title: Pharmacokinetic profile after multiple deltoid or gluteal intramuscular injections of paliperidone palmitate in patients with schizophrenia.
abstract: Paliperidone palmitate (PP) is a once-monthly long-acting injectable antipsychotic approved for the treatment of schizophrenia in many countries. To evaluate the different injection-site options, we compared the pharmacokinetic profile of paliperidone after multiple injections of PP 100 mg eq. (156 mg of PP, equivalent to 100 mg of paliperidone) on days 1, 8, 36, and 64 into the deltoid (n = 24) or gluteal muscle (n = 25) in patients with schizophrenia. After four injections in the deltoid muscle, paliperidone exposure was higher for AUCτ and Cmax , compared with the gluteal muscle (geometric mean AUCτ -based ratio: 120% [90% CI: 93.1-154.7%], and geometric mean Cmax -based ratio: 130% [90% CI: 100.6-168.9%]). The mean [SD] fluctuation index was higher, with a larger interpatient variability, after deltoid-injections (75.9% [30.9%]) than gluteal-injections (58.5% [14.3%]). The median tmax was similar for both sites. PP was generally tolerable in patients, with more favorable local-site tolerability for gluteal-injection. In conclusion, to achieve therapeutic-concentrations quickly, the first-two injections of PP are best administered into the deltoid muscle, whereas thereafter maintenance-injections can be administered either in the deltoid or gluteal muscle.
authors.affiliation: Division of Janssen Pharmaceutica NV, Janssen Research & Development, Beerse, Belgium.
authors.forename: Stefaan
authors.initials: S
authors.lastname: Rossenu
authors.affiliation: Division of Janssen Pharmaceutica NV, Janssen Research & Development, Beerse, Belgium.
authors.forename: Adriaan
authors.initials: A
authors.lastname: Cleton
authors.affiliation: Janssen Research & Development, LLC, Raritan, NJ, USA.
authors.forename: David
authors.initials: D
authors.lastname: Hough
authors.affiliation: Division of Janssen Pharmaceutica NV, Janssen Research & Development, Beerse, Belgium.
authors.forename: Herta
authors.initials: H
authors.lastname: Crauwels
authors.affiliation: Division of Janssen Pharmaceutica NV, Janssen Research & Development, Beerse, Belgium.
authors.forename: An
authors.initials: A
authors.lastname: Vandebosch
authors.affiliation: Janssen Research & Development, LLC, Raritan, NJ, USA.
authors.forename: Joris
authors.initials: J
authors.lastname: Berwaerts
authors.affiliation: Division of Janssen Pharmaceutica NV, Janssen Research & Development, Beerse, Belgium.
authors.forename: Marielle
authors.initials: M
authors.lastname: Eerdekens
authors.affiliation: Division of Janssen Pharmaceutica NV, Janssen Research & Development, Beerse, Belgium.
authors.forename: Virginie
authors.initials: V
authors.lastname: Herben
authors.affiliation: Division of Janssen Pharmaceutica NV, Janssen Research & Development, Beerse, Belgium.
authors.forename: Marc
authors.initials: M
authors.lastname: De Meulder
authors.affiliation: Division of Janssen Pharmaceutica NV, Janssen Research & Development, Beerse, Belgium.
authors.forename: Bart
authors.initials: B
authors.lastname: Remmerie
authors.affiliation: Institute of Clinical Pharmacology, Clinical Hospital Centre, Zagreb, Croatia.
authors.forename: Igor
authors.initials: I
authors.lastname: Francetic
mesh_terms: D000293:Adolescent; D000328:Adult; D000368:Aged; D014150:Antipsychotic Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002081:Buttocks; D017523:Croatia; D057645:Deltoid Muscle; D016903:Drug Monitoring / Q000379:methods; D005260:Female; D006801:Humans; D007273:Injections, Intramuscular; D008297:Male; D008657:Metabolic Clearance Rate; D008875:Middle Aged; D000068882:Paliperidone Palmitate / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D012559:Schizophrenia / Q000097:blood / Q000175:diagnosis / Q000188:drug therapy*; D012565:Schizophrenic Psychology; D016896:Treatment Outcome; D055815:Young Adult
chemical_list: D014150:Antipsychotic Agents; D000068882:Paliperidone Palmitate
keywords: atypical long-acting injectable; deltoid and gluteal muscle; paliperidone palmitate; pharmacokinetics; schizophrenia