Pharmacokinetic profile after multiple deltoid or gluteal intramuscular injections of paliperidone palmitate in patients with schizophrenia. Issue 4 (28th August 2014)

• Record Type: Journal Article
• Authors: Rossenu, Stefaan; Cleton, Adriaan; Hough, David; Crauwels, Herta; Vandebosch, An; Berwaerts, Joris; Eerdekens, Marielle; Herben, Virginie; De Meulder, Marc; Remmerie, Bart; Francetic, Igor
• Is Part Of: Clinical pharmacology in drug development. Volume 4:Issue 4(2015:Jul./Aug.)
• Page Start: 270
• Page End: 278
• Publication Date: 2014-08-28
• Subjects: Drugs -- Testing -- Periodicals; Drug development -- Periodicals; Clinical pharmacology -- Periodicals; 615.580724
• DOI: 10.1002/cpdd.144
• Languages: English
• ISSNs: 2160-7648

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <sec id="cpdd144-sec-0001" sec-type="section"> <p>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 AUC_τ and C_max, compared with the gluteal muscle (geometric mean AUC_τ‐based ratio: 120% [90% CI: 93.1–154.7%], and geometric mean C_max‐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 t_max 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.</p> </sec> </abstract>