Pharmacokinetic evaluation of tapentadol extended-release tablets in healthy subjects

Zannikos, Peter; Smit, Johan W.; Stahlberg, Henning; Wenge, Birger; Hillewaert, Vera; Etropolski, Mila

doi:10.5055/jom.2013.0171

Cited by 18 publications

(9 citation statements)

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“…The formulations of tapentadol ER used in the two studies differed; a conventional hypromellose-based formulation was used in the first study [ 18 ], while a new formulation of tapentadol ER, with a high mechanical strength resulting from a polyethylene oxide matrix and melt extrusion manufacturing process, was used in the second study [ 19 ]. Bioequivalence has generally been demonstrated for these two formulations [ 21 ]. In addition, the enrolment criteria related to glycaemic control differed in the two studies.…”

Section: Discussionmentioning

confidence: 99%

“…The first study [ 18 ] used the conventional hypromellose-based formulation employed in other phase 3 clinical trials [ 12 , 13 , 20 ], while the second study [ 19 ] used a new formulation of tapentadol ER that has a high mechanical strength resulting from a polyethylene oxide matrix and melt extrusion manufacturing process, is less susceptible to crushing or extraction than the conventional hypromellose-based formulation and is intended to reduce the potential for tampering with the tablet that might overcome the extended-release characteristics. The new formulation of tapentadol ER, which has a similar release profile to the hypromellose-based formulation [ 21 ], has been approved for the management of chronic pain in the United States.…”

Section: Methodsmentioning

confidence: 99%

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A Pooled Analysis Evaluating the Efficacy and Tolerability of Tapentadol Extended Release for Chronic, Painful Diabetic Peripheral Neuropathy

Schwartz¹,

Etropolski

Shapiro

et al. 2014

Clin Drug Investig

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Background and ObjectiveData from two similarly designed studies of tapentadol extended release (ER) for managing neuropathic pain associated with diabetic peripheral neuropathy (DPN; NCT00455520, NCT01041859) in adults were pooled for this analysis, allowing a detailed evaluation of efficacy in patient subgroups and secondary endpoints.MethodsIn each study, patients were titrated to their optimal dose of open-label tapentadol ER [100–250 mg twice daily (bid)] over 3 weeks. Patients with ≥1-point improvement in average pain intensity [11-point numerical rating scale (NRS)] were randomized (1:1) to receive placebo or tapentadol ER during a 12-week, double-blind maintenance period.ResultsMean (standard deviation [SD]) changes in pain intensity from baseline to week 12 of maintenance in the placebo (n = 343) and tapentadol ER (n = 360) groups, respectively, were 1.28 (2.41) and 0.08 (1.87) [least squares mean difference (LSMD): −1.14 (95 % confidence interval [CI]: −1.435, −0.838); P < 0.001, in favour of tapentadol ER]. Significant between-group differences were also observed in changes from the start of the double-blind treatment period to the double-blind endpoint for the Short Form-36 physical functioning, role-physical, bodily pain, social functioning and role-emotional subscale and physical component summary scores, and the EuroQol 5-Dimension health status index (all P < 0.05, in favour of tapentadol ER). No clinically relevant differences were observed in the efficacy of tapentadol ER across patient subgroups divided by age, sex, race, opioid experience and pain intensity. Incidences of treatment-emergent adverse events were 56.0 % (192/343) with placebo and 74.7 % (269/360) with tapentadol ER during maintenance.ConclusionResults of this pooled analysis indicate that tapentadol ER was effective for managing DPN-related pain, and provided consistent analgesic efficacy across different patient subgroups.

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Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

A Pooled Analysis Evaluating the Efficacy and Tolerability of Tapentadol Extended Release for Chronic, Painful Diabetic Peripheral Neuropathy

Schwartz¹,

Etropolski

Shapiro

et al. 2014

Clin Drug Investig

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show abstract

“…This new formulation of tapentadol ER (approved for the management of chronic pain in the U.S.) has a similar release profile to the conventional hypromellose-based formulation (12). This study also included the validated Neuropathic Pain Symptom Inventory (NPSI) as a neuropathic pain-specific efficacy instrument (13).…”

Section: Methodsmentioning

confidence: 99%

A Randomized Withdrawal, Placebo-Controlled Study Evaluating the Efficacy and Tolerability of Tapentadol Extended Release in Patients With Chronic Painful Diabetic Peripheral Neuropathy

