Literature DB >> 20875374

A thorough QT/QTc study of multiple doses of tapentadol immediate release in healthy subjects.

C Oh1, J Rengelshausen, B Mangold, M Etropolski, C Rauschkolb, S S Wang, D Upmalis, T Häufel.   

Abstract

OBJECTIVE: This randomized, double-blind, placebo- and positive-controlled 4-way crossover study evaluated the effects of tapentadol immediate release (IR) on the QT/QTc interval.
MATERIALS AND METHODS: Healthy subjects received tapentadol IR 100 mg or 150 mg, or placebo, every 6 h on Days 1 and 2, with a >= 7-day washout between treatments. Moxifloxacin 400 mg was the positive control. Serial triplicate 12-lead electrocardiograms (ECGs) were performed; the Fridericia correction (QTcF) was the primary correction method. Serial blood sampling was performed for pharmacokinetic analyses.
RESULTS: Of the 75 subjects who were randomized, 68 received at least 1 dose of study medication, and 59 completed the study. Upper limits of the 90% confidence intervals (CIs) for the difference in mean DeltaQTcF between tapentadol IR 100 or 150 mg and placebo were < 10 ms (non-inferiority criterion) for all time points. The lower limit of the 90% CI for mean DeltaQTcF between moxifloxacin and placebo exceeded 5 ms from 1 to 6 h after dosing, establishing assay sensitivity. No subject had a postdose QTc interval > 480 ms, change from baseline > 60 ms, or clinically relevant change in heart rate or other ECG variables. Steady-state concentrations were reached within 18 to 24 h. Common adverse events were vertigo (central nervous system (CNS) origin), headache, somnolence, nausea, vomiting, and feeling drunk.
CONCLUSION: Therapeutic and supratherapeutic doses of tapentadol do not affect the QT/QTc interval.

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Year:  2010        PMID: 20875374     DOI: 10.5414/cpp48678

Source DB:  PubMed          Journal:  Int J Clin Pharmacol Ther        ISSN: 0946-1965            Impact factor:   1.366


  8 in total

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Authors:  Sheridan M Hoy
Journal:  Drugs       Date:  2012-02-12       Impact factor: 9.546

2.  Effect of nalmefene 20 and 80 mg on the corrected QT interval and T-wave morphology: a randomized, double-blind, parallel-group, placebo- and moxifloxacin-controlled, single-centre study.

Authors:  Jørgen Matz; Claus Graff; Petri J Vainio; Antero Kallio; Astrid Maria Højer; Johannes J Struijk; Jørgen K Kanters; Mads P Andersen; Egon Toft
Journal:  Clin Drug Investig       Date:  2011-11-01       Impact factor: 2.859

Review 3.  Tapentadol in pain management: a μ-opioid receptor agonist and noradrenaline reuptake inhibitor.

Authors:  Craig T Hartrick; Richard J Rozek
Journal:  CNS Drugs       Date:  2011-05       Impact factor: 5.749

Review 4.  Tapentadol Prolonged Release: A Review in Pain Management.

Authors:  Emma D Deeks
Journal:  Drugs       Date:  2018-11       Impact factor: 9.546

5.  Tapentadol shows lower intrinsic efficacy at µ receptor than morphine and oxycodone.

Authors:  Preeti Manandhar; Mark Connor; Marina Santiago
Journal:  Pharmacol Res Perspect       Date:  2022-02

6.  Patient considerations in the use of tapentadol for moderate to severe pain.

Authors:  Nalini Vadivelu; Yili Huang; Brian Mirante; Michael Jacoby; Ferne R Braveman; Roberta L Hines; Raymond Sinatra
Journal:  Drug Healthc Patient Saf       Date:  2013-07-03

Review 7.  Cardiac Arrest Following Drug Abuse with Intravenous Tapentadol: Case Report and Literature Review.

Authors:  Misbahuddin Khaja; George Lominadze; Konstantin Millerman
Journal:  Am J Case Rep       Date:  2017-07-21

8.  Tapentadol Versus Tramadol: A Narrative and Comparative Review of Their Pharmacological, Efficacy and Safety Profiles in Adult Patients.

Authors:  Lucien Roulet; Victoria Rollason; Jules Desmeules; Valérie Piguet
Journal:  Drugs       Date:  2021-07-01       Impact factor: 9.546

  8 in total

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