Painkiller

Why Tapentadol 100mg is the UK’s Preferred Choice for Managing Chronic Pain

Introduction

Chronic or long standing persistent pain that hampers the facets of daily affects ⅓ rd to
almost ½ of the population in the UK along with putting a dent in the economy of the nation.
While opioids are the chief treatment plan for long-standing pain conditions, they are often
addictive in addition to having a wide range of side effects that can cause serious problems
for the patients.

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The need is for a safe and effective option for chronic pain that can work on a wide range of
conditions, and Tapendol has been widely regarded as the best solution.

Before understanding Tapentadol, it is important to have a brief understanding of chronic pain and opioids.

Chronic pain is classified as a period of algesia lasting for 12 weeks or more that impairs an individuals working abilities, and limits their daily activities, resulting in impaired work
quality, academic complications and an overall negative impact on the quality of life.

Back and neck pain, Fibromyalgia, diabetic neuropathy-induced pain, arthritis, and cancer-
related pain are some of the types of chronic pain that require frequent analgesics to ease the discomfort of the patient.

Among the treatment options, opioids are considered most handy as they block the pain
signals between the body and the brain.

Tapentadol is a combination of mu-opioid receptor agonist and a norepinephrine reuptake
inhibitor that gives it the double advantage of being effective for several chronic pain
conditions along with having less adverse effects and addiction potential than conventional
opioids.

Animal studies have shown that despite having a 50-fold lower binding affinity to mu-opioid
receptors, it is only two to three times less than morphine. Unlike other opiates that
negatively impact neurogenesis in the process of exerting their analgesic effects, Tapentadol
doesn’t adversely impact cell survival or reduce neurite outgrowth. On the contrary, it
counteracts the adverse mu-opioid receptor effects on the hippocampal neurons and exhibits
pro-neurogenic and anti-apoptotic effects by activating the Beta-2 and Alpha-2 adrenergic
receptors, respectively.
 
Nerve damage is one of the chief reasons for chronic neuropathic pain and neurogenesis or the process of creating new neurons is crucial for neuropathic pain relief. The hippocampus
is the area of the brain responsible for emotion, memory and learning. Additionally. Hippocampal neurons play an important role in pain management especially of inflammatory and neural origin.
 
Through inhibition of glutamatergic synaptic transmission without impacting postsynaptic
receptor sensitivity, Tapentadol suppresses neuronal hyperexcitability in the hippocampal
area. That combined with its lower affinity with mu-opioid receptors promotes hippocampal
neurogenesis that helps relieve chronic neuropathic pain.

It has a potential role in cancer pain.

Pain plays an integral part in the diagnosis and treatment of cancer. In research conducted in 11 European countries, more than 50% of cancer patients said that their quality of life was not a priority for healthcare professionals.

Because of its combination of neuropathic and nociceptive origin, it becomes difficult to treat cancer pain with conventional analgesics. Tapentadol, because of its unique mechanism and molecular structure, has the potential to be a feasible solution to the problem.

In a European trial conducted to evaluate the impact of Tapentadol for moderate to severe malignant tumor-related pain, 496 patients with cancer-related pain were assigned Tapentadol 100-250 mg or Morphine 40-100 mg twice daily for two weeks. The majority of the patients suffered from cancer of the breast, respiratory tract, or prostrate, and 80% had metastasis in the bones and lymph nodes.

Patients in the Tapentadol group reported an effectiveness in moderate to severe pain than morphine. Those with neuropathic pain showed a higher response rate to Tapentadol with significantly lower adverse effects. Most importantly, gastrointestinal disorders were 29.6% less in the Tapentadol group in comparison to 46.8% in the morphine group.

conclusion

Tapentadol has the potential to enhance conditioned pain modulation in fibromyalgia
patients along with providing significant pain relief in osteoarthritis patients. It even has
anxiolytic activity that enhances its role as an analgesic and muscle relaxant. Despite its
numerous advantages, it should be used with utmost caution as per the advice of the
physician, as it can elevate the serotonin concentration and is contraindicated in pregnant
women and people with hepatic and renal impairments.

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