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Chemical Compound Review

Invega     3-[2-[4-(6- fluorobenzo[d]isoxazol-3-yl)- 1...

Synonyms: Paliperidone, PALLIPERIDONE, CHEMBL1621, Invega (TN), SureCN436689, ...
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Disease relevance of R 76477


Psychiatry related information on R 76477


High impact information on R 76477


Biological context of R 76477


Anatomical context of R 76477


Associations of R 76477 with other chemical compounds


Gene context of R 76477


Analytical, diagnostic and therapeutic context of R 76477

  • Endpoint steady-state plasma levels of risperidone and 9-hydroxyrisperidone were analyzed by high performance liquid chromatography with ultraviolet detection [21].
  • The primary efficacy variable was the time of first recurrence of schizophrenia symptoms, which included predefined changes in symptom scores, psychiatric hospitalization, self-injury, and suicidal or aggressive behavior during the double-blind phase (paliperidone ER or placebo treatment) [22].
  • In this randomized, double-blind, placebo-controlled, multicenter study, patients' symptoms were stabilized during an 8-week run-in and a 6-week stabilization phases using open-label, flexibly dosed paliperidone ER (3-15 mg once daily, starting dose = 9 mg) [22].
  • The interaction of risperidone, 9-hydroxyrisperidone (the principal active metabolite), and clozapine with neurotransmitter receptors was investigated in vitro using animal brain tissue homogenates and cloned human receptors expressed in cells and ex vivo using quantitative receptor autoradiography in rat and guinea pig brain sections [15].
  • The patients received risperidone orally (dose range, 0.5-11 mg per day) and had concentrations of risperidone and the active metabolite 9-hydroxyrisperidone measured at steady state by a new, rapid, and sensitive method of high-performance liquid chromatography (HPLC) [23].


