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. 2019 Jun 28:12:1925-1936.
doi: 10.2147/JPR.S197348. eCollection 2019.

First evaluation of tapentadol oral solution for the treatment of moderate to severe acute pain in children aged 6 to <18

Julia C Finkel  1 , Jutta Goldberg  2 , Ronald Rosenburg  2 , Jay Ariyawansa  3 , Tao Sun  3 , Rachel Ochs-Ross  3 , Peter Zannikos  3 , Liping Zhang  3 , Mila Etropolski  3
Affiliations

First evaluation of tapentadol oral solution for the treatment of moderate to severe acute pain in children aged 6 to <18

Julia C Finkel et al. J Pain Res. .

Abstract

Background: This is the first clinical trial in the global pediatric clinical development program for the use of the analgesic tapentadol in children and adolescents.

Patients and methods: This multicenter, open-label clinical trial investigated pharmacokinetics, safety and tolerability, and efficacy of tapentadol and its major metabolite tapentadol-O-glucuronide after administration of a single dose of tapentadol oral solution (OS) in pediatric patients aged 6 to <18 years experiencing moderate to severe acute pain after surgery. Efficacy (change in pain intensity after tapentadol intake) was assessed in an exploratory manner using the McGrath Color Analog Scale and Faces Pain Scale-Revised. Adverse events were monitored throughout the trial.

Results: Forty-four patients who received a single dose of 1 mg/kg tapentadol OS were included in this investigation. Maximum serum concentrations of tapentadol (111 ng/mL) and tapentadol-O-glucuronide (2,400 ng/mL) observed in this trial were within the range of individual maximum concentrations observed in healthy adults administered a comparable dose (range for tapentadol 23.2-129 ng/mL, for tapentadol-O-glucuronide 1,040-4,070 ng/mL). Following tapentadol administration, pain intensity scores improved from baseline at all timepoints. Treatment-emergent adverse events, none of which were serious, were experienced by 45.5% of the patients; the most commonly reported were vomiting (29.5%) and nausea (9.1%).

Conclusions: Tapentadol OS administered as a single dose of 1 mg/kg in children aged 6 to <18 years was generally well tolerated and produced similar serum concentrations as administration of 50-100 mg tapentadol immediate-release tablets in adults. A decrease in postsurgical pain was observed using exploratory subject-reported pain assessments. Tapentadol OS may provide a new treatment option in the management of moderate to severe acute pain in children and adolescents.

Keywords: acute pain; children; efficacy and safety; pharmacokinetics; tapentadol; µ-opioid.

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Conflict of interest statement

Jutta Goldberg is an employee of Grünenthal GmbH. Ronald Rosenburg was an employee of Grünenthal GmbH at the time the trial was conducted. Jay Ariyawansa, Tao Sun, Rachel Ochs-Ross, Peter Zannikos, Liping Zhang, and Mila Etropolski are employees of Janssen Pharmaceutical. Julia C Finkel reports grants from Janssen, during the conduct of the study. The authors report no other conflicts of interest in this work.

Figures

Figure 1
Figure 1
Individual serum concentrations of tapentadol in pediatric patients in the age groups from 12 to <18 years (N=30) and from 6 to <12 years (N=14).
Figure 2
Figure 2
Mean pain intensity over time in (A) patients aged from 12 to <18 years and (B) patients aged from 6 to <12 years. Abbreviations: CAS, Color Analog Scale; EOT, end of trial; EW, early withdrawal.
See this image and copyright information in PMC

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