MOR-NRI: different concepts meeting the complexity of pain (tapentadol)
Current treatment of chronic pain is largely based on the severity of pain – but does this still meet the increasing awareness that most chronic pain conditions are multifactorial in nature, e.g. nociceptive and neuropathic components present?
In order to allow a more targeted approach to the choice of pharmacological treatment, ideally, clinicians would identify the specific causal mechanisms underlying each patient's symptoms.
However, identifying these mechanisms in practice is difficult, as one mechanism can produce different symptoms and one symptom can be produced by different mechanisms.1
Where the pathophysiology of a medical condition is multifactorial in nature, the optimal therapeutic strategy is to use drugs addressing different mechanisms. Since most commonly available analgesic drugs predominantly affect only a single pain modulation system (opiodergic/monoaminergic system), combination therapy is frequently required but often limited due to the increased risk of side effects.2
In consequence, low patient compliance or even treatment discontinuations may occur (Vicious Circle) hampering the therapy success.2
Tapentadol – combined mechanisms of action in one molecule
Tapentadol is the only centrally acting analgesic available with a combined mechanism of action "MOR-NRI" in a single molecule.
It acts as a µ-opioid-receptor agonist (MOR) as well as a noradrenaline reuptake inhibitor (NRI), with proven efficacy in nociceptive pain and neuropathic pain.3
MOR-NRI combine strong efficacy in nociceptive and neuropathic pain with superior tolerability compared to classical strong opioids, enabling patients to stay on their therapy and improve their quality of life.4,5,6
1 Woolf CJ et al. Neuropathic pain: aetiology, symptoms, mechanisms, and management. Lancet. 1999; 353:1959-1964.
2 Varrassi G et al. Pharmacological treatment of chronic pain – the need for CHANGE. Curr Med Res Opin. 2010; 26(5):1231-1245.
3 Tzschentke TM et al. Tapentadol hydrochloride: A next generation, centrally acting analgesic with two mechanisms of action in a single molecule. Drugs of Today 2009; 45:483-96.
4 Kress HG et al. Tapentadol Prolonged Release for Managing Moderate to Severe, Chronic Malignant Tumor-Related Pain. Pain Physician. 2014; 17: 329-343.
5 Lange B et al. Efficacy and safety of tapentadol prolonged release for chronic osteoarthritis pain and low back pain. Adv Ther 2010; 27(6):381-99.
6 Binder A et al. Safety and tolerability of tapentadol prolonged release (PR) versus oxycodone/naloxone PR for severe chronic low back pain with a neuropathic pain component. Poster presented at PAIN Week September 2014, Las Vegas, USA.