Tuesday, 2 February 2016

Will Endomorphin Be The Replacement For Opioids For Neuropathy Patients?

Today's post from sciencedaily.com (see link below) follows on from yesterday's post about endomorphin and its potential for chronic pain patients but whereas yesterday's post was from a national newspaper, this one is from the ever-reliable Sciencedaily.com and confirms what you may have read yesterday. If the predictions are correct, then commercially produced endomorphin may replace opioids as the pain killers of choice for those who've tried everything else and as a bonus, will deliver none of the side effects associated with opioids. This is fantastic news for long-term pain patients who not only have to manage their opioid prescriptions properly but have to face the wagging finger of media stigma, however unjust that may be. We still have to wait two years before the first human trials but the eventual benefits may make the wait easier.

New drug could be safer, non-addictive alternative to morphine
 January 28, 2016 Source: Tulane University

The peptide-based drugs, which mimic a natural brain chemical, target the same pain-relieving opioid receptor as morphine

Researchers at Tulane University and Southeast Louisiana Veterans Health Care System have developed a painkiller that is as strong as morphine but isn't likely to be addictive and with fewer side effects, according to a new study in the journal Neuropharmacology.

Using rats, scientists compared several engineered variants of the neurochemical endomorphin, which is found naturally in the body, to morphine to measure their effectiveness and side effects. The peptide-based drugs target the same pain-relieving opioid receptor as morphine.

Opium-based drugs are the leading treatments for severe and chronic pain, but they can be highly addictive. Their abuse results in thousands of overdose deaths in the United States annually. They can cause motor impairment and potentially fatal respiratory depression. Patients also build up tolerance over time, increasing the risk for abuse and overdose.

"These side effects were absent or reduced with the new drug," said lead investigator James Zadina, VA senior research career scientist and professor of medicine, pharmacology and neuroscience at Tulane University School of Medicine. "It's unprecedented for a peptide to deliver such powerful pain relief with so few side effects."

In the study, the new endomorphin drug produced longer pain relief without substantially slowing breathing in rats; a similarly potent dosage of morphine produced significant respiratory depression. Impairment of motor coordination, which can be of particular importance to older adults, was significant after morphine but not with the endomorphin drug.

The new drug produced far less tolerance than morphine and did not produce spinal glial cell activation, an inflammatory effect of morphine known to contribute to tolerance.

Scientists conducted several experiments to test whether the drug would be addictive. One showed that although rats would spend more time in a compartment where they had received morphine, the new drug did not affect this behavior. Another test showed that when the press of a bar produced an infusion of drug, the rats only increased efforts to obtain morphine and not the new drug. The tests are predictive of human drug abuse, Zadina said.

Researchers hope to begin human clinical trials of the new drug within the next two years.

Story Source:

The above post is reprinted from materials provided by Tulane University. Note: Materials may be edited for content and length.

Journal Reference:

James E. Zadina, Mark R. Nilges, Jenny Morgenweck, Xing Zhang, Laszlo Hackler, Melita B. Fasold. Endomorphin analog analgesics with reduced abuse liability, respiratory depression, motor impairment, tolerance, and glial activation relative to morphine. Neuropharmacology, 2016; 105: 215 DOI: 10.1016/j.neuropharm.2015.12.024

Tulane University. "New drug could be safer, non-addictive alternative to morphine: The peptide-based drugs, which mimic a natural brain chemical, target the same pain-relieving opioid receptor as morphine." ScienceDaily. ScienceDaily, 28 January 2016. .


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