Paliperidone-ER: First atypical antipsychotic with oral extended release formulation

Expert Review of Neurotherapeutics

Volumn 8, Issue 2, 2008, Pages 193-200

  Lautenschlager, Marion ^a   Heinz, Andreas ^a  

^a CHARITÉ UNIVERSITÄTSMEDIZIN BERLIN   (Germany)

Author keywords

9 hydroxyrisperidone; Atypical antipsychotic; Cytochrome P450 2D6 (CYP2D6); Hepatic metabolism; OROS extended release; Paliperidone; Renal elimination; Risperidone

Indexed keywords

3 HYDROXYRISPERIDONE; ATYPICAL ANTIPSYCHOTIC AGENT; DRUG METABOLITE; HYDROMORPHONE; METHYLPHENIDATE; MUSCARINIC RECEPTOR; PALIPERIDONE; PLACEBO; RISPERIDONE; SEROTONIN 2A RECEPTOR; UNCLASSIFIED DRUG;

AKATHISIA; BINDING AFFINITY; CLINICAL FEATURE; CLINICAL STUDY; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG DELIVERY SYSTEM; DRUG EFFICACY; DRUG FORMULATION; DRUG HALF LIFE; DRUG SAFETY; DRUG STRUCTURE; DRUG TOLERABILITY; ELDERLY CARE; EXTRAPYRAMIDAL SYMPTOM; HUMAN; IMPOTENCE; LONG TERM CARE; MONOTHERAPY; MOTOR DYSFUNCTION; NONHUMAN; ORTHOSTATIC HYPOTENSION; PARKINSON DISEASE; PSYCHOSIS; RANDOMIZED CONTROLLED TRIAL; RECURRENT DISEASE; REVIEW; SCHIZOPHRENIA; SIDE EFFECT; SUSTAINED RELEASE PREPARATION; TACHYCARDIA; TARDIVE DYSKINESIA; TREATMENT DURATION; WEIGHT GAIN;

ADMINISTRATION, ORAL; ANIMALS; ANTIPSYCHOTIC AGENTS; CLINICAL TRIALS AS TOPIC; DELAYED-ACTION PREPARATIONS; HUMANS; ISOXAZOLES; PYRIMIDINES; SCHIZOPHRENIA;

EID: 39549095838     PISSN: 14737175     EISSN: 17448360     Source Type: Journal    
DOI: 10.1586/14737175.8.2.193     Document Type: Review

References (29)

