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Morphine Substitute – What To Expect In The New Pain Medication?

The leading therapies for acute and chronic pain are morphine-based drugs, but they can be highly addictive. The misuse contributes annually to thousands of overdose deaths in the United States. Motor dysfunction and potentially lethal respiratory depression may be caused by them. Over time, patients also build up tolerance, raising the likelihood of misuse and overdose. Morphine has been discovered and widely applied to clinical entities[1] for such a long period. Scientists have made progress to create a safe morphine substitute that can manage chronic pain.

“With the new medication, these side effects were absent or decreased”, said by James Zadina, VA Senior Research Career Scientist and Professor of Medicine, Pharmacology and Neuroscience at the School of Medicine of Tulane University. With so few side effects, it’s unprecedented for a peptide to provide such strong pain relief.

The new drug developed much less tolerance than morphine and did not produce activation of the spinal glial cell, a morphine inflammatory effect known to lead to tolerance. Scientists have performed several experiments to test whether the drug would be addictive. Researchers are hoping to begin clinical human trials of the new drug within the next two years.

What Do You Know About Morphine Substitute

Scientists have created a synthetic medication that may be a morphine substitute for medicinal use, public health, cancer pain, health care et al. During Covid-19 pandemics, researchers discovered that engineered endomorphin forms[2], a naturally occurring chemical in the body, are as effective as morphine when it comes to killing pain. On top of that, the medication does not contain any of the undesirable side effects that come with opium-based drugs – such as being highly addictive. It is also safe to use for respiratory depression, pain relief, cancer pain, and motor impairment et al, nevertheless it has side effects also on the opioid receptor.

Experiments on new morphine substitute

At this point, the results apply only to experiments in rats[3], but a positive introduction to what might be a powerful and less troublesome painkiller. Motor control disorders were also not apparent in rats given endomorphin, although severe deficiency of morphine in animals could be observed. 

In addition, the engineered medication also developed even less resistance than morphine. To assess the addictive levels of the new medication, the researchers performed a variety of experiments. They claimed that these tests were indicative of human drug addiction and also its side effects. If we are aiming to offer patients informed choice and optimal symptom control, comparisons among morphine substitution are necessary. Improved comprehension of early-stage or non-malignant chronic pain patients will improve treatment and optimize patients’ functional ability and quality of life.

The goal of palliation is to prescribe powerful analgesics with a half-life hours so that we can manage the pain easily. Modified formulations are extremely helpful once dose requirements have stabilized, allowing longer dose intervals and simultaneously maintaining the flexibility to make dose alterations without risk of accumulation. Potency and length of operation are also important relevant features.

Theoretically, morphine sets the gold standard: four-hour clinical duration of action allows for a regular review of controlling unmodified pains. . When stabilized, sustained-release formulations minimize the dose frequency to once or twice daily. Sudden pain is under control with extra doses of the unmodified drug. It was calculated as 1/6 of the total 24-hour opioid dose requirement.

Drugs with a very short half-life (pethidine, for example) are unsuitable due to the need for repeat dosing, which can cause the build-up of toxic metabolites. Drugs with inherently long half-lives (e.g. methadone) are useful for long-term maintenance but can be difficult to treat safely with  unstable pain.

morphine substitute
Morphine can treat various pains

New Pain Medication Laws 2020

The CDC Guidance[4] addresses patient-centered care procedures, including careful review, public health, evaluation of all potential therapies, and respiratory depression,  drugs, appropriate risk monitoring, and safe elimination of opioids. The three main focus areas of the Guideline are as follows:

Regulation on whether to start or resume opioids for severe pain 

  • Selection of non-pharmacological therapy, non-opioid pharmacological therapy, opioid therapy
  • Establishing care targets.
  • Discussion of risks and benefits of treatment with patients

Opioid selection, dosage, duration, follow-up, and discontinuation of drugs.               

  • Selection of immediate-release or extended-release and long-acting opioids 
  • Dosage considerations                                                                                
  • Duration of treatment                                                               
  • Considerations for follow-up and discontinuation of opioid therapy

Assessing risk and addressing harms of opioid use                                     

  • Evaluation of risk factors for opioid-related harms and ways to mitigate patient risk.                                                                                                                                                
  • Review of prescription drug monitoring program (PDMP) data                                                
  • Use of urine drug testing.                                                                     
  • Considerations for co-prescribing benzodiazepines                                        

Arrangement of treatment for opioid use disorder

Improving the way opioids are administered will guarantee that patients have access to a better and more reliable chronic pain management. More than 11,5 million Americans aged 12 and older reported misusing prescription opioids in 2016.

