Tested a drug that strengthens the analgesic effect of opioids without increasing constipation

March 31, 2014

Scientists from the University of Granada have taken part, alongside the Esteve laboratory, in the development of a new drug that multiplies the analgesic effect of opioids (drugs for treating intense pain), without increasing constipation, one of the most common side-effects of these drugs, among which is morphine.

This important scientific breakthrough has been published in The Journal of Pharmacology and Experimental Therapeutics, and has been chosen as its outstanding article in the month of January. So far, the University of Granada researchers have published the results from testing this molecule on mice.

Opium derivates have been used since ancient times to treat pain. Currently, these and similar products (opioids) are the drugs used to treat various types of intense pain, such as post-operatory pain, cancer pain or internal-organ pain. The prolonged use of opioids causes strong constipation, which is a substantial drawback to their administration, since it substantially diminishes patient well-being.

The recently-published article proves that S1RA, a drug that blocks the sigma-1 receptor, manages to multiply solely the beneficial effect of the opioids; that is, their pain-killing properties.

The sigma-1 receptor is a very small protein that acts as a neuro-modulator, physically linking to other proteins (among which are the opioid receptors) and modifying their function.

As Enrique Cobos del Moral, one of the authors and a researcher at the University of Granada Institute of Neuroscience, explains, opioids are basically "centrally-acting" drugs; that is, they act directly upon the brain and the spinal medula. However, when opioids are associated with sigma-1 receptor blockers, their pain-killing effects are brought about by acting upon other areas; specifically, on the peripheral nervous system. From this, it is deduced that the sigma-1 receptor is a biological brake that prevents peripheral opioid analgesia, and that this brake can be eliminated by pharmacological treatment so as to increase the pain-killing power of opioids.

This scientific breakthrough is of huge importance for the well-being of patients suffering from pain, since, in the short term, it will allow the development of more efficient painkillers with fewer side-effects.

Esteve is working on the development of this medication, which is currently in Clinical Phase II
-end-
References:

Modulation of Peripheral μ-Opioid Analgesia by sigma1 Receptors
Sánchez-Fernández C, Montilla-García Á, González-Cano R, Nieto FR, Romero L, Artacho-Cordón A, Montes R, Fernández-Pastor B, Merlos M, Baeyens JM, Entrena JM, Cobos EJ.

The Journal of Pharmacology and Experimental Therapeutics. 348:32, January 2014 http://dx.doi.org/10.1124/jpet.113.208272

University of Granada

Related Pain Articles from Brightsurf:

Pain researchers get a common language to describe pain
Pain researchers around the world have agreed to classify pain in the mouth, jaw and face according to the same system.

It's not just a pain in the head -- facial pain can be a symptom of headaches too
A new study finds that up to 10% of people with headaches also have facial pain.

New opioid speeds up recovery without increasing pain sensitivity or risk of chronic pain
A new type of non-addictive opioid developed by researchers at Tulane University and the Southeast Louisiana Veterans Health Care System accelerates recovery time from pain compared to morphine without increasing pain sensitivity, according to a new study published in the Journal of Neuroinflammation.

The insular cortex processes pain and drives learning from pain
Neuroscientists at EPFL have discovered an area of the brain, the insular cortex, that processes painful experiences and thereby drives learning from aversive events.

Pain, pain go away: new tools improve students' experience of school-based vaccines
Researchers at the University of Toronto and The Hospital for Sick Children (SickKids) have teamed up with educators, public health practitioners and grade seven students in Ontario to develop and implement a new approach to delivering school-based vaccines that improves student experience.

Pain sensitization increases risk of persistent knee pain
Becoming more sensitive to pain, or pain sensitization, is an important risk factor for developing persistent knee pain in osteoarthritis (OA), according to a new study by researchers from the Université de Montréal (UdeM) School of Rehabilitation and Hôpital Maisonneuve Rosemont Research Centre (CRHMR) in collaboration with researchers at Boston University School of Medicine (BUSM).

Becoming more sensitive to pain increases the risk of knee pain not going away
A new study by researchers in Montreal and Boston looks at the role that pain plays in osteoarthritis, a disease that affects over 300 million adults worldwide.

Pain disruption therapy treats source of chronic back pain
People with treatment-resistant back pain may get significant and lasting relief with dorsal root ganglion (DRG) stimulation therapy, an innovative treatment that short-circuits pain, suggests a study presented at the ANESTHESIOLOGY® 2018 annual meeting.

Sugar pills relieve pain for chronic pain patients
Someday doctors may prescribe sugar pills for certain chronic pain patients based on their brain anatomy and psychology.

Peripheral nerve block provides some with long-lasting pain relief for severe facial pain
A new study has shown that use of peripheral nerve blocks in the treatment of Trigeminal Neuralgia (TGN) may produce long-term pain relief.

Read More: Pain News and Pain Current Events
Brightsurf.com is a participant in the Amazon Services LLC Associates Program, an affiliate advertising program designed to provide a means for sites to earn advertising fees by advertising and linking to Amazon.com.