Tag: pain relievers

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Dependence on Pain Medication is on the Rise

On By ModernMedia
Photo by Towfiqu Barbhuiya on Unsplash

Dependence on pain medication is on the rise due to lack of vigilance by medical professionals, according to a new study from the University of Surrey. In the paper published in the journal Pain and Therapy, patients dependent on pain medication describe feelings of ‘living in a haze’ and being ignored and misunderstood by the medical profession.

In the first study of its kind in the UK, Louise Norton and Dr Bridget Dibb from the University of Surrey investigated the experiences of patients dependent on medication for chronic pain. Pharmacological treatment for chronic pain usually involves potentially addictive substances such as non-steroidal anti-inflammatory drugs, gabapentinoids, and opioids. Increased prescription levels of such pain relief medications have been associated with heightened levels of overdose and misuse.

Dr Bridget Dibb, Senior Lecturer in Health Psychology at the University of Surrey, said: “An increasing number of people are experiencing chronic pain, which can interfere with their daily life and lead to depression and anxiety. Medication can help alleviate pain and return a sense of normalcy to a person’s life; however, there is a risk of dependence, which can potentially cause damage to vital organs, including the liver and kidneys.

“The first step to tackle this problem is to learn more about a person’s experience, how they perceive their dependence and how they interact with others, including the medical profession.”

To learn more, interviews were carried out with nine participants who had become dependent on pain medication. Participants spoke about how their dependence on pain medication resulted in them feeling not fully present and removed from their lives due to the side effects of the treatment. Many also expressed frustration about the lack of alternative treatment options available on the NHS to manage their pain, with medications being too readily prescribed.

The majority of participants also spoke about their negative interactions with medical professionals, with some attributing the cause of their dependence on them. Many believed a lack of continuity between doctors led to missed opportunities in spotting their dependence, enabling it to continue.

Louise Norton added: “Relationships with medical professionals substantially affect the experiences of those with painkiller dependence. Doctors can often be seen as authority figures due to their expertise and so patients may be apprehensive to question their treatment options. However, through providing patients with thorough information, doctors can enable more shared-decision making in which patients feel better supported and equipped to manage their chronic pain.”

Researchers noted participants felt stigmatised when speaking with others about their dependence due to a lack of understanding about their reliance to prescribed pain medications. Such interactions left participants feeling ashamed and critical of themselves.

Dr Dibb added: “Those with a dependence on prescription painkillers not only have to navigate their reliance on the medication but the shame and guilt associated with such a need. Combining this with feelings of being misunderstood and ignored by medical professionals, they have a lot of emotional needs to be managed alongside their physical pain. To prevent this from happening medical professionals need to be more vigilant when prescribing medication and ensure that their patients are fully aware of the risk of dependence before they begin treatment.”

Source: University of Surrey

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New Compound Outperforms Gabapentin for Pain Relief

On By ModernMedia
Photo by Louis Reed on Unsplash

A new compound reversed four types of chronic pain in animal studies, according to new research published online in the Proceedings of the National Academy of Sciences (PNAS). It outperformed gabapentin without troublesome side effects, providing a promising candidate for treating pain.

Researchers led by NYU College of Dentistry’s Pain Research Center developed this small molecule, which binds to an inner region of a calcium channel to indirectly regulate it.

Calcium channels play a central role in pain signaling, in part through the release of neurotransmitters such as glutamate and GABA – “the currency of the pain signal,” according to Rajesh Khanna, director of the NYU Pain Research Center and professor of molecular pathobiology. The Cav2.2 (or N-type) calcium channel is the target for three clinically available drugs, including gabapentin and pregabalin, which are widely used to treat nerve pain and epilepsy.

Gabapentin mitigates pain by binding to the outside of the Cav2.2 calcium channel, affecting the channel’s activity. However, like many pain medications, gabapentin use often comes with side effects.

“Developing effective pain management with minimal side effects is crucial, but creating new therapies has been challenging,” said Khanna, the senior author of the PNAS study. “Rather than directly going after known targets for pain relief, our lab is focused on indirectly targeting proteins that are involved in pain.”

Inside the channel

Khanna has long been interested in a protein called CRMP2, a key regulator of the Cav2.2 calcium channel that binds to the channel from the inside. He and his colleagues previously discovered a peptide derived from CRMP2 that could uncouple CRMP2 from the calcium channel. When this peptide – calcium channel-binding domain 3 (CBD3) – was delivered to cells, it acted as a decoy, blocking CRMP2 from binding to the inside of the calcium channel. This resulted in less calcium entering the calcium channel and less neurotransmitter release, which translated to less pain in animal studies.

Peptides are difficult to synthesise as drugs because they are short-acting and easily degrade in the stomach, so the researchers sought to create a small molecule drug based on CBD3. Starting with the 15 amino acids that make up the CBD3 peptide, they honed in on two amino acids that studies showed were responsible for inhibiting calcium influx and mitigating pain.

