Grünenthal Pharma launches Spain Palexia ® retard, a new generation of central action analgesics

-Palexia ® retard is the representative of a new generation of analgesics of central action called MOR-NRI1, 2

– has shown broad efficacy in severe chronic pain, whether of origin nociceptivo or neuropático3-7

-sinérgico8 (MOR-NRI) and dual action mechanism provides an efficiency comparable to the of the classic powerful opioids such as oxycodonewith a lower incidence of reactions adverse that they lead to a lower rate of terminations of tratamientos3-6.

Madrid, September of 2011. Grünenthal Pharma, pharmaceutical company relating to the treatment against pain worldwide, launches in Spain tapentadol, already available in hospitals and in Spanish pharmacies under the name Palexia ® retard. Tapentadol retard is the first molecular entity developed for the treatment of severe chronic pain on the market since more than 25 años2, as well as representative of a new generation of so-called central action analgesics MOR-NRI1, 2 (the µ-opioid receptor agonist and norepinephrine reuptake inhibitor). The results of numerous studies show that Palexia ® retard is effective in nociceptivo pain and neuropathic pain, as demonstrated in models preclínicos9 and clinical studies on indications of severe chronic pain as lumbar pain crónico3, arthrosis of knee 4 or polyneuropathy diabética7.

Complementary mechanisms of action

Tapentadol combines in a single molecule a mechanism of dual and synergistic action and presents únicas2 pharmacokinetic characteristics, 8, 10. Both the agonismo µ-opioid (MOR), such as the inhibition of reuptake of norepinephrine (NRI), contribute complementary and sinérgica8 to the effectiveness of tapentadol in conditions of nociceptivo and neuropático9 pain. At the spinal level, tapentadol reduces transmission of painful signal via ascending through the activation of the µ-opioids recipient pre and post synaptic. In addition, tapentadol inhibits reuptake of norepinephrine (NA) in via downward, increasing levels of it in the synaptic cleft. This NA join α2 receptors, thus reducing the transmission of the dolor10. The combination of these two mechanisms of action in a single molecule can be advantageous in indications that often involve both components of pain, nociceptivo and neuropathic, as chronic low back pain intensa3.

This dual and synergistic action in the same molecule mechanism provides efficient both in pain nociceptivo as neuropathic, as well as a saving effect µ-opioid, giving rise to a smaller number of adverse effects usually associated with powerful opioid clásicos10.

Improving the control of pain

Pain is a serious health problem with more than six million Spaniards (17,25%), and if we speak of chronic pain, 20% of the population of Europe is affected by él11. Numerous studies have shown that pain has an impact very negatively on the quality of life of patients. In fact, more than half of people with severe pain (53%) recognize that they have been forced to reduce or limit their usual social activities. It is also closely linked to low labour productivity: 39,39% of people who suffer severe pain are absent from their jobs, compared with a 3.32% of the population not as padece12.

Currently, pharmacological treatment of severe chronic pain is typically inefficient due to the difficulty of maintaining the balance between adequate pain relief and an acceptable tolerability. This is what is known as the vicious circle, of which often is the interruption of treatment. Patients with chronic pain leave more frequently its treatment with opioids because of adverse effects that due to lack of eficacia13.

The best approach to pain needs to identify its mechanism and their symptoms and decide as well, the most appropriate for different types of dolor14 treatment, 15. The mechanisms of modulation Palexia ® MOR-NRI retard contributes to the analgesic effect and are complementarios1, 10.

Also, tapentadol has been included as a narcotic substance in Spain following the recent adoption of Royal Decree 1194 / 2011, which regulates the procedure by which a substance is considered narcotic.

About Grünenthal

Grünenthal is a pharmaceutical company concerning the treatment of pain worldwide, both for patients and for doctors and health managers. Innovation is one of its fundamental principles and one of the keys to be leaders in the global market for moderate to severe pain. Grünenthal is an independent German company family-owned, with offices in 36 countries around the world. Founded in 1946, Grünenthal has 347 employees in the region of Iberia and approximately 4,900 at the global level. In 2009 global sales figures reached 881 million euros. Also, Grünenthal Pharma ranked 17 in the Group of companies of between 250 and 500 employees in the prestigious ranking ‘ Best WorkPlaces 2011 Spain ’, produced by Great Place to Work ®

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