Vinik¹,

et al. 2014

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OBJECTIVEThis study evaluated the efficacy and tolerability of tapentadol extended release (ER) for the management of chronic pain associated with diabetic peripheral neuropathy (DPN). RESEARCH DESIGN AND METHODSAdults with moderate to severe DPN pain were titrated to tapentadol ER 100-250 mg bid during a 3-week open-label period; patients with ‡1-point reduction in pain intensity (11-point numerical rating scale) at end of titration were randomized to receive placebo or tapentadol ER (optimal dose from titration) for 12 weeks (double-blind, fixed-dose maintenance phase). The primary end point was mean change in average pain intensity from the start to week 12 (last observation carried forward [LOCF]) of the double-blind maintenance phase. RESULTSA total of 358 patients completed the titration period; 318 patients (placebo, n = 152; tapentadol ER, n = 166) were randomized and received one or more doses of double-blind study medication. Mean (SD) pain intensity (observed case) was 7.33 (1.30) at the start and 4.16 (2.12) at week 3 of the open-label titration period (mean [SD] change, -3.22 [1.97]). The mean (SD) change in pain intensity (LOCF) from start of double-blind treatment to week 12 was as follows: placebo, 1.30 (2.43); tapentadol ER, 0.28 (2.04; least squares mean difference, -0.95 [95% CI -1.42 to -0.49]; P < 0.001). Treatment-emergent adverse events ( ‡10%) in the tapentadol ER group during the double-blind maintenance phase were nausea (21.1%) and vomiting (12.7%). CONCLUSIONSTapentadol ER (100-250 mg bid) was effective and well tolerated for the management of moderate to severe chronic pain associated with DPN.

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“…None of the metabolites appear to contribute to the analgesic action. In a pharmacokinetic study of tapentadol PR (polyethylene-oxide-based tablets) of doses ranging from 50 to 250 mg in healthy subjects, maximum concentrations ( C max ) were typically observed 5 h after dosing with terminal half-life values ranging from 4.4 to 5.9 h [ 30 ]. Trough concentrations increased during repeat dosing and achieved a steady state after the third dose.…”

Section: Pharmacokinetics Of Tapentadolmentioning

confidence: 99%

“…When tapentadol PR 250 mg was consumed with a high-fat meal, C max and the area under the concentration-time curve (AUC) increased by an average of less than 17%. Thus, tapentadol PR can be considered to have consistent pharmacokinetic parameter values after single and repeated dosing and may be administered with or without food [ 30 ].…”

Section: Pharmacokinetics Of Tapentadolmentioning

confidence: 99%

Tapentadol Extended Release in the Treatment of Severe Chronic Low Back Pain and Osteoarthritis Pain

et al. 2018

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Tapentadol is a novel pain reliever with apparently synergistic dual mechanisms of action, capable of addressing both nociceptive and neuropathic components of chronic pain. As an effective analgesic with good tolerability, tapentadol may be appropriate for patients suffering from severe chronic pain associated with low back pain (LBP) or osteoarthritis (OA). Efficacy studies of tapentadol in populations of patients with severe chronic LBP or OA pain suggest that tapentadol is non-inferior to oxycodone. Its tolerability, especially with respect to gastrointestinal (GI) side effects, may be better than that of other strong opioids in clinical trials and analyses of multiple trials. Patient satisfaction with tapentadol extended release for chronic noncancer pain syndromes is good. Although tapentadol has an opioid component with abuse liability, it appears to be a difficult opioid for tampering with less appeal to abusers than other opioids. For patients with severe LBP and OA pain, tapentadol appears to hold promise as a safe, effective therapeutic option.

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Pharmacokinetic evaluation of tapentadol extended-release tablets in healthy subjects

Cited by 18 publications

References 0 publications

A Pooled Analysis Evaluating the Efficacy and Tolerability of Tapentadol Extended Release for Chronic, Painful Diabetic Peripheral Neuropathy

A Pooled Analysis Evaluating the Efficacy and Tolerability of Tapentadol Extended Release for Chronic, Painful Diabetic Peripheral Neuropathy

A Randomized Withdrawal, Placebo-Controlled Study Evaluating the Efficacy and Tolerability of Tapentadol Extended Release in Patients With Chronic Painful Diabetic Peripheral Neuropathy

Tapentadol Extended Release in the Treatment of Severe Chronic Low Back Pain and Osteoarthritis Pain

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