title: Aripiprazole Once-Monthly 400 mg: Comparison of Pharmacokinetics, Tolerability, and Safety of Deltoid Versus Gluteal Administration.
abstract: Two open-label, randomized, parallel-arm studies compared pharmacokinetics, safety, and tolerability of aripiprazole once-monthly 400 mg following deltoid vs gluteal injection in patients with schizophrenia.
  
  
  
  In the single-dose study, 1 injection of aripiprazole once-monthly 400 mg in the deltoid (n=17) or gluteal (n=18) muscle (NCT01646827) was administered. In the multiple-dose study, the first aripiprazole once-monthly 400 mg injection was administered in either the deltoid (n=71) or gluteal (n=67) muscle followed by 4 once-monthly deltoid injections (NCT01909466).
  
  
  
  After single-dose administration, aripiprazole exposure (area under the concentration-time curve) was similar between deltoid and gluteal administrations, whereas median time to maximum plasma concentration was shorter (7.1 [deltoid] vs 24.1 days [gluteal]) and maximum concentration was 31% higher after deltoid administration. In the multiple-dose study, median time to maximum plasma concentration for deltoid administration was shorter (3.95 vs 7.1 days), whereas aripiprazole mean trough concentrations, maximum concentration, and area under the concentration-time curve were comparable between deltoid and gluteal muscles (historical data comparison). Multiple-dose pharmacokinetic results for the major metabolite, dehydro-aripiprazole, followed a similar pattern to that of the parent drug for both deltoid and gluteal injection sites. Safety and tolerability profiles were similar after gluteal or deltoid injections. Based on observed data, minimum aripiprazole concentrations achieved by aripiprazole once-monthly 400 mg are comparable with those of oral aripiprazole 15 to 20 mg/d.
  
  
  
  The deltoid muscle is a safe alternative injection site for aripiprazole once-monthly 400 mg in patients with schizophrenia.
authors.affiliation: Otsuka Pharmaceutical Development & Commercialization, Inc., Rockville, Maryland; Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, New Jersey; H. Lundbeck A/S, Valby, Denmark; Lundbeck LLC, Deerfield, Illinois.
authors.forename: Arash
authors.initials: A
authors.lastname: Raoufinia
authors.affiliation: Otsuka Pharmaceutical Development & Commercialization, Inc., Rockville, Maryland; Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, New Jersey; H. Lundbeck A/S, Valby, Denmark; Lundbeck LLC, Deerfield, Illinois.
authors.forename: Timothy
authors.initials: T
authors.lastname: Peters-Strickland
authors.affiliation: Otsuka Pharmaceutical Development & Commercialization, Inc., Rockville, Maryland; Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, New Jersey; H. Lundbeck A/S, Valby, Denmark; Lundbeck LLC, Deerfield, Illinois.
authors.forename: Anna-Greta
authors.initials: AG
authors.lastname: Nylander
authors.affiliation: Otsuka Pharmaceutical Development & Commercialization, Inc., Rockville, Maryland; Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, New Jersey; H. Lundbeck A/S, Valby, Denmark; Lundbeck LLC, Deerfield, Illinois.
authors.forename: Ross A
authors.initials: RA
authors.lastname: Baker
authors.affiliation: Otsuka Pharmaceutical Development & Commercialization, Inc., Rockville, Maryland; Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, New Jersey; H. Lundbeck A/S, Valby, Denmark; Lundbeck LLC, Deerfield, Illinois.
authors.forename: Anna
authors.initials: A
authors.lastname: Eramo
authors.affiliation: Otsuka Pharmaceutical Development & Commercialization, Inc., Rockville, Maryland; Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, New Jersey; H. Lundbeck A/S, Valby, Denmark; Lundbeck LLC, Deerfield, Illinois.
authors.forename: Na
authors.initials: N
authors.lastname: Jin
authors.affiliation: Otsuka Pharmaceutical Development & Commercialization, Inc., Rockville, Maryland; Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, New Jersey; H. Lundbeck A/S, Valby, Denmark; Lundbeck LLC, Deerfield, Illinois.
authors.forename: Patricia
authors.initials: P
authors.lastname: Bricmont
authors.affiliation: Otsuka Pharmaceutical Development & Commercialization, Inc., Rockville, Maryland; Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, New Jersey; H. Lundbeck A/S, Valby, Denmark; Lundbeck LLC, Deerfield, Illinois.
authors.forename: Jennifer
authors.initials: J
authors.lastname: Repella
authors.affiliation: Otsuka Pharmaceutical Development & Commercialization, Inc., Rockville, Maryland; Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, New Jersey; H. Lundbeck A/S, Valby, Denmark; Lundbeck LLC, Deerfield, Illinois.
authors.forename: Robert D
authors.initials: RD
authors.lastname: McQuade
authors.affiliation: Otsuka Pharmaceutical Development & Commercialization, Inc., Rockville, Maryland; Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, New Jersey; H. Lundbeck A/S, Valby, Denmark; Lundbeck LLC, Deerfield, Illinois.
authors.forename: Peter
authors.initials: P
authors.lastname: Hertel
authors.affiliation: Otsuka Pharmaceutical Development & Commercialization, Inc., Rockville, Maryland; Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, New Jersey; H. Lundbeck A/S, Valby, Denmark; Lundbeck LLC, Deerfield, Illinois.
authors.forename: Frank
authors.initials: F
authors.lastname: Larsen
mesh_terms: D000293:Adolescent; D000328:Adult; D000704:Analysis of Variance; D014150:Antipsychotic Agents / Q000097:blood* / Q000627:therapeutic use; D019540:Area Under Curve; D000068180:Aripiprazole / Q000097:blood* / Q000627:therapeutic use; D002081:Buttocks / Q000294:innervation*; D004305:Dose-Response Relationship, Drug; D005260:Female; D005500:Follow-Up Studies; D006801:Humans; D007273:Injections, Intramuscular; D008297:Male; D008875:Middle Aged; D012559:Schizophrenia / Q000097:blood* / Q000188:drug therapy; D012782:Shoulder / Q000294:innervation*; D055815:Young Adult
chemical_list: D014150:Antipsychotic Agents; D000068180:Aripiprazole
keywords: antipsychotic; aripiprazole once-monthly 400 mg; injection site; pharmacokinetics; safety/tolerability