“At that point, we realised that these two amino acids could be the building blocks for designing a small molecule,” said Khanna.

From 27 million to one

In collaboration with colleagues at the University of Pittsburgh, the researchers ran a computer simulation that screened a library of 27 million compounds to look for a small molecule that would “match” the CBD3 amino acids.

The simulation narrowed the library down to 77 compounds, which the researchers experimentally tested to see if they lessened the amount of calcium influx. This further pared the pool down to nine compounds, which were assessed using electrophysiology to measure decreases in electrical currents through the calcium channels.

One compound, which the researchers named CBD3063, emerged as the most promising candidate for treating pain. Biochemical tests revealed that CBD3063 disrupted the interaction between the CaV2.2 calcium channel and CRMP2 protein, reduced calcium entering the channel, and lessened the release of neurotransmitters.

“Many scientists have screened the same library of compounds, but have been trying to block the calcium channel from the outside. Our target, these two amino acids from CRMP2, is on the inside of the cell, and this indirect approach may be the key to our success,” said Khanna.

Four labs, four types of pain

Khanna’s lab then tested CBD3063 with mouse models for pain related to injury. The compound was effective in alleviating pain in both male and female mice – and notably, in a head-to-head test with the drug gabapentin, the researchers needed to use far less CBD3063 (1–10mg) than gabapentin (30 mg) to reduce pain.

To explore whether CBD3063 helped with different types of chronic pain, Khanna partnered with researchers at Virginia Commonwealth University, Michigan State University, and Rutgers University. Collaborators ran similar studies administering CBD3063 to treat animal models of chemotherapy-induced neuropathy, inflammatory pain, and trigeminal nerve pain – all successfully reversing pain, similar to gabapentin.

But unlike gabapentin, the use of CBD3063 did not come with side effects, including sedation, changes to cognition such as memory and learning, or changes to heart rate and breathing.

What’s next

The researchers are continuing to study CBD3063, refining its chemical composition and running additional tests to study the compound’s safety and assess if tolerance develops.

Long-term, they hope to bring a CBD3063-derived drug to clinical trials in an effort to offer new options for safe and effective pain relief.

“Identifying this first-in-class small molecule has been the culmination of more than 15 years of research. Though our research journey continues, we aspire to present a superior successor to gabapentin for the effective management of chronic pain,” said Khanna.

Source: New York University

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Only 30% of Adults Discuss OTC Pain Relievers with Doctors Despite Hypertension Risk

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Only about 30% of US adults have spoken with their health care professional about the adverse effects some over-the-counter (OTC) pain relievers can have on blood pressure. The findings are part of a recent online poll commissioned by the American Heart Association.

Some pain relievers may raise blood pressure, according to the American Heart Association’s most recent Guideline for the Prevention, Detection, Evaluation and Management of High Blood Pressure. 

“It’s paramount that people who have high blood pressure, or are at risk for it, understand the effects associated with some over-the-counter pain relievers,” said Mitchell S. V. Elkind, MD, MS, FAHA, chief clinical science officer of the American Heart Association and a tenured professor of neurology and epidemiology at Columbia University. “A conversation with a health care professional about pain relief options is essential to preventing and managing high blood pressure.”

High blood pressure affects almost half of all people in the US. According to the American Heart Association’s recent poll, of those who have been diagnosed with high blood pressure, white and Asian adults (40%) are significantly less likely than Black (54.2%) and Hispanic (54.1%) adults to have ever discussed the effect some pain relievers have on blood pressure with a health care professional.
“Some over-the-counter pain relievers are safer than others,” added Elkind. “A conversation with a health care professional regularly about medications you or a loved one takes is an important step in finding safe options and controlling blood pressure.”

The poll conducted by Big Village, a collaborative and consultative research firm, also looked at how often people used OTC pain relievers. Of the close to 3000 US adults aged 18 and older surveyed, nearly 50% took medication for pain once a week or more. Adults aged 45-54 take them most frequently of all age groups polled. Additional findings include:

  • Gen X, people born from 1965 to 1980, are significantly more likely than other generations to take OTC pain relievers multiple times a day, but only 41% of Gen X would initially ask a health care professional for alternative pain relief even if they knew some OTC pain relievers can raise a person’s blood pressure.
  • Gen Z, people born from 1997 to 2012, are significantly less likely (30.5%) than any other generation to initially ask their health care professional for alternative pain relief if they knew some OTC pain relievers can raise a person’s blood pressure.
  • 61% of all respondents had not discussed the effect some over-the-counter pain relievers have on blood pressure with a health care professional.
  • 22% would research an alternative pain reliever online, second only to discussing with a health care professional.

Source: American Heart Association