title: A comparison of serum prolactin concentrations after administration of paliperidone extended-release and risperidone tablets in patients with schizophrenia.
abstract: Increases in serum prolactin concentrations after administration of risperidone have been attributed, by some, to the availability of paliperidone in plasma. This double-blind, randomized, parallel-group study in patients with schizophrenia compared serum prolactin concentrations following the administration of paliperidone extended-release and risperidone immediate-release tablets. At steady state, the doses administered resulted in a similar exposure to paliperidone and the pharmacologically active fraction of risperidone (i.e. risperidone + paliperidone), respectively. Eligible patients were randomized to either paliperidone extended-release 12 mg on days 1-6 or risperidone immediate-release 2 mg on day 1 and 4 mg on days 2-6. Mean serum prolactin concentrations increased on day 1 (C(max): 71.8 ng/ml and 89.7 ng/ml reached at 6.5 hours and 2.6 hours for paliperidone extended-release and risperidone immediate-release, respectively). On day 6, serum prolactin concentration-time profiles were similar for both treatments, with overall higher serum prolactin concentrations than on day 1 (AUC(0-24 h): 1389 and 842 ng h/ml, and 1306 and 741 ng.h/ml on day 6 and day 1 for paliperidone extended-release and risperidone immediate-release, respectively). These results indicate that paliperidone extended-release 12 mg and risperidone immediate-release 4 mg, administered over a period of 6 days, lead to similar elevations in serum prolactin concentrations.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, Titusville, NJ 08560, USA. JBerwaer@its.jnj.com
authors.forename: Joris
authors.initials: J
authors.lastname: Berwaerts
authors.forename: Adriaan
authors.initials: A
authors.lastname: Cleton
authors.forename: Stefaan
authors.initials: S
authors.lastname: Rossenu
authors.forename: Krishna
authors.initials: K
authors.lastname: Talluri
authors.forename: Bart
authors.initials: B
authors.lastname: Remmerie
authors.forename: Luc
authors.initials: L
authors.lastname: Janssens
authors.forename: Sandra
authors.initials: S
authors.lastname: Boom
authors.forename: Michelle
authors.initials: M
authors.lastname: Kramer
authors.forename: Mariëlle
authors.initials: M
authors.lastname: Eerdekens
mesh_terms: D000293:Adolescent; D000328:Adult; D014150:Antipsychotic Agents / Q000008:administration & dosage / Q000009:adverse effects* / Q000627:therapeutic use; D019540:Area Under Curve; D003692:Delayed-Action Preparations; D004311:Double-Blind Method; D004359:Drug Therapy, Combination; D005260:Female; D006801:Humans; D007024:Hypotension, Orthostatic / Q000139:chemically induced; D007555:Isoxazoles / Q000008:administration & dosage / Q000009:adverse effects* / Q000627:therapeutic use; D008297:Male; D008875:Middle Aged; D000068882:Paliperidone Palmitate; D011388:Prolactin / Q000097:blood*; D011569:Psychiatric Status Rating Scales; D011743:Pyrimidines / Q000008:administration & dosage / Q000009:adverse effects* / Q000627:therapeutic use; D018967:Risperidone / Q000008:administration & dosage / Q000009:adverse effects* / Q000627:therapeutic use; D012559:Schizophrenia / Q000188:drug therapy*; D055815:Young Adult
chemical_list: D014150:Antipsychotic Agents; D003692:Delayed-Action Preparations; D007555:Isoxazoles; D011743:Pyrimidines; D011388:Prolactin; D018967:Risperidone; D000068882:Paliperidone Palmitate