NEW DRUG… if proven safe in humans and truly non-addicting – could replace opiates ?

An end to morphine? New drug could provide safer painkiller alternative amid opioid epidemic 

http://www.dailymail.co.uk/health/article-3745809/An-end-morphine-New-drug-provide-safer-painkiller-alternative-amid-opioid-epidemic.html

Morphine may finally be sidelined in favor of a new safer painkiller, scientists claim. 

Researchers have spent decades searching for a safer non-addictive alternative to the potentially lethal opium.

Despite its dangers, no other drug has ever rivaled its efficient pain-numbing qualities. 

But this week, a new study has identified a compound that could do the trick – without the lethal side-effects. 

Researchers have spent decades searching for a safer non-addictive alternative to the potentially lethal opium - to no avail. But a new study claims to have made a breakthrough

Researchers have spent decades searching for a safer non-addictive alternative to the potentially lethal opium – to no avail. But a new study claims to have made a breakthrough

A team at the University of California at San Francisco found PZM21 effectively blocked pain by attaching itself to the same molecular receptor ‘switch’ targeted by morphine.

It did not share the same deadly side effects as morphine, especially suppressing breathing in higher doses.

Scientists also believe the drug is unlikely to be addictive – a major problem associated with morphine and other opioid drugs such as heroin.

If successful, the discovery could be a lifeline for millions of people amid a rapidly worsening painkiller-addiction epidemic in the United States.

Morphine, a natural extract of the opium poppy first isolated in the 19th century, revolutionized medicine and surgery with its extraordinary ability to dull pain.

However, the drug has to be administered with great care and can easily kill by interfering with breathing.

Professor Brian Shoichet, from the University of California at San Francisco, US, who co-led the new research, said: ‘Morphine transformed medicine. 

HOW MORPHINE WORKS

Morphine binds with receptors on the surface of nerve cells.

When that happens, there is a chain reaction along the cell, gradually numbing it so it is not so sensitive to pain.

The cell’s reactions become slow, meaning they take too long to pass pain signals through the body for it to be felt.

The drug also taps into the brain, slowing down perception skills, making the patient monumentally drowsy.

Too much can overwhelm the body, ultimately killing the patient.

It can also cause other issues, such as constipation (by slowing the receptors in the gut) and breathing problems (by targeting the lungs).

‘There are so many medical procedures we can do now because we know we can control the pain afterwards. But it’s obviously dangerous too.

‘People have been searching for a safer replacement for standard opioids for decades.’

The international scientists adopted an unusual drug discovery approach by avoiding the normal trial-and-error method of screening different compounds.

They started with the ‘mu opioid receptor’, the brain cell molecule through which morphine operates. 

Molecules of morphine fit the receptor like a key in a three-dimensional lock, triggering a signalling process that causes a cascade of effects.

To find a molecule that bound to the receptor in just the way they wanted, the researchers used powerful computer software to simulate different configurations of millions of drug candidates.

Over a period of two weeks, the team performed roughly four trillion of these ‘virtual experiments’.

In the end, they had a shortlist of 23 candidates. 

Further tests identified one especially promising molecule, whose chemical potency was then boosted 1000-fold to produce PZM21.

More work is needed to confirm that the drug is safe in humans and truly non-addictive, say the scientists, whose findings are published in the journal Nature.

They claim the new drug could be a game-changer in pain management and provide a solution to the major problem of painkiller addiction. 

5 Responses

  1. Where does this leave the 5.5 billion people who do not have access to inexpensive morphine for even end-stage pain relief? If political barriers prove to be so sturdy, just imagine how much impenetrable the economic barriers or a newly patented drug will be. Count me skeptical too.

  2. When? How long will the testing and adaption to patients be?

  3. Wouldn’t this be wonderful! I hope it is deemed safe! It’s wonderful that people are doing research around safe pain medicines!

  4. This would be such a great time for this discovery ! But they would still have to go through human testing and FDA approval correct Steve ?

  5. Mu receptor agonists have been proven over and over to be addictive (heroin in early 1900’s, meperidine in 1940’s, pentazocine in the 1970’s, buprenorphine and relatives in 1990’s).

    Please excuse my skepticism…

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