Abstract

TORRES MORERA, L. M.. Tapentadol retard for severe chronic pain. Rev. Soc. Esp. Dolor [online]. 2011, vol.18, n.5, pp.283-290. ISSN 1134-8046.

Since the first orally administered morphine was introduced in Spain back in 1988 the bioavailability of potent opioid drugs to be administered via a route other than the intravenous one has increasingly evolved. Formulations allowing these drugs to be absorbed via the skin or oral mucosa have made a major difference in the administration of analgesic medication. Later still, novel immediate-release or controlled-release forms have finished off the positive efficacy and safety profile of these new opioid drugs. Tapentadol retard is a latest-generation, central-acting pain killer that was approved by the EMA (European Medicines Agency) in 2010 and recently by Agencia Española de Medicamentos y Productos Sanitarios (AEMPS) for the treatment of severe chronic pain. The synergy between its two mechanisms of action - μ-opioid agonism and noradrenaline uptake inhibition -- allows approaching pain from two different physiological aspects. Tapentadol retard is rapidly absorbed following oral administration, and excreted almost exclusively by the kidneys. While the analgesic efficacy of other opioids, including codeine and tramadol, depend upon their metabolic actions, the analgesia resulting from tapentadol administration derives from its primary molecule's action, with no active metabolites involved. The papers analyzed in this review show the efficacy of tapentadol retard in the management of moderate to severe pain in patients with chronic low-back pain, chronic knee or hip osteoarthritis, and diabetic neuropathy. Regarding safety, this drug has a superior tolerability profile when compared to current opioid analgesics, which confers a significant potential for the treatment of pain resulting from chronic conditions. This literature review analyzes tapentadol retard's mechanism of action, pharmacokinetics, pharmacodynamics, efficacy, and safety, as well as its exchangeability for opioid pain killers.

Keywords : Tapentadol; Chronic pain; Opioid.

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