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A single‐dose, open‐label, parallel, randomized, dose‐proportionality study of paliperidone after intramuscular injections of paliperidone palmitate in the deltoid or gluteal muscle in patients with schizophrenia
Author(s) -
Cleton Adriaan,
Rossenu Stefaan,
Crauwels Herta,
Berwaerts Joris,
Hough David,
Gopal Srihari,
Eerdekens Marielle,
Vandebosch An,
Remmerie Bart,
De Meulder Marc,
Fernández Clara M. Rosso
Publication year - 2014
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/jcph.295
Subject(s) - paliperidone palmitate , deltoid curve , medicine , deltoid muscle , intramuscular injection , paliperidone , urology , area under the curve , anesthesia , surgery , risperidone , schizophrenia (object oriented programming) , psychiatry
Paliperidone palmitate (PP) is a long‐acting injectable (LAI) antipsychotic, developed for monthly intramuscular (i.m.) administration into deltoid/gluteal muscle, approved for the treatment of schizophrenia in many countries. To assess the options for i.m. injection sites, dose‐proportionality of PP was investigated after injection of a single dose (25–150 mg eq.) of PP in either gluteal (n = 106) or deltoid (n = 95) muscle of schizophrenic patients. Overall, mean (geometric) area under plasma concentration–time curve from time zero to infinity (AUC ∞ ) of paliperidone increased proportionally with increasing PP doses, regardless of injection site. Mean maximum plasma concentration (C max ) was slightly less than dose‐proportional for both injection sites at PP doses >50 mg eq. Mean C max was higher after injection in the deltoid compared with the gluteal muscle, except for the 100 mg eq. dose, while AUC ∞ for both injection sites was comparable at all doses. Median time to reach C max (t max ) ranged from 13–14 days after deltoid and 13–17 days after gluteal injection across all doses. Single PP injections in deltoid and gluteal muscles in the dose range of 25–150 mg eq. were generally tolerable both locally and systemically.

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