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Detected analgesic without side effects as morphine replacement
Morphine is a painkiller that is only approved for the most severe pain. The overdose of the drug can have life-threatening effects on us and morphine can also make patients quickly addicted. Researchers have now discovered that a synthetic drug is similarly effective against pain, but without the typical side effects and the fast-growing addiction to opioids.
An international team of scientists from the University of California at San Francisco, Stanford University and the Friedrich Alexander University of Erlangen-Nuremberg found in a study that a new synthetic drug can combat the pain as effectively as morphine. However, there is no danger of becoming addicted to the new drug called PZM21. The physicians published the results of their study in the journal "Nature".
Certain pain killers can cause severe side effects, addiction and even death. Scientists found a new powerful analgesic that has no side effects and no addiction. (Image: lovegtr35 / fotolia.com) PZM21 does not slow or block breathing
A study on mice revealed that the new substance activates a known molecular pathway in our brain that triggers pain suppression. But unlike pain killers like morphine and prescription drugs like oxycodone, Oxycontin does not slow or block our normal breathing, the researchers explain.
Consumption and abuse of opioids has reached epidemic proportions
The use of opioids results in approximately 30,000 deaths each year in the United States alone, due to the attenuation of the respiratory center, say the authors. The ever-growing overdose of opioid painkillers is also causing more and more people to die. Consumption and abuse has now reached epidemic proportions in the United States, warn the medical profession.
PZM21 is not addictive
The new drug, PZM21, did not make the lab mice addicted, though mice are addicted to morphine and other pharmaceutical pain killers just as quickly as we humans, the researchers say. In the experiments, the rodents showed no preference between PZM21 or an administered neutral saline solution.
New medication does not slow down breathing and does not cause constipation
PZM21 provides long-lasting analgesia (pain therapy) and does not slow our breathing. In addition, the drug causes no blockages, explain the scientists. In the United States, there are now extra drugs to relieve the obstructed by opioids intestine.
Opium and its derivatives are still the main painkiller in severe pain
For the past 4,000 years, people have used opium and its derivatives to fight pain and create euphoric feelings. Even in our age of modern medicine, morphine remained the main painkiller in severe pain, say the experts. The substance derived from the opium poppy, for example, is used for recovery after surgery or used for the immediate treatment of severe wounds and pain.
The search for a safe replacement for Opioide has been going on for decades
The dangers of opium are obvious, says author Professor Brian Shoichet of the University of California School of Pharmacy. People need a safe replacement for opioids. The search has been going on for decades now, the expert adds. Most efforts were aimed at optimizing the chemical structure of the drug. This should eliminate the side effects.
Researchers are focusing on opioid receptors in the brain
However, researchers at Stanford University, the University of North Carolina and the Friedrich Alexander University in Germany used a different radical approach to problem solving. They focused on the so-called opioid receptors in the brain, which trigger a chemical response to suppress pain when activated.
Doctors are taking a new approach to problem solving
The physicians were looking for a molecule that can successfully dock at a receptor without docking to a second receptor. Docking on the second receptor would trigger the unwanted response of addiction to the drug, the researchers explain. Traditional forms of drug research do not really help here. However, when the physicians began to work on the structure of the receptor that was to be addressed, there were hardly any limitations in the investigations.
Computer simulations are investigating three million commercially available compounds
Using computer simulations, the researchers examined three million commercially available compounds and additionally considered one million possible configurations for each compound. So they wanted to determine which configuration works best with the receptor. In a laboratory trial, the cost of examining trillion configurations would have been prohibitively expensive and time-consuming, the researchers say.
Investigations are the first step in the development of the perfect painkiller
Finally, the scientists found an active ingredient that showed in further analysis that, although it triggered the good molecular signaling pathways, it did not activate any negative signaling pathways. The new investigation was a first step in developing a perfect medication for pain, say the experts. However, PZM21 still has many hurdles to overcome before it is available as a drug in our pharmacies.
Further research is urgently needed before the drug enters the market
Further clinical studies must first prove that PZM21 is safe for humans. This process can typically take up to a decade to complete, the scientists explain. Future research must also show whether the drug in humans or mice leads to a tolerance or resistance. By such a drug could lose its analgesic effectiveness over time, the experts add. (As)