abstract

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Paliperidone suppresses the development of the aggressive phenotype in a developmentally sensitive animal model of escalated aggression

et al. 2008

View full text Add to dashboard Cite

show abstract

“…It is also used for schizophrenia and schizoaffective disorder. Paliperidone (9-OH-risperidone) is a receptor monoaminergic antagonist that exhibits the characteristic dopamine type 2 (D2) and serotonin (5-hydroxytryptamine 5-HT) type 2A (5-HT2A) antagonism of antipsychotic drugs 4,5 . An extensive literature survey is carried out and very few spectrophotometric 6 methods were found so far.…”

Section: Introductionmentioning

confidence: 99%

Spectrophotometric Methods for the Quantitative Estimation of Paliperidone in Formulations

2014

Chem Sci Trans

View full text Add to dashboard Cite

Two simple, sensitive and economical spectrophotometric methods have been developed and validated for the determination of paliperidone in pharmaceutical dosage forms. The methods were based on the formation of colored complex of Paliperidone with different reagents. The absorbance of the formed colored complex is measured at the wavelength of maximum absorbance of the complex 665 nm and 555 nm respectively against the reagent blank treated similarly. These methods have different linearity ranges observed in the concentration ranges of 1-6 and 10-60 μg/mL with correlation coefficient of 0.998 for both the methods. Statistical analysis indicates that the proposed methods are reproducible and selective for the estimation of Paliperidone in bulk drug and in its tablet dosage form.

show abstract

“…More recently, interest has turned to the active metabolites of atypical antipsychotic drugs in the hope that they might have increased efficacy over the parent drug and a reduced incidence of side effects. The active metabolite of risperidone, 9-OH-risperidone (paliperidone [Invega®]) from Janssen Pharmaceuticals, has recently met FDA approval and is being used clinically for the treatment of schizophrenia in the US (Dlugosz and Nasrallah 2007;Dolder et al 2008). The active metabolite for clozapine, N-desmethylclozapine (Li et al 2005), was being developed by Acadia Pharmaceuticals, as ACP-104, for the treatment of schizophrenia; however, a recent press release (Reuters, June 16 2008) reported that ACP-104 did not display antipsychotic efficacy compared to placebo in Phase IIb clinical trials.…”

Section: Introductionmentioning

confidence: 99%

Discriminative stimulus properties of atypical and typical antipsychotic drugs: a review of preclinical studies

Porter

Prus

2008

Psychopharmacology

View full text Add to dashboard Cite

Background Drug discrimination is an increasingly valuable behavioral assay for the preclinical development of antipsychotic drugs. The majority of studies have used the atypical antipsychotic clozapine because it displays robust discriminative stimulus properties and is the "prototypical" or "gold standard" atypical antipsychotic against which other antipsychotics will undoubtedly be compared for many years. Objectives Pharmacological mechanisms mediating the discriminative stimulus properties of antipsychotics used as training drugs and the usefulness of drug discrimination for distinguishing typical and atypical antipsychotics were reviewed. Results Clozapine appears to have a compound cue involving antagonism of two or more receptors. While muscarinic receptor antagonism is a prominent factor for mediation of clozapine's cue in rats with a 5.0-mg/kg training dose, there are differences in clozapine's cue with a low training dose and in pigeons and mice. With a low training dose, clozapine has consistently produced full or partial generalization to atypical but not to typical antipsychotics. Although not evaluated as extensively, the atypical antipsychotics quetiapine and ziprasidone also appear to generalize to atypical but not typical antipsychotics. This has not been the case for other antipsychotic drugs (olanzapine, chlorpromazine, haloperidol) used as training drugs. Conclusions There are important differences in discriminative stimulus properties both between and within atypical and typical antipsychotics and across species. While lowdose clozapine discrimination in rats appears to provide a more sensitive behavioral assay for distinguishing atypical from typical antipsychotics, the extent to which clozapine's discriminative stimulus properties are predictive of its antipsychotic effects remains to be determined.

show abstract

Paliperidone for schizophrenia

Cited by 68 publications

References 36 publications

Paliperidone suppresses the development of the aggressive phenotype in a developmentally sensitive animal model of escalated aggression

Paliperidone suppresses the development of the aggressive phenotype in a developmentally sensitive animal model of escalated aggression

Spectrophotometric Methods for the Quantitative Estimation of Paliperidone in Formulations

Discriminative stimulus properties of atypical and typical antipsychotic drugs: a review of preclinical studies

Contact Info

Product

Resources

About