A comparison of serum prolactin concentrations after administration of paliperidone extended-release and risperidone tablets in patients with schizophrenia.
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.
Berwaerts
Joris
J
Johnson & Johnson Pharmaceutical Research and Development, Titusville, NJ 08560, USA. JBerwaer@its.jnj.com
Cleton
Adriaan
A
Rossenu
Stefaan
S
Talluri
Krishna
K
Remmerie
Bart
B
Janssens
Luc
L
Boom
Sandra
S
Kramer
Michelle
M
Eerdekens
Mariëlle
M
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
D014150:Antipsychotic Agents; D003692:Delayed-Action Preparations; D007555:Isoxazoles; D011743:Pyrimidines; D011388:Prolactin; D018967:Risperidone; D000068882:Paliperidone Palmitate