Dosing and switching strategies for paliperidone palmitate: Based on population pharmacokinetic modelling and clinical trial data

CNS Drugs

Volumn 25, Issue 10, 2011, Pages 829-845

  Samtani, Mahesh N ^a   Gopal, Srihari ^a   Gassmann Mayer, Cristiana ^a   Alphs, Larry ^b   Palumbo, Joseph M ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

^b JANSSEN RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Intramuscular; Liver dysfunction; Paliperidone; Pharmacokinetic modelling; Population pharmacokinetics; Renal impairment; Schizophrenia.

Indexed keywords

DOPAMINE 2 RECEPTOR; NEUROLEPTIC AGENT; PALIPERIDONE; RISPERIDONE;

BODY MASS; BODY WEIGHT; CREATININE CLEARANCE; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG HALF LIFE; DRUG SENSITIVITY; DRUG SUBSTITUTION; DRUG TOLERABILITY; GENDER; HUMAN; KIDNEY DISEASE; LIVER DISEASE; PRIORITY JOURNAL; REVIEW;

ANTIPSYCHOTIC AGENTS; CLINICAL TRIALS AS TOPIC; HUMANS; INJECTIONS, INTRAMUSCULAR; ISOXAZOLES; MODELS, BIOLOGICAL; PALMITATES; SCHIZOPHRENIA;

EID: 80053043482     PISSN: 11727047     EISSN: 11791934     Source Type: Journal    
DOI: 10.2165/11591690-000000000-00000     Document Type: Review

References (42)