Multicentre trials in palliative care have been slow to develop. There are logistical problems of financing and organizing trials across a large number of small units and difficulties in developing scientifically sound procedures that meet the needs of terminally ill patients both clinically and ethically. Recruitment tends to be slow, attrition rates high, and assessment of effects confounded by patients having multiple problems and requiring different treatment modalities.

CDC created and released the CDC Guidance for Prescription Opioids for Chronic Pain to provide guidelines for adults 18 years and over in primary care settings. Recommendations center on the use of opioids in the management of chronic pain (pain more than 3 months or after natural tissue healing) beyond active cancer treatment, palliative care, and end-of-life care.

Alternative opioids to morphine

Morphine is an extremely powerful narcotic pain medication originating from one of three opioid types. However uncommon true medical allergy to morphine is, some people are still allergic to morphine, and many others suffer from serious side effects attributable to morphine. Usually, morphine can relieve relatively high to extremely severe levels of pain, such as after surgery or severe injury. As a result, for those who are either allergic or have adverse effects with morphine, clinicians may provide alternatives instead.

Generally, there are three distinct groups of opioids: phenanthrenes, phenylpiperidine, and phenylheptane. Morphine, along with codeine, oxycodone, and hydrocodone, all belong to the phenanthrene class. A medication from another class of opioids, such as fentanyl, from the phenylpiperidine class, can be administered as a morphine replacement .

In addition, studies finds that non-steroidal anti-inflammatory medications (NSAIDs) are also alternatives to morphine. A patient who has demonstrated a true aversion to opioids may have their pain treated by NSAIDs. 

Ibuprofen is an example of an ANSID that can help control discomfort. Acetaminophen is another non-narcotic analgesic that can be used as an antidote to morphine. Effectiveness is the issue for NSAIDs and other non-opioids pain relievers. Although they can be very useful in treating mild to moderate pain and are mostly well tolerated, they can be very ineffective in treating extreme pain and can be dangerous at high doses.

In most cases, doctors will find an opioid proxy for pain relief, blood pressure, respiratory depression, or pain control. They have to consider the previous medical condition and opioid reaction because a side effect can be extremely serious if given the wrong opioid receptor. In certain cases, drug adverse effects are due to dosing rather than to the drugs itself. If controlled doses of morphine are inadequate, switching to another type of drug also relieves the problem one from another.

When you are not sure about your reaction with opioids or other opiates, or you are scheduled for surgery, speak to your doctor beforehand about it. And if you suspect that you are allergic to a narcotic pain reliever for acute or chronic pain, call the doctor immediately.

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  1. Surg. Lieut. J. A. McLachlin. 1945. THE INTRAVENOUS USE OF NOVOCAINE AS A SUBSTITUTE FOR MORPHINE IN POSTOPERATIVE CARE, vol 12. Available from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1581839/pdf/canmedaj00583-0159.pdf
  2. Amy K.Feehan, JennyMorgenweck, et al. 2017. Novel Endomorphin Analogs Are More Potent and Longer-Lasting Analgesics in Neuropathic, Inflammatory, Postoperative, and Visceral Pain Relative to Morphine, 18(12), 1526 – 1541 . The Journal of Pain. Available from: https://www.sciencedirect.com/science/article/abs/pii/S1526590017306983
  3. Vasudeva Raghavendra, Flobert Y Tanga & Joyce A DeLeo. 2003 [Oct 8, 2003]. Attenuation of Morphine Tolerance, Withdrawal-Induced Hyperalgesia, and Associated Spinal Inflammatory Immune Responses by Propentofylline in Rats. Available from: https://www.nature.com/articles/1300315
  4. Deborah Dowell, Tamara M. Haegerich, Roger Chou. 2016 [April 16, 2016]. CDC Guideline for Prescribing Opioids for Chronic Pain—United States, 2016. Available from: https://jamanetwork.com/journals/jama/fullarticle/2503508
  5. John Traynor. Traynor Lab. Department of pharmacology. Available from: https://sites.google.com/a/umich.edu/traynor-lab/