1. Aravagiri M, Marder SR. Brain, plasma and tissue pharmacokinetics of risperidone and 9-hydroxyrisperidone after separate oral administration to rats. Psychopharmacology 159, 424-431 (2002).
2. Swanson J, Gupta S, Lam A et al. Development of a new once-a-day formulation of methylphenidate for the treatment of attention-deficit/ hyperactivity disorder: proof-of-concept and proof-ofproduct studies. Arch. Gen. Psychiatry 60(2), 204-211 (2003).
3. Palangio M, Northfelt DW, Portenoy RK et al. Dose conversion and titration with a novel, once-daily, OROS® osmotic technology, extended-release hydromorphone formulation in the treatment of chronic malignant or nonmalignant pain. J. Pain Symptom Manage. 23, 355-368 (2002).
4. Conley R, Sathyan G, Prosser J, Gupta SK. Review of the clinical spectrum of the osmotic-controlled release oral delivery system (OROS® ) and application in central nervous system disorders. Presented at: Collegium Internationale Neuro-Psychopharmacologicum 25th Biennial Congress. Chicago, IL, USA, 9-13 July 2006.
5. Leysen JE, Janssen PM, Megens AA, Schotte A. Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J. Clin. Psychiatry 55(Suppl.), 5-12 (1994).
6. Megens AA, Awouters FH, Schotte A et al. Survey on the pharmacodynamics of the new antipsychotic risperidone. Psychopharmacology 114(1), 9-23 (1994).
7. 2A receptor occupancy and safety profile of paliperidone ER in healthy subjects. Presented at: European College of Neuropsychopharmacology Congress. Amsterdam, The Netherlands, 21-25 October 2005 (Poster).
8. Fang J, Bourin M, Baker GB. Metabolism of risperidone to 9-hydroxyrisperidone by human cytochromes P450 2D6 and 3A4. Naunyn- Schmiedeberg's Arch. Pharmacol. 359, 147-151(1999). •• This study shows the effects of cytochrome P450 inhibition and induction on the metabolism of risperidone.
9. Sachse C, Brockmöller J, Bauer S, Roots I. Cytochrome P450 2D6 variants in a Caucasian population: allele frequencies and phenotypic consequences. Am. J. Hum. Genet. 60, 284-295 (1997).
10. Scordo MG, Spina E, Facciolà G, Avenoso A, Johansson I, Dahl ML. Cytochrome P450 2D6 genotype and steady state plasma levels of risperidone and 9-hydroxyrisperidone. Psychopharmacology 147, 300-305 (1999).
11. Berecz R, Llerena A, de la Rubia A et al. Relationship between risperidone and 9-hydroxy-risperidone plasma concentrations and CYP2D6 enzyme activity in psychiatric patients. Pharmacopsychiatry 35, 231-234 (2002).
12. Mihara K, Kondo T, Yasui-Furukori N et al. Effects of various CYP2D6 genotypes on the steady-state plasma concentrations of risperidone and its active metabolite, 9-hydroxyrisperidone, in Japanese patients with schizophrenia. Ther. Drug Monit. 25(3), 287-293 (2003).
13. Yasui-Furukori N, Mihara K, Kondo T et al. Effects of CYP2D6 genotypes on plasma concentrations of risperidone and enantiomers of 9-hydroxyrisperidone in Japanese patients with schizophrenia. J. Clin. Pharmacol. 43(2), 122-127 (2007).
14. 14C-paliperidone 1 mg in healthy subjects. Presented at: European College of Neuropsychopharmacology Congress. Amsterdam, Netherlands, 21-25 October 2005 (Abstract).
15. Goff DC, Cather C, Evins AE et al. Medical morbidity and mortality in schizophrenia: guidelines for psychiatrists. J. Clin. Psychiatr. 66, 183-194 (2005).
16. Gagnon D, Adriaenssen I, Nasrallah H, Morosini PL. Reliability, validity and sensitivity to change of the Personal and Social Performance scale in patients with stable schizophrenia. Presented at: Collegium Internationale Neuro-Psychopharmacologicum 25th Biennial Congress. Chicago, IL, USA, 9-13 July 2006 (Abstract).
17. Morosini PL, Magliano L, Brambilla L, Ugolini S, Pioli R. Development, reliability and acceptability of a new version of the DSM-IV Social and Occupational Functioning Assessment Scale (SOFAS) to assess routine social functioning. Acta Psychiatr. Scand. 101, 323-329 (2000). •• Contains the original description of the Personal and Social Performance-Score.
18. Kane J, Canas F, Kramer M et al. Treatment of schizophrenia with paliperidone extended-release tablets: a 6-week placebo-controlled trial, Schizophr. Res. 90, 147-161 (2007) • One of three double-blind 6-week studies investigating paliperidone in the treatment of schizophrenia.
19. Davidson M, Emsley R, Kramer M et al. Efficacy, safety and effect on functioning of paliperidone extended-release tablets in schizophrenia: an international 6-week placebo-controlled study. Schizophr. Res. 93, 117-130 (2007). • One of three double-blind 6-week studies investigating paliperidone in the treatment of schizophrenia.
20. Marder SR, Kramer M, Ford L et al. Efficacy and safety of paliperidone extended-release tablets: results of a 6-week, randomized, placebo-controlled study. Biol. Psychiatry 62, 1363-1370 (2007). • One of three double-blind 6-week studies investigating paliperidone in the treatment of schizophrenia.
21. Swartz MS, Perkins OD, Stroup TS et al. Effects of antipsychotic medications on psychosocial functioning in patients with chronic schizophrenia: findings from the NIMH CATIE study. Am. J. Psychiatry 164(3), 428-436 (2007).
22. Meltzer H, Kramer M, Gassmann-Mayer C, Lim P, Bobo W, Eerdekens M. Efficacy and tolerability of oral paliperidone extended-release tablets in the treatment of acute schizophrenia: pooled data from three 6-week placebo-controlled studies. Presented at: Collegium Internationale Neuro-Psychopharmacologicum 25th Biennial Congress. Chicago, IL, USA, 9-13 July 2006.
23. Knegtering R, Baselmans P, Castelein S, Bosker F, Bruggeman R, van den Bosch RJ. Predominant role of the 9-hydroxy metabolite of risperidone in elevating blood prolactin levels. Am. J. Psychiatry 162, 1010-1012 (2005).
24. Melkersson KI. Prolactin elevation of the antipsychotic risperidone is predominantly related to its 9-hydroxy metabolite. Hum. Psychopharmacol. 21, 529-532 (2006).
25. Meyer J, Kramer M, Kostic D, Lane R, Lim P, Eerdekens MM. Metabolic outcomes in patients with schizophrenia treated with oral paliperidone extended-release tablets: pooled analysis of three 6-week placebo-controlled studies. Presented at: Collegium Internationale Neuro-Psychopharmacologicum 25th Biennial Congress. Chicago, IL, USA, 9-13 July 2006.
26. Kramer M, Simpson G, Maciulis V et al. Paliperidone extended-release tablets for prevention of symptom recurrence in patients with schizophrenia. A randomized, double-blind, placebo-controlled study J. Clin. Psychopharmacol. 27, 6-14 (2007). •• Longest long-term study published to date on paliperidone-extended release.
27. Kramer M, Ford L, Gassmann-Mayer C, Lim P, Eerdekens M. A six-week placebo-controlled study on the safety and tolerability of flexible doses of oral paliperidone extended-release tablets in the treatment of schizophrenia in elderly patients. Presented at: American Psychiatric Association Congress. Toronto, Canada, 20-25 May 2006.
28. De Deyn PP, Buitelaar J. Risperidone in the management of agitation and aggression associated with psychiatric disorders. Eur. Psychiatry 21, 21-28 (2006).
29. Bass DM, Prevo M, Waxman DS. Gastrointestinal safety of an extendedrelease, nondeformable, oral dosage form (OROS): a retrospective study. Drug Saf. 25(14), 1021-1033 (2002). •• Thorough retrospective study regarding the safety of the osmotic-controlled release oral delivery system application form.