  1. Effects of various CYP2D6 genotypes on the steady-state plasma concentrations of risperidone and its active metabolite, 9-hydroxyrisperidone, in Japanese patients with schizophrenia. Mihara, K., Kondo, T., Yasui-Furukori, N., Suzuki, A., Ishida, M., Ono, S., Kubota, T., Iga, T., Takarada, Y., de Vries, R., Kaneko, S. Therapeutic drug monitoring. (2003) [Pubmed]
  2. Plasma concentrations of risperidone and 9-hydroxyrisperidone during combined treatment with paroxetine. Spina, E., Avenoso, A., Facciolà, G., Scordo, M.G., Ancione, M., Madia, A. Therapeutic drug monitoring. (2001) [Pubmed]
  3. Effect of fluvoxamine on plasma risperidone concentrations in patients with schizophrenia. D'Arrigo, C., Migliardi, G., Santoro, V., Morgante, L., Muscatello, M.R., Ancione, M., Spina, E. Pharmacol. Res. (2005) [Pubmed]
  4. Cytochrome P450 3A inhibitor itraconazole affects plasma concentrations of risperidone and 9-hydroxyrisperidone in schizophrenic patients. Jung, S.M., Kim, K.A., Cho, H.K., Jung, I.G., Park, P.W., Byun, W.T., Park, J.Y. Clin. Pharmacol. Ther. (2005) [Pubmed]
  5. Effect of verapamil on pharmacokinetics and pharmacodynamics of risperidone: in vivo evidence of involvement of P-glycoprotein in risperidone disposition. Nakagami, T., Yasui-Furukori, N., Saito, M., Tateishi, T., Kaneo, S. Clin. Pharmacol. Ther. (2005) [Pubmed]
  6. Pharmacokinetics of the novel antipsychotic agent risperidone and the prolactin response in healthy subjects. Huang, M.L., Van Peer, A., Woestenborghs, R., De Coster, R., Heykants, J., Jansen, A.A., Zylicz, Z., Visscher, H.W., Jonkman, J.H. Clin. Pharmacol. Ther. (1993) [Pubmed]
  7. Dose-dependent interaction of paroxetine with risperidone in schizophrenic patients. Saito, M., Yasui-Furukori, N., Nakagami, T., Furukori, H., Kaneko, S. Journal of clinical psychopharmacology. (2005) [Pubmed]
  8. A colloidal graphite-coated emitter for sheathless capillary electrophoresis/nanoelectrospray ionization mass spectrometry. Zhu, X., Thiam, S., Valle, B.C., Warner, I.M. Anal. Chem. (2002) [Pubmed]
  9. Cytochrome P450 2D6 genotype and steady state plasma levels of risperidone and 9-hydroxyrisperidone. Scordo, M.G., Spina, E., Facciolà, G., Avenoso, A., Johansson, I., Dahl, M.L. Psychopharmacology (Berl.) (1999) [Pubmed]
  10. Pharmacokinetics and tolerability of long-acting risperidone in schizophrenia. Eerdekens, M., Van Hove, I., Remmerie, B., Mannaert, E. Schizophr. Res. (2004) [Pubmed]
  11. Effect of venlafaxine on the pharmacokinetics of risperidone. Amchin, J., Zarycranski, W., Taylor, K.P., Albano, D., Klockowski, P.M. Journal of clinical pharmacology. (1999) [Pubmed]
  12. The complexity of active metabolites in therapeutic drug monitoring of psychotropic drugs. Hendset, M., Haslemo, T., Rudberg, I., Refsum, H., Molden, E. Pharmacopsychiatry (2006) [Pubmed]
  13. Metabolism of risperidone to 9-hydroxyrisperidone by human cytochromes P450 2D6 and 3A4. Fang, J., Bourin, M., Baker, G.B. Naunyn Schmiedebergs Arch. Pharmacol. (1999) [Pubmed]
  14. Transfer of risperidone and 9-hydroxyrisperidone into human milk. Ilett, K.F., Hackett, L.P., Kristensen, J.H., Vaddadi, K.S., Gardiner, S.J., Begg, E.J. The Annals of pharmacotherapy. (2004) [Pubmed]
  15. Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. Leysen, J.E., Janssen, P.M., Megens, A.A., Schotte, A. The Journal of clinical psychiatry. (1994) [Pubmed]
  16. Comparison of prolactin concentrations between haloperidol and risperidone treatments in the same female patients with schizophrenia. Yasui-Furukori, N., Kondo, T., Suzuki, A., Mihara, K., Kaneko, S. Psychopharmacology (Berl.) (2002) [Pubmed]
  17. Pharmacokinetic and safety assessments of concurrent administration of risperidone and donepezil. Zhao, Q., Xie, C., Pesco-Koplowitz, L., Jia, X., Parier, J.L. Journal of clinical pharmacology. (2003) [Pubmed]
  18. Different enantioselective 9-hydroxylation of risperidone by the two human CYP2D6 and CYP3A4 enzymes. Yasui-Furukori, N., Hidestrand, M., Spina, E., Facciolá, G., Scordo, M.G., Tybring, G. Drug Metab. Dispos. (2001) [Pubmed]
  19. Paliperidone for treatment of schizophrenia. Nussbaum, A.M., Stroup, T.S. Schizophr. Bull (2008) [Pubmed]
  20. Effects of various factors on steady-state plasma concentrations of risperidone and 9-hydroxyrisperidone: lack of impact of MDR-1 genotypes. Yasui-Furukori, N., Mihara, K., Takahata, T., Suzuki, A., Nakagami, T., De Vries, R., Tateishi, T., Kondo, T., Kaneko, S. British journal of clinical pharmacology. (2004) [Pubmed]
  21. Risperidone in acutely exacerbated schizophrenia: dosing strategies and plasma levels. Lane, H.Y., Chiu, W.C., Chou, J.C., Wu, S.T., Su, M.H., Chang, W.H. The Journal of clinical psychiatry. (2000) [Pubmed]
  22. Paliperidone extended-release tablets for prevention of symptom recurrence in patients with schizophrenia: a randomized, double-blind, placebo-controlled study. Kramer, M., Simpson, G., Maciulis, V., Kushner, S., Vijapurkar, U., Lim, P., Eerdekens, M. Journal of clinical psychopharmacology (2007) [Pubmed]
  23. Therapeutic drug monitoring of risperidone using a new, rapid HPLC method: reappraisal of interindividual variability factors. Balant-Gorgia, A.E., Gex-Fabry, M., Genet, C., Balant, L.P. Therapeutic drug monitoring. (1999) [Pubmed]
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