title: 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.
abstract: 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 (Cmax ) was slightly less than dose-proportional for both injection sites at PP doses >50 mg eq. Mean Cmax 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 Cmax (tmax ) 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.
authors.affiliation: Janssen Research & Development, Division of Janssen Pharmaceutica NV, Beerse, Belgium.
authors.forename: Adriaan
authors.initials: A
authors.lastname: Cleton
authors.forename: Stefaan
authors.initials: S
authors.lastname: Rossenu
authors.forename: Herta
authors.initials: H
authors.lastname: Crauwels
authors.forename: Joris
authors.initials: J
authors.lastname: Berwaerts
authors.forename: David
authors.initials: D
authors.lastname: Hough
authors.forename: Srihari
authors.initials: S
authors.lastname: Gopal
authors.forename: Marielle
authors.initials: M
authors.lastname: Eerdekens
authors.forename: An
authors.initials: A
authors.lastname: Vandebosch
authors.forename: Bart
authors.initials: B
authors.lastname: Remmerie
authors.forename: Marc
authors.initials: M
authors.lastname: De Meulder
authors.forename: Clara M
authors.initials: CM
authors.lastname: Rosso
mesh_terms: D000328:Adult; D014150:Antipsychotic Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D002081:Buttocks; D005260:Female; D006801:Humans; D007273:Injections, Intramuscular; D007555:Isoxazoles / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D008875:Middle Aged; D018482:Muscle, Skeletal; D000068882:Paliperidone Palmitate; D011569:Psychiatric Status Rating Scales; D011743:Pyrimidines / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D012559:Schizophrenia / Q000188:drug therapy / Q000378:metabolism*; D012782:Shoulder
chemical_list: D014150:Antipsychotic Agents; D007555:Isoxazoles; D011743:Pyrimidines; D000068882:Paliperidone Palmitate
keywords: dose-proportionality; long-acting injectable; paliperidone palmitate; schizophrenia