The life expectancy of cancer patients has significantly improved due to advancements in early diagnosis and treatment of the disease. Therefore, it is more likely that patients will perceive their particular cancer pain as chronic pain. As a result, long-term management of cancer-related pain and the pain associated with oncological therapy is crucial for all patients and a problem for all health providers.
Tapentadol is a centrally-acting analgesic drug with synergistic mechanisms of action. It acts at the µ-opioid receptor and inhibits noradrenaline reuptake. Tapentadol is, therefore, regarded as the pioneer of the MOR-NRI drug class.
Tapentadol has been evaluated on various cancer patient populations (opioid-naive and -pretreated), including those with pain of mixed causes, advanced cancer, and advanced-stage patients. Let us see this in detail.
In 2019, the United States reported 1,752,735 new cancer cases, and 599,589 people died of cancer. After heart disease, cancer is the second leading cause of death in the US.
"Cancer Statistics, 2022," published in the American Cancer Society Journal, states that an estimated 1.9 million new cancer cases will be diagnosed and 609,360 cancer deaths in the United States in 2022. This estimate excludes basal and squamous cell skin cancers, as cancer registries do not require reporting them.
Tapentadol is a centrally-acting analgesic that works by a dual mechanism. It acts by activating mu-opioid receptors and inhibiting norepinephrine reuptake. It helps to relieve moderate to severe pain in adults.
Tapentadol is distinct from classic opioids and thus may be suitable for chronic, neuropathic, and mixed pain. Therefore, it can be considered a general-purpose analgesic for moderate to severe cancer pain in opioid-naive and opioid-pretreated patients.
Cancer is a category of disorders marked by uncontrolled cell proliferation and invasion into other body regions. Cancers result from specific changes at the molecular level in response to various stimuli.
Numerous factors are known to increase the risk of cancer:
People who have cancer may experience moderate to severe pain. As cancer progresses, pain can become worse. It can dull aching, stabbing, or burning. Most cancer pain is manageable, and controlling your pain is essential for treatment.
Acute pain: Acute pain is short-lived. The cause can be easily identified, such as an activity that causes it. The pain goes away when the wound heals.
Chronic pain: Chronic pain may be due to cancer pressing on the nerves or to chemicals produced by a tumor. Nerve changes resulting from cancer treatment can also cause pain. Chronic pain lasts long after the injury or treatment and can range from mild to severe.
Somatic pain: The patient feels pain in body parts, such as bones, muscles, joints, and ligaments. It may be aching, dull, or throbbing in nature.
Neuropathic pain: Caused by pressure on nerves or the spinal cord or by nerve damage. People often experience it as a burning or tingling sensation.
Visceral pain- Viscera are the soft, internal organs in areas of the body, such as the chest, abdomen, and pelvis. The patient feels pain in an organ in one of these areas. The origin of the pain is difficult to pinpoint because it is diffuse and widespread.
Tapentadol provides excellent analgesia with good tolerability. It combines opioid receptor agonist activity with norepinephrine reuptake (NRI) suppression.
Tapentadol may benefit cancer patients who experience frequent nausea, vomiting, constipation, or other events that reduce their quality of life. Its fewer gastrointestinal side effects and favorable Safety profile make Tapentadol an appealing option for some cancer patients.
Tapentadol reduces pain through two action modes: MOR(mu-opioid receptor) agonism and NRI (noradrenaline reuptake inhibition). Compared to delta- and kappa-opioid receptors, it has a more than or equal to a ten-fold affinity for MOR. Tapentadol has a 44-fold reduced affinity for MOR than Morphine.
NRI raises noradrenaline (NA) levels, which activates inhibitory alpha-2 receptors to provide analgesia. Its opioid-sparing actions are a result of this dual mode of action. Although Tapentadol has a negligible effect on serotonin reuptake, it does have an analgesic effect.
In a four-week prospective study by Mercadante et al., 50 opioid-naive cancer patients with moderate-to-severe pain participated; each patient received 50 mg of Tapentadol PR twice daily, and doses were adjusted following the patients' clinical responses. Thirty-nine patients completed the study in total.
As of the first week, pain intensity was significantly reduced compared to the baseline, and the study's duration improved the quality of life. Individuals who previously used NSAIDs or paracetamol tolerated Tapentadol well with little to no side effects. There was no worsening clinical status—Tapentadol in cancer pain management: a prospective open-label study.
Brunetti et al. investigated the Safety and effectiveness of Tapentadol PR in a retrospective trial. The study included 36 challenging patients with hematological malignancies and uncontrolled pain. Overall, there was a reduction in pain intensity without any pertinent adverse events—Tapentadol PR for pain syndromes in actual-life patients with hematological malignancy.
Design the dosing regimen based on the severity of pain and previous treatment experience. Patients should begin treatment with 50 mg of Tapentadol administered every 4 to 6 hours. If the first dose did not provide adequate pain relief, initiate the second one hour later.
Side effects are undesired effects that occur after taking the drug. These can be expected or severe side effects. Talk to your doctor if any of the symptoms appear.
|Common Side Effects||Serious Side Effects|
|Drowsiness or dizziness||Fainting|
|Dry mouth||Fast, slow, or pounding heartbeat|
|Nausea or vomiting||Severe dizziness|
|Itching||Signs of an allergic reaction|
Treatment options for cancer pain include non-opioid analgesics, opioid analgesics, radiation therapy, and surgery. Adjuvant medications are also essential for pain control.
Pain can be a long-term side effect of cancer treatment. It is important to tell your doctor or nurse about persistent or new pain so they can help you manage it. Many effective treatments can relieve pain at all stages and for all types of cancer.
Interestingly, a Cochrane review from 2015 found that Tapentadol proved to be at least as effective in relieving cancer patients' pain as morphine or oxycodone.
Tapentadol's lower incidence of gastrointestinal side effects and generally positive Safety profile make it a suitable alternative for cancer pain patients. Another significant benefit of Tapentadol in cancer patients receiving intensive pharmacological therapy is its minimal likelihood of experiencing drug-drug interactions. Tapentadol can be regarded as an acceptable option for supportive treatment in those cancer patients who are most at risk and likely to develop gastrointestinal side effects.
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