Comparative pharmacokinetics and bioavailability of tapentadol following oral administration of immediate- and prolonged-release formulations

Göhler, Karin; Brett, Martin; Smit, Johan W.; Rengelshausen, Jens; Terlinden, Rolf

doi:10.5414/cp201722

Cited by 27 publications

(19 citation statements)

References 21 publications

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“…Tapentadol reaches maximum serum concentrations 3–6 h after PR tablet administration [23, 24] and, when the tablets are taken twice daily, steady-state levels are attained on day 2 and the accumulation ratio is ≈ 1.5 [23]. Tapentadol PR tablets can be taken without regard to food [23].…”

Section: Pharmalogical Propertiesmentioning

confidence: 99%

Tapentadol Prolonged Release: A Review in Pain Management

Deeks

2018

Drugs

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Tapentadol prolonged release (tapentadol PR) [Palexia® SR in EU] is a long-acting tablet formulation of the strong central analgesic tapentadol, which acts as both a μ-opioid receptor (MOR) agonist and a noradrenaline reuptake inhibitor. Tapentadol PR is approved for chronic pain in various countries, with its EU indication (severe chronic pain manageable only with opioid analgesics) being the focus here. Well-designed trials and clinical practice data support tapentadol PR use in this setting. Short term, tapentadol PR was an effective and generally well tolerated analgesic for moderate to severe pain of varying aetiologies, including neuropathic pain. It provided analgesia at least as good as that of conventional strong opioids and appeared more favourable in terms of gastrointestinal tolerability, likely due to less potent MOR binding. Severe back pain with a neuropathic component responded well to moderate-dose tapentadol PR in some patients, while for others, an increase to the maximum recommended tapentadol PR dosage provided analgesia at least as good as that of moderate-dose tapentadol PR plus pregabalin and appeared to have some CNS tolerability benefits. Data also support the use of tapentadol PR in opioid rotation, including when conventional opioids are intolerable. Longer-term data in musculoskeletal pain conditions indicate continued benefit over up to 2 years’ treatment with tapentadol PR with no evidence of tolerance. Thus, tapentadol PR is a useful option for the management of severe chronic pain.

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Section: Pharmalogical Propertiesmentioning

confidence: 99%

Tapentadol Prolonged Release: A Review in Pain Management

Deeks

2018

Drugs

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“…in Arzneimittel-Forschung/Drug Research in 1978 as a comparative clinical study (Rost and Schenck 1978 ). The discovery and identification of tramadol and its unique mechanism of action lead to the development of a newer tramadol-like agent named tapentadol which is currently available in the market and promoted to have better safety profile than tramadol (Giorgi et al 2012 ; Mercadante et al 2012 , 2013 ; Cepeda et al 2013 ; Gohler et al 2013 ; Lee et al 2013 ; Schwittay et al 2013 ; Singh et al 2013 ; Fejos et al 2014 ).…”

Section: Discussionmentioning

confidence: 99%

Worldwide research productivity on tramadol: a bibliometric analysis

et al. 2016

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BackgroundPain management and safe use of analgesics is an important medical issue. Tramadol is an old analgesic with controversial properties. Evaluation of worldwide scientific output on tramadol has not been explored. Therefore, the main objective of this study was to give a bibliometric overview of global research productivity on tramadol.MethodsSciVerse Scopus was used to retrieve and quantitatively and qualitatively analyze worldwide publications on tramadol.ResultsA total of 2059 original and review research articles on tramadol were retrieved from Scopus. Forty-six documents (2.23 %) were published in Anesthesia and Analgesia Journal whereas 30 (1.46 %) were published in Arzneimittel Forschung Drug Research Journal. Retrieved tramadol documents were published from 71 countries and appeared in 160 peer reviewed journals. Although the United States of America (259; 12.86 %) had the largest contribution to tramadol publications; the contribution by other countries like Turkey (232; 11.27) India (189; 8.09 %) and Germany (176; 8.56 % was not far away from that of USA. The most productive institution was Grunenthal, Germany (47; 2.28 %) followed by Tehran University of Medical Sciences, Iran (29; 1.41 %), and, Ortho-McNeil Pharmaceutical Incorporated, USA (25; 1.21 %). Of the 2059 documents, there were 370 documents about dependence. The leading institution in documents pertaining to tramadol dependence was Grunenthal GmbH (18; 4.86 %) followed by Ortho-McNeil Pharmaceutical Incorporated (17; 4.59 %).ConclusionsThe current study showed that there is an obvious interest in tramadol research. More efforts are needed to clarify the abuse potential and safety profile of tramadol to help in determining the legal status of tramadol. Collaboration among pharmaceutical industry, clinical researchers and academic institutions can improve research quantity and quality on tramadol.

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“…conducted three randomized, open-label, cross-over studies evaluating the absolute and relative bioavailabilities of tapentadol IR and tapentadol ER in healthy subjects, under a fasted state, which was demonstrated to be 32% for both IR and ER formulations [26]. More details are listed in Table 1.…”

Section: Pharmacokinetics and Metabolismmentioning

confidence: 99%