Population Pharmacokinetics of a Novel Once-Every 3 Months Intramuscular Formulation of Paliperidone Palmitate in Patients with Schizophrenia

Abstract

The final model with two saturable absorption processes provided a good description of the pharmacokinetic characteristics of paliperidone after intramuscular administration of its long-acting 3-month formulation palmitate ester. In addition to the structural covariates (creatinine clearance on CL, body mass index on V, and injection volume on both absorption rates), injection site and sex were identified as covariates on k of the slow absorption process (k). Clinical trial registration numbers: NCT01559272, NCT01529515, and NCT01515423.

Time to onset and time to resolution of extrapyramidal symptoms in patients with exacerbated schizophrenia treated with 3-monthly vs once-monthly paliperidone palmitate

“…This is consistent with PK modeling that demonstrated similar plasma exposure between equivalent doses of the two formulations. 17 , 18 During the DB phase, EPS-related TEAE rates were generally numerically lower for both PP3M and PP1M compared with the first 17 weeks (OL phase), consistent with previous observations of EPS-related TEAE rates for PP1M. 9 , 12 , 19 There were no consistent, substantial, or significant differences in the overall incidence of EPS-related TEAEs, TTO, and TTR between the PP3M- and PP1M-treated groups.…”

“… 8 Peak drug plasma concentrations were achieved within 30–33 days after a single injection of PP3M over the dose range of 175–525 mg eq. 17 Yet, the incidence of EPS-related TEAEs was similar between the PP3M and PP1M treatment groups; furthermore, TTO and TTR of EPS were also not meaningfully longer for PP1M.…”

Evaluations of muscle echogenicities in patients treated with second generation long acting injectable antipsychotics

“…Yuko YASUHARA 1) , Tetsuya TANIOKA 1) , Kensaku TAKASE 2) , Yueren ZHAO 3) , Kazushi MOTOKI 4) , Takaharu AZEKAWA Risperidone long-acting injection (RLAI) 4,5) was the first SG-LAI. Since then, two other SG-LAIs, paliperidone LAI (PLAI 6) ), and aripiprazole LAI (ALAI) 7) have become available in Japan.…”

“…These LAIs are administered by intramuscular (IM) injection. A single injection effect lasts within the range of 1 week to 3 months, depending on the compound and formulation 2,3) .…”

“…These LAIs are administered by intramuscular (IM) injection. A single injection effect lasts within the range of 1 week to 3 months, depending on the compound and formulation 2,3) . Our previous study evaluated the B-mode findings of the muscle infiltrated with second generation long acting injectable antipsychotics (SG-LAIs).…”