1. American Psychiatric Association. Diagnostic and statistical manual of mental disorders. 4th ed. Arlington (VA): American Psychiatric Publishing, Inc., 1994
2. Keith SJ, Kane JM. Partial compliance and patient consequences in schizophrenia: our patients can do better. J Clin Psychiatry 2003 Nov; 64 (11): 1308-15 (Pubitemid 37490235)
3. Andreasen NC. Symptoms, signs, and diagnosis of schizophrenia. Lancet 1995 Aug; 346 (8973): 477-81
4. Invega Sustenna™: US prescribing information [online]. Available from URL: http://www.invegasustenna.com/in vegasustenna/shared/pi/ invegasustenna.pdf [Accessed 2009 Sep]
5. Bloch Y, Mendlovic S, Strupinsky S, et al. Injections of depot antipsychotic medications in patients suffering from schizophrenia: do they hurt? J Clin Psychiatry 2001 Nov; 62 (11): 855-9 (Pubitemid 33131171)
6. Lindenmayer JP, Jarboe K, Bossie CA, et al. Minimal injection site pain and high patient satisfaction during treatment with long-acting risperidone. Int Clin Psychopharmacol 2005 Jul; 20 (4): 213-21 (Pubitemid 40896376)
7. Lasser R, Bossie C, Gharabawi G, et al. Patients with schizophrenia previously stabilized on conventional depot antipsychotics experience significant clinical improvements following treatment with long-acting risperidone. Eur Psychiatry 2004 Jun; 19: 219-25 (Pubitemid 38766136)
8. Gopal S, Gassmann-Mayer C, Palumbo J, et al. Practical guidance for dosing and switching paliperidone palmitate treatment in patients with schizophrenia. Curr Med Res Opin 2010 Feb; 26 (2): 377-87
9. Gopal S, Lindenmayer J, Hough D, et al. Safety and tolerability profiles of paliperidone palmitate injected into either the deltoid or gluteus muscle in patients with schizophrenia. 60th Annual Meeting of the Institute of Psychiatric Services; 2008 May 3-8; Chicago (IL)
10. Nasrallah H, Gopal S, Gassman-Mayer C, et al. Efficacy and safety of three doses of paliperidone palmitate, an investigational long-acting injectable antipsychotic, in schizophrenia [poster no. 125]. 60th AnnualMeeting of the Institute of Psychiatric Services; 2008 May 3-8; Chicago (IL)
11. Kramer M, Litman R, Lane R, et al. Efficacy and tolerability of paliperidone palmitate: 9-week, placebocontrolled study in schizophrenia patients. Biol Psychiatry 2008; 63: 1S-319S
12. Hough D, Lindenmayer JP, Gopal S, et al. Safety and tolerability of deltoid and gluteal injections of paliperidone palmitate in schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry 2009 Aug; 33 (6): 1022-31
13. Pandina G, Lindenmayer J, Lull J, et al. A randomized, double-blind, placebo-controlled, dose-response study to assess efficacy and safety of paliperidone palmitate in adult subjects with schizophrenia [poster no. 31]. Annual Meeting of the International Congress of Schizophrenia Research; 2009 Mar 27-28; San Diego (CA)
14. Samtani M, Gopal S, Kern Sliwa J, et al. Paliperidone palmitate dosing in special populations: guidance based on pharmacokinetic modeling and simulation [poster no. K4]. American Conference on Pharmacometrics; 2009 Oct 4-7; Mashantucket (CT)
15. Samtani M, Gopal S, Kern Sliwa J, et al. Management of missed paliperidone palmitate doses based on pharmacokinetic modeling and simulation [poster no. II-62]. New Clinical Drug Evaluation Unit Annual Meeting; 2009 Jun 29-Jul 2; Hollywood (FL)
16. Samtani M, Gopal S, Kern Sliwa J, et al. Switching to paliperidone palmitate from other antipsychotics: guidance based on pharmacokinetic modeling and simulations [poster no. I-68]. New Clinical Drug Evaluation Unit Annual Meeting; 2009 Jun 29-Jul 2; Hollywood (FL)
17. Samtani M, Haskins J, Alphs L, et al. Maintenance dosing of once-monthly (4-weekly) paliperidone palmitate in schizophrenia: pharmacokinetic rationale based on population simulations [poster no. 21]. Annual Meeting of the College of Psychiatric and Neurologic Pharmacists; 2009 Apr 19-20; Jacksonville (FL)
18. Samtani M, Kern Sliwa J, Haskins J, et al. Initiation dosing of deltoid intramuscular paliperidone palmitate in schizophrenia: pharmacokinetic rationale based on modeling and simulation [poster no. 19]. Annual Meeting of the College of Psychiatric and Neurologic Pharmacists; 2009 Apr 19-20; Jacksonville (FL)
19. Samtani M, Vermeulen A, Stuyckens K. Population pharmacokinetics of intramuscular paliperidone palmitate in patients with schizophrenia: a novel once-monthly longacting formulation of atypical antipsychotic. Clin Pharmacokinet 2009 Sep; 48 (9): 585-600
20. Cirincione B, Redman M, Fiedler-Kelley J, et al. Population pharmacokinetics of paliperidone ER in healthy subjects and patients with schizophrenia [poster no. PI-21]. Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics; 2007 Mar 21-24; Anaheim (CA)
21. Samtani M, Gopal S, Kern Sliwa J, et al. Switching to paliperidone palmitate from other depot antipsychotics: guidance based on pharmacokinetic simulations [abstract no. 1839]. Annual Meeting of the Population Approach Group in Europe; 2010 Jun 9-11; Berlin
22. Karlsson P, Dencker E, Nyberg S, et al. Pharmacokinetics and dopamine D2 and serotonin 5-HT2A receptor occupancy of paliperidone in healthy subjects: two open-label single-dose studies [abstract no. PIII-57]. Clin Pharm Ther 2006; 79 (2): 74
23. Nordstrom AL, Farde L, Wiesel FA, et al. Central D2-dopamine receptor occupancy in relation to antipsychotic drug effects: a double-blind PET study of schizophrenic patients. Biol Psychiatry 1993 Feb; 33 (4): 227-35 (Pubitemid 23091497)
24. Nyberg S, Farde L, Halldin C, et al. D2 dopamine receptor occupancy during low-dose treatment with haloperidol decanoate. Am J Psychiatry 1995 Feb; 152 (2): 173-8
25. Kapur S, Remington G, Jones C, et al. High levels of dopamine D2 receptor occupancy with low-dose haloperidol treatment: a PET study. Am J Psychiatry 1996 Jul; 153 (7): 948-50 (Pubitemid 26225470)
26. Cleton A, Rossenu S, Crauwels H, et al. Assessment of the dose proportionality of paliperidone palmitate 25, 50, 100 and 150mg eq., a new long-acting injectable antipsychotic, following administration in the deltoid or gluteal muscles [poster no. PI-74]. Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics; 2008 Apr 2-5; Orlando (FL)
27. Cleton A, Rossenu S, Hough D, et al. Evaluation of the pharmacokinetic profile of deltoid versus gluteal intramuscular injections of paliperidone palmitate in patients with schizophrenia [poster no. PI-75]. Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics; 2008 Apr 2-5; Orlando (FL)
28. Invega™: US prescribing information [online]. Available from URL: http://www.janssencns.com/invega-prescribinginformation [Accessed 2011 Jul 21]
29. Fleischhacker W, Gopal S, Samtani M, et al. Optimization of the dosing strategy for the long-acting injectable antipsychotic paliperidone palmitate: results of two randomized double-blind studies and population pharmacokinetic simulations [poster no. 21]. Annual Meeting of American College of Neuropsychopharmcologists; 2008 Dec 7-11; Scottsdale (AZ)
30. Ereshefsky L. Pharmacokinetics and drug interactions: update for new antipsychotics. J Clin Psychiatry 1996; 57 Suppl. 11: 12-25 (Pubitemid 26389782)
31. Mauri MC, Volonteri LS, Colasanti A, et al. Clinical pharmacokinetics of atypical antipsychotics: a critical review of the relationship between plasma concentrations and clinical response. Clin Pharmacokinet 2007; 46 (5): 359-88 (Pubitemid 46686464)
32. VermeirM, Boom S, Naessens I, et al. Absorption, metabolism and excretion of paliperidone, a new monoaminergic antagonist, in humans.DrugMetab Dispos 2008Apr; 36 (4): 769-79 (Pubitemid 351468385)
33. Wikipidea, The Free Encyclopedia. Typical antipsychotic [online]. Available from URL: http://enwikipediaorg/wiki/Typical-antipsychotic [Accessed 2009 Aug 27]
34. Altamura AC, Sassella F, Santini A, et al. Intramuscular preparations of antipsychotics: uses and relevance in clinical practice. Drugs 2003; 63 (5): 493-512 (Pubitemid 36337728)
35. Levron JC, Ropert R. Clinical pharmacokinetics of haloperidol decanoate: comparison with other prolonged-action neuroleptics. L'Encephale 1987 Mar-Apr; 13 (2): 83-7 (Pubitemid 17073995)
36. Kane JM, Aguglia E, Altamura AC, et al. Guidelines for depot antipsychotic treatment in schizophrenia: European Neuropsychopharmacology Consensus Conference in Siena, Italy. Eur Neuropsychopharmacol 1998 Feb; 8 (1): 55-66
37. Gefvert O, Eriksson B, Persson P, et al. Pharmacokinetics and D2 receptor occupancy of long-acting injectable risperidone (Risperdal Consta™) in patients with schizophrenia. Int J Neuropsychopharmacol 2005 Mar; 8 (1): 27-36 (Pubitemid 40388811)
38. Boom S, Thyssen A, Crauwels H, et al. The influence of hepatic impairment on the pharmacokinetics of paliperidone. Int J Clin Pharmacol Ther 2009 Oct; 47 (10): 606-16
39. Jann MW, Ereshefsky L, Saklad SR. Clinical pharmacokinetics of the depot antipsychotics. Clin Pharmacokinet 1985 Jul-Aug; 10 (4): 315-33 (Pubitemid 15005994)
40. Ereshefsky L, Saklad SR, Tran-Johnson T, et al. Kinetics and clinical evaluation of haloperidol decanoate loading dose regimen. Psychopharmacol Bull 1990; 26 (1): 108-14 (Pubitemid 20322255)
41. Ereshefsky L, Toney G, Saklad SR, et al. A loading-dose strategy for converting from oral to depot haloperidol. Hosp Community Psychiatry 1993 Dec; 44 (12): 1155-61 (Pubitemid 24002835)
42. Wei FC, Jann MW, Lin HN, et al. A practical loading dose method for converting schizophrenic patients from oral to depot haloperidol therapy. J Clin Psychiatry 1996 Jul; 57 (7): 298-302 (Pubitemid 26251109)