Tapentadol prolonged release (PR) for the treatment of moderate to severe
chronic pain combines 2 modes of action. These are μ-
opioid receptor agonism and
noradrenaline reuptake inhibition in a single molecule that allow higher
analgesic potency through modulation of different pharmacological targets within the
pain transmitting systems. At the same time, this can also serve as a clue for modulation of different
pain-generating mechanisms according to nociceptive, neuropathic, or mixed
pain conditions.
Tapentadol PR has now been on the market for 5 years, with over 4.6 million people treated worldwide. A panel of
pain specialists convened in Germany to review the clinical program and to discuss the role of
tapentadol PR in the management of chronic
pain. The clinical study program demonstrated effective and generally well-tolerated treatment for up to 2 years in a broad range of
chronic pain conditions, including those with
neuropathic pain components. This was confirmed in routine clinical practice observations. Head-to-head studies with World Health Organization (WHO) III
opioids such as
oxycodone controlled release and
oxycodone/
naloxone PR showed at least comparable
pain relief in the treatment of moderate-to-severe
musculoskeletal pain. Rotation from poorly tolerated WHO III
opioids to
tapentadol PR provided effective
pain relief and better symptom control for
musculoskeletal pain compared to previous medication. Functionality, health status and quality of life also improved under
tapentadol PR treatment. The gastrointestinal tolerability profile was more favorable compared to other tested WHO III
opioids.
Tapentadol PR has a good safety profile and no evidence of acquired tolerance from the long-term data so far collected. Overall,
tapentadol PR represents an effective and generally well-tolerated alternative to "classical" opioidergic drugs.