Drug that strengthens analgesic effect of opioids without increasing constipation tested

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 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 . 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 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 .

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.

More information: "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. 348:32–45, January 2014. dx.doi.org/10.1124/jpet.113.208272

add to favorites email to friend print save as pdf

Related Stories

FDA orders starker warnings on opioid painkillers

Sep 10, 2013

The Food and Drug Administration is requiring stronger warning labels on prescription painkillers like OxyContin, in the government's latest attempt to reduce overdose deaths caused by the long-acting medications.

Recommended for you

Health care M&A leads global deal surge

18 hours ago

In a big year for deal making, the health care industry is a standout. Large drugmakers are buying and selling businesses to control costs and deploy surplus cash. A rising stock market, tax strategies and ...

US approves new, hard-to-abuse hydrocodone pill (Update)

Nov 20, 2014

U.S. government health regulators on Thursday approved the first hard-to-abuse version of the painkiller hydrocodone, offering an alternative to a similar medication that has been widely criticized for lacking ...

Soaring generic drug prices draw Senate scrutiny

Nov 20, 2014

Some low-cost generic drugs that have helped restrain health care costs for decades are seeing unexpected price spikes of up to 8,000 percent, prompting a backlash from patients, pharmacists and now Washington ...

Only half of patients take their medications as prescribed

Nov 20, 2014

The cost of patients not taking their medications as prescribed can be substantial in terms of their health. Although a large amount of research evidence has tried to address this problem, there are no well-established ...

User comments

Adjust slider to filter visible comments by rank

Display comments: newest first

DonGateley
not rated yet Mar 28, 2014
And this might be helping people in agony when?

Please sign in to add a comment. Registration is free, and takes less than a minute. Read more

Click here to reset your password.
Sign in to get notified via email when new